SP600125

目录号: HY-12041 纯度: 99.73%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

SP600125 是一种口服有效的，可逆的，ATP竞争性的 JNK 抑制剂，抑制 JNK1， JNK2 和 JNK3 的 IC₅₀ 分别为 40，40，90 nM。SP600125 是一种有效的铁死亡 (ferroptosis) 抑制剂。SP600125 能诱导膀胱癌细胞自噬 (autophagy) 向凋亡 (apoptosis) 的转化。

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SP600125 Chemical Structure

CAS No. : 129-56-6

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥605	In-stock
5 mg	￥343	In-stock
10 mg	￥550	In-stock
50 mg	￥850	In-stock
100 mg	￥1250	In-stock
200 mg	￥2250	In-stock
500 mg	￥4800	In-stock
1 g		询价
5 g		询价

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Customer Review

MCE 顾客使用本产品发表的 455 篇科研文献

RT-PCR

: SP600125 purchased from MCE. Usage Cited in: Cytotherapy. 2023 Mar 6;S1465-3249(23)00037-3. [Abstract]; SP600125 (10 μM; 24 h) decreases the protein levels of p-JNK and p-c-Jun in THP-1 and U937 cells.

: SP600125 purchased from MCE. Usage Cited in: Exp Neurol. 2020 Sep;331:113374. [Abstract]; Effects of SP600125 attenuated p-JNK and RIPK3-mediated necroptosis after I/R injury. Representative western blot images and quantification of the protein expression of p-JNK, IL-6, pRIPK3 and AIF in the group pretreated with SP600125 before I/R.

: SP600125 purchased from MCE. Usage Cited in: Chem Biol Interact. 2019 Sep 1;310:108748. [Abstract]; Followed by 10 μM SP600125 incubation for 3 or 6 h, the protein levels of t-JNK, p-JNK, t-c-Jun and p-c-Jun in MC3T3-E1 cells are detected by western blotting.

: SP600125 purchased from MCE. Usage Cited in: J Cell Biochem. 2019 Mar;120(3):3898-3910. [Abstract]; Cells pretreated with SP600125 show a decreased proapoptotic Bax expression and increase antiapoptotic Bcl-2 formation when JNK pathway is blocked. Inhibition of p38 by SB202190 significantly enhanced Bcl-2 expression. Pretreatment with BAY 11-7082 to inhibit NF‐κB markedly enhance Baxm and decrease Bcl-2 expression compared with the ACR-treated group.

: SP600125 purchased from MCE. Usage Cited in: Acta Biochim Biophys Sin (Shanghai). 2019 Apr 1;51(4):365-374. [Abstract]; MAPKs inhibitors suppress LPS-induced COX-2 expression and AKT1 phosphorylation. RAW264.7 cells are pretreated for 1 h with U0126, SB202190, SP600125 alone, or all the three inhibitors, respectively, and then exposed to 40 ng/ml LPS for 30 min or 12 h. The phosphorylated protein kinases and COX-2 expression are detected by western blot analysis using their corresponding antibodies.

: SP600125 purchased from MCE. Usage Cited in: J Autoimmun. 2018 May;89:30-40. [Abstract]; The protein expression of S100A7 in keratinocytes incubated with DMSO or JNK inhibitor SP600125 for 48 h after transfection with siRNA for 24 h.

: SP600125 purchased from MCE. Usage Cited in: J Neuroinflammation. 2018 Oct 19;15(1):291. [Abstract]; Blocking the three MAPK signaling pathways through specific inhibitors (U0126; SB202190; and SP600125) significantly decrease the infection-induced neuroinflammatory response via real-time PCR analysis.

: SP600125 purchased from MCE. Usage Cited in: J Neuroinflammation. 2018 Oct 19;15(1):291. [Abstract]; Blocking the three MAPK signaling pathways through specific inhibitors (U0126; SB202190; and SP600125) significantly decrease the infection-induced neuroinflammatory response via real-time PCR analysis.

: SP600125 purchased from MCE. Usage Cited in: J Neuroinflammation. 2018 Jun 15;15(1):184. [Abstract]; Representative immunoblots of total lysates from BV2 cells treated with MPP+or/and U0126 (10 μM), SP600125 (SP, 10 μM) and SB203580 (SB, 10 μM) using the antibodies against DICER.

: SP600125 purchased from MCE. Usage Cited in: Cell Mol Life Sci. 2018 Mar;75(6):1117-1132. [Abstract]; Sertoli cells (SC) are pretreated with the SP600125 for 1 h followed by a 24-h treatment with MC-LR. Expression levels of MMP-8, c-Jun, c-Fos, p-ERK, ERK, p-JNK, and JNK are determined by western blotting.

: SP600125 purchased from MCE. Usage Cited in: Cell Mol Life Sci. 2018 Jul;75(14):2627-2641. [Abstract]; RAW264.7 macrophages are pre-treated with the inhibitor of ERK, JNK, P38, P65, and AKT signal pathway.Western blot analyzes the non- and phosphorylation of ERK, JNK, P38, P65, and AKT.

: SP600125 purchased from MCE. Usage Cited in: Phytomedicine. 2018 Mar 15;42:152-163. [Abstract]; Cells are pretreated with SP600125 (20 μM), SB203580 (20 μM) or U0126 (20 μM) in presence or absence of KLA, then incubated with LPS (1 μg/mL) for certain time. Cell lysates are subjected to western blot.

: SP600125 purchased from MCE. Usage Cited in: Free Radic Biol Med. 2018 Jun 2;124:205-213. [Abstract]; Total and phosphorylation levels of JNK in MCF7 and MDAMB231 after SP600125 treatment at 24 h.

: SP600125 purchased from MCE. Usage Cited in: Br J Pharmacol. 2018 Dec;175(23):4338-4352. [Abstract]; Treatment of macrophages with inhibitor of p38 (SB203580) or JNK (SP600125) inhibits the synthesis of pro-IL-1β in ZFP91-overexpressing THP-1 cells.

: SP600125 purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Oct 3;108:1294-1302. [Abstract]; The protein levels of IL-1β and TNF-α are sharply downregulated by the addition of inhibitors SB203580, SP600125, and U0126.

: SP600125 purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Oct 3;108:1294-1302. [Abstract]; As for both 0 g and 3 g groups, the p-ERK1/2/ERK1/2 is notably reduced by inhibitors SB203580, SP600125, and U0126.

: SP600125 purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Oct 3;108:1294-1302. [Abstract]; The protein level of MMP-9 is downregulated by inhibitors SB203580, SP600125, and U0126.

: SP600125 purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Oct 3;108:1294-1302. [Abstract]; As for both 0 g and 3 g groups, the p-JNK1&JNK1 is downregulated by inhibitors SB203580, SP600125, and U0126.

: SP600125 purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Oct 3;108:1294-1302. [Abstract]; As for both 0 g and 3 g groups, the p-p38&p38 is downregulated by inhibitors SB203580, SP600125, and U0126.

: SP600125 purchased from MCE. Usage Cited in: J Agric Food Chem. 2018 Jun 27;66(25):6317-6325. [Abstract]; HepG2 cells are pre-incubated with 20 µM SB203580, SP600125 and PD98059 for 1 h and then treated with tangeretin(20µM) for 24 h.

: SP600125 purchased from MCE. Usage Cited in: FASEB J. 2018 May;32(5):2722-2734. [Abstract]; Cultured L02 cells exposed to 1% BSA or 200 mM PA for 12 h are pretreated with JNK inhibitor (SP600125) for 2 h. Intracellular and released HMGB1 are analyzed.

: SP600125 purchased from MCE. Usage Cited in: Sci Rep. 2018 Apr 23;8(1):6379. [Abstract]; Immunoblot analysis of lysates from Anisomycin pre-treatment cells reveals an increase of CHIP protein compared with OGD treated only cells, contrasting with a decrease in RIPK3 and p-MLKL protei. Pre-treatment cells with SP600125 results in the expected attenuation in JNK phosphorylation levels.

: SP600125 purchased from MCE. Usage Cited in: Onco Targets Ther. 2018 Nov 28;11:8435-8444. [Abstract]; Western blot results of active caspase 3 and JNK pathway-related genes in the treatment of CON, XRCC1-ON and SP600125.

: SP600125 purchased from MCE. Usage Cited in: J Mol Endocrinol. 2018 Feb;60(2):145-157. [Abstract]; SP600125 decreases Keap1 expression through inhibition of JNK activity.

: SP600125 purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2018 Sep 5;503(2):903-909. [Abstract]; Inactivation of JNK using SP600125 in the PTP1B overexpressing cancer cells largely restores the expression levels of Twist, vimentin and Ecadherin.

: SP600125 purchased from MCE. Usage Cited in: bioRxiv. August 2, 2018.; AGS-EBV and B95.8 cells are pretreated with SP600125 (0, 50, and 100 nM) for 24. Equal amounts of cell lysates are prepared and western blot analysis is performed to determine the levels of total and phosphorylated ERKs, p38, and JNKs and EBV lytic proteins.

: SP600125 purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2018;46(5):1779-1792. [Abstract]; Western blot bands of p38, phospho-p38, ZO-1, Clau-din-1, and Occludin. JNK inhibitor SP600125 and p38 inhibitor SB203580 are used.

: SP600125 purchased from MCE. Usage Cited in: Cell Death Differ. 2017 Mar;24(3):492-499. [Abstract]; LPS stimulates ICER expression via p38-CREB pathway. Effect of MAPK and IKK inhibitors on LPS-induced CREB phosphorylation in peritoneal macrophages.

: SP600125 purchased from MCE. Usage Cited in: Cancer Lett. 2017 Feb 16;393:22-32. [Abstract]; Effects of p38 MAPK inhibitor (SB203580), ERK inhibitor (U0126), JNK inhibitor (SP600125), caspase inhibitor (Z-VAD-FMK) and NAC on SGC-7901 and MGC-803 treated with DOX/VCPA combination treatment. VCPA pretreatment strategy is the same as above. SB203580 (20 μM), U0126 (10 μM), SP600125 (20 μM), Z-VAD-FMK (10 μM) and NAC (5 mM) are treated 2 h before DOX (2 μg/mL) added into the culture, respectively. MAPK pathway protein levels are determined.

: SP600125 purchased from MCE. Usage Cited in: Oncoimmunology. 2017 Dec 26;7(4):e1412910. [Abstract]; The down-regulated phosphorylation of SAPK/JNK pathway by 10µM SP600125 is detected in RAW264.7 by Western blot. The down-regulated phosphorylation of SAPK/JNK pathway by 15mg/kg SP600125 is detected in peritoneal macrophages in vivo by Western blot.

: SP600125 purchased from MCE. Usage Cited in: Int J Mol Med. 2017 Jan;39(1):71-80. [Abstract]; Inhibition of c-Jun N-terminal kinase (JNK) expression enhances the promoting effects of miR-214 on adipocyte differentiation and decreases p-JNK protein expression in bone marrow-derived mesenchymal stem cells (BMSCs) following the overexpression of miR-214. p-JNK protein expression is even more significantly suppressed by treatment of the cells with JNK inhibitor as shown by (A) western blot analysis and (B) statistical analysis of p-JNK protein expression.

: SP600125 purchased from MCE. Usage Cited in: Chem Biol Interact. 2017 Nov 1;277:62-73. [Abstract]; Effects of silencing p53 on colistin-induced ROS production and p-JNK expression level in PC-12 cells. The protein levels of p53. The protein levels of p-JNK by western blot.

: SP600125 purchased from MCE. Usage Cited in: Mol Immunol. 2017 Jul;87:161-170. [Abstract]; Effect of TLR2 on autophagy activation via ERK signaling pathway in MG-infected RAW264.7 cells. RAW264.7 cells transfected with TLR2 siRNA/control siRNA are infected with MG for 30 min prior to SP600125. The expression levels of Beclin1, LC3-II/I, p-JNK, p-ERK1/2 and p-p38 are examined by Western blot. The GAPDH level was used as the internal standard.

: SP600125 purchased from MCE. Usage Cited in: Oxid Med Cell Longev. 2017;2017:7426458. [Abstract]; Representative immunoblot analysis of p53, p16, p21, and retinoblastoma protein (Rb) in NP cells.

: SP600125 purchased from MCE. Usage Cited in: Oxid Med Cell Longev. 2017;2017:6175841. [Abstract]; Involvements of MAPK signaling pathway in CPS-induced apoptosis in ALI cultures of sheep bronchial epithelial cells. Cells are pretreated with SP600125 (a JNK inhibitor, 20 μM) for 1 h, followed by exposure to CPS (100 ng/mL) or MO (MOI = 30) for 48 h. Cell lysates are subjected to Western blotting analysis using indicated antibodies.

: SP600125 purchased from MCE. Usage Cited in: Oncotarget. 2016 Dec 20;7(51):85079-85096. [Abstract]; IL-37b inhibits TNF-α mediated activation of the pSmad3L/c-myc pathway but potentiates pSmad3C/ p21 expression in SMMC-7721 cells. Serum-starved LV_NC and LV_IL1F7b-infected SMMC-7721 cells are incubated for 8 h in the absence or presence of 10 μM SP600125 and are then treated for 30 mins with 400 pM TNF-α. Expression of endogenous Smad3 phosphorylation, p21, and c-myc is analyzed in Western blot using specific Abs.

: SP600125 purchased from MCE. Usage Cited in: J Mol Cell Cardiol. 2015 Dec;89(Pt B):268-79. [Abstract]; Dose response of MAPK and Akt inhibitors on cardiac fibroblast-derived exosomes (Exo)-induced activation of MAPKs and Akt. Neonatal rat cardiomyocytes are treated with or without Exo (50 μg/mL), U0126, SP600125, MK-2206, and SB023580 for 20 min and subjected to Western blot analysis. The results are from 4 separate experiments.

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JNK1 JNK2 JNK3 JNK

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

SP600125 is an orally active, reversible, and ATP-competitive JNK inhibitor with IC₅₀s of 40, 40 and 90 nM for JNK1, JNK2 and JNK3, respectively. SP600125 is a potent ferroptosis inhibitor. SP600125 induces the transformation of bladder cancer cells from autophagy to apoptosis^[1]^[2]^[3].

IC₅₀ & Target^[1]

JNK1

40 nM (IC₅₀)

JNK2

40 nM (IC₅₀)

JNK3

90 nM (IC₅₀)

Autophagy

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
786-0	IC₅₀	27.1 μM Compound: SP600125	Antiproliferative activity against human 786-0 cells measured after 48 hrs by SRB assay Antiproliferative activity against human 786-0 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
A498	IC₅₀	7.03 μM Compound: SP600125	Antiproliferative activity against human A498 cells measured after 48 hrs by SRB assay Antiproliferative activity against human A498 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
A549	IC₅₀	14.93 μM Compound: SP600125	Antiproliferative activity against human A549 cells measured after 48 hrs by SRB assay Antiproliferative activity against human A549 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
ACHN	IC₅₀	6.64 μM Compound: SP600125	Antiproliferative activity against human ACHN cells measured after 48 hrs by SRB assay Antiproliferative activity against human ACHN cells measured after 48 hrs by SRB assay	[PMID: 35764033]
BT-549	IC₅₀	30.76 μM Compound: SP600125	Antiproliferative activity against human BT-549 cells measured after 48 hrs by SRB assay Antiproliferative activity against human BT-549 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
CAKI-1	IC₅₀	3.56 μM Compound: SP600125	Antiproliferative activity against human CAKI-1 cells measured after 48 hrs by SRB assay Antiproliferative activity against human CAKI-1 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
CCRF-CEM	IC₅₀	16.03 μM Compound: SP600125	Antiproliferative activity against human CCRF-CEM cells measured after 48 hrs by SRB assay Antiproliferative activity against human CCRF-CEM cells measured after 48 hrs by SRB assay	[PMID: 35764033]
COLO 205	IC₅₀	19.54 μM Compound: SP600125	Antiproliferative activity against human COLO 205 cells measured after 48 hrs by SRB assay Antiproliferative activity against human COLO 205 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
DU-145	IC₅₀	28.18 μM Compound: SP600125	Antiproliferative activity against human DU-145 cells measured after 48 hrs by SRB assay Antiproliferative activity against human DU-145 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
EKVX	IC₅₀	20.04 μM Compound: SP600125	Antiproliferative activity against human EKVX cells measured after 48 hrs by SRB assay Antiproliferative activity against human EKVX cells measured after 48 hrs by SRB assay	[PMID: 35764033]
HCC 2998	IC₅₀	9.62 μM Compound: SP600125	Antiproliferative activity against human HCC 2998 cells measured after 48 hrs by SRB assay Antiproliferative activity against human HCC 2998 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
HCT-116	IC₅₀	44.57 μM Compound: SP600125	Antiproliferative activity against human HCT-116 cells measured after 48 hrs by SRB assay Antiproliferative activity against human HCT-116 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
HCT-15	IC₅₀	8.04 μM Compound: SP600125	Antiproliferative activity against human HCT-15 cells measured after 48 hrs by SRB assay Antiproliferative activity against human HCT-15 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
HL-60(TB)	IC₅₀	42.07 μM Compound: SP600125	Antiproliferative activity against human HL-60(TB) cells measured after 48 hrs by SRB assay Antiproliferative activity against human HL-60(TB) cells measured after 48 hrs by SRB assay	[PMID: 35764033]
HOP-62	IC₅₀	69.34 μM Compound: SP600125	Antiproliferative activity against human HOP-62 cells measured after 48 hrs by SRB assay Antiproliferative activity against human HOP-62 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
HOP-92	IC₅₀	37.58 μM Compound: SP600125	Antiproliferative activity against human HOP-92 cells measured after 48 hrs by SRB assay Antiproliferative activity against human HOP-92 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
Hs-578T	IC₅₀	55.08 μM Compound: SP600125	Antiproliferative activity against human Hs-578T cells measured after 48 hrs by SRB assay Antiproliferative activity against human Hs-578T cells measured after 48 hrs by SRB assay	[PMID: 35764033]
HT-29	IC₅₀	25.88 μM Compound: SP600125	Antiproliferative activity against human HT-29 cells measured after 48 hrs by SRB assay Antiproliferative activity against human HT-29 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
IGROV-1	IC₅₀	11.35 μM Compound: SP600125	Antiproliferative activity against human IGROV-1 cells measured after 48 hrs by SRB assay Antiproliferative activity against human IGROV-1 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
K562	IC₅₀	48.64 μM Compound: SP600125	Antiproliferative activity against human K562 cells measured after 48 hrs by SRB assay Antiproliferative activity against human K562 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
KM12	IC₅₀	2.62 μM Compound: SP600125	Antiproliferative activity against human KM12 cells measured after 48 hrs by SRB assay Antiproliferative activity against human KM12 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
M14	IC₅₀	> 100 μM Compound: SP600125	Antiproliferative activity against human M14 cells measured after 48 hrs by SRB assay Antiproliferative activity against human M14 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
Malme-3M	IC₅₀	16.41 μM Compound: SP600125	Antiproliferative activity against human Malme-3M cells measured after 48 hrs by SRB assay Antiproliferative activity against human Malme-3M cells measured after 48 hrs by SRB assay	[PMID: 35764033]
MCF7	IC₅₀	48.98 μM Compound: SP600125	Antiproliferative activity against human MCF7 cells measured after 48 hrs by SRB assay Antiproliferative activity against human MCF7 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
MDA-MB-231	IC₅₀	65.31 μM Compound: SP600125	Antiproliferative activity against human MDA-MB-231 cells measured after 48 hrs by SRB assay Antiproliferative activity against human MDA-MB-231 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
MDA-MB-435	IC₅₀	12.82 μM Compound: SP600125	Antiproliferative activity against human MDA-MB-435 cells measured after 48 hrs by SRB assay Antiproliferative activity against human MDA-MB-435 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
MOLT-4	IC₅₀	20.37 μM Compound: SP600125	Antiproliferative activity against human MOLT-4 cells measured after 48 hrs by SRB assay Antiproliferative activity against human MOLT-4 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
MONO-MAC-6	IC₅₀	5.2 μM Compound: SP600125	Inhibition of JNK in human MONO-MAC-6 cells assessed as reduction in LPS-induced IL6 production preincubated for 30 mins followed by LPS-stimulation and measured after 24 hrs by ELISA Inhibition of JNK in human MONO-MAC-6 cells assessed as reduction in LPS-induced IL6 production preincubated for 30 mins followed by LPS-stimulation and measured after 24 hrs by ELISA	[PMID: 30347329]
NCI/ADR-RES	IC₅₀	22.59 μM Compound: SP600125	Antiproliferative activity against human NCI-ADR-RES cells measured after 48 hrs by SRB assay Antiproliferative activity against human NCI-ADR-RES cells measured after 48 hrs by SRB assay	[PMID: 35764033]
NCI-H226	IC₅₀	22.86 μM Compound: SP600125	Antiproliferative activity against human NCI-H226 cells measured after 48 hrs by SRB assay Antiproliferative activity against human NCI-H226 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
NCI-H23	IC₅₀	23.77 μM Compound: SP600125	Antiproliferative activity against human NCI-H23 cells measured after 48 hrs by SRB assay Antiproliferative activity against human NCI-H23 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
NCI-H322M	IC₅₀	24.95 μM Compound: SP600125	Antiproliferative activity against human NCI-H322M cells measured after 48 hrs by SRB assay Antiproliferative activity against human NCI-H322M cells measured after 48 hrs by SRB assay	[PMID: 35764033]
NCI-H460	IC₅₀	9.86 μM Compound: SP600125	Antiproliferative activity against human NCI-H460 cells measured after 48 hrs by SRB assay Antiproliferative activity against human NCI-H460 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
NCI-H522	IC₅₀	12.19 μM Compound: SP600125	Antiproliferative activity against human NCI-H522 cells measured after 48 hrs by SRB assay Antiproliferative activity against human NCI-H522 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
OVCAR-3	IC₅₀	15.31 μM Compound: SP600125	Antiproliferative activity against human OVCAR-3 cells measured after 48 hrs by SRB assay Antiproliferative activity against human OVCAR-3 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
OVCAR-4	IC₅₀	31.91 μM Compound: SP600125	Antiproliferative activity against human OVCAR-4 cells measured after 48 hrs by SRB assay Antiproliferative activity against human OVCAR-4 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
OVCAR-5	IC₅₀	24.38 μM Compound: SP600125	Antiproliferative activity against human OVCAR-5 cells measured after 48 hrs by SRB assay Antiproliferative activity against human OVCAR-5 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
OVCAR-8	IC₅₀	22.03 μM Compound: SP600125	Antiproliferative activity against human OVCAR-8 cells measured after 48 hrs by SRB assay Antiproliferative activity against human OVCAR-8 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
PC-3	IC₅₀	23.28 μM Compound: SP600125	Antiproliferative activity against human PC-3 cells measured after 48 hrs by SRB assay Antiproliferative activity against human PC-3 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
RPMI-8226	IC₅₀	18.79 μM Compound: SP600125	Antiproliferative activity against human RPMI-8226 cells measured after 48 hrs by SRB assay Antiproliferative activity against human RPMI-8226 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
RXF 393	IC₅₀	20.75 μM Compound: SP600125	Antiproliferative activity against human RXF 393 cells measured after 48 hrs by SRB assay Antiproliferative activity against human RXF 393 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
SF-268	IC₅₀	18.45 μM Compound: SP600125	Antiproliferative activity against human SF-268 cells measured after 48 hrs by SRB assay Antiproliferative activity against human SF-268 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
SF-295	IC₅₀	22.49 μM Compound: SP600125	Antiproliferative activity against human SF-295 cells measured after 48 hrs by SRB assay Antiproliferative activity against human SF-295 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
SF-539	IC₅₀	32.21 μM Compound: SP600125	Antiproliferative activity against human SF-539 cells measured after 48 hrs by SRB assay Antiproliferative activity against human SF-539 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
SK-MEL-2	IC₅₀	28.97 μM Compound: SP600125	Antiproliferative activity against human SK-MEL-2 cells measured after 48 hrs by SRB assay Antiproliferative activity against human SK-MEL-2 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
SK-MEL-28	IC₅₀	37.5 μM Compound: SP600125	Antiproliferative activity against human SK-MEL-28 cells measured after 48 hrs by SRB assay Antiproliferative activity against human SK-MEL-28 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
SK-MEL-5	IC₅₀	14.62 μM Compound: SP600125	Antiproliferative activity against human SK-MEL-5 cells measured after 48 hrs by SRB assay Antiproliferative activity against human SK-MEL-5 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
SK-OV-3	IC₅₀	20.99 μM Compound: SP600125	Antiproliferative activity against human SK-OV-3 cells measured after 48 hrs by SRB assay Antiproliferative activity against human SK-OV-3 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
SN12C	IC₅₀	14.76 μM Compound: SP600125	Antiproliferative activity against human SN12C cells measured after 48 hrs by SRB assay Antiproliferative activity against human SN12C cells measured after 48 hrs by SRB assay	[PMID: 35764033]
SNB-19	IC₅₀	50 μM Compound: SP600125	Antiproliferative activity against human SNB-19 cells measured after 48 hrs by SRB assay Antiproliferative activity against human SNB-19 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
SNB-75	IC₅₀	16.9 μM Compound: SP600125	Antiproliferative activity against human SNB-75 cells measured after 48 hrs by SRB assay Antiproliferative activity against human SNB-75 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
SR	IC₅₀	13.09 μM Compound: SP600125	Antiproliferative activity against human SR cells measured after 48 hrs by SRB assay Antiproliferative activity against human SR cells measured after 48 hrs by SRB assay	[PMID: 35764033]
SW-620	IC₅₀	10.91 μM Compound: SP600125	Antiproliferative activity against human SW-620 cells measured after 48 hrs by SRB assay Antiproliferative activity against human SW-620 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
T47D	IC₅₀	> 100 μM Compound: SP600125	Antiproliferative activity against human T47D cells measured after 48 hrs by SRB assay Antiproliferative activity against human T47D cells measured after 48 hrs by SRB assay	[PMID: 35764033]
TK-10	IC₅₀	5.93 μM Compound: SP600125	Antiproliferative activity against human TK-10 cells measured after 48 hrs by SRB assay Antiproliferative activity against human TK-10 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
U-251	IC₅₀	23.07 μM Compound: SP600125	Antiproliferative activity against human U-251 cells measured after 48 hrs by SRB assay Antiproliferative activity against human U-251 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
UACC-257	IC₅₀	29.51 μM Compound: SP600125	Antiproliferative activity against human UACC-257 cells measured after 48 hrs by SRB assay Antiproliferative activity against human UACC-257 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
UACC-62	IC₅₀	14.55 μM Compound: SP600125	Antiproliferative activity against human UACC-62 cells measured after 48 hrs by SRB assay Antiproliferative activity against human UACC-62 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
UO-31	IC₅₀	10.54 μM Compound: SP600125	Antiproliferative activity against human UO-31 cells measured after 48 hrs by SRB assay Antiproliferative activity against human UO-31 cells measured after 48 hrs by SRB assay	[PMID: 35764033]
WI-38	IC₅₀	> 20 μM Compound: SP600125	Antiproliferative activity against human WI-38 cells measured by MTT assay Antiproliferative activity against human WI-38 cells measured by MTT assay	[PMID: 35764033]

体外研究
(In Vitro)

SP600125 是 JNK2 的 ATP 竞争性抑制剂，K_i 值为 0.19±0.06 μM。SP600125 在 Jurkat T 细胞中抑制 c-Jun 的磷酸化，IC₅₀ 为 5 μM 至 10 μM。在 CD4⁺ 细胞中，例如从人脐带血或外周血中分离的 Th0 细胞，SP600125 阻断细胞活化和分化并抑制炎症基因 COX-2、IL-2、IL-10、IFN-γ 和 TNF-α，IC₅₀ 为 5 μM 至 12 μM^[1]。
在小鼠 β 细胞 MIN6 中，SP600125 (20 μM) 诱导 p38 MAPK 的磷酸化及其下游 CREB 依赖性启动子激活^[2]。
在 HCT116 细胞中，SP600125 (20 μM) 阻断 G2 期到有丝分裂的转变并诱导核内复制。SP600125 的这种能力独立于 JNK 抑制，但由于其抑制 Aurora A 和 Polo 样激酶 1 上游的 CDK1-细胞周期蛋白 B 激活^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

SP600125 (15 mg/kg 或 30 mg/kg；静脉注射) 显著抑制 TNF-α 血清水平，而 30 mg/kg 口服施用后，则剂量依赖性地阻断 TNF-α 表达^[1]。
SP600125 在大鼠体内减轻 LPS 诱导的 ALI。SP600125 组大鼠 BALF 中 TNF-α和 IL-6 的表达水平显著降低^[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

220.23

Formula

C₁₄H₈N₂O

CAS 号

129-56-6

性状

固体

颜色

Yellow to green

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : 12.5 mg/mL (56.76 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	4.5407 mL	22.7035 mL	45.4071 mL
5 mM	0.9081 mL	4.5407 mL	9.0814 mL
10 mM	0.4541 mL	2.2704 mL	4.5407 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.08 mg/mL (9.44 mM); 悬浊液; 超声助溶

此方案可获得 2.08 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

方案一

请依序添加每种溶剂： Corn Oil
Solubility: 1 mg/mL (4.54 mM); 悬浊液; 超声助溶 (<80°C)
方案二

请依序添加每种溶剂： 1% CMC-Na/saline water
Solubility: 3.33 mg/mL (15.12 mM); 悬浊液; 超声助溶

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.73%

选择批次：

Data Sheet (654 KB) SDS (393 KB)

COA (292 KB) HNMR (255 KB) LCMS (98 KB) 元素分析报告 (216 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Bennett BL, et al. SP600125, an anthrapyrazolone inhibitor of Jun N-terminal kinase. Proc Natl Acad Sci U S A, 2001, 98(24), 13681-13686. [Content Brief]

[2]. Vaishnav D, et al. SP600125, an inhibitor of c-jun N-terminal kinase, activates CREB by a p38 MAPK-mediated pathway. Biochem Biophys Res Commun, 2003, 307(4), 855-860. [Content Brief]

[3]. Kim JA, et al. SP600125 suppresses Cdk1 and induces endoreplication directly from G2 phase, independent of JNK inhibition. Oncogene, 2010, 29(11), 1702-1716. [Content Brief]

[4]. Zheng Y, et al. JNK inhibitor SP600125 protects against lipopolysaccharide-induced acute lung injury via upregulation ofclaudin-4. Exp Ther Med. 2014 Jul;8(1):153-158. [Content Brief]

[5]. Zhang H, et al. SP600125 Suppresses Keap1 Expression and Results in NRF2-mediated Prevention of Diabetic Nephropathy. J Mol Endocrinol. J Mol Endocrinol. 2018 Feb;60(2):145-157. [Content Brief]

[6]. Yatsushige H, et al. Role of c-Jun N-terminal kinase in cerebral vasospasm after experimental subarachnoid hemorrhage. Stroke. 2005 Jul;36(7):1538-43. [Content Brief]

Cell Assay ^[1]	Determination of mRNA half-life is performed essentially, except that CD14⁺ cells are stimulated with (bacterial) lipopolysaccharide (LPS; 50 ng/mL) for 2 h before addition of actinomycin D (5 μg/mL). SP600125 (25 μM) or vehicle (0.5% DMSO vol/vol) is added immediately following the actinomycin D. Analysis is performed by using real-time reverse transcription (RT)-PCR. Total RNA is extracted with an RNeasy Mini kit. TNF mRNA is measured by real time RT-PCR, using a TNF Taqman probe. All data are normalized by using glyceraldehyde-3-phosphate dehydrogenase (GAPDH) expression. The TNF-α forward primer is 5′-CTGGCCCAGGCAGTCAGAT-3′ and the reverse primer is 5′-TATCTCTCAGCTCCACGCCATT-3′. The Taqman probe sequence is 5′-FAM-CCTGTAGCCCATGTTGTAGCAAACCCTCA-TAMRA-3′^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]^[4]	Mice^[1] Female CD-1 mice (8-10 weeks of age) are dosed i.v. or per oswith SP600125 in PPCES vehicle (30% PEG-400/20% polypropylene glycol/15% Cremophor EL/5% ethanol/30% saline), final volume of 5 mL/kg, 15 min before i.v. injection with LPS in saline (0.5 mg/kg). At 90 min, a terminal bleed is obtained from the abdominal vena cava, and the serum is recovered. Samples are analyzed for mouse TNF-α by using an ELISA. Rats^[4] A total of 40 male Wistar rats are randomly divided into four groups (n=10): the control group, LPS group, normal saline group (NS) and the SP600125 group. Acute lung injury (ALI) is induced via intratracheal injection of LPS. Normal saline or SP600125 is administered via intraperitoneal injection (15 mg/kg) 10 min after the LPS injection. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Bennett BL, et al. SP600125, an anthrapyrazolone inhibitor of Jun N-terminal kinase. Proc Natl Acad Sci U S A, 2001, 98(24), 13681-13686. [Content Brief] [2]. Vaishnav D, et al. SP600125, an inhibitor of c-jun N-terminal kinase, activates CREB by a p38 MAPK-mediated pathway. Biochem Biophys Res Commun, 2003, 307(4), 855-860. [Content Brief] [3]. Kim JA, et al. SP600125 suppresses Cdk1 and induces endoreplication directly from G2 phase, independent of JNK inhibition. Oncogene, 2010, 29(11), 1702-1716. [Content Brief] [4]. Zheng Y, et al. JNK inhibitor SP600125 protects against lipopolysaccharide-induced acute lung injury via upregulation ofclaudin-4. Exp Ther Med. 2014 Jul;8(1):153-158. [Content Brief] [5]. Zhang H, et al. SP600125 Suppresses Keap1 Expression and Results in NRF2-mediated Prevention of Diabetic Nephropathy. J Mol Endocrinol. J Mol Endocrinol. 2018 Feb;60(2):145-157. [Content Brief] [6]. Yatsushige H, et al. Role of c-Jun N-terminal kinase in cerebral vasospasm after experimental subarachnoid hemorrhage. Stroke. 2005 Jul;36(7):1538-43. [Content Brief]

SP600125 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	4.5407 mL	22.7035 mL	45.4071 mL	113.5177 mL
	5 mM	0.9081 mL	4.5407 mL	9.0814 mL	22.7035 mL
	10 mM	0.4541 mL	2.2704 mL	4.5407 mL	11.3518 mL
	15 mM	0.3027 mL	1.5136 mL	3.0271 mL	7.5678 mL
	20 mM	0.2270 mL	1.1352 mL	2.2704 mL	5.6759 mL
	25 mM	0.1816 mL	0.9081 mL	1.8163 mL	4.5407 mL
	30 mM	0.1514 mL	0.7568 mL	1.5136 mL	3.7839 mL
	40 mM	0.1135 mL	0.5676 mL	1.1352 mL	2.8379 mL
	50 mM	0.0908 mL	0.4541 mL	0.9081 mL	2.2704 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SP600125129-56-6SP 600125SP-600125JNKAutophagyApoptosisFerroptosisc-Jun N-terminal kinasereversibleATP-competitivephosphorylationInhibitorinhibitorinhibit

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