Adezmapimod (Synonyms: SB 203580; RWJ 64809)

目录号: HY-10256 纯度: 99.96%: FAQs
Data Sheet SDS COA 产品使用指南技术支持

Adezmapimod (SB 203580) 是一种选择性的，ATP 竞争性的 p38 MAPK 抑制剂，对 SAPK2a/p38 和 SAPK2b/p38β2 的 IC₅₀ 分别为 50 nM 和 500 nM。Adezmapimod 抑制 LCK，GSK3β 和 PKBα，IC₅₀ 比 SAPK2a/p38 高 100-500 倍。Adezmapimod 不抑制 JNK 活性，是一种自噬 (autophagy) 和线粒体自噬 (mitophagy) 激活剂。

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Adezmapimod Chemical Structure

CAS No. : 152121-47-6

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥412	In-stock
5 mg	￥375	In-stock
10 mg	￥600	In-stock
25 mg	￥979	In-stock
50 mg	￥1400	In-stock
100 mg	￥2100	In-stock
200 mg	￥3225	In-stock
500 mg	￥5338	In-stock
1 g		询价
5 g		询价

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Customer Review

Other Forms of Adezmapimod:

Adezmapimod hydrochloride In-stock

MCE 顾客使用本产品发表的 459 篇科研文献

IHC

: Adezmapimod purchased from MCE. Usage Cited in: Biomaterials. 2018 Aug;175:19-29. [Abstract]; Western blotting analysis showing the related protein expression (MHC, MyoD, p38α, phospho-p38α) of C2C12 myoblasts after incubated for 6 days in DM containing 40 μg/mL AuNPs and Au-AgNPs in the presence or absence of SB203580 (SB).

: Adezmapimod purchased from MCE. Usage Cited in: PLoS Biol. 2018 May 11;16(5):e2004225. [Abstract]; Representative western blots of p-CREB (Ser133) and UCP-1 in iWAT from C57BL/6J mice after 4 wk of SB203580 treatment. These mice are exposed to cold for 2 d before analysis.

: Adezmapimod 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.

: Adezmapimod 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.

: Adezmapimod 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.

: Adezmapimod 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.

: Adezmapimod 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.

: Adezmapimod 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.

: Adezmapimod 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.

: Adezmapimod 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.

: Adezmapimod purchased from MCE. Usage Cited in: Acta Physiol (Oxf). 2018 Feb;222(2). [Abstract]; P38 inhibitor SB203580 pretreatment also decreases p-HSP27 and MMP9 levels induced by MICAL2-overexpression.

: Adezmapimod 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.

: Adezmapimod purchased from MCE. Usage Cited in: Front Immunol. 2018 Dec 7;9:2854. [Abstract]; Neutrophils are pretreated with inhibitor of p38 MAPK (SB203580) and ERK1/2 (U0126), and the cells are then incubated with either SS2 ZY05719 or PMA for 3 h. Immunofluorescence is performed.

: Adezmapimod purchased from MCE. Usage Cited in: Am J Physiol Cell Physiol. 2018 Aug 1;315(2):C225-C235. [Abstract]; Western blot analysis shows that inhibiting MAPK cannot completely reverse increased expression of RNF2 and CDDP resistance of OC cells.

: Adezmapimod purchased from MCE. Usage Cited in: J Cell Mol Med. 2018 Nov;22(11):5450-5467. [Abstract]; Treatment with SB203580 significantly abolishes siPlectin-stimulated p38 activation.

: Adezmapimod purchased from MCE. Usage Cited in: FASEB J. 2019 Feb;33(2):2435-2450. [Abstract]; Bile acids (BAs) cause nuclear translocation of NF-kB p65, an effect that is abolished by SB203580.

: Adezmapimod purchased from MCE. Usage Cited in: J Endod. 2018 May;44(5):751-758. [Abstract]; p38 MAPK inhibition enhances DPC-Exos–induced tube formation. (A) p38 MAPK activity is measured by detecting Phospho-p38 MAPK. The ratio between Phospho-p38 MAPK and the p38 MAPK band is used for quantification. (B) The effects of VEGF-A and KDR expression after p38 MAPK inhibitor SB203580 treatment on DPC-Exos-stimulated HUVECs.

: Adezmapimod purchased from MCE. Usage Cited in: J Cell Biochem. 2018 Dec 2. [Abstract]; Western analysis of protein expression in the treatment of miR-543 and SB 203580.

: Adezmapimod purchased from MCE. Usage Cited in: J Cell Biochem. 2018 Nov;119(10):8450-8459. [Abstract]; Western blot results show a reduction in phosphorylated p38 MAPK in ADSCs after treatment with 20 μM SB203580, 20 μM SP600125, or 20 μM PD98059 for 1 hour.

: Adezmapimod purchased from MCE. Usage Cited in: BMC Pulm Med. 2018 Nov 27;18(1):178. [Abstract]; P-p38 and P-Hsp27 are detected by western blotting with the treatment of LPS, SB203580 and SB203580+ LPS.

: Adezmapimod purchased from MCE. Usage Cited in: BMC Pulm Med. 2018 Nov 27;18(1):178. [Abstract]; P-p38 and P-Hsp27 are detected by western blotting with the treatment of LPS, SB203580 and SB203580+ LPS.

: Adezmapimod 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.

: Adezmapimod 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.

: Adezmapimod 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.

: Adezmapimod purchased from MCE. Usage Cited in: Free Radic Biol Med. 2017 Nov;112:49-59. [Abstract]; Cells are pre-treated with ERK (U1026) and p38 (SB203580) inhibitors, followed by GL-V9 treatment for 24 h. Western blot is performed to analyze NAG-1 expression.

: Adezmapimod purchased from MCE. Usage Cited in: Hum Mol Genet. 2017 Sep 15;26(18):3553-3563. [Abstract]; Immunofluorescence analysis for expression of the I-cell marker ΔNP63 on proximal sections of ureters explanted from E12.5 wildtype (control) embryos and cultured for 6 d in the presence of solvent (DMSO) (A), the AKT inhibitor (AKT-i) MK2206 (B), the P38 inhibitor (P38-i) SB203580 (C), the ERK1/2 inhibitor (ERK1/2-i) PD98059 (D) or combinations as indicated (E and F).

: Adezmapimod purchased from MCE. Usage Cited in: Biochem Cell Biol. 2017 Feb;95(1):64-68. [Abstract]; The involvement of the p38 MAPK signaling pathways in lactoferrin-induced differentiation of HaCaT keratinocytes. HaCaT cells are differentiated in the presence or absence of 10 μM bovine Lactoferrin for 5 days. PD98059 (40 μM), SB203580 (10 μM), or LY294002 (10 μM) are added at the same time. Cell differentiation is evaluated by the expression levels of Involucrin and Filaggrin. GAPDH is used as a loading control.

: Adezmapimod purchased from MCE. Usage Cited in: Biomed Res. 2017; 28 (8): 3383-3386; Effects of various protease inhibitors on HO-1 and P-gp protein expressions.

: Adezmapimod purchased from MCE. Usage Cited in: Int J Clin Exp Med. 2017;10(9):13542-13549.; SB203580 decreases the expression ratio of p-p38 and p38 to inhibit activation of p38 MARK pathway.

: Adezmapimod purchased from MCE. Usage Cited in: China Biotechnology. 2017, 37(12): 40-48.; The Western blot analysis of HOG1 and Phospho-HOG1.

: Adezmapimod purchased from MCE. Usage Cited in: Oncotarget. 2017 Oct 19;8(60):101965-101983. [Abstract]; Representative western blot analysis of P-gp, p38 MAPK and phospho-p38 MAPK expression in MCF-7/MDR and K562/MDR cells treated with 10 μM SB203580 for 48 hr.

: Adezmapimod 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 SB203580 (a P38 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.

: Adezmapimod purchased from MCE. Usage Cited in: Chin Arch Otolaryngol Head Neck Surg. 2016,23(01):49-52.; Effect of p38MAPK inhibitor on the soft palate reconstruction of the rats with chronic intermittent hypoxia.

: Adezmapimod 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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p38 MAPK p38α p38β MAPK13 p38δ p38γ

生物活性
纯度 & 产品资料
参考文献

生物活性

Adezmapimod (SB 203580) is a selective and ATP-competitive p38 MAPK inhibitor with IC₅₀s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod inhibits LCK, GSK3β and PKBα with IC₅₀s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod does not disrupt JNK activity and is an autophagy and mitophagy activator^[1].

IC₅₀ & Target^[1]

p38

50 nM (IC₅₀)

p38β2

500 nM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
BMDC	IC₅₀	3.45 μM Compound: SB203580	Antiinflammatory activity in C57BL/6 mouse BMDCs assessed as inhibition of LPS-stimulated IL12 production treated 1 hr before LPS challenge measured 18 hrs post stimulation by ELISA Antiinflammatory activity in C57BL/6 mouse BMDCs assessed as inhibition of LPS-stimulated IL12 production treated 1 hr before LPS challenge measured 18 hrs post stimulation by ELISA	[PMID: 23484668]
BMDC	IC₅₀	3.5 μM Compound: SB203580	Anti-inflammatory activity in C57BL/6 mouse BMDC assessed as inhibition of LPS-induced IL-6 production pretreated for 1 hr followed by LPS-stimulation after 18 hrs by ELISA Anti-inflammatory activity in C57BL/6 mouse BMDC assessed as inhibition of LPS-induced IL-6 production pretreated for 1 hr followed by LPS-stimulation after 18 hrs by ELISA	[PMID: 28009172]
BMDC	IC₅₀	3.5 μM Compound: SB203580	Antiinflammatory activity in C57BL/6 mouse BMDC cells assessed as inhibition of LPS-induced IL-6 production preincubated for 1 hr prior to LPS-stimulation measured after 18 hrs by ELISA Antiinflammatory activity in C57BL/6 mouse BMDC cells assessed as inhibition of LPS-induced IL-6 production preincubated for 1 hr prior to LPS-stimulation measured after 18 hrs by ELISA	[PMID: 24047259]
BMDC	IC₅₀	3.53 μM Compound: SB203580	Antiinflammatory activity in C57BL/6 mouse BMDC assessed as inhibition of LPS-stimulated IL-6 production preincubated for 1 hr before LPS-stimulation measured after 16 hrs by ELISA Antiinflammatory activity in C57BL/6 mouse BMDC assessed as inhibition of LPS-stimulated IL-6 production preincubated for 1 hr before LPS-stimulation measured after 16 hrs by ELISA	[PMID: 22071304]
BMDC	IC₅₀	3.56 μM Compound: SB203580	Antiinflammatory activity against in C57BL/6 mouse BMDC assessed as inhibition of LPS-stimulated IL6 production compound pre-incubated for 1 hr before LPS challenge by ELISA Antiinflammatory activity against in C57BL/6 mouse BMDC assessed as inhibition of LPS-stimulated IL6 production compound pre-incubated for 1 hr before LPS challenge by ELISA	[PMID: 23200246]
BMDC	IC₅₀	5 μM Compound: SB203580	Anti-inflammatory activity in C57BL/6 mouse BMDC assessed as inhibition of LPS-induced IL12 p40 production pretreated for 1 hr followed by LPS-stimulation after 18 hrs by ELISA Anti-inflammatory activity in C57BL/6 mouse BMDC assessed as inhibition of LPS-induced IL12 p40 production pretreated for 1 hr followed by LPS-stimulation after 18 hrs by ELISA	[PMID: 28009172]
BMDC	IC₅₀	5 μM Compound: SB203580	Antiinflammatory activity in C57BL/6 mouse BMDC cells assessed as inhibition of LPS-induced IL-12 p40 production preincubated for 1 hr prior to LPS-stimulation measured after 18 hrs by ELISA Antiinflammatory activity in C57BL/6 mouse BMDC cells assessed as inhibition of LPS-induced IL-12 p40 production preincubated for 1 hr prior to LPS-stimulation measured after 18 hrs by ELISA	[PMID: 24047259]
BMDC	IC₅₀	5 μM Compound: SB203580	Antiinflammatory activity in wild-type C57BL/6 mouse BMDCs assessed as inhibition of IL-12 p40 production incubated for 1 hr prior to LPS challenge measured after 16 hrs by ELISA Antiinflammatory activity in wild-type C57BL/6 mouse BMDCs assessed as inhibition of IL-12 p40 production incubated for 1 hr prior to LPS challenge measured after 16 hrs by ELISA	[PMID: 23395633]
BMDC	IC₅₀	5.02 μM Compound: SB203580	Antiinflammatory activity in C57BL/6 mouse BMDC assessed as inhibition of LPS-stimulated IL-12p40 production preincubated for 1 hr before LPS-stimulation measured after 16 hrs by ELISA Antiinflammatory activity in C57BL/6 mouse BMDC assessed as inhibition of LPS-stimulated IL-12p40 production preincubated for 1 hr before LPS-stimulation measured after 16 hrs by ELISA	[PMID: 22071304]
BMDC	IC₅₀	5.21 μM Compound: SB203580	Antiinflammatory activity in C57BL/6 mouse BMDCs assessed as inhibition of LPS-stimulated IL-12p40 production treated 1 hr before LPS challenge measured 18 hrs post stimulation by ELISA Antiinflammatory activity in C57BL/6 mouse BMDCs assessed as inhibition of LPS-stimulated IL-12p40 production treated 1 hr before LPS challenge measured 18 hrs post stimulation by ELISA	[PMID: 23484668]
BMDC	IC₅₀	5.67 μM Compound: SB203580	Antiinflammatory activity against in C57BL/6 mouse BMDC assessed as inhibition of LPS-stimulated IL12 production compound pre-incubated for 1 hr before LPS challenge by ELISA Antiinflammatory activity against in C57BL/6 mouse BMDC assessed as inhibition of LPS-stimulated IL12 production compound pre-incubated for 1 hr before LPS challenge by ELISA	[PMID: 23200246]
BMDC	IC₅₀	7.2 μM Compound: SB203580	Anti-inflammatory activity in C57BL/6 mouse BMDC assessed as inhibition of LPS-induced TNFalpha production pretreated for 1 hr followed by LPS-stimulation after 18 hrs by ELISA Anti-inflammatory activity in C57BL/6 mouse BMDC assessed as inhibition of LPS-induced TNFalpha production pretreated for 1 hr followed by LPS-stimulation after 18 hrs by ELISA	[PMID: 28009172]
BMDC	IC₅₀	7.24 μM Compound: SB203580	Antiinflammatory activity in C57BL/6 mouse BMDC assessed as inhibition of LPS-stimulated TNF-alpha production preincubated for 1 hr before LPS-stimulation measured after 16 hrs by ELISA Antiinflammatory activity in C57BL/6 mouse BMDC assessed as inhibition of LPS-stimulated TNF-alpha production preincubated for 1 hr before LPS-stimulation measured after 16 hrs by ELISA	[PMID: 22071304]
BMDC	IC₅₀	7.37 μM Compound: SB203580	Antiinflammatory activity against in C57BL/6 mouse BMDC assessed as inhibition of LPS-stimulated TNFalpha production compound pre-incubated for 1 hr before LPS challenge by ELISA Antiinflammatory activity against in C57BL/6 mouse BMDC assessed as inhibition of LPS-stimulated TNFalpha production compound pre-incubated for 1 hr before LPS challenge by ELISA	[PMID: 23200246]
BMDC	IC₅₀	7.5 μM Compound: SB203580	Antiinflammatory activity in C57BL/6 mouse BMDC cells assessed as inhibition of LPS-induced TNFalpha production preincubated for 1 hr prior to LPS-stimulation measured after 18 hrs by ELISA Antiinflammatory activity in C57BL/6 mouse BMDC cells assessed as inhibition of LPS-induced TNFalpha production preincubated for 1 hr prior to LPS-stimulation measured after 18 hrs by ELISA	[PMID: 24047259]
BMDC	IC₅₀	7.53 μM Compound: SB203580	Antiinflammatory activity in C57BL/6 mouse BMDCs assessed as inhibition of LPS-stimulated TNF-alpha production treated 1 hr before LPS challenge measured 18 hrs post stimulation by ELISA Antiinflammatory activity in C57BL/6 mouse BMDCs assessed as inhibition of LPS-stimulated TNF-alpha production treated 1 hr before LPS challenge measured 18 hrs post stimulation by ELISA	[PMID: 23484668]
HEK293	EC₅₀	0.06 μM Compound: SB 203580	Inhibition of recombinant Nanoluc-tagged p38alpha (unknown origin) expressed in HEK293 cells incubated for 2 to 3 mins by NanoBRET assay Inhibition of recombinant Nanoluc-tagged p38alpha (unknown origin) expressed in HEK293 cells incubated for 2 to 3 mins by NanoBRET assay	[PMID: 31520926]
HeLa	IC₅₀	0.1 μM Compound: SB-203580	Inhibition of Tat-induced HIV1 LTR transactivation in human HeLa cells assessed as CAT expression after 2 days Inhibition of Tat-induced HIV1 LTR transactivation in human HeLa cells assessed as CAT expression after 2 days	[PMID: 18926711]
HL-60	IC₅₀	50.5 μM Compound: SB-203580	Antiinflammatory activity in PMA-stimulated human HL60 cells assessed as inhibition of LPS-induced TNFalpha production preincubated for 30 mins before LPS challenge measured after 24 hrs by ELISA Antiinflammatory activity in PMA-stimulated human HL60 cells assessed as inhibition of LPS-induced TNFalpha production preincubated for 30 mins before LPS challenge measured after 24 hrs by ELISA	[PMID: 22621841]
HL-60	IC₅₀	52.2 μM Compound: SB203580	Antiinflammatory activity in human HL-60 derived macrophage-like cells assessed as inhibition of LPS-induced IL-6 production treated 30 mins before LPS stimulation measured after 24 hrs by ELISA Antiinflammatory activity in human HL-60 derived macrophage-like cells assessed as inhibition of LPS-induced IL-6 production treated 30 mins before LPS stimulation measured after 24 hrs by ELISA	[PMID: 23811089]
HL-60	IC₅₀	52.2 μM Compound: SB-203580	Antiinflammatory activity in PMA-stimulated human HL60 cells assessed as inhibition of LPS-induced IL-6 production preincubated for 30 mins before LPS challenge measured after 24 hrs by ELISA Antiinflammatory activity in PMA-stimulated human HL60 cells assessed as inhibition of LPS-induced IL-6 production preincubated for 30 mins before LPS challenge measured after 24 hrs by ELISA	[PMID: 22621841]
HL-60	IC₅₀	8.6 μM Compound: SB203580	Antiinflammatory activity in human HL-60 derived macrophage-like cells assessed as inhibition of LPS-induced TNFalpha production treated 30 mins before LPS stimulation measured after 24 hrs by ELISA Antiinflammatory activity in human HL-60 derived macrophage-like cells assessed as inhibition of LPS-induced TNFalpha production treated 30 mins before LPS stimulation measured after 24 hrs by ELISA	[PMID: 23811089]
PBMC	IC₅₀	> 10 μM Compound: SB-203580	Antiinflammatory activity in human PBMCs assessed as inhibition of LPS-induced IL6 release incubated for 15 mins prior to LPS challenge measured after 24 hrs by HTRF assay Antiinflammatory activity in human PBMCs assessed as inhibition of LPS-induced IL6 release incubated for 15 mins prior to LPS challenge measured after 24 hrs by HTRF assay	[PMID: 23411072]
PBMC	IC₅₀	0.34 μM Compound: SB-203580	Antiinflammatory activity in human PBMCs assessed as inhibition of LPS-induced IL1-beta release incubated for 15 mins prior to LPS challenge measured after 24 hrs by HTRF assay Antiinflammatory activity in human PBMCs assessed as inhibition of LPS-induced IL1-beta release incubated for 15 mins prior to LPS challenge measured after 24 hrs by HTRF assay	[PMID: 23411072]
PBMC	IC₅₀	1 μM Compound: SB-203580	Antiinflammatory activity in human PBMCs assessed as inhibition of LPS-induced TNFalpha release incubated for 15 mins prior to LPS challenge measured after 24 hrs by HTRF assay Antiinflammatory activity in human PBMCs assessed as inhibition of LPS-induced TNFalpha release incubated for 15 mins prior to LPS challenge measured after 24 hrs by HTRF assay	[PMID: 23411072]
PBMC	IC₅₀	160 nM Compound: 4	Inhibition of staphylococcal enterotoxin B(SEB) stimulated tumor necrosis factor alpha (TNF-alpha) production by human peripheral blood mononuclear cells(PBMCs) Inhibition of staphylococcal enterotoxin B(SEB) stimulated tumor necrosis factor alpha (TNF-alpha) production by human peripheral blood mononuclear cells(PBMCs)	[PMID: 9784093]
PBMC	IC₅₀	25 nM Compound: 4	Inhibition of LPS-stimulated TH+NF-alphs production by human peripheral blood mononuclear cells (PBMCs) Inhibition of LPS-stimulated TH+NF-alphs production by human peripheral blood mononuclear cells (PBMCs)	[PMID: 9784093]
Peritoneal macrophage cell	IC₅₀	0.22 μM Compound: 10, SB-203580	Antiinflammatory activity in BALB/c mouse peritoneal macrophages assessed as inhibition of LPS-induced TNFalpha production treated 1 hr before LPS challenge measured after 24 hrs by ELISA Antiinflammatory activity in BALB/c mouse peritoneal macrophages assessed as inhibition of LPS-induced TNFalpha production treated 1 hr before LPS challenge measured after 24 hrs by ELISA	[PMID: 22647219]
Sf9	IC₅₀	0.035 μM Compound: SB203580	Inhibition of recombinant human full-length N-terminal GST-tagged P38 alpha MAPK expressed in baculovirus infected Sf9 insect cells using p38 peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins in presen Inhibition of recombinant human full-length N-terminal GST-tagged P38 alpha MAPK expressed in baculovirus infected Sf9 insect cells using p38 peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins in presen	[PMID: 31445234]
Sf9	IC₅₀	10 nM Compound: 2, SB-203580	Inhibition of full-length FLAG-6His-TEV tagged human RIP2 expressed in Sf9 cells assessed as reduction in autophosphorylation pre-incubated for 30 mins followed by incubation with ATP for 2 hrs by ADP-Glo assay Inhibition of full-length FLAG-6His-TEV tagged human RIP2 expressed in Sf9 cells assessed as reduction in autophosphorylation pre-incubated for 30 mins followed by incubation with ATP for 2 hrs by ADP-Glo assay	[PMID: 26455654]
Sf9	IC₅₀	200 nM Compound: 2, SB-203580	Inhibition of full-length FLAG-6His-TEV tagged human RIP2 expressed in Sf9 cells by fluorescent polarization assay Inhibition of full-length FLAG-6His-TEV tagged human RIP2 expressed in Sf9 cells by fluorescent polarization assay	[PMID: 26455654]
SW1353	IC₅₀	50 nM Compound: 1	Inhibition of IL-6 production by SW1353 cells treated with both cytokines IL-1 and TNF-alpha. Inhibition of IL-6 production by SW1353 cells treated with both cytokines IL-1 and TNF-alpha.	[PMID: 11140741]
THP-1	IC₅₀	0.07 μM Compound: SB-203580	Inhibition of tumor necrosis factor alpha release by THP-1 cells Inhibition of tumor necrosis factor alpha release by THP-1 cells	[PMID: 15658855]
THP-1	IC₅₀	20 nM Compound: SB 203580	Inhibition of LPS-induced TNFalpha production in human THP1 cells incubated for 1 hr followed by LPS stimulation and measured after 4 hrs by TR-FRET method Inhibition of LPS-induced TNFalpha production in human THP1 cells incubated for 1 hr followed by LPS stimulation and measured after 4 hrs by TR-FRET method	[PMID: 31520926]
THP-1	IC₅₀	72 nM Compound: SB-203580	Inhibitory activity against TNF-alpha production using lipopolysaccharide stimulated human monocytic cells Inhibitory activity against TNF-alpha production using lipopolysaccharide stimulated human monocytic cells	[PMID: 12729637]

体外研究
(In Vitro)

Adezmapimod (SB 203580) (用 0-30 μM 预孵育 1 小时并在 20 ng/mL IL-2 存在下培养 24 小时) 防止 IL-2 诱导的原代人 T 细胞、鼠 CT6 T 细胞增殖或 BAF F7 B 细胞，IC₅₀ 为 3-5 μM^[1]。
SB203580 阻断 PKB 磷酸化 (IC₅₀ 3-5 微米)。SB203580 在 CT6 和活化的人 T 细胞以及 IL-2 反应性 BA/F3 F7 B 细胞中以剂量依赖性方式抑制 Ser473 的磷酸化^[1]。

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

Cell Proliferation Assay^[1]

Cell Line:	CT6, BA/F3 cell line F7, and PBMC/T cells
Concentration:	0-30 μM
Incubation Time:	Preincubated with 0-30 μM SB203580 for 1 h and cultured for 24 h in the presence of 20 ng/mL IL-2
Result:	Prevented the IL-2-induced proliferation of primary human T cells, murine CT6 T cells, or BAF F7 B cells with an IC₅₀ of 3-5 μM.

Western Blot Analysis^[1]

Cell Line:	CT6 cells, activated human T cells, and BA/F3 F7 cells
Concentration:	0-30 μM
Incubation Time:	Preincubated with 0-30 μM SB203580 for 1 h before stimulating with 20 ng/mL IL-2 for 5 min
Result:	Inhibited the phosphorylation of PKB at Ser473 in a dose-dependent manner.

体内研究
(In Vivo)

Adezmapimod (SB 203580) (5 mg/kg/天；每天腹膜内注射，连续 16 天，在雌性无染色体 Nu/Nu 小鼠中) 处理，与平行处理的 p38TM 肿瘤相比，p38WT 肿瘤的肿瘤负荷明显更小^[1]。

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

Animal Model:	Six-week-old female atymic Nu/Nu mice CAL27 p38WT and p38TM tumors^[1]
Dosage:	5 mg/kg/day
Administration:	Intra peritoneal injected daily for 16 consecutive days
Result:	After 2 weeks treatment, CAL27 p38WT tumors were significantly smaller; CAL27 p38TM tumors were not affected by the p38 inhibitor (n=10).

分子量

377.43

Formula

C₂₁H₁₆FN₃OS

CAS 号

152121-47-6

性状

固体

颜色

White to light yellow

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 : 20 mg/mL (52.99 mM; 超声助溶 (<60°C); 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	2.6495 mL	13.2475 mL	26.4950 mL
5 mM	0.5299 mL	2.6495 mL	5.2990 mL
10 mM	0.2649 mL	1.3247 mL	2.6495 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： 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.5 mg/mL (6.62 mM); 澄清溶液
方案二

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2 mg/mL (5.30 mM); 澄清溶液; 超声助溶

此方案可获得 2 mg/mL的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.0 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。
方案三

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2 mg/mL (5.30 mM); 澄清溶液; 超声助溶

此方案可获得 2 mg/mL的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案四

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: 2 mg/mL (5.30 mM); 澄清溶液; 超声助溶

此方案可获得 2 mg/mL的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
方案五

请依序添加每种溶剂： 2% DMSO 40% PEG300 5% Tween-80 53% Saline
Solubility: ≥ 1 mg/mL (2.65 mM); 澄清溶液
方案六

请依序添加每种溶剂： 2% DMSO 98% (20% SBE-β-CD in Saline)
Solubility: ≥ 1 mg/mL (2.65 mM); 澄清溶液

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： 50% PEG300 50% Saline
Solubility: 10 mg/mL (26.49 mM); 悬浊液; 超声助溶
方案二

请依序添加每种溶剂： 0.5% CMC-Na/saline water
Solubility: 16.67 mg/mL (44.17 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: 99.96%

选择批次：

Data Sheet (647 KB) SDS (393 KB)

COA (290 KB) LCMS (255 KB) 元素分析报告 (214 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Davies SP, et al. Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105. [Content Brief]

[2]. Lali FV, et al. The pyridinyl imidazole inhibitor SB203580 blocks phosphoinositide-dependent protein kinase activity, protein kinase B phosphorylation, and retinoblastoma hyperphosphorylation in interleukin-2-stimulated T cells independently of p38 mitogen-activated protein kinase. J Biol Chem. 2000 Mar 10;275(10):7395-402. [Content Brief]

[3]. Leelahavanichkul K, et al. A role for p38 MAPK in head and neck cancer cell growth and tumor-induced angiogenesis and lymphangiogenesis. Mol Oncol. 2014 Feb;8(1):105-18. [Content Brief]

Adezmapimod 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	2.6495 mL	13.2475 mL	26.4950 mL	66.2374 mL
	5 mM	0.5299 mL	2.6495 mL	5.2990 mL	13.2475 mL
	10 mM	0.2649 mL	1.3247 mL	2.6495 mL	6.6237 mL
	15 mM	0.1766 mL	0.8832 mL	1.7663 mL	4.4158 mL
	20 mM	0.1325 mL	0.6624 mL	1.3247 mL	3.3119 mL
	25 mM	0.1060 mL	0.5299 mL	1.0598 mL	2.6495 mL
	30 mM	0.0883 mL	0.4416 mL	0.8832 mL	2.2079 mL
	40 mM	0.0662 mL	0.3312 mL	0.6624 mL	1.6559 mL
	50 mM	0.0530 mL	0.2649 mL	0.5299 mL	1.3247 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.

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Adezmapimod (Synonyms: SB 203580; RWJ 64809)

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MCE 顾客使用本产品发表的 459 篇科研文献

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完整储备液配制表

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Adezmapimod (Synonyms: SB 203580; RWJ 64809)

Customer Review

Other Forms of Adezmapimod:

Adezmapimod 相关抗体

MCE 顾客使用本产品发表的 459 篇科研文献

Adezmapimod 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 p38 MAPK 亚型特异性产品:

生物活性

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参考文献

Adezmapimod 相关抗体:

摩尔计算器

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