GPP78 (Synonyms: CAY10618)

目录号: HY-14374 纯度: ≥99.0%: FAQs
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GPP78 (CAY10618) 是一种有效的烟酰胺磷酸核糖转移酶 (Nampt) 抑制剂，对 NAD 消耗的 IC₅₀ 为 3 nM。GPP78 通过诱导自噬对神经母细胞瘤细胞 SH-SY5Y 具有毒性，IC₅₀ 为 3.8 nM。GPP78 具有抗癌和抗炎作用。

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GPP78 Chemical Structure

CAS No. : 1202580-59-3

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规格	价格	是否有货	数量
1 mg (11.38 mM * 200 μL in Methanol)	￥1150	In-stock
5 mg (11.38 mM * 1 mL in Methanol)	￥3500	In-stock

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MCE 顾客使用本产品发表的 1 篇科研文献

•Sci Signal. 2021 Jun 8;14(686):eabc7405. [Abstract]

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生物活性
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参考文献

生物活性

GPP78 (CAY10618) is a potent Nampt inhibitor with an IC₅₀ of 3.0 nM for nicotinamide adenine dinucleotide (NAD) depletion. GPP78 is cytotoxic to neuroblastoma cell line SH-SY5Y cells with an IC₅₀ of 3.8 nM by inducing autophagy. GPP78 has anti-cancer and anti-inflammatory effects^[1]^[2].

IC₅₀ & Target

Nampt^[1];
Autophagy^[1]

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
786-0	GI₅₀	7.33 μM Compound: 8	Growth inhibition of human 786-0 cells by sulforhodamine B assay Growth inhibition of human 786-0 cells by sulforhodamine B assay	[PMID: 19961183]
A498	GI₅₀	1.59 x 10^-5 M Compound: 8	Growth inhibition of human A498 cells by sulforhodamine B assay Growth inhibition of human A498 cells by sulforhodamine B assay	[PMID: 19961183]
A549	GI₅₀	2.1 μM Compound: 8	Growth inhibition of human A549 cells by sulforhodamine B assay Growth inhibition of human A549 cells by sulforhodamine B assay	[PMID: 19961183]
ACHN	GI₅₀	1.87 x 10^-5 M Compound: 8	Growth inhibition of human ACHN cells by sulforhodamine B assay Growth inhibition of human ACHN cells by sulforhodamine B assay	[PMID: 19961183]
BT-549	GI₅₀	1.7 μM Compound: 8	Growth inhibition of human BT549 cells by sulforhodamine B assay Growth inhibition of human BT549 cells by sulforhodamine B assay	[PMID: 19961183]
CAKI-1	GI₅₀	7.76 x 10^-1 μM Compound: 8	Growth inhibition of human Caki1 cells by sulforhodamine B assay Growth inhibition of human Caki1 cells by sulforhodamine B assay	[PMID: 19961183]
CCRF-CEM	GI₅₀	3.28 μM Compound: 8	Growth inhibition of human CCRF-CEM cells by sulforhodamine B assay Growth inhibition of human CCRF-CEM cells by sulforhodamine B assay	[PMID: 19961183]
COLO 205	GI₅₀	1.18 μM Compound: 8	Growth inhibition of human COLO205 cells by sulforhodamine B assay Growth inhibition of human COLO205 cells by sulforhodamine B assay	[PMID: 19961183]
DU-145	GI₅₀	7.02 x 10^-1 μM Compound: 8	Growth inhibition of human DU145 cells by sulforhodamine B assay Growth inhibition of human DU145 cells by sulforhodamine B assay	[PMID: 19961183]
EKVX	GI₅₀	8.46 μM Compound: 8	Growth inhibition of human EKVX cells by sulforhodamine B assay Growth inhibition of human EKVX cells by sulforhodamine B assay	[PMID: 19961183]
HCC 2998	GI₅₀	7 x 10^-1 μM Compound: 8	Growth inhibition of human HCC2998 cells by sulforhodamine B assay Growth inhibition of human HCC2998 cells by sulforhodamine B assay	[PMID: 19961183]
HCT-116	GI₅₀	4.03 x 10^-2 μM Compound: 8	Growth inhibition of human HCT116 cells by sulforhodamine B assay Growth inhibition of human HCT116 cells by sulforhodamine B assay	[PMID: 19961183]
HCT-15	GI₅₀	2.57 x 10^-1 μM Compound: 8	Growth inhibition of human HCT15 cells by sulforhodamine B assay Growth inhibition of human HCT15 cells by sulforhodamine B assay	[PMID: 19961183]
HOP-62	GI₅₀	2.38 x 10^-5 M Compound: 8	Growth inhibition of human HOP62 cells by sulforhodamine B assay Growth inhibition of human HOP62 cells by sulforhodamine B assay	[PMID: 19961183]
HOP-92	GI₅₀	9.74 x 10^-5 M Compound: 8	Growth inhibition of human HOP92 cells by sulforhodamine B assay Growth inhibition of human HOP92 cells by sulforhodamine B assay	[PMID: 19961183]
Hs-578T	GI₅₀	2.04 x 10^-5 M Compound: 8	Growth inhibition of human Hs 578T cells by sulforhodamine B assay Growth inhibition of human Hs 578T cells by sulforhodamine B assay	[PMID: 19961183]
HT-29	GI₅₀	4.6 x 10^-1 μM Compound: 8	Growth inhibition of human HT-29 cells by sulforhodamine B assay Growth inhibition of human HT-29 cells by sulforhodamine B assay	[PMID: 19961183]
IGROV-1	GI₅₀	2.72 x 10^-1 μM Compound: 8	Growth inhibition of human IGROV1 cells by sulforhodamine B assay Growth inhibition of human IGROV1 cells by sulforhodamine B assay	[PMID: 19961183]
KM12	GI₅₀	1.03 μM Compound: 8	Growth inhibition of human KM12 cells by sulforhodamine B assay Growth inhibition of human KM12 cells by sulforhodamine B assay	[PMID: 19961183]
LOX IMVI	GI₅₀	1.01 x 10^-5 M Compound: 8	Growth inhibition of human LOXIMVI cells by sulforhodamine B assay Growth inhibition of human LOXIMVI cells by sulforhodamine B assay	[PMID: 19961183]
M14	GI₅₀	1.66 x 10^-1 μM Compound: 8	Growth inhibition of human M14 cells by sulforhodamine B assay Growth inhibition of human M14 cells by sulforhodamine B assay	[PMID: 19961183]
Malme-3M	GI₅₀	1.22 x 10^-5 M Compound: 8	Growth inhibition of human MALME-3M cells by sulforhodamine B assay Growth inhibition of human MALME-3M cells by sulforhodamine B assay	[PMID: 19961183]
MCF7	GI₅₀	3.42 μM Compound: 8	Growth inhibition of human MCF7 cells by sulforhodamine B assay Growth inhibition of human MCF7 cells by sulforhodamine B assay	[PMID: 19961183]
MDA-MB-231	GI₅₀	2.09 x 10^-5 M Compound: 8	Growth inhibition of human MDA-MB-231 cells by sulforhodamine B assay Growth inhibition of human MDA-MB-231 cells by sulforhodamine B assay	[PMID: 19961183]
MDA-MB-435	GI₅₀	3.99 x 10^-1 μM Compound: 8	Growth inhibition of human MDA-MB-435 cells by sulforhodamine B assay Growth inhibition of human MDA-MB-435 cells by sulforhodamine B assay	[PMID: 19961183]
MDA-MB-468	GI₅₀	7.34 μM Compound: 8	Growth inhibition of human MDA-MB-468 cells by sulforhodamine B assay Growth inhibition of human MDA-MB-468 cells by sulforhodamine B assay	[PMID: 19961183]
NCI/ADR-RES	GI₅₀	8.14 x 10^-2 μM Compound: 8	Growth inhibition of human NCI/ADR-RES cells by sulforhodamine B assay Growth inhibition of human NCI/ADR-RES cells by sulforhodamine B assay	[PMID: 19961183]
NCI-H226	GI₅₀	1.55 x 10^-5 M Compound: 8	Growth inhibition of human NCI-H226 cells by sulforhodamine B assay Growth inhibition of human NCI-H226 cells by sulforhodamine B assay	[PMID: 19961183]
NCI-H23	GI₅₀	1.51 x 10^-5 M Compound: 8	Growth inhibition of human NCI-H23 cells by sulforhodamine B assay Growth inhibition of human NCI-H23 cells by sulforhodamine B assay	[PMID: 19961183]
NCI-H322M	GI₅₀	2.31 x 10^-5 M Compound: 8	Growth inhibition of human NCI-H322M cells by sulforhodamine B assay Growth inhibition of human NCI-H322M cells by sulforhodamine B assay	[PMID: 19961183]
NCI-H460	GI₅₀	7.24 x 10^-1 μM Compound: 8	Growth inhibition of human NCI-H460 cells by sulforhodamine B assay Growth inhibition of human NCI-H460 cells by sulforhodamine B assay	[PMID: 19961183]
NCI-H522	GI₅₀	9.14 x 10^-2 μM Compound: 8	Growth inhibition of human NCI-H522 cells by sulforhodamine B assay Growth inhibition of human NCI-H522 cells by sulforhodamine B assay	[PMID: 19961183]
OVCAR-3	GI₅₀	5.19 μM Compound: 8	Growth inhibition of human OVCAR-3 cells by sulforhodamine B assay Growth inhibition of human OVCAR-3 cells by sulforhodamine B assay	[PMID: 19961183]
OVCAR-4	GI₅₀	3.16 x 10^-5 M Compound: 8	Growth inhibition of human OVCAR4 cells by sulforhodamine B assay Growth inhibition of human OVCAR4 cells by sulforhodamine B assay	[PMID: 19961183]
OVCAR-5	GI₅₀	2.68 x 10^-1 μM Compound: 8	Growth inhibition of human OVCAR5 cells by sulforhodamine B assay Growth inhibition of human OVCAR5 cells by sulforhodamine B assay	[PMID: 19961183]
OVCAR-8	GI₅₀	5.74 x 10^-2 μM Compound: 8	Growth inhibition of human OVCAR8 cells by sulforhodamine B assay Growth inhibition of human OVCAR8 cells by sulforhodamine B assay	[PMID: 19961183]
PC-3	GI₅₀	4.67 x 10^-1 μM Compound: 8	Growth inhibition of human PC3 cells by sulforhodamine B assay Growth inhibition of human PC3 cells by sulforhodamine B assay	[PMID: 19961183]
RXF 393	GI₅₀	1 x 10^-4 M Compound: 8	Growth inhibition of human RXF393 cells by sulforhodamine B assay Growth inhibition of human RXF393 cells by sulforhodamine B assay	[PMID: 19961183]
SF-268	GI₅₀	2.47 x 10^-5 M Compound: 8	Growth inhibition of human SF268 cells by sulforhodamine B assay Growth inhibition of human SF268 cells by sulforhodamine B assay	[PMID: 19961183]
SF-295	GI₅₀	6.55 x 10^-1 μM Compound: 8	Growth inhibition of human SF295 cells by sulforhodamine B assay Growth inhibition of human SF295 cells by sulforhodamine B assay	[PMID: 19961183]
SF-539	GI₅₀	6.18 x 10^-2 μM Compound: 8	Growth inhibition of human SF539 cells by sulforhodamine B assay Growth inhibition of human SF539 cells by sulforhodamine B assay	[PMID: 19961183]
SH-SY5Y	IC₅₀	3.8 nM Compound: 8	Cytotoxicity against human SH-SY5Y cells assessed as cell viability after 48 hrs by MTT assay Cytotoxicity against human SH-SY5Y cells assessed as cell viability after 48 hrs by MTT assay	[PMID: 19961183]
SK-MEL-2	GI₅₀	1.28 x 10^-5 M Compound: 8	Growth inhibition of human SK-MEL-2 cells by sulforhodamine B assay Growth inhibition of human SK-MEL-2 cells by sulforhodamine B assay	[PMID: 19961183]
SK-MEL-28	GI₅₀	1.59 μM Compound: 8	Growth inhibition of human SK-MEL-28 cells by sulforhodamine B assay Growth inhibition of human SK-MEL-28 cells by sulforhodamine B assay	[PMID: 19961183]
SK-MEL-5	GI₅₀	2.64 x 10^-5 M Compound: 8	Growth inhibition of human SK-MEL-5 cells by sulforhodamine B assay Growth inhibition of human SK-MEL-5 cells by sulforhodamine B assay	[PMID: 19961183]
SK-OV-3	GI₅₀	2.05 x 10^-5 M Compound: 8	Growth inhibition of human SKOV3 cells by sulforhodamine B assay Growth inhibition of human SKOV3 cells by sulforhodamine B assay	[PMID: 19961183]
SN12C	GI₅₀	4.26 x 10^-2 μM Compound: 8	Growth inhibition of human SN12C cells by sulforhodamine B assay Growth inhibition of human SN12C cells by sulforhodamine B assay	[PMID: 19961183]
SNB-19	GI₅₀	4.5 x 10^-1 μM Compound: 8	Growth inhibition of human SNB19 cells by sulforhodamine B assay Growth inhibition of human SNB19 cells by sulforhodamine B assay	[PMID: 19961183]
SNB-75	GI₅₀	2.98 x 10^-5 M Compound: 8	Growth inhibition of human SNB75 cells by sulforhodamine B assay Growth inhibition of human SNB75 cells by sulforhodamine B assay	[PMID: 19961183]
SW-620	GI₅₀	6.15 x 10^-2 μM Compound: 8	Growth inhibition of human SW620 cells by sulforhodamine B assay Growth inhibition of human SW620 cells by sulforhodamine B assay	[PMID: 19961183]
T47D	GI₅₀	1.23 μM Compound: 8	Growth inhibition of human T47D cells by sulforhodamine B assay Growth inhibition of human T47D cells by sulforhodamine B assay	[PMID: 19961183]
TK-10	GI₅₀	1.82 x 10^-5 M Compound: 8	Growth inhibition of human TK10 cells by sulforhodamine B assay Growth inhibition of human TK10 cells by sulforhodamine B assay	[PMID: 19961183]
U-251	GI₅₀	5.21 x 10^-1 μM Compound: 8	Growth inhibition of human U251 cells by sulforhodamine B assay Growth inhibition of human U251 cells by sulforhodamine B assay	[PMID: 19961183]
UACC-257	GI₅₀	1.33 x 10^-5 M Compound: 8	Growth inhibition of human UACC257 cells by sulforhodamine B assay Growth inhibition of human UACC257 cells by sulforhodamine B assay	[PMID: 19961183]
UACC-62	GI₅₀	1.33 x 10^-5 M Compound: 8	Growth inhibition of human UACC62 cells by sulforhodamine B assay Growth inhibition of human UACC62 cells by sulforhodamine B assay	[PMID: 19961183]
UO-31	GI₅₀	1.69 x 10^-5 M Compound: 8	Growth inhibition of human UO31 cells by sulforhodamine B assay Growth inhibition of human UO31 cells by sulforhodamine B assay	[PMID: 19961183]

体外研究
(In Vitro)

GPP78 (Compound 8; 10 nM; 24-40 hours; SH-SY5Y cells) treatment with cells, punctate staining of LC3-II and the formation of autophagolysosomes are observable. LC3-II is membrane-bound and is present in autophagosomes^[1].
GPP78 (Compound 8) inhibits the growth of most cell lines tested, with nanomolar potency (GI₅₀) in cell lines derived from leukemia, lung, CNS, colon, melanoma, ovarian, renal, and prostate cancers. GPP78 appears truly cytotoxic in melanoma cell lines, while in the others it is mainly cytostatic^[1].

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

Western Blot Analysis^[1]

Cell Line:	SH-SY5Y cells
Concentration:	10 nM
Incubation Time:	24 hours, 40 hours
Result:	Punctate staining of LC3-II and the formation of autophagolysosomes were observable.

体内研究
(In Vivo)

GPP78 (10 mg/kg; intraperitoneal injection; daily; 1 hour or 6 hours after SCI; for 19 days; male adult CD1 mice) treatment reduces the severity of spinal cord trauma in SCI mice^[2].

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

Animal Model:	Male adult CD1 mice (25-30 g) with spinal cord injury (SCI)^[2]
Dosage:	10 mg/kg
Administration:	Intraperitoneal injection; daily; 1 hour or 6 hours after SCI; for 19 days
Result:	Significantly reduced the demyelination associated with SCI. And significantly ameliorated the functional deficits induced by SCI.

分子量

439.55

Formula

C₂₇H₂₉N₅O

CAS 号

1202580-59-3

性状

液体

颜色

Colorless to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Solution, -20°C, 2 years

纯度 & 产品资料

纯度: ≥99.0%

选择批次：

Data Sheet (533 KB) SDS (419 KB)

COA (259 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Colombano G, et al. A novel potent nicotinamide phosphoribosyltransferase inhibitor synthesized via click chemistry. J Med Chem. 2010 Jan 28;53(2):616-23. [Content Brief]

[2]. Esposito E, et al. The NAMPT inhibitor FK866 reverts the damage in spinal cord injury. J Neuroinflammation. 2012 Apr 10;9:66. [Content Brief]

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The dilution calculator equation

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

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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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GPP78 (Synonyms: CAY10618)

Customer Review

MCE 顾客使用本产品发表的 1 篇科研文献

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