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Merck

SML2001

Sigma-Aldrich

GSK′843

≥98% (HPLC)

别名:

3-(5-Benzothiazolyl)-7-(1,3-dimethyl-1H-pyrazol-5-yl)-thieno[3,2-c]pyridin-4-amine, GSK 843, GSK-843, GSK843

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About This Item

经验公式(希尔记法):
C19H15N5S2
分子量:
377.49
MDL號碼:
分類程式碼代碼:
12352200
NACRES:
NA.77

化驗

≥98% (HPLC)

形狀

powder

顏色

white to beige

溶解度

DMSO: 2 mg/mL, clear

儲存溫度

2-8°C

生化/生理作用

GSK′843 is a potent ATP-competitive RIP3 (RIPK3) kinase inhibitor (IC50 = 6.5 nM) with much reduced or little affinity toward 262 other kinases (IC50 >1 μM against 10 μM ATP in competitive binding assay), including RIP5. GSK′843 effectively suppresses TNF/Z-VAD-FMK/IAP agonist treatment-induced necrosis induction in both human and murine cell cultures (EC50 ranges from <0.12 to 3 μM), while inducing apoptosis in the absence of caspase inhibitor as a result of caspase 8 activation via RHIM-driven recruitment to assemble a Casp8-FADD-cFLIP complex independent of pronecrotic kinase activities and MLKL.

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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分析证书(COA)

Lot/Batch Number

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Pratyusha Mandal et al.
Molecular cell, 56(4), 481-495 (2014-12-03)
Receptor-interacting protein kinase 3 (RIP3 or RIPK3) has emerged as a central player in necroptosis and a potential target to control inflammatory disease. Here, three selective small-molecule compounds are shown to inhibit RIP3 kinase-dependent necroptosis, although their therapeutic value is

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