SML2001
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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关于此项目
经验公式（希尔记法）:
C19H15N5S2
化学文摘社编号:
分子量:
377.49
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
产品名称
GSK′843, ≥98% (HPLC)
SMILES string
[s]1c2c(nc1)cc(cc2)c3c4c([s]c3)c(cnc4N)c5[n](nc(c5)C)C
InChI key
BPKSNNJTKPIZKR-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Biochem/physiol Actions
A potent ATP-competitive RIP3 (RIPK3) kinase inhibitor that suppresses necrosis induction in both human and murine cell cultures.
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.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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
William J Kaiser et al.
The Journal of biological chemistry, 288(43), 31268-31279 (2013-09-11)
Toll-like receptor (TLR) signaling is triggered by pathogen-associated molecular patterns that mediate well established cytokine-driven pathways, activating NF-κB together with IRF3/IRF7. In addition, TLR3 drives caspase 8-regulated programmed cell death pathways reminiscent of TNF family death receptor signaling. We find
N Preyat et al.
Cell death and differentiation, 23(1), 29-40 (2015-05-23)
Cellular necrosis has long been regarded as an incidental and uncontrolled form of cell death. However, a regulated form of cell death termed necroptosis has been identified recently. Necroptosis can be induced by extracellular cytokines, pathogens and several pharmacological compounds
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