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GW806742X is an ATP site-targeing kinase inhibitor (IC50 in nM = 2/VEGFR2, 15/SRC, 47/C-FMS, 851/GSK3, 9016/ERBB2, 9120/FGFR) with potent antiproliferation activity against cancer cultures (IC50 in nM = 5/HUVEC-v, 424/HUVEC-b, 81/HEF, 453/MDA468, 470/A375P, 693/HT29, 734/PC3), GW806742X is now better known as Compound 1 for its anti-necroptosis activity via affinity interaction with MLKL pseudokinase domain (Kd = 9.3 μM), thereby preventing the 4HB domain from exerting its necroptototic effect following RIPK3-mediated pseudokinase domain phosphorylation. GW806742X inhibits TSQ (1 ng/mL TNF, 500 nM Smac-mimetic, 10 μM Q-VD-Oph) treatment-induced necroptosis of mouse dermal fibroblasts (IC50 <50 nM) with >50-fold greater potency than Nec-1, while reduced efficiency is only observed in the presence of supraphysiological TNF concentrations of 100 ng/mL (IC50 = 100-500 nM; Max efficacy ~50%).
| Molecular Weight | 573.55 |
| Formula | C25H22F3N7O4S |
| CAS Number | 579515-63-2 |
| Solubility (25°C) | DMSO: ≥ 30 mg/mL |
| Storage | 4°C, dry, sealed |
| Related Necroptosis Products |
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| Necrosulfonamide
Necrosulfonamide is a necroptosis inhibitor which selectively targeting the mixed lineage kinase domain-like protein (MLKL) with IC50 value of 124 nM in human HT-29. Necrosulfonamide prevents MLKL-RIP1-RIP3 necrosome complex from interacting with its downstream effectors. |
| GSK2982772
GSK2982772 is a potent, selective receptor interacting protein kinase 1 (RIPK1) inhibitor with IC50 values of 16 nM and 20 nM against human and monkey RIP1, respectively. |
| GSK547
GSK547 is a potent and highly selective inhibitor of receptor-interacting protein kinase 1 (RIPK1) and also inhibits necroptosis. |
| PK68
PK68 is a potent and selective type II RIPK1 inhibitor with an IC50 value of approximately 90 nM that inhibits RIPK1-dependent necroptosis. It can be used in studies related to inflammatory diseases and cancer metastasis. |
| GSK-843
GSK-843 is a potent receptor-interacting protein kinase 3 (RIP3 or RIPK3) inhibitor, which binds RIP3 kinase domain with an IC50 of 8.6 nM, and inhibits kinase activity with an IC50 of 6.5 nM. |
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