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GW806742X

Cat. No. M8758
GW806742X Structure
Size Price Availability Quantity
5mg USD 48  USD48 In stock
10mg USD 78  USD78 In stock
25mg USD 145  USD145 In stock
50mg USD 230  USD230 In stock
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Quality Control & Documentation
Biological Activity

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%).

Chemical Information
Molecular Weight 573.55
Formula C25H22F3N7O4S
CAS Number 579515-63-2
Solubility (25°C) DMSO: ≥ 30 mg/mL
Storage 4°C, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Hildebrand JM, et al. Proc Natl Acad Sci U S A. Activation of the pseudokinase MLKL unleashes the four-helix bundle domain to induce membrane localization and necroptotic cell death.

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TC13172 

TC13172 is an inhibitor of MLKL and necroptosis that acts on HT-29 cells with an EC50 value of 2 nM.

GW806742X hydrochloride

GW806742X hydrochloride is an ATP mimetic and potent inhibitor of MLKL and necroptosis, slowing down MLKL membrane translocation and binding to the MLKL pseudokinase domain with a Kd value of 9.3 μM. GW806742X hydrochloride has anti-VEGFR2 activity (IC50=2 nM). GW806742X hydrochloride has anti-VEGFR2 activity (IC50=2 nM).

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.

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.

  Catalog
Abmole Inhibitor Catalog




Keywords: GW806742X supplier, Necroptosis, inhibitors, activators


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