GW-806742X
| Code | Size | Price |
|---|
| SYN-1215-M100 | 100 mg | Enquire |
Quantity:
| SYN-1215-M001 | 1 mg | £115.00 |
Quantity:
| SYN-1215-M005 | 5 mg | £233.00 |
Quantity:
| SYN-1215-M010 | 10 mg | £385.00 |
Quantity:
| SYN-1215-M050 | 50 mg | £1,006.00 |
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
Ambient
Storage:
+4°C
Documents
Further Information
Alternate Names/Synonyms:
AC1NS7PT; AGN-PC-0LQ49Y
Appearance:
Solid.
CAS:
579515-63-2
EClass:
32160000
Form (Short):
liquid
InChi:
InChI=1S/C25H22F3N7O4S/c1-35(22-13-14-30-23(34-22)31-18-3-2-4-21(15-18)40(29,37)38)19-9-5-16(6-10-19)32-24(36)33-17-7-11-20(12-8-17)39-25(26,27)28/h2-15H,1H3,(H2,29,37,38)(H,30,31,34)(H2,32,33,36)
InChiKey:
SNRUTMWCDZHKKM-UHFFFAOYSA-N
Long Description:
Chemical. CAS: 579515-63-2. Formula: C25H22F3N7O4S. MW: 573.6. Potent protein kinase VEGFR2 inhibitor (2nm range). Binds to the pseudokinase domain of MLKL and blocks cell death by necroptosis, as well. With regards to its role in necroptosis, it is an ATP-mimetic that was shown to bind recombinant mouse MLKL pseudokinase domain, which showed inhibited TSQ-induced death of mouse dermal fibroblasts by delaying MLKL translocation to the membrane. Appears therefore to be a valuable reagent to inhibit necroptosis. It also provides an important proof-of-principle that targeting catalytically-dead pseudoenzymes represents a feasible, emerging therapeutic avenue.
Molecular Formula:
C25H22F3N7O4S
Molecular Weight:
573.6
Package Type:
Plastic Vial
Product Description:
Potent protein kinase VEGFR2 inhibitor (2nm range). Binds to the pseudokinase domain of MLKL and blocks cell death by necroptosis, as well. With regards to its role in necroptosis, it is an ATP-mimetic that was shown to bind recombinant mouse MLKL pseudokinase domain, which showed inhibited TSQ-induced death of mouse dermal fibroblasts by delaying MLKL translocation to the membrane. Appears therefore to be a valuable reagent to inhibit necroptosis. It also provides an important proof-of-principle that targeting catalytically-dead pseudoenzymes represents a feasible, emerging therapeutic avenue.
Purity:
>95%
Solubility Chemicals:
Soluble in DMSO.
Transportation:
Non-hazardous
UNSPSC Category:
Protein Kinase Modulators
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 2 years after receipt when stored at -20°C.
References
Discovery of a novel and potent series of dianilinopyrimidineurea and urea isostere inhibitors of VEGFR2 tyrosine kinase: D.M. Sammond, et al.; Bioorg. Med. Chem Lett. 15, 3519 (2005) | Activation of the pseudokinase MLKL unleashes the four-helix bundle domain to induce membrane localization and necroptotic cell death: J.M. Hildebrand, et al.; PNAS 111, 15072 (2014) | Identification and structure-function analysis of subfamily selective G protein-coupled receptor kinase inhibitors: K.T. Homan, et al.; ACS Chem. Biol. 10, 310 (2015) | Neutrophil necroptosis is triggered by ligation of adhesion molecules following GM-CSF priming: X. Wang, et al.; J. Immunol. 197, 4090 (2016)