Product overview

Name GSK'872
Alternative names GSK2399872A
Purity >98%
Description

Potent, selective RIP3 inhibitor. Necroptosis inhibitor.

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Biological Data

Biological description

Potent and selective RIP3 inhibitor. Binds to the RIP3 kinase domain (IC50 = 1.3 nM) and inhibits kinase activity with an IC50 of 1.3 nM. Demonstrates >1000-fold selectivity for RIP3 compared with >300 different kinases. Inhibits necroptosis, TLR3-, TNF-α- and virus-induced necrosis. Also induces caspase8-mediated apoptosis in a concentration-dependent manner (at higher concentration such as 3-10 µM).

Solubility & Handling

Storage instructions -20°C
Solubility overview Soluble in DMSO (100 mM), and in ethanol (100 mM)
Important This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use

Calculators

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Dilution

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Chemical Data

Purity >98%
Chemical name N-5-Benzothiazolyl-6-[(1-methylethyl)sulfonyl]-4-quinolinamine
Molecular Weight 383.5
Chemical structure  Chemical Structure
Molecular Formula C19H17N3O2S2
CAS Number 1346546-69-7
PubChem identifier 54674134
SMILES CC(C)S(=O)(=O)C1=CC2=C(C=CN=C2C=C1)NC3=CC4=C(C=C3)SC=N4
InChi InChI=1S/C19H17N3O2S2/c1-12(2)26(23,24)14-4-5-16-15(10-14)17(7-8-20-16)22-13-3-6-19-18(9-13)21-11-25-19/h3-12H,1-2H3,(H,20,22)
InChiKey ZCDBTQNFAPKACC-UHFFFAOYSA-N
MDL number MFCD30481302
Appearance Yellow solid

References for GSK'872

References are publications that support the biological activity of the product
  • RIP3 induces apoptosis independent of pronecrotic kinase activity.

    Mandal P et al (2014) Molecular cell 56 : 481-95
  • Toll-like receptor 3-mediated necrosis via TRIF, RIP3, and MLKL.

    Kaiser WJ et al (2013) The Journal of biological chemistry 288 : 31268-79
  • Mixed lineage kinase domain-like protein mediates necrosis signaling downstream of RIP3 kinase.

    Sun L et al (2012) Cell 148 : 213-27

3 Item(s)