| Identification | Back Directory | [Name]
3-(1,3-benzothiazol-5-yl)-7-(1,3-dimethyl-1H-pyrazol-5-yl)thieno[3,2-c]pyridin-4-amine | [CAS]
1601496-05-2 | [Synonyms]
GSK-843
Thieno[3,2-c]pyridin-4-amine, 3-(5-benzothiazolyl)-7-(1,3-dimethyl-1H-pyrazol-5-yl)-
3-(1,3-benzothiazol-5-yl)-7-(1,3-dimethyl-1H-pyrazol-5-yl)thieno[3,2-c]pyridin-4-amine | [Molecular Formula]
C19H15N5S2 | [MOL File]
1601496-05-2.mol | [Molecular Weight]
377.49 |
| Chemical Properties | Back Directory | [Boiling point ]
640.0±55.0 °C(Predicted) | [density ]
1.54±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Solid | [pka]
5.62±0.40(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
GSK-843 (GSK'843) is a 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. GSK-843 can be used for the research of inflammation[1][2]. | [Biological Activity]
GSKμ843 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. GSKμ843 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. | [IC 50]
RIPK3 | [storage]
Store at -20°C | [References]
[1] Mandal P, et al. RIP3 induces apoptosis independent of pronecrotic kinase activity. Mol Cell. 2014 Nov 20;56(4):481-95. DOI:10.1016/j.molcel.2014.10.021
[2] Kaiser WJ, et al. Toll-like receptor 3-mediated necrosis via TRIF, RIP3, and MLKL. J Biol Chem. 2013 Oct 25;288(43):31268-79. DOI:10.1074/jbc.M113.462341 |
|
|