产品介绍
Product Description
Biochem/physiol Actions
A potent ATP-competitive RIP3 (RIPK3) kinase inhibitor that suppresses necrosis induction in both human and murine cell cultures.
GSK′843 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. GSK′843 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.
技术参数
Specifications
| assay | ≥98% (HPLC) |
| form | powder |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear |
| storage temp. | 2-8°C |
| SMILES string | [s]1c2c(nc1)cc(cc2)c3c4c([s]c3)c(cnc4N)c5[n](nc(c5)C)C |
| InChI key | BPKSNNJTKPIZKR-UHFFFAOYSA-N |

