SML2001

GSK′843

≥98% (HPLC)

• Synonym(s): 3-(5-Benzothiazolyl)-7-(1,3-dimethyl-1H-pyrazol-5-yl)-thieno[3,2-c]pyridin-4-amine, GSK 843, GSK-843, GSK843
• Empirical Formula (Hill Notation): C₁₉H₁₅N₅S₂
• CAS Number: 1601496-05-2
• Molecular Weight: 377.49
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD30536593
• Assay: ≥98% (HPLC)
• Form: powder

Properties

• 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

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.

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable