SML2001

GSK′843

≥98% (HPLC)

• 동의어(들): 3-(5-Benzothiazolyl)-7-(1,3-dimethyl-1H-pyrazol-5-yl)-thieno[3,2-c]pyridin-4-amine, GSK 843, GSK-843, GSK843
• 실험식(Hill 표기법): C₁₉H₁₅N₅S₂
• CAS Number: 1601496-05-2
• Molecular Weight: 377.49
• MDL number: MFCD30536593
• UNSPSC 코드: 12352200
• NACRES: NA.77

속성

• 분석: ≥98% (HPLC)
• 양식: powder
• 색상: white to beige
• solubility: DMSO: 2 mg/mL, clear
• 저장 온도: 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

설명

생화학적/생리학적 작용

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.

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable