SML2001

GSK′843

≥98% (HPLC)

• Synonym(e): 3-(5-Benzothiazolyl)-7-(1,3-dimethyl-1H-pyrazol-5-yl)-thieno[3,2-c]pyridin-4-amine, GSK 843, GSK-843, GSK843
• Empirische Formel (Hill-System): C₁₉H₁₅N₅S₂
• CAS-Nummer: 1601496-05-2
• Molekulargewicht: 377.49
• MDL-Nummer: MFCD30536593
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Assay: ≥98% (HPLC)
• Form: powder
• Farbe: white to beige
• Löslichkeit: DMSO: 2 mg/mL, clear
• Lagertemp.: 2-8°C

Beschreibung

Biochem./physiol. Wirkung

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.

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable