SML3850

I-BET432

≥98% (HPLC)

• Synonym(s): (R)-7-((R)-1,2-Dihydroxyethyl)-1,3-dimethyl-5-(1-methyl-1H-pyrazol-4-yl)-1H-benzo[d]azepin-2(3H)-one, GSK 3740432, GSK-3740432, GSK3740432
• Empirical Formula (Hill Notation): C₁₈H₂₁N₃O₃
• Molecular Weight: 327.38
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: -10 to -25°C

Description

Biochem/physiol Actions

I-BET432 is a bromodomain (BrD) inhibitor with selectivity toward the BET family of bromodomain-containing proteins (BrD1/2 pKd = 8.3/8.1 (BRD2), 8.5/8.1 (BRD3), 8.3/8.2 (BRD4), 8.3/7.8 (BRDT) by DiscoRx BROMOscan) with little or no affinity toward bromodomain-containng proteins (BCPs) and BrDs, including CREBBP, TRIM24, EP300, WDR9 BD2, PBRM1 BD2, TAF1 BD2, BAZ2A (pKd <5.9 from DiscoRx BROMOscan panel). I-BET432 inhibits LPS-stimulated MCP-1 production from human white blood cells (pIC50 = 7.4) with oral availability and good in vivo pharmacokinetic properties.

Orally available bromodomain (BrD) inhibitor with selectivity toward the BET family of bromodomain-containing proteins BRD2/3/4 and BRDT.

Safety Information

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