| Bioactivity | I-BET432 is a BET inhibitor. I-BET432 inhibits BRD4 N-terminal bromodomain (BD1) and the C-terminal bromodomain (BD2) with pIC50 values of 7.5 and 7.2, respectively. I-BET432 can be used as an oral candidate quality molecule for the research of multiple oncology and inflammatory diseases[1]. |
| Invitro | I-BET432 inhibits BRD4 BD1 and BD2 with pIC50 values of 7.5 and 7.2, respectively[1].I-BET432 inhibits human whole blood MCP-1 with an pIC50 value of 7.4[1].I-BET432 inhibits hERG with an pIC50 value ＜4.3[1]. |
| In Vivo | I-BET432 shows great oral bioavailability in rats and dogs[1].1.19Pharmacokinetic Properties of I-BET432 in Rats and Dogs[1]. |
| Name | I-BET432 |
| Formula | C18H21N3O3 |
| Molar Mass | 327.38 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Humphreys PG, et al. Identification and Optimization of a Ligand-Efficient Benzoazepinone Bromodomain and Extra Terminal (BET) Family Acetyl-Lysine Mimetic into the Oral Candidate Quality Molecule I-BET432. J Med Chem. 2022 Nov 24;65(22):15174-15207. |