I-BET762 (GSK525762) is a novel, highly potent, selective and cell permeable inhibitor of the bromodomain and extra terminal (BET) family protein BRD4 with an IC50 of ~35 nM. It suppresses the production of proinflammatory proteins by macrophages and blocks acute inflammation. It is highly selective over other bromodomain-containing proteins. In vivo studies using I-BET762 have demonstrated efficacy in a range of oncology and immunoinflammatory models. I-BET762 is currently in clinical development for oncology indication.
CAS Number: 1260907-17-2
Molecular Weight: 423.90
Chemical Name: (S)-2-(6-(4-chlorophenyl)-8-methoxy-1-methyl-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)-N-ethylacetamide
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 50 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
I-BET762 was used at 0.5-1 µM final concentration in various in vitro assays.
I-BET762 could be dosed to the mice by oral administration at 10-30 mg/kg once per day.
- Mirguet O, et al. Discovery of epigenetic regulator I-BET762: lead optimization to afford a clinical candidate inhibitor of the BET bromodomains. (2013) J Med Chem. 56(19):7501-15.
- Zhao Y, et al. The making of I-BET762, a BET bromodomain inhibitor now in clinical development. (2013) J Med Chem. 56(19):7498-500.
Products are for research use only. Not for human use.
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