I-BET151 (GSK1210151A) is a novel and selective inhibitor of the bromodomain and extra terminal (BET) family proteins BRD2, BRD3, and BRD4 with IC50 of ~0.5 μM, 0.25 μM, and 0.79 μM respectively. It has profound effects on human and murine MLL-fusion leukaemic cell lines, through the induction of early cell cycle arrest and apoptosis. The mode of action of I-BET151 is, at least in part, due to the inhibition of transcription at key genes (BCL2, C-MYC and CDK6) through the displacement of BRD3/4, PAFc and SEC components from chromatin. In vivo studies indicate that I-BET151 can provide survival benefit in two distinct mouse models of murine MLL–AF9 and human MLL–AF4 leukaemia. I-BET151 is also an ApoA1 upregulator that was also found to mediate potent anti-inflammatory effects. It showed a broad anti-inflammatory profile in a LPS-challenged Balb/C mouse model.
CAS Number: 1300031-49-5
Molecular Weight: 415.44
Chemical Name: 7-(3,5-dimethylisoxazol-4-yl)-8-methoxy-1-((R)-1-(pyridin-2-yl)ethyl)-1H-imidazo[4,5-c]quinolin-2(3H)-one
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 100mM
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: ≥360 days 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-BET151 was used at 10 µM final concentration in various in vitro assays.
IP administration of I-BET151 at 30 mg/kg once per day was shown to provide survival benefit in two distinct mouse models of murine MLL–AF9 and human MLL–AF4 leukaemia. Oral administration of I-BET151 at 10 mg/kg once per day in mice showed efficacy in acute inflammation mouse model.
- Dawson MA, et al. Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia. (2011) Nature. 478(7370):529-33.
- Mirguet O, et al. From ApoA1 upregulation to BET family bromodomain inhibition: discovery of I-BET151. (2012) Bioorg Med Chem Lett. 22(8):2963-7.
- Seal J, et al. Identification of a novel series of BET family bromodomain inhibitors: binding mode and profile of I-BET151 (GSK1210151A). (2012) Bioorg Med Chem Lett. 22(8):2968-72.
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