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Background: Bromodomains have an important role in the targeting of chromatin-modifying enzymes to specific sites, including methyltransferases, HATs and transcription factors and regulate diverse biological processes from cell proliferation and differentiation to energy homeostasis and neurological processes. Optimized to retain excellent BET target potency and selectivity while enhancing the in vivo pharmacokinetics and terminal half-life to enable prolonged in vivo studies.
Biological Activity: I-BET151 (GSK1210151A) is a novel selective BET inhibitor for BRD2, BRD3 and BRD4 with IC50 of 0.5 µM, 0.25 µM, and 0.79 µM, respectively.
CAS Number: 1300031-49-5
Description: I-BET151(GSK1210151A) is a BET bromodomain inhibitor. I-BET151 displays potent binding affinity to BRD2, BRD3 and BRD4 with Kd of 0.02-0.1 µM. I-BET151 (0.5 or 5 µM) inhibits the binding of BETs (BRD2, BRD3, BRD4, and BRD9) but not the binding of 23 other bromodomain proteins. I-BET151 also blocks recruitment of BET to chromatin.
Solubility: Soluble in DMSO 83 mg/ml (199 mM), water < 1 mg/ml (<1 mM), ethanol 27 mg/ml (64 mM)
Storage Stability: Store at or below -20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.
Target: BET
Biosafety Level: Not applicable (BSL-1)
References: Dawson et al. (2011). Nature 478: 529.
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