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Products are for research use only. Not for human use. We do not sell to patients.
(GSK1210151A; I-BET 151; GSK-1210151A; GSK 1210151A)
I-BET151 Chemical Structure
|Product name: I-BET151|
|Cat. No.: HY-13235|
I-BET151(GSK1210151A) is a BET bromodomain inhibitor(pIC50=6.1,BRD4); I-BET151 blocks recruitment of BET to chromatin .
IC50 value: 6.1(pIC50) 
Target: BET bromodomain
I-BET151 induces apoptosis and G0/G1 cell cycle arrest in MLL-fusion leukemic cell lines in vitro (IC50 values are 15, 26, 120 and 192 nM for NOMO1, MV4;11, MOLM13 and RS4;11 cell lines respectively). I-BET151 reduces BCL2 expression in NOMO1 cells. I-BET151 improves survival in two rodents models of MLL-fusion leukemia in vivo.
|M.Wt||415.44||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
DMSO 100 mM Ethanol 100 mM
|1 mg||5 mg||10 mg|
|1 mM||2.4071 mL||12.0354 mL||24.0709 mL|
|5 mM||0.4814 mL||2.4071 mL||4.8142 mL|
|10 mM||0.2407 mL||1.2035 mL||2.4071 mL|
. Seal, Jonathan; Lamotte, Yann; Donche, Frederic et al. Identification of a novel series of BET family bromodomain inhibitors: Binding mode and profile of I-BET151 (GSK1210151A). Bioorganic & Medicinal Chemistry Letters (2012), 22(8), 2968-2972.
. Mirguet, Olivier; Lamotte, Yann; Donche, Frederic et al. From ApoA1 upregulation to BET family bromodomain inhibition: Discovery of I-BET151. Bioorganic & Medicinal Chemistry Letters (2012), 22(8), 2963-2967.
. Dawson, Mark A.; Prinjha, Rab K.; Dittman, Antje et al. Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia. Nature (London, United Kingdom) (2011), 478(7370), 529-533.
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