Apoptosis
MAO
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Product name : GSK 1210151A (I-BET151)
Item : cc415
Price : 200mg, $750;500mg, $1190; 1g $1890; 2g, $2995
contact : Send inquiry to: info@acesobio.com,or by fax to: 1-845-673-1239.
CAS : 1300031-49-5
Molecular Weight : 415.44
Formula : C₂₃H₂₁N₅O₃
Storage : at -20°C
Additional information : We offer significant discount for bulky quantity order
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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 GSK 1210151A can provide survival benefit in two distinct mouse models of murine MLL–AF9 and human MLL–AF4 leukaemia. GSK-1210151A 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. [1][2]
Reference:
[1] Nature 2011, 478, 529-533.
[2] Bioorg. Med. Chem. Lett. 2012, 22, 2968-2972.
Chemical Information
PLEASE KEEP THE PRODUCT UNDER -20℃ FOR LONG-TERM STORAGE.
NOT FOR HUMAN OR VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.
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