I-BET151 (GSK1210151A) (Synonyms: GSK1210151A) |
Catalog No.GC15747 |
I-BET151 (GSK1210151A) (GSK1210151A) est un inhibiteur du bromodomaine BET qui inhibe BRD4, BRD2 et BRD3 avec pIC50 de 6,1, 6,3 et 6,6, respectivement.
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Cas No.: 1300031-49-5
Sample solution is provided at 25 µL, 10mM.
I-BET151 (GSK1210151A) is a selective inhibitor of BET with pIC50 value of 6.1 [1].
BET (bromo and extraterminal) is a member of bromodomain family and has been shown to be associated with a variety of diseases (human squamous cell carcinoma and other cancers). BET inhibitor has been implicated as a promising therapy for human cancer treatment [2].
I-BET151 is a selective BET inhibitor and has the similar inhibition function as TMZ. When tested with 6 myeloma cell lines, I-BET151 treatment decreased cells percent in S/G2 phase and increased cell apoptosis in a time- and dose- dependent manner [2]. In globlastoma cell line U87MG, administration of I-BET151 arrested cells in the G1 phase and reduced cell proliferation ability [3].
When treated with myeloma implanted mouse model with I-BET151, it reduced tumor volume in a four- or five- fold compared with control group [2]. In immunocompromised mouse model with U87MG cells xenograft, administration of I-BET151 in a concentration of 10 mg/kg i.p. daily significantly reduced tumor volume compared with saline treated group [3].
References:
[1]. Seal, J., et al., Identification of a novel series of BET family bromodomain inhibitors: binding mode and profile of I-BET151 (GSK1210151A). Bioorg Med Chem Lett, 2012. 22(8): p. 2968-72.
[2]. Chaidos, A., et al., Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762. Blood, 2014. 123(5): p. 697-705.
[3]. Chan, C.H., et al., BET bromodomain inhibition suppresses transcriptional responses to cytokine-Jak-STAT signaling in a gene-specific manner in human monocytes. Eur J Immunol, 2015. 45(1): p. 287-97.
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