UMB-32 |
| رقم الكتالوجGC14168 |
يربط UMB-32 ، وهو مثبط قوي وانتقائي BRD4 ، BRD4 بـ Kd البالغ 550 نانومتر ، و IC50 لـ 637 نانومتريُظهر UMB-32 أيضًا فاعلية ضد TAF1 ، وهو عامل نسخ يحتوي على البرومودومين
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1635437-39-6
Sample solution is provided at 25 µL, 10mM.
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UMB-32 is a potent, selective inhibitor of the BET bromodomain BRD4 [1]. The BET family (BRD2, BRD3, BRD4, and BRDT) functions as transcriptional coactivator proteins. BET bromodomains are also important mediators of cell cycle progression and facilitate developmental transitions such as spermiogenesis. Deregulation of BET bromodomain function has been observed in numerous malignancies. BET bromodomain inhibition has contributed new insights into gene regulation and emerged as a promising therapeutic strategy in cancer [1].
In vitro: UMB-32 bound to BRD4 with a Kd value of 550 nM and 724 nM cellular potency in BRD4-dependent lines. UMB-32 showed potency against TAF1, a bromodomain-containing transcription factor. UMB-32 showed markedly increased potency for the BET proteins associated with a dramatic improvement in selectivity. UMB-32 potently bound to the TAF1 and TAF1L with the Kd values of 560nM and 1.3 μM, respectively [1].
Reference:
[1] McKeown M R, Shaw D L, Fu H, et al. Biased multicomponent reactions to develop novel bromodomain inhibitors[J]. Journal of medicinal chemistry, 2014, 57(21): 9019-9027.
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