| CAS NO: | 1635437-39-6 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 361.4 |
| Cas No. | 1635437-39-6 |
| Formula | C21H23N5O |
| Solubility | ≤20mg/ml in ethanol;10mg/ml in DMSO;20mg/ml in dimethyl formamide |
| Chemical Name | N-(1,1-dimethylethyl)-2-[4-(3,5-dimethyl-4-isoxazolyl)phenyl]-imidazo[1,2-a]pyrazin-3-amine |
| Canonical SMILES | CC(C)(C)NC1=C(N=C2N1C=CN=C2)C3=CC=C(C4=C(C)ON=C4C)C=C3 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
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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