Bromosporine

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Bromosporine

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1619994-69-2

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议
50mg	电议

产品介绍

Bromosporine 是一种有效的 BET 抑制剂，对 PCAF 的 IC50 值为 2.1 μM。溴孢菌素可以阻滞细胞周期并诱导癌细胞凋亡。当与 5-FU 联合使用时，溴孢菌素在异种移植小鼠模型中表现出优异的抗肿瘤活性。 Bromosporine 可以增加 HIV-1 潜伏期模型中的 CDK9 T 环磷酸化，从而保护重新激活 HIV-1 复制免受潜伏期。溴孢菌素可用于研究结直肠癌、急性髓性白血病 (AML) 和艾滋病。

Cas No.	1619994-69-2
化学名	ethyl (3-methyl-6-(4-methyl-3-(methylsulfonamido)phenyl)-[1,2,4]triazolo[4,3-b]pyridazin-8-yl)carbamate
Canonical SMILES	CC1=C(NS(C)(=O)=O)C=C(C2=NN3C(C(NC(OCC)=O)=C2)=NN=C3C)C=C1
分子式	C₁₇H₂₀N₆O₄S
分子量	404.44
溶解度	≥ 40.4 mg/mL in DMSO
储存条件	Store at -20℃
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
产品描述	Bromosporine is a broad spectrum inhibitor of bromodomains with IC50 value of 0.41 μM, 0.29μM, 0.122μM for BRD2, BRD4 and BRD9, respectively [1]. Bromodomains is a 110 amino acid protein domain which can recognize monoacetylated lysine residues and play a pivotal role in the targeting of chromatin-modifying enzymes to specific sites. It has been revealed that proteins contained BRDs involves in the development of many diseases, including cancers, inflammatory diseases and neurological diseases. It is also reported that Bromosporine functioned on BAZ2A, BRPF3, CECR2, FALZ and TIF-1α with IC50 value of 9.36μM, 48.11μM, 0.017μM, 5.655μM and 12.38μM, respectively [1]. Reference: [1]. University of Oxford. Structural Genomics Consortium Nuffield Dept. of Clinical Medicine. 15th Hellenic Symposium of Medicinal Chemistry Athens, 30, May, 2012.