|(3-甲基-6-(4-甲基-3-(甲基磺酰胺基)苯基)-[1,2,4]三唑并[4,3-b]哒嗪-8-基)氨基甲酸乙酯|CsnPharm

CAS No.: 1619994-69-2

Bromosporine Catalog No. CSN15855

Synonyms: Bromosporine

Bromosporine inhibits various bromodomains including BRD2, BRD4, BRD9 and CECR2 with IC50s of 0.41 μM, 0.29 μM, 0.122 μM and 0.017 μM respectively.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 CECR2

IC50:0.017μM Bromodomain 9

IC50:0.122μM Bromodomain 4

IC50:0.29μM Bromodomain 2

IC50:0.41μM
描述Bromodomains are protein interaction modules that play an important role in the targeting of chromatin-modifying enzymes to specific sites. Bromodomain-containing proteins are involved in a variety of biological processes, including cell proliferation, differentiation, energy homeostasis, and neurological function. Bromosporine is a broad spectrum inhibitor for bromodomains with IC50 values of 0.41, 0.29, and 0.122μM for BRD2, BRD4, and BRD9, respectively. It also exhibited inhibitory activities against BAZ2A, BRPF3, CECR2, FALZ, and TIF1α with IC50 values of 9.36, 48.11, 0.017, 5.655, and 12.38μM, respectively^[3]. Bromosporine at a concentration of 10μM resulted in a temperature shift of 4.4, 5.9, 5.3, 5.9, 6.9, 6.2, 7.3, 5.2, 8.3, 0.4, 1.3, 5.2, 0.9, 0.9, 1.2, 0.4, -0.2, 3.9, and 3.4°C for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1), BRD4(2), BRDT(1), BRDT(2), CECR2, PB1(5), TAF1(1), TAF1(2), TAF1L(1), TAF1L(2), BAZ2A, TIF1α, ATAD2, BRD9, and CREBBP, respectively. Bromosporine also showed moderate cytotoxicity in HeLa cells at a concentration of 18µM^[4]. Bromosporine can potently reactivate latent HIV-1 replication in a dose- and time-dependent manner^[5].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4725 mL
- 12.3627 mL
- 24.7253 mL
- 5 mM
- 0.4945 mL
- 2.4725 mL
- 4.9451 mL
- 10 mM
- 0.2473 mL
- 1.2363 mL
- 2.4725 mL

技术信息

CAS号

1619994-69-2

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H20N6O4S

运输

蓝冰

分子量

404.44

别名

Bromosporine

溶解度

DMSO	79.0 mg/mL (195.3 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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靶点	Description	IC50
CECR2		IC50:0.017μM
Bromodomain 9		IC50:0.122μM
Bromodomain 4		IC50:0.29μM
Bromodomain 2		IC50:0.41μM

Bromosporine Catalog No. CSN15855

靶点选择性

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