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Bromosporine

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Chemical Structure| 1619994-69-2 同义名 : -
CAS号 : 1619994-69-2
货号 : A104099
分子式 : C17H20N6O4S
纯度 : 99%+
分子量 : 404.443
MDL号 : MFCD26142669
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(123.63 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • bromodomain

    CECR2, IC50:17 nM

  • BET

    BRD2, IC50:0.29 μM

    BRD9, IC50:0.122 μM
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.47mL

0.49mL

0.25mL

12.36mL

2.47mL

1.24mL

24.73mL

4.95mL

2.47mL
参考文献

[1]Roberts TC, Etxaniz U, et al. BRD3 and BRD4 BET Bromodomain Proteins Differentially Regulate Skeletal Myogenesis. Sci Rep. 2017 Jul 21;7(1):6153.

[2]Picaud S, Leonards K, et al. Promiscuous targeting of bromodomains by bromosporine identifies BET proteins as master regulators of primary transcription response in leukemia. Sci Adv. 2016 Oct 12;2(10):e1600760.

[3]University of Oxford. Structural Genomics Consortium Nuffield Dept. of Clinical Medicine. 15th Hellenic Symposium of Medicinal Chemistry Athens, 30, May, 2012

[4]Bromosporine (BSP)

[5]Pan H, Lu P, Shen Y, et al. The bromodomain and extraterminal domain inhibitor bromosporine synergistically reactivates latent HIV-1 in latently infected cells. Oncotarget. 2017;8(55):94104-94116.