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CAS No.: 1440209-96-0

BRD73954 Catalog No. CSN17366

Synonyms: BRD73954

BRD73954 is a selective inhibitor of HDAC6 and HDAC8 with IC50 of 36 nM and 120 nM, respectively.

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400-920-2911

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技术信息

生物活性

描述Histone deacetylases (HDAC) are a class of enzymes that catalyze the removal of acetyl groups from an amino acid on a histone or a non-histone protein. BRD73954 is a small molecule HDAC inhibitor that exhibits selective and potent inhibitory effects against HDAC6 (IC50 = 0.036 ± 0.018μM) and HDAC8 (IC50 = 0.12 ± 0.064μM). It shows reduced inhibitory potency toward HDAC1, HDAC2, HDAC3, and HDAC7 with IC50 values of 12 ± 2.0, 9.0 ± 6.6, 23 ± 10, and 14 ± 1.7μM, respectively. The IC50 values of BRD73954 for HDAC4, HDAC5, and HDAC9 are over 33μM. Treatment of HeLa cells with BRD73954 (10μM) for 48 hours induced α-tubulin acetylation, but did not affect the acetylation state of H3.^[2]
作用机制BRD73954 is a small molecule HDAC inhibitor with the most potent inhibitory effect toward HDAC6 and HDAC8. It adopts an optimal binding pose in the catalytic domain of HDAC6, forming key H-bonds with His130, His131, and Tyr302. When docking into HDAC8, BRD73954 achieves optimal chelation geometry and forms key H-bonds with His129 and His130.^[2]
参考文献

[1] Olson DE, Wagner FF, et al. Discovery of the first histone deacetylase 6/8 dual inhibitors. J Med Chem. 2013 Jun 13;56(11):4816-20.
[2] Olson DE, Wagner FF, Kaya T, Gale JP, Aidoud N, Davoine EL, Lazzaro F, Weïwer M, Zhang YL, Holson EB. Discovery of the first histone deacetylase 6/8 dual inhibitors. J Med Chem. 2013 Jun 13;56(11):4816-20

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
- 3.5173 mL
- 17.5864 mL
- 35.1729 mL
- 5 mM
- 0.7035 mL
- 3.5173 mL
- 7.0346 mL
- 10 mM
- 0.3517 mL
- 1.7586 mL
- 3.5173 mL

技术信息

CAS号

1440209-96-0

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C16H16N2O3

运输

蓝冰

分子量

284.31

别名

BRD73954

溶解度

DMSO	290.0 mg/mL (1020.0 mM)
Water	insoluble

动物实验配方

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