BRD73954

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Chemical Structure| 1440209-96-0 同义名 : -
CAS号 : 1440209-96-0
货号 : A985320
分子式 : C16H16N2O3
纯度 : 99%
分子量 : 284.31
MDL号 : MFCD26383435
存储条件：

Pure form Inert atmosphere,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(87.93 mM)，配合低频超声助溶，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

  • HDAC8

    HDAC8, IC50:120 nM

  • HDAC6

    HDAC6, IC50:36 nM
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]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.52mL

0.70mL

0.35mL

17.59mL

3.52mL

1.76mL

35.17mL

7.03mL

3.52mL
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