HPOB

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Chemical Structure| 1429651-50-2 同义名 : -
CAS号 : 1429651-50-2
货号 : A392083
分子式 : C17H18N2O4
纯度 : 97%
分子量 : 314.34
MDL号 : MFCD27952937
存储条件：

Pure form Sealed in dry,2-8°C

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

DMSO: 50 mg/mL(159.07 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, IC50:2.8 μM

  • HDAC10

    HDAC10, IC50:3.0 μM

  • HDAC3

    HDAC3, IC50:1.7 μM

  • HDAC6

    HDAC6, IC50:56 nM
描述 HPOB is a selective HDAC6 inhibitor with IC50 value of 56nM, exhibiting at least 30-fold selectivity to HDAC6 over other HDACs. Treatment with HPOB at concentration of 8-32μM for 72h led to cell growth inhibition of normal (HFS) and transformed (LNCaP, A549, and U87) cells but did not induce cell death. HPOB at concentration of 4-16μM caused accumulation of acetylated α-tubulin and acetylated peroxiredoxin, both of which are HDAC6 substrates, in normal (HFS) and transformed (LNCAP, U87, and A549) cells post 24-hour treatment, without effect on acetylated histones. HPOB only inhibited the catalytic activity but not the ubiquitin-binding activity of HDAC6. HPOB had the therapeutic potential in combination therapy to enhance the potency of anticancer drugs including, etoposide, doxorubicin and SAHA in vitro, and enhance anticancer effects of SAHA (50mg/kg) in mice bearing human prostate cancer CWR22 xenograft at dose of 300mg/kg, i.p., for 25 days.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.18mL

0.64mL

0.32mL

15.91mL

3.18mL

1.59mL

31.81mL

6.36mL

3.18mL
参考文献

[1]Li ZY, Li QZ, et al. HPOB, an HDAC6 inhibitor, attenuates corticosterone-induced injury in rat adrenal pheochromocytoma PC12 cells by inhibiting mitochondrial GR translocation and the intrinsic apoptosis pathway. Neurochem Int. 2016 Oct;99:239-251.

[2]Lee JH, Mahendran A, et al. Development of a histone deacetylase 6 inhibitor and its biological effects. Proc Natl Acad Sci U S A. 2013 Sep 24;110(39):15704-9.