HPOB
目录号: PL04939 纯度: ≥95%
CAS No. :1429651-50-2
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中文名称
HPOB
中文别名
HPOB 抑制剂;HPOB
英文名称
HPOB
英文别名
HPOB;Benzeneacetamide, 4-[(hydroxyamino)carbonyl]-N-(2-hydroxyethyl)-N-phenyl-;4-[(Hydroxyamino)carbonyl]-N-(2-hydroxyethyl)-N-phenyl-benzeneacetamide
Cas No.
1429651-50-2
分子式
C17H18N2O4
分子量
314.34
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
HPOB 是一种高效、选择性的 HDAC6 抑制剂,IC50 为 56 nM。HPOB 显示对其他 HDAC 的效力降低了 30 倍以上。HPOB 提高 DNA 损伤抗癌药物在转化细胞中的有效性。HPOB 不阻断 HDAC6 的泛素结合活性。
生物活性
HPOB is a highly potent and selective inhibitor of HDAC6 with an IC 50 of 56 nM. HPOB displays >30 fold less potent against other HDACs. HPOB enhances the effectiveness of DNA-damaging anticancer agents in transformed cells but not normal cells. HPOB does not block the ubiquitin-binding activity of HDAC6.
性状
Solid
IC50 & Target[1][2]
HDAC6 0.056 μM (IC50) HDAC3/NCOR2 1.7 μM (
体外研究(In Vitro)
HPOB (8, 16, or 32 μM; 72 hours) inhibits growth, however, not viability, of normal or transformed cells.
In normal (HFS) and transformed (LNCAP, U87, and A549) cells, HPOB causes accumulation of acetylated α-tubulin and acetylated peroxiredoxin, substrates of HDAC6, but not of acetylated histones. HPOB enhances etoposide-, doxorubicin-, and SAHA-induced transformed cell ((LNCAP, U87, and A549 cells) death but not normal cell death.
In LNCaP cells cultured with HPOB and etoposide, there was an increase in cleaved PARP, a marker of apoptosis. Combination of HPOB with etoposide increased the accumulation of DNA damage compared with etoposide alone as evidenced by accumulation of γH2AX in LNCaP cells.
HPOB attenuates corticosterone-induced injury in rat adrenal pheochromocytoma PC12 cells by inhibiting mitochondrial GR translocation and the intrinsic apoptosis pathwa
体内研究(In Vivo)
HPOB (300 mg/kg; i.p.; daily for 18 days) and SAHA (50 mg/kg) causes suppression of the growth of established CWR22 tumors. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Nude mice (
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Lee JH 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.
[2]. Li ZY 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;99:239-51.
溶解度数据
In Vitro: DMSO : 50 mg/mL (159.06 mM; Need ultrasonic)配制储备液
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2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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