HPOB

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的选择性 HDAC6 抑制剂 (IC50=56 nM)。

A potent and selective HDAC6 inhibitor (IC50=56 nM); shows IC50>1.7 uM for the other HDACs, more potent than tubacin; selectively inhibits HDAC6 catalytic activity in vivo and in vitro; causes growth inhibition of normal and transformed cells but does not induce cell death; enhances the effectiveness of DNA-damaging anticancer drugs in transformed cells but not normal cells.

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 pathway.Cell Proliferation Assay Cell Line:Normal human foreskin fibroblast (HFS), LNCaP, A549, U87 cellsConcentration:8, 16, or 32 μM Incubation Time:72 hours Result:Inhibited cell growth of normal and transformed cells in a concentration-dependent mannerbut do not induce cell death of normal or transformed cells.

HPOB (300 mg/kg; i.p.; daily for 18 days) and SAHA (50 mg/kg) causes suppression of the growth of established CWR22 tumors. Animal Model:Nude mice (CWR22 human prostate cancer xenograf)Dosage:300 mg/kg Administration:I.p.; daily for 18 days Result:Combination with SAHA showed significant shrinkage of CWR22 tumors.

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Cell Cycle/DNA Damage

HDAC

HDAC1|HDAC10|HDAC3|HDAC6|HDAC8

Cancer

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1429651-50-2

314.3358

C17H18N2O4

>98% (HPLC)

10 mM in DMSO

C1=CC=C(C=C1)N(CCO)C(=O)CC2=CC=C(C=C2)C(=O)NO

Benzeneacetamide, 4-[(hydroxyamino)carbonyl]-N-(2-hydroxyethyl)-N-phenyl-

(-20℃)

With Ice Pack

≥ 2 years