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HPOB

CAS No. : 1429651-50-2

MCE 站：HPOB

产品活性：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。

研究领域：Cell Cycle/DNA Damage  |  Epigenetics  |  Apoptosis

作用靶点：HDAC  |  Apoptosis

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 pathway.

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.

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