HPOB

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HPOB  纯度: ≥95.0%

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。

HPOB

HPOB Chemical Structure

CAS No. : 1429651-50-2

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥550 In-stock
5 mg ¥500 In-stock
10 mg ¥800 In-stock
25 mg ¥1600 In-stock
50 mg ¥2400 In-stock
100 mg ¥3900 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

HPOB 相关产品

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生物活性

HPOB is a highly potent and selective inhibitor of HDAC6 with an IC50 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[1].

IC50 & Target[1]

HDAC6

0.056 μM (IC50)

HDAC3/NCOR2

1.7 μM (IC50)

HDAC8

2.8 μM (IC50)

HDAC1

2.9 μM (IC50)

HDAC10

3.0 μM (IC50)

HDAC2

4.4 μM (IC50)

体外研究
(In Vitro)

HPOB (8, 16, or 32 μM; 72 hours) inhibits growth, however, not viability, of normal or transformed cells[1].
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[1].
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[1].
HPOB attenuates corticosterone-induced injury in rat adrenal pheochromocytoma PC12 cells by inhibiting mitochondrial GR translocation and the intrinsic apoptosis pathway[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

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

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[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Nude mice (CWR22 human prostate cancer xenograf)[1]
Dosage: 300 mg/kg
Administration: I.p.; daily for 18 days
Result: Combination with SAHA showed significant shrinkage of CWR22 tumors.

分子量

314.34

Formula

C17H18N2O4

CAS 号

1429651-50-2

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
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (159.06 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.1813 mL 15.9063 mL 31.8127 mL
5 mM 0.6363 mL 3.1813 mL 6.3625 mL
10 mM 0.3181 mL 1.5906 mL 3.1813 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.95 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.95 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (7.95 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.95 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.95 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.95 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
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.

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