HPOB|cas:1429651-50-2|西域试剂

HPOB,95.0%

产品编号：Bellancom-19747| CAS NO：1429651-50-2| 分子式：C₁₇H₁₈N₂O₄| 分子量：314.34

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货号	价格	库存与货期
Bellancom-19747	￥500.00	杭州北京（现货）
Bellancom-19747	￥800.00	杭州北京（现货）
Bellancom-19747	￥1600.00	杭州北京（现货）
Bellancom-19747	￥2400.00	杭州北京（现货）
Bellancom-19747	￥3900.00	杭州北京（现货）

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HPOB

产品介绍

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 损伤抗癌活性分子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 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.

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

HPOB (300 mg/kg; i.p.; daily for 18 days) and SAHA (50 mg/kg) causes suppression of the growth of established CWR22 tumors.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

HPOB (300 mg/kg; i.p.; daily for 18 days) and SAHA (50 mg/kg) causes suppression of the growth of established CWR22 tumors.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

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。