1. Cell Cycle/DNA Damage Epigenetics Apoptosis
  2. HDAC Apoptosis
  3. Purinostat mesylate

Purinostat mesylate 是 HDAC 的选择性抑制剂。Purinostat mesylate 抑制 I 型和 IIb 型 HDACs 的 IC50 值在 0.81-11.5 nM 之间。Purinostat mesylate 诱导 LAMA84 和 188 BL-2 细胞凋亡,影响细胞周期,在体内表现出较强的抗白血病作用。Purinostat mesylate 可用于淋巴细胞白血病的研究。

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Purinostat mesylate Chemical Structure

Purinostat mesylate Chemical Structure

CAS No. : 2650188-32-0

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10 mM * 1 mL in DMSO ¥7227
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1 mg ¥2250
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5 mg ¥5600
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Customer Review

Other Forms of Purinostat mesylate:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Purinostat mesylate is a selective inhibitor of HDAC. Purinostat mesylate inhibits class I and class IIb HDACs with IC50s from 0.81 to 11.5 nM. Purinostat mesylate induces apoptosis and affects cell cycle of LAMA84 and 188 BL-2 cells, and shows potently anti-leukemia effects in vivo. Purinostat mesylate can be used for the research of lymphoblastic leukemia[1].

IC50 & Target

HDAC1

0.81 nM (IC50)

HDAC10

1.1 nM (IC50)

HDAC2

1.4 nM (IC50)

HDAC3

1.7 nM (IC50)

HDAC8

3.8 nM (IC50)

HDAC6

11.5 nM (IC50)

HDAC5

426 nM (IC50)

HDAC7

590 nM (IC50)

HDAC9

622 nM (IC50)

HDAC4

1072 nM (IC50)

HDAC11

3349 nM (IC50)

体外研究
(In Vitro)

Purinostat mesylate (1-10 μM) inhibits HDAC1, 2, 3 and 8 with IC50s of 0.81, 1.4, 1.7 and 3.8 nM, inhibits HDAC6 and 10 with IC50s of 11.5 and 1.1 nM, and inhibits HDAC4, 5, 7, 9 and 11 with IC50s of 1072, 426, 690, 622 and 3348 nM, respectively[1].
Purinostat mesylate (0-60 nM; 24 h) induces apoptosis and affects cell cycle of LAMA84 and 188 BL-2 cells[1].

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

Cell Proliferation Assay[1]

Cell Line: LAMA84 and 188 BL-2 cell lines
Concentration: 0-80 nM
Incubation Time: 24, 48 and 72 hours
Result: Significantly inhibited cell proliferation of LAMA84 and 188 BL-2 cells.

Apoptosis Analysis[1]

Cell Line: LAMA84 and 188 BL-2 cell lines
Concentration: 0-60 nM
Incubation Time: 24 hours
Result: Induced apoptosis of LAMA84 and 188 BL-2 cells.

Cell Cycle Analysis[1]

Cell Line: LAMA84 and 188 BL-2 cell lines
Concentration: 0-40 nM
Incubation Time: 24 hours
Result: Dose-dependently blocked cell cycle progression at G0/G1 phase.

Western Blot Analysis[1]

Cell Line: LAMA84 and 188 BL-2 cell lines
Concentration: 0-40 nM
Incubation Time: 24 hours
Result: Dose-dependently increased the 191 levels of Ac-H3 and Ac-H4, and decreased HSP90.
体内研究
(In Vivo)

Purinostat mesylate (5-10 mg/kg; i.p. three times a week for 5 weeks) effectively suppresses leukemia progression in vivo[1].
Purinostat mesylate (5-10 mg/kg; i.v. three times a week for 8 weeks) shows potently anti-leukemia effects in BCR-ABL(T315I)-induced primary B-ALL mice[1].

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

Animal Model: Non-irradiated C57BL/6 recipient mice with BL-2 cells injection[1]
Dosage: 5 and 10 mg/kg
Administration: Intraperitoneal injection; 5-10 mg/kg three times a week; for five weeks
Result: Significantly prolonged the overall survival rate and suppressed leukemia progression of mice, and no tumor cell was detected after stopped treatment.
Animal Model: Non-irradiated C57BL/6 recipient mice with BL-2 secondary transplantation[1]
Dosage: 10 mg/kg
Administration: Intravenous injection; 10 mg/kg three times a week
Result: Completely eliminated GFP+B220+ cells in spleens on day 3 with two times treatment and this complete inhibition was maintained for 26 days duration of treatment.
Animal Model: B-ALL mouse with BCR-ABL(T315I)-induced leukemia[1]
Dosage: 5 and 10 mg/kg
Administration: Intravenous injection; 5 and 10 mg/kg three times a week; for 8 weeks
Result: Significantly prolonged survival rate of BCR-ABL(T315I)-induced B-ALL mice. Survived all mice after treatment for 42 days.
分子量

586.62

Formula

C24H30N10O6S

CAS 号
性状

固体

颜色

Off-white to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 35 mg/mL (59.66 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7047 mL 8.5234 mL 17.0468 mL
5 mM 0.3409 mL 1.7047 mL 3.4094 mL
查看完整储备液配制表

* 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 (sealed storage, away from moisture)。-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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
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体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

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体积 (start)

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体积 (final)

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动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

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动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 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 (sealed storage, away from moisture)。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7047 mL 8.5234 mL 17.0468 mL 42.6170 mL
5 mM 0.3409 mL 1.7047 mL 3.4094 mL 8.5234 mL
10 mM 0.1705 mL 0.8523 mL 1.7047 mL 4.2617 mL
15 mM 0.1136 mL 0.5682 mL 1.1365 mL 2.8411 mL
20 mM 0.0852 mL 0.4262 mL 0.8523 mL 2.1309 mL
25 mM 0.0682 mL 0.3409 mL 0.6819 mL 1.7047 mL
30 mM 0.0568 mL 0.2841 mL 0.5682 mL 1.4206 mL
40 mM 0.0426 mL 0.2131 mL 0.4262 mL 1.0654 mL
50 mM 0.0341 mL 0.1705 mL 0.3409 mL 0.8523 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
Purinostat mesylate
目录号:
HY-150109
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