2. Cell Cycle/DNA Damage Epigenetics Apoptosis
  3. HDAC Apoptosis
  4. 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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Purinostat mesylate 相关抗体

Top Publications Citing Use of Products

查看 HDAC 亚型特异性产品:

查看所有亚型
HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

  • 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.

Purinostat mesylate 相关抗体:

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
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Purinostat mesylate 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

Purinostat2650188-32-0HDACApoptosisHistone deacetylasesselectiveBCR-ABLB-cell acutelymphoblastic leukemiamouse modelsuperior efficiencyLAMA84188 BL-2Inhibitorinhibitorinhibit

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