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。
| 生物活性 | Purinostat mesylate is a selective inhibitor ofHDAC. Purinostat mesylate inhibits class I and class IIb HDACs withIC50s from 0.81 to 11.5 nM. Purinostat mesylate inducesapoptosisand 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].
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].
| 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 | |
| Formula | |
| 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. |
m.cnreagent.com