2650188-32-0
2650188-32-0 structure
- Name: Purinostat mesylate
- Chemical Name: Purinostat mesylate
- CAS Number: 2650188-32-0
- Molecular Formula: C24H30N10O6S
- Molecular Weight: 586.62
- Catalog: Signaling Pathways Apoptosis Apoptosis
- Create Date: 2022-10-16 12:16:13
- Modify Date: 2024-01-13 17:45:06
-
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].
| Name | Purinostat mesylate |
|---|
| Description | 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]. |
|---|---|
| Related Catalog | |
| 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) |
| 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. |
| 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. |
| References |
| Molecular Formula | C24H30N10O6S |
|---|---|
| Molecular Weight | 586.62 |