Droxinostat

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Droxinostat (NS-41080) 是一种选择性 HDAC 抑制剂，对 HDAC3、HDAC6 和 HDAC8 的 IC50 分别为 16.9、2.47 和 1.46 uM。

Droxinostat (NS-41080) is a selective HDAC inhibitor with IC50 of 16.9, 2.47 and 1.46 uM for HDAC3, HDAC6 and HDAC8, respectively; does not inhibit HDAC1, HDAC2, HDAC4, HDAC5, HDAC7, HDAC9, and HDAC10 with IC50 of >20 uM; sensitizes malignant cells to death receptor ligands FAS and TRAIL sensitization with IC50 of 20 and 39 uM, respectively; decreases the expression of the caspase-8 inhibitor FLIP, downregulates c-FLIP(L) and c-FLIP(S) mRNA and protein levels, causes PARP degradation, reduces cell survival, and induces apoptosis in MCF-7 breast cancer cells.

Droxinostat selectively inhibits HDAC3, HDAC6, and HDAC8 with IC50 values of 16.9 μM, 2.47 μM, and 1.46 μM, respectively.Droxinostat (0, 10, 20, or 40 μM; 48 h) suppresses HDAC3 expression and induces acetylation of histones H3 and H4.Droxinostat (0, 10, 20, 40, and 80 μM; 0, 24, 48, 72, 96, and 120 h) inhibits cell proliferation and colony formation in HepG2 and SMMC-7721 cells.Droxinostat (0 to 80 μM; 48 h) induces hepatoma cell apoptosis by activating mitochondrial apoptotic pathways and downregulating FLIP. Western Blot Analysis Cell Line:SMMC-7721 and HepG2 (Human liver carcinoma cell lines)Concentration:0, 10, 20, or 40 μM Incubation Time:48 h Result:Significantly decreased the expression of HDAC3 with dose-dependent in HepG2 and SMMC-7721 cell lines.Significantly enhanced the expression of acetyl-H3 (Ac-H3) and acetylH4 (Ac-H4) in HepG2 and SMMC-7721 cells in a dose-dependent manner.Upregulated the levels of phospho-p53 and cleaved caspase 3 protein and downregulated the levels of Bcl-2.Markedly increased the Bax/Bcl-2 ratio in a dose-dependent manner and increased the expression of cleaved PARP protein in HepG2 cells in a dose-dependent manner.Significant reduced the FLIP expression and enhanced caspase 8 activity in both HepG2 and SMMC-7721cell.Cell Proliferation Assay Cell Line:SMMC-7721 and HepG2 Concentration:0, 10, 20, 40, and 80 μM Incubation Time:0, 24, 48, 72, 96, and 120 h Result:Decreased the viability with a time-and dose-dependent in both cell lines.Apoptosis Analysis Cell Line:SMMC-7721 and HepG2 Concentration:0 to 80 μM Incubation Time:48 h Result:Clearly led to dose-dependent apoptosis, but did not induce hepatoma cell apoptosis at 10 μM and had an apoptotic effect at a starting concentration of 20 μM.RT-PCRCell Line:SMMC-7721 and HepG2 Concentration:20 μM and 40 μM Incubation Time:48 h Result:Significantly increased the mRNA levels of Bax and p53 genes associated with the mitochondrial p53 apoptosis pathway in a dose-dependent manner in HepG2 and SMMC-7721 cells.Significantly increased the Bcl-2 mRNA levels in SMMC-7721 cells at a concentration of 40 uM and also increased the Bax/Bcl-2 mRNA ratio.

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NS 41080 | NS-41080 | NS41080

Cell Cycle/DNA Damage

HDAC

HDAC10|HDAC3|HDAC6|HDAC8|HDAC9

Cancer

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99873-43-5

243.7

C11H14ClNO3

>98% (HPLC)

10 mM in DMSO

O=C(NO)CCCOC1=CC=C(Cl)C=C1C

Butanamide, 4-(4-chloro-2-methylphenoxy)-N-hydroxy-

(-20℃)

With Ice Pack

≥ 2 years