NCH-51

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

NCH-51 是 NCH-31 的 S-异丁酰前药，NCH-31 是一种有效的 HDAC 抑制剂，对 HDAC1 的 IC50 为 48 nM。

NCH-51 is the S-isobutyryl prodrug of NCH-31, which is a potent HDAC inhibitor with IC50 of 48 nM for HDAC1, inhibits cell proliferation of NCI-H460 and MDA-MB-231 with IC50 of 2.1 and 4.4 uM; inhibits the cell growth of a variety of lymphoid malignant cells through apoptosis induction, more effectively than SAHA, upregulates p21 and downregulated anti-apoptotic molecules including survivin, bcl-w and c-FLIP; also induces expression of latent HIV-1 through the Sp1 sites with minimal cytotoxicit in latently infected-cells.

PTACH (compound 51) treatment elevates the levels of acetylated histone H4 and p21WAF1/CIP1 in a dose-dependent manner.In cancer cell growth inhibition assay, PTACH (compound 51) shows strong activity. PTACH inhibits various cancer cells with EC50 values of 2.3 μM, 9.1 μM, 3.0 μM, 2.6 μM, 1.1 μM, 4.5 μM, 2.4 μM, 5.0 μM, and 4.5 μM for MDA-MB-231, SNB-78, HCT116, NCI-H226, LOX-IMVI, SK-OV-3, RXF-631L, St-4, and DU-145 cells, respectively.PTACH (NCH-51) augments the HIV-1 production in latently infected OM10.1 cells and such reactivation is associated with a loss of HDAC1 occupancy and subsequent hyperacetylation of histones in nuc-1 at the HIV-1 promoter. Western Blot Analysis Cell Line:HCT 116 cells Concentration:1 μM, 5 μM, 25 μM Incubation Time:8 hours Result:Gave rise to elevated and dose-dependent levels of acetylated histone H4 and p21WAF1/CIP1.

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NCH51

Cell Cycle/DNA Damage

HDAC

HDAC

Cancer

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848354-66-5

390.5627

C20H26N2O2S2

>98% (HPLC)

10 mM in DMSO

CC(C)C(SCCCCCCC(NC1=NC(C2=CC=CC=C2)=CS1)=O)=O

Propanethioic acid, 2-methyl-, S-[7-oxo-7-[(4-phenyl-2-thiazolyl)amino]heptyl] ester

(-20℃)

With Ice Pack

≥ 2 years