| Bioactivity | PTACH (NCH-51) is a potent HDAC inhibitor with IC50s of 48 nM, 32 nM, and 41 nM for HDAC1, HDAC4, and HDAC6, respectively. PTACH exerts potent growth inhibition against various cancer cells (EC50s of 1.1-9.1 µM) [1][2]. | ||||||||||||
| Invitro | PTACH (compound 51) treatment elevates the levels of acetylated histone H4 and p21WAF1/CIP1 in a dose-dependent manner[1].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[1].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[2]. Western Blot Analysis[1] Cell Line: | ||||||||||||
| Name | PTACH | ||||||||||||
| CAS | 848354-66-5 | ||||||||||||
| Formula | C20H26N2O2S2 | ||||||||||||
| Molar Mass | 390.56 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Suzuki T, et al. Novel inhibitors of human histone deacetylases: design, synthesis, enzyme inhibition, and cancer cell growth inhibition of SAHA-based non-hydroxamates. J Med Chem. 2005 Feb 24;48(4):1019-1032. [2]. Ann Florence B Victoriano, et al. Novel histone deacetylase inhibitor NCH-51 activates latent HIV-1 gene expression. FEBS Lett. 2011 Apr 6;585(7):1103-11. |