PTACH

PTACH
  • CAS No.:848354-66-5
Other grades of this product :
PTACH Basic information
Product Name:PTACH
Synonyms:Cpd 51, S-[6-(4-Phenyl-2-thiazolylcarbamoyl)hexyl] thioisobutyrate;2-MethylpropanethioicacidS-[7-oxo-7-[(4-phenyl-2-thiazolyl)amino]heptyl]ester;NCH 51;S-(7-Oxo-7-((4-phenylthiazol-2-yl)amino)-heptyl) 2-methylpropanethioate;PTACH (NCH-51);HDAC Inhibitor XXII, NCH51;Propanethioic acid,2-methyl-, S-[7-oxo-7-[(4-phenyl-2-thiazolyl)amino]heptyl] ester;NCH51, >98%
CAS:848354-66-5
MF:C20H26N2O2S2
MW:390.56
EINECS:
Product Categories:
Mol File:848354-66-5.mol
PTACH Chemical Properties
Melting point 127-128 °C(Solv: hexane (110-54-3); ethyl acetate (141-78-6))
density 1.181±0.06 g/cm3(Predicted)
storage temp. 2-8°C
solubility DMSO: soluble26mg/mL
form White powder
pka9.52±0.50(Predicted)
Safety Information
Hazard Codes Xi
Risk Statements 41
Safety Statements 26-39
WGK Germany 3
MSDS Information
PTACH Usage And Synthesis
UsesNCH 51 is a Histone deacetylase inhibitor.
General DescriptionA cell-permeable S-isobutyryl prodrug that is processed intracellularly to form the potent HDAC inhibitor NCH-31 (IC50 = 48 and 170 nM, respectively, using partially purified HDAC1 or HeLa nuclear extract) that is predicted to exhibit a similar HADC binding mode as that of SAHA with its sulfhydryl replacing SAHA′s hydroxamate as the active-site zinc-targeting group. NCH-51 is shown to exhibit comparable antiproliferative (mean IC50 = 3.8 μM vs. 3.7 μM for SAHA; 48 h treatment) and apoptotic activity as SAHA against various cancer cell lines, but not PBMCs from 4 healthy individuals (IC50 >30 μM with either drug), and the antioxidant N-Acetyl-L-Cysteine (NAC; Cat. No. 106425) at 2 mM is reported to abolish the cell-growth inhibition caused by either 3 μM NCH-51 or SAHA in the Multiple Myeloma U266 cultures. Half-life in human plasma at 37 °C = 24 h.
Biological ActivityHistone deacetylase (HDAC) inhibitor. Inhibits growth of various cancer cells in vitro (EC 50 = 1.1-9.1 μ M).
Biochem/physiol ActionsHDAC inhibitor; more potent than the majority of HDAC inhibitors except for SAHA (gold standard).
references[1]. suzuki t, hisakawa s, itoh y, et al. identification of a potent and stable antiproliferative agent by the prodrug formation of a thiolate histone deacetylase inhibitor. bioorg med chem lett, 2007, 17(6): 1558-1561. [2]. suzuki t, nagano y, kouketsu a, 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, 48(4): 1019-1032.[3]. sanda t, okamoto t, uchida y, et al. proteome analyses of the growth inhibitory effects of nch-51, a novel histone deacetylase inhibitor, on lymphoid malignant cells. leukemia, 2007, 21(11): 2344-2353. [4]. victoriano af, imai k, togami h, et al. novel histone deacetylase inhibitor nch-51 activates latent hiv-1 gene expression. febs lett, 2011, 585(7): 1103-1111.
PTACH Preparation Products And Raw materials

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