CPTH2

Research use only, not for human use.

CPTH2 is a specific histone acetyltransferase inhibitor modulating Gcn5 network in vitro and in vivo.

CPTH2 is a specific histone acetyltransferase inhibitor modulating Gcn5 network in vitro and in vivo, inhibits H3 acetylation and induces cell-cycle perturbation and apoptosis in U-937 cells; increases E1A CR3 transactivation of human adenovirus through inhibition of HAT GCN5, also reduces virus yield during infection; induces apoptosis and decreases the invasiveness of a ccRCC cell line through the inhibition of KAT3B.

CPTH2 (100 μM; 12, 24, 48 hours) causes a decrease in cell proliferation after as early as 12 h with a further significant reduction after 48 h stimulation. CPTH2 (100 μM; 12 or 48 hours) causes a comparable drop of the activity in both cell lines. CPTH2 (100 μM; 48 hours) produces a drastic increase in apoptotic/dead cell population after 48 h. CPTH2 (100 μM; 12, 24, 48 hours) shows a reduced acetylation of both global AcH3 histone and H3AcK18. CPTH2 (100 μM; 24, 48 hours) is capable to counteract invasion and migration of ccRCC-786-O cells in culture. CPTH2 (0.2, 0.5, 1 mM) inhibits the growth of a GCN5 deleted strain and a single catalytic mutant E173H. CPTH2 (0.6, 0.8 mM; for 24 hours) inhibits histone H3 acetylation in yeast cell cultures. CPTH2 inhibits the Gcn5p dependent functional network. Cell Proliferation Assay Cell Line:Papillary thyroid (K1) and clear cell Renal Cell Carcinoma (ccRCC-786-O) cell lines Concentration:100 μM Incubation Time:12, 24, 48 hoursResult:Caused a decrease in cell proliferation after as early as 12 h with a further significant reduction after 48 h stimulation. Cell Viability Assay Cell Line:K1 and ccRCC-786-O cell lines Concentration:100 μM Incubation Time:24 hours (K1 cell) and 48 hours (ccRCC-786-O cell)Result:Caused a comparable drop of the activity in both cell lines.Apoptosis Analysis Cell Line:ccRCC-786-O cells Concentration:100 μM Incubation Time:48 hours Result:Produced a drastic increase in apoptotic/dead cell population after 48 h.Western Blot Analysis Cell Line:ccRCC-786-O cells Concentration:100 μM Incubation Time:12, 24, 48 hours Result:Showed a reduced acetylation of both global AcH3 histone and H3AcK18.

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CPTH2 | CPTH 2 | CPTH-2

Chromatin/Epigenetic

HAT

HAT

Cancer

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357649-93-5

291.797

C14H14ClN3S

>98% (HPLC)

In Vitro:?DMSO : 16.67 mg/mL (57.13 mM)

ClC1=CC=C(C2=CSC(N/N=C3CCCC/3)=N2)C=C1

N-[4-(4-Chloro-phenyl)-thiazol-2-yl]-N'-cyclopentylidene-hydrazine

(-20℃)

With Ice Pack

≥ 2 years