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CPTH2 hydrochloride

Names

[ CAS No. ]:
2108899-91-6

[ Name ]:
CPTH2 hydrochloride

[Synonym ]:
4-(4-Chlorophenyl)-2-(2-cyclopentylidenehydrazino)-1,3-thiazole hydrochloride (1:1)
Cyclopentanone, 2-[4-(4-chlorophenyl)-2-thiazolyl]hydrazone, hydrochloride (1:1)
CPTH2 (hydrochloride)

Biological Activity

[Description]:

CPTH2 hydrochloride is a potent histone acetyltransferase (HAT) inhibitor. CPTH2 hydrochloride selectively inhibits the acetylation of histone H3 by Gcn5. CPTH2 hydrochloride induces apoptosis and decreases the invasiveness of a clear cell renal carcinoma (ccRCC) cell line through the inhibition of acetyltransferase p300 (KAT3B)[1][2].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis
Research Areas >> Cancer
Signaling Pathways >> Epigenetics >> Histone Acetyltransferase

[Target]

GCN5

p300


[In Vitro]

CPTH2 (100 μM; 12, 24, 48 hours) hydrochloride causes a decrease in cell proliferation after as early as 12 h with a further significant reduction after 48 h stimulation[1]. CPTH2 (100 μM; 12 or 48 hours) hydrochloride causes a comparable drop of the activity in both cell lines[1]. CPTH2 (100 μM; 48 hours) hydrochloride produces a drastic increase in apoptotic/dead cell population after 48 h[1]. CPTH2 (100 μM; 12, 24, 48 hours) hydrochloride shows a reduced acetylation of both global AcH3 histone and H3AcK18[1]. CPTH2 (100 μM; 24, 48 hours) hydrochloride is capable to counteract invasion and migration of ccRCC-786-O cells in culture[1]. CPTH2 (0.2, 0.5, 1 mM) hydrochloride inhibits the growth of a GCN5 deleted strain and a single catalytic mutant E173H[2]. CPTH2 (0.6, 0.8 mM; for 24 hours) hydrochloride inhibits histone H3 acetylation in yeast cell cultures[2]. CPTH2 hydrochloride inhibits the Gcn5p dependent functional network[2]. Cell Proliferation Assay[1] Cell Line: Papillary thyroid (K1) and clear cell Renal Cell Carcinoma (ccRCC-786-O) cell lines Concentration: 100 μM Incubation Time: 12, 24, 48 hours Result: Caused a decrease in cell proliferation after as early as 12 h with a further significant reduction after 48 h stimulation. Cell Viability Assay[1] 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[1] 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[1] 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.

[References]

[1]. Cocco E, et al. KAT3B-p300 and H3AcK18/H3AcK14 levels are prognostic markers for kidney ccRCC tumoraggressiveness and target of KAT inhibitor CPTH2. Clin Epigenetics. 2018 Apr 4;10:44.

[2]. Chimenti F, et al. A novel histone acetyltransferase inhibitor modulating Gcn5 network: cyclopentylidene-[4-(4'-chlorophenyl)thiazol-2-yl)hydrazone. J Med Chem. 2009 Jan 22;52(2):530-6.

Chemical & Physical Properties

[ Molecular Formula ]:
C14H15Cl2N3S

[ Molecular Weight ]:
328.260

[ Exact Mass ]:
327.036377

Safety Information

[ Hazard Codes ]:
Xi


Related Compounds