CPTH2

Modify Date: 2024-01-07 23:17:42

CPTH2 Structure
CPTH2 structure
 Common Name CPTH2
CAS Number 357649-93-5 Molecular Weight 291.79900
Density N/A Boiling Point N/A
Molecular Formula C14H14ClN3S Melting Point N/A
MSDS Chinese USA Flash Point N/A

 Use of CPTH2


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

 Names

Name 4-(4-chlorophenyl)-N-(cyclopentylideneamino)-1,3-thiazol-2-amine
Synonym More Synonyms

 CPTH2 Biological Activity

Description CPTH2 is a potent histone acetyltransferase (HAT) inhibitor. CPTH2 selectively inhibits the acetylation of histone H3 by Gcn5. CPTH2 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
Target

GCN5

p300

In Vitro 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[1]. CPTH2 (100 μM; 12 or 48 hours) causes a comparable drop of the activity in both cell lines[1]. CPTH2 (100 μM; 48 hours) produces a drastic increase in apoptotic/dead cell population after 48 h[1]. CPTH2 (100 μM; 12, 24, 48 hours) shows a reduced acetylation of both global AcH3 histone and H3AcK18[1]. CPTH2 (100 μM; 24, 48 hours) is capable to counteract invasion and migration of ccRCC-786-O cells in culture[1]. CPTH2 (0.2, 0.5, 1 mM) inhibits the growth of a GCN5 deleted strain and a single catalytic mutant E173H[2]. CPTH2 (0.6, 0.8 mM; for 24 hours) inhibits histone H3 acetylation in yeast cell cultures[2]. CPTH2 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 C14H14ClN3S
Molecular Weight 291.79900
Exact Mass 291.06000
PSA 65.52000
LogP 4.87840
Storage condition 2-8°C

 Safety Information

RIDADR NONH for all modes of transport

 Precursor & DownStream

Precursor  2

DownStream  0

 Articles1

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 Synonyms

cpth2
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Related Compounds: More...
CPTH2 hydrochloride
2108899-91-6
Chemsrc provides CPTH2(CAS#:357649-93-5) MSDS, density, melting point, boiling point, structure, formula, molecular weight etc. Articles of CPTH2 are included as well.>> amp version: CPTH2

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