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).

Product information

CAS Number: 357649-93-5

Molecular Weight: 291.80

Formula: C14H14ClN3S

Chemical Name: 4-(4-chlorophenyl)-2-(2-cyclopentylidenehydrazin-1-yl)-1, 3-thiazole

Smiles: ClC1=CC=C(C=C1)C1=CSC(NN=C2CCCC2)=N1

InChiKey: YYTHPXHGWSAKIZ-UHFFFAOYSA-N

InChi: InChI=1S/C14H14ClN3S/c15-11-7-5-10(6-8-11)13-9-19-14(16-13)18-17-12-3-1-2-4-12/h5-9H,1-4H2,(H,16,18)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 25 mg/mL (85.68 mM; Need ultrasonic) Ethanol : 1 mg/mL (3.43 mM; Need ultrasonic) H2O : < 0.1 mg/mL (insoluble)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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. 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.

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.

Products are for research use only. Not for human use.