1. Epigenetics Apoptosis
  2. Histone Acetyltransferase Apoptosis
  3. CPTH2 hydrochloride

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).

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CPTH2 hydrochloride Chemical Structure

CPTH2 hydrochloride Chemical Structure

CAS No. : 2108899-91-6

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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].

IC50 & Target[1][2]

GCN5

 

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

328.26

Formula

C14H15Cl2N3S

CAS No.
SMILES

ClC1=CC=C(C2=CSC(N/N=C3CCCC/3)=N2)C=C1.[H]Cl

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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References
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CPTH2 hydrochloride Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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CPTH2 hydrochloride
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