2. Epigenetics
    Apoptosis
  3. Histone Acetyltransferase
    Apoptosis
  4. CPTH2

CPTH2 

Cat. No.: HY-W013274 Purity: 99.79%
COA Handling Instructions

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).

For research use only. We do not sell to patients.

CPTH2 Chemical Structure

CPTH2 Chemical Structure

CAS No. : 357649-93-5

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Based on 1 publication(s) in Google Scholar

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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].

IC50 & Target[1]

GCN5

 

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].

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

291.80

Appearance

Solid

Formula

C14H14ClN3S
CAS No.
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
In Vitro: 

DMSO : 16.67 mg/mL (57.13 mM; ultrasonic and warming and heat to 60°C)

Ethanol : 1 mg/mL (3.43 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (ultrasonic) (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4270 mL 17.1350 mL 34.2701 mL
5 mM 0.6854 mL 3.4270 mL 6.8540 mL
10 mM 0.3427 mL 1.7135 mL 3.4270 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.67 mg/mL (5.72 mM); Suspended solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.79%

COA (246 KB) HNMR (116 KB) RP-HPLC (181 KB)

Handling Instructions (2659 KB)
References
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Help & FAQs
  • 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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Keywords:

CPTH2357649-93-5CPTH 2CPTH-2Histone AcetyltransferaseApoptosisHATsHAThistoneH3apoptosiscarcinomaccRCCacetyltransferaseKAT3BGcn5pInhibitorinhibitorinhibit

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