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

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CPTH2 Chemical Structure

CPTH2 Chemical Structure

CAS No. : 357649-93-5

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO USD 154 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of CPTH2:

CPTH2 Related Antibodies

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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

 

Cellular Effect
Cell Line Type Value Description References
BTI-TN-5B1-4 IC50
262 nM
Compound: 2
Inhibition of human recombinant MAOB expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as hydrogen peroxide production from p-tyramine by amplex red assay
Inhibition of human recombinant MAOB expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as hydrogen peroxide production from p-tyramine by amplex red assay
[PMID: 20579890]
BTI-TN-5B1-4 IC50
7160 nM
Compound: 2
Inhibition of human recombinant MAOA expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as hydrogen peroxide production from p-tyramine by amplex red assay
Inhibition of human recombinant MAOA expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as hydrogen peroxide production from p-tyramine by amplex red assay
[PMID: 20579890]
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].

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

CPTH2 Related Antibodies

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

Formula

C14H14ClN3S
CAS No.
Appearance

Solid

Color

White to off-white

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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

H2O : < 0.1 mg/mL (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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a suspended solution of ≥ 1.67 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.82%

SDS (393 KB)

COA (247 KB) RP-HPLC (258 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 3.4270 mL 17.1350 mL 34.2700 mL 85.6751 mL
DMSO 5 mM 0.6854 mL 3.4270 mL 6.8540 mL 17.1350 mL
10 mM 0.3427 mL 1.7135 mL 3.4270 mL 8.5675 mL
15 mM 0.2285 mL 1.1423 mL 2.2847 mL 5.7117 mL
20 mM 0.1714 mL 0.8568 mL 1.7135 mL 4.2838 mL
25 mM 0.1371 mL 0.6854 mL 1.3708 mL 3.4270 mL
30 mM 0.1142 mL 0.5712 mL 1.1423 mL 2.8558 mL
40 mM 0.0857 mL 0.4284 mL 0.8568 mL 2.1419 mL
50 mM 0.0685 mL 0.3427 mL 0.6854 mL 1.7135 mL
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CPTH2 Related Classifications

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.

Keywords:

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

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