2. Epigenetics
  3. Histone Acetyltransferase Epigenetic Reader Domain
  4. CBP/p300-IN-20

CBP/p300-IN-20 is a potent and selective p300/CBP inhibitor, with a pIC50 of 10.1 for p300. CBP/p300-IN-20 can be used for the research of cancer.

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

CBP/p300-IN-20 Chemical Structure

CBP/p300-IN-20 Chemical Structure

CAS No. : 2999742-92-4

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5 mg USD 560 In-stock
10 mg USD 900 In-stock
25 mg USD 1800 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

CBP/p300-IN-20 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

CBP/p300-IN-20 is a potent and selective p300/CBP inhibitor, with a pIC50 of 10.1 for p300. CBP/p300-IN-20 can be used for the research of cancer[1].

IC50 & Target[1]

CBP/p300

10.1 (pIC50)

In Vitro

CBP/p300-IN-20 (compound 28) decreases Myc protein in cell-based cMyc HTRF assay, with a pEC50 of 8.5[1].
CBP/p300-IN-20 (1 μM) shows 97% inhibition for p300 and 80% inhibition for CPB[1].
CBP/p300-IN-20 (0.3-1000 nM; 2 h) decreases H3K18 and H3K27 acetylation without affecting H3K9 acetylation and total H3 in COLO 320HSR cells[1].

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

CBP/p300-IN-20 Related Antibodies

Western Blot Analysis[1]

Cell Line: COLO 320HSR cells
Concentration: 0.3, 1, 3, 10, 30, 100, 300, 1000 nM
Incubation Time: 2 hours
Result: Caused a rapid concentration-dependent decrease in H3K18 and H3K27 acetylation without affecting H3K9 acetylation and total H3.
In Vivo

CBP/p300-IN-20 (compound 28) (0.54 mg/kg; i.v.) exhibits Cmax (210 ng/mL), AUC0→∞ (102 h•ng/mL), CL (95 mL/min/kg), and T1/2 (0.3 h) in rats[1].

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

477.87

Formula

C22H19ClF3N5O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C([C@@H]1N(C(C2(CC(F)(F)C2)C3=CC=C(Cl)C=C3)=O)C[C@H](F)C1)NC4=CC=C5NN=CC5=N4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 200 mg/mL (418.52 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0926 mL 10.4631 mL 20.9262 mL
5 mM 0.4185 mL 2.0926 mL 4.1852 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: ≥ 5 mg/mL (10.46 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 5 mg/mL (10.46 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
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).
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
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. 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
DMSO 1 mM 2.0926 mL 10.4631 mL 20.9262 mL 52.3155 mL
5 mM 0.4185 mL 2.0926 mL 4.1852 mL 10.4631 mL
10 mM 0.2093 mL 1.0463 mL 2.0926 mL 5.2315 mL
15 mM 0.1395 mL 0.6975 mL 1.3951 mL 3.4877 mL
20 mM 0.1046 mL 0.5232 mL 1.0463 mL 2.6158 mL
25 mM 0.0837 mL 0.4185 mL 0.8370 mL 2.0926 mL
30 mM 0.0698 mL 0.3488 mL 0.6975 mL 1.7438 mL
40 mM 0.0523 mL 0.2616 mL 0.5232 mL 1.3079 mL
50 mM 0.0419 mL 0.2093 mL 0.4185 mL 1.0463 mL
60 mM 0.0349 mL 0.1744 mL 0.3488 mL 0.8719 mL
80 mM 0.0262 mL 0.1308 mL 0.2616 mL 0.6539 mL
100 mM 0.0209 mL 0.1046 mL 0.2093 mL 0.5232 mL
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CBP/p300-IN-20 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:

CBP/p300-IN-202999742-92-4Histone AcetyltransferaseEpigenetic Reader DomainHATsHATH3K18H3K27acetylationH3K9total H3Inhibitorinhibitorinhibit

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