1. Epigenetics
  2. Histone Acetyltransferase
  3. CBP/p300-IN-5

P300/CBP-IN-5 is a potent p300/CBP histone acetyltransferase inhibitor extracted from patent WO2016044770A1, Example 715, has an IC50 of 18.8 nM.

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

CBP/p300-IN-5 Chemical Structure

CBP/p300-IN-5 Chemical Structure

CAS No. : 1889284-33-6

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Description

P300/CBP-IN-5 is a potent p300/CBP histone acetyltransferase inhibitor extracted from patent WO2016044770A1, Example 715, has an IC50 of 18.8 nM[1].

IC50 & Target

CBP/p300

 

In Vitro

P300/CBP-IN-5 inhibits p300 LnCap-FGC cellls proliferation with an IC50 of 14.8 nM. P300/CBP-IN-5 inhibits H3K27Ac with an IC50 value of 4.6 nM in PC-3 cells[1].

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

In Vivo

The effect of P300/CBP-IN-5 (Example 715) on tumor growth is evaluated in subcutaneous, SuDHL-8 (B-cell lymphoma) and 22RV1 (prostate) xenograft tumors implanted in SCID female mice. Human cancer cells are inoculated subcutaneously into the right hind flank of female SCID mice on study day 0. Administration of P300/CBP-IN-5 (7.5 mg/kg/day) is initiated at the time of size match. P300/CBP-IN-5 induces significant tumor growth inhibition in multiple xenograft tumor models (the tumor growth inhibition of 62% in SuDHL-8 xenograft tumor model; 48% in 22RV1 xenograft tumor model)[1].

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

Molecular Weight

618.55

Formula

C29H27F5N6O4

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(CN(C1=O)C(N[C@@]21C[C@H](C3=C2C=CC(C4=CN(N=C4)CC(NC)=O)=C3)F)=O)N([C@H](C(F)(F)F)C)CC5=CC=C(C=C5)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 60 mg/mL (97.00 mM; Need ultrasonic and warming; 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 1.6167 mL 8.0834 mL 16.1668 mL
5 mM 0.3233 mL 1.6167 mL 3.2334 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)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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.
Calculation results:
Working solution concentration: mg/mL
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 1.6167 mL 8.0834 mL 16.1668 mL 40.4171 mL
5 mM 0.3233 mL 1.6167 mL 3.2334 mL 8.0834 mL
10 mM 0.1617 mL 0.8083 mL 1.6167 mL 4.0417 mL
15 mM 0.1078 mL 0.5389 mL 1.0778 mL 2.6945 mL
20 mM 0.0808 mL 0.4042 mL 0.8083 mL 2.0209 mL
25 mM 0.0647 mL 0.3233 mL 0.6467 mL 1.6167 mL
30 mM 0.0539 mL 0.2694 mL 0.5389 mL 1.3472 mL
40 mM 0.0404 mL 0.2021 mL 0.4042 mL 1.0104 mL
50 mM 0.0323 mL 0.1617 mL 0.3233 mL 0.8083 mL
60 mM 0.0269 mL 0.1347 mL 0.2694 mL 0.6736 mL
80 mM 0.0202 mL 0.1010 mL 0.2021 mL 0.5052 mL
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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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Product Name:
CBP/p300-IN-5
Cat. No.:
HY-100132
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