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P300-IN-6

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Catalog No. T218495 Copy Product Info
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P300-IN-6 is an orally active inhibitor of the histone acetyltransferase (HAT) p300 domain, with an IC50 value of 7 nM in humans. It suppresses c-Myc expression, reduces H3K18ac and H3K27ac levels, and inhibits cancer cell proliferation. Additionally, P300-IN-6 hinders tumor growth in xenograft mouse models and is suitable for research in multiple myeloma.

P300-IN-6

Cas No. 3034595-62-2
Pack SizePriceUSA StockGlobal StockQuantity
10 mgInquiry10-14 weeks10-14 weeks
50 mgInquiry10-14 weeks10-14 weeks
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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For research use only—not for human use. No sales to individuals. Use as intended only.
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Product Introduction

Bioactivity
Description
P300-IN-6 is an orally active inhibitor of the histone acetyltransferase (HAT) p300 domain, with an IC50 value of 7 nM in humans. It suppresses c-Myc expression, reduces H3K18ac and H3K27ac levels, and inhibits cancer cell proliferation. Additionally, P300-IN-6 hinders tumor growth in xenograft mouse models and is suitable for research in multiple myeloma.
Targets & IC50
p300 HAT:7 nM
In vitro
P300-IN-6 (Compound B6) is a potent inhibitor of the recombinant human p300 HAT domain, with an IC₅₀ of 7 nM. It effectively suppresses the proliferation of human multiple myeloma OPM-2 cells, showing an IC₅₀ of 8.8 nM. At a concentration of 100 nM over six days, P300-IN-6 achieves 70-80% growth inhibition of human prostate cancer 22RV1 cells. Additionally, in the range of 1-20 nM over 24 hours, it dose-dependently inhibits c-Myc expression and reduces H3K18ac/H3K27ac levels in OPM-2 and 22RV1 cells.
In vivo
P300-IN-6 (Compound B6) administered at a dose of 20 mg/kg via gavage once daily for 17 days achieved 60% tumor growth inhibition in the OPM-2 multiple myeloma xenograft model in mice.
Chemical Properties
Molecular Weight454.52
FormulaC26H26N6O2
Cas No.3034595-62-2
SmilesCN1C=2C(=CC=C(NC([C@H](NC[C@@H](C)C3=CC=C(C#N)C=C3)C4=CC=CC=C4)=O)N2)N(C)C1=O
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 µL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
µL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
Related Tags: P300-IN-6 in vivo | P300-IN-6 in vitro | P300-IN-6 formula | P300-IN-6 molecular weight