research use only

CP2 Histone Demethylase inhibitor

Cat.No.S8601

CP2 is a cyclic peptide that inhibits the JmjC histone demethylases KDM4 with IC50 values of 42 nM and 29 nM for KDM4A and KDM4C, respectively.

Chemical Structure

Molecular Weight: 2010.15

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.36%

99.36

Related Targets	Epigenetic Reader Domain HDAC JAK Histone Methyltransferase AMPK PKC PARP HIF Histone Acetyltransferase Aurora Kinase Sirtuin PRMT EZH1/2 DNA Methyltransferase Pim LSD1 MLL JMJD G9a/GLP NSD FTO MicroRNA PAD SETD SMYD DOT1 COMT WDR5 HNMT SAM MTase
Related Products	GSK-J4 Hydrochloride SP2509 CPI-455 HCl Iadademstat (ORY-1001) 2HCl GSK-LSD1 2HCl JIB-04 OG-L002 ML324 IOX1 GSK J1 CPI-455

Chemical Information, Storage & Stability

Molecular Weight	2010.15	Formula	C₉₂H₁₂₀N₂₄O₂₆S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	no CAS	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC(C)C1NC(=O)C(CC2=CC=C(O)C=C2)NNC(CC(O)=O)C(=O)C(=O)CSCC(NC(=O)C(NC(=O)C(CC3=CC=C(O)C=C3)NC(=O)C(CC4=C[NH]C5=C4C=CC=C5)NC(=O)C(CCCNC(N)=N)NC(=O)C(CC6=C[NH]C7=C6C=CC=C7)NC(=O)CNC(=O)C(CO)NC(=O)C(CCCNC

Solubility

In vitro
Batch:

Water : 100 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (2.49mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.250mg/ml (0.62mM)	Taking the 1 mL working solution as an example, add 50 μL of 25 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	KDM4C ^[1] (Cell-free assay) 29 nM KDM4A ^[1] (Cell-free assay) 42 nM
In vitro	CP2 uniquely binds in the KDM4A substrate-binding pocket. It binds differently to, but competes with, histone substrates in the active site^[1].
References	https://www.nature.com/articles/ncomms14773

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT01241812	Completed	Knee Osteoarthritis	University of British Columbia\|Canadian Arthritis Network	October 2010	Not Applicable
NCT00261846	Completed	Chronic Myeloid Leukemia	Pfizer	January 18 2006	Phase 2

Tech Support

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