2. Epigenetics
  3. Histone Demethylase
  4. CPI-455 hydrochloride

CPI-455 hydrochloride is a specific, pan-KDM5 inhibitor with an IC50 of 10 nM for KDM5A. CPI-455 hydrochloride mediates KDM5 inhibition, elevates global levels of H3K4me3, and decreases the number of drug-tolerant persister cancer cells in multiple cancer cell line models treated with standard chemotherapy or targeted agents.

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CPI-455 hydrochloride

CPI-455 hydrochloride Chemical Structure

CAS No. : 2095432-28-1

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Based on 10 publication(s) in Google Scholar

Other Forms of CPI-455 hydrochloride:

CPI-455 hydrochloride Related Antibodies

Top Publications Citing Use of Products

View All Histone Demethylase Isoform Specific Products:

View All Isoforms
KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6 KDM7

  • Biological Activity

  • Purity & Documentation

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Description

CPI-455 hydrochloride is a specific, pan-KDM5 inhibitor with an IC50 of 10 nM for KDM5A. CPI-455 hydrochloride mediates KDM5 inhibition, elevates global levels of H3K4me3, and decreases the number of drug-tolerant persister cancer cells in multiple cancer cell line models treated with standard chemotherapy or targeted agents[1].

IC50 & Target

KDM5

 

In Vitro

CPI-455 hydrochloride mediates KDM5 inhibition, elevates global levels of H3K4 trimethylation (H3K4me3) and decreases the number of DTPs in multiple cancer cell line models treated with standard chemotherapy or targeted agents[1].
CPI-455 hydrochloride, with high measured affinity for the target KDM5 proteins. Within 24 hours, increases in H3K4me3, are observed after exposure to either of the two active compounds, CPI-455 and CPI-766, in a dosedependent manner. IC50 calculation for KDM5 Inhibitor CPI0455 in 3 luminal breast cancer cell lines MCF-7, T-47 and EFM-19 are 35.4, 26.19 and 16.13 μM, respectively[2].

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

CPI-455 hydrochloride Related Antibodies
In Vivo

Dual blockade of B7-H4 and KDM5B (CPI-455 hydrochloride, 50/70 mg/kg, ip, daily) in mice elicits protective immunity[2].

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

314.77

Formula

C16H15ClN4O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

N#CC1=C2NC(C3=CC=CC=C3)=C(C(C)C)C(N2N=C1)=O.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 8.33 mg/mL (26.46 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 3.1769 mL 15.8846 mL 31.7692 mL
5 mM 0.6354 mL 3.1769 mL 6.3538 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 (sealed storage, away from moisture). 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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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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Volume (start)

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Concentration (final)

C2

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Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

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g

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(per animal)

μL

Number of animals

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 (sealed storage, away from moisture). 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 3.1769 mL 15.8846 mL 31.7692 mL 79.4231 mL
5 mM 0.6354 mL 3.1769 mL 6.3538 mL 15.8846 mL
10 mM 0.3177 mL 1.5885 mL 3.1769 mL 7.9423 mL
15 mM 0.2118 mL 1.0590 mL 2.1179 mL 5.2949 mL
20 mM 0.1588 mL 0.7942 mL 1.5885 mL 3.9712 mL
25 mM 0.1271 mL 0.6354 mL 1.2708 mL 3.1769 mL
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CPI-455 hydrochloride 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:

CPI-4552095432-28-1CPI455CPI 455Histone DemethylaseInhibitorinhibitorinhibit

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