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CPI 455
- Soluble in DMSO
- MF: C16H14N4O
- MW: 278.31
Description
CPI-455 is a potent and selective KDM5 histone demethylase inhibitor with an IC50 value of 10 nM for inhibition of full-length KDM5A. CPI-455 specifically increases histone H3 lysine 4 (H3K4) methylation in multiple cellular contexts, demonstrating robust target engagement and modulation of epigenetic regulation.
The KDM5 family of lysine demethylases (KDM5A-D) regulates gene expression through removal of methyl groups from H3K4, an epigenetic mark associated with active transcription. Aberrant KDM5 activity has been linked to cancer progression, transcriptional plasticity, and the emergence of drug-tolerant persister (DTP) cells. CPI-455 reduces survival of drug-tolerant cancer cells and serves as a high-quality chemical probe for investigating KDM5-dependent disease biology, epigenetic regulation, and therapeutic resistance mechanisms.
Key Features
- Potent and selective KDM5 inhibitor
- IC50: 10 nM for full-length KDM5A
- Increases cellular H3K4 methylation
- Reduces survival of drug-tolerant cancer cells
- Widely used chemical probe for KDM5 biology
Applications
- KDM5 and histone demethylase research
- Epigenetics and chromatin biology studies
- H3K4 methylation investigations
- Cancer biology and drug tolerance research
- Target validation and transcriptional regulation studies
Related Product
CPI-4203 (Axon 2622) is a structurally related but approximately 25-fold less potent KDM5 inhibitor that has been used as a comparator and control compound in KDM5 target validation studies. CPI-455 and CPI-4203 were reported together in the original Nature publication describing selective KDM5 inhibition.
More Information
| Parent CAS No. | 1628208-23-0 |
|---|---|
| Chemical Name | 6-isopropyl-7-oxo-5-phenyl-4,7-dihydropyrazolo[1,5-a]pyrimidine-3-carbonitrile |
| SMILES | C12=C(C#N)C=NN1C(=O)C(C(C)C)=C(C1=CC=CC=C1)N2 |
| MFCD | N.A. |
| InChi | InChI=1S/C16H14N4O/c1-10(2)13-14(11-6-4-3-5-7-11)19-15-12(8-17)9-18-20(15)16(13)21/h3-7,9-10,19H,1-2H3 |
| InChiKey | DHXKRMSKXLDZGY-UHFFFAOYSA-N |
| CID | 78426698 |
| Short Description | KDM5 inhibitor |
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