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CPI 4203
- Soluble in DMSO
- MF: C16H14N4O
- MW: 278.31
Description
CPI-4203 is a selective KDM5 histone demethylase inhibitor with an IC50 value of 250 nM for inhibition of full-length KDM5A. CPI-4203 is structurally related to the potent KDM5 inhibitor CPI-455 (Axon 2573) but is approximately 25-fold less potent, making it a useful comparator and control compound for KDM5 inhibition studies.
The KDM5 family of lysine demethylases (KDM5A-D) regulates gene expression through demethylation of histone H3 lysine 4 (H3K4), a key epigenetic mark associated with active transcription. KDM5 proteins have been implicated in cancer progression, transcriptional regulation, cellular plasticity, and drug resistance. CPI-4203 serves as a valuable tool for validating KDM5-dependent biological effects and is commonly used alongside CPI-455 in epigenetics and chromatin biology research.
Key Features
- Selective KDM5 histone demethylase inhibitor
- IC50: 250 nM for full-length KDM5A
- Structurally related to CPI-455
- Approximately 25-fold less potent than CPI-455
- Useful control compound for KDM5 studies
Applications
- KDM5 and histone demethylase research
- Epigenetics and chromatin biology studies
- H3K4 methylation investigations
- Cancer biology and transcriptional regulation research
- KDM5 target validation experiments
More Information
| Parent CAS No. | 1628214-07-2 |
|---|---|
| Chemical Name | 6-ethyl-7-oxo-5-o-tolyl-4,7-dihydropyrazolo[1,5-a]pyrimidine-3-carbonitrile |
| SMILES | C12=C(C#N)C=NN1C(=O)C(CC)=C(C1=C(C)C=CC=C1)N2 |
| MFCD | N.A. |
| InChi | InChI=1S/C16H14N4O/c1-3-12-14(13-7-5-4-6-10(13)2)19-15-11(8-17)9-18-20(15)16(12)21/h4-7,9,19H,3H2,1-2H3 |
| InChiKey | OXELDRCVUWWSFZ-UHFFFAOYSA-N |
| CID | 90442348 |
| Short Description | KDM5 inhibitor |
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