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KDM5 inhibitor compound 48
- Soluble in DMSO
- MF: C17H20N6O
- MW: 324.38
Description
KDM5 inhibitor compound 48 is a potent, selective and orally bioavailable KDM5 histone demethylase inhibitor with an IC50 value of 15.1 nM for KDM5A. The compound demonstrates improved cellular activity with an EC50 value of 0.34 μM for increasing H3K4me3 levels in PC9 cells, reflecting effective target engagement in cells.
The KDM5 family of lysine demethylases (KDM5A-D) regulates gene expression through removal of methyl groups from histone H3 lysine 4 (H3K4). Aberrant KDM5 activity has been implicated in cancer progression, epigenetic plasticity, drug resistance, and transcriptional regulation. KDM5 inhibitor compound 48 serves as a valuable chemical probe for studying KDM5 biology and epigenetic regulation in vivo and in vitro.
Key Features
- Potent and selective KDM5 inhibitor
- IC50: 15.1 nM for KDM5A
- EC50: 0.34 μM for H3K4me3 elevation in PC9 cells
- Orally bioavailable compound
- Chemical probe suitable for in vivo KDM5 studies
Applications
- KDM5 and histone demethylase research
- Epigenetics and chromatin regulation studies
- H3K4 methylation investigations
- Cancer biology and drug resistance research
- In vivo target validation studies
More Information
| Parent CAS No. | 1628210-26-3 |
|---|---|
| Chemical Name | 5-(1-tert-Butyl-1H-pyrazol-4-yl)-6-isopropyl-7-oxo-4,7-dihydropyrazolo[1,5-a]pyrimidine-3-carbonitrile |
| SMILES | N12N=CC(C#N)=C1NC(C1=CN(C(C)(C)C)N=C1)=C(C(C)C)C2=O |
| MFCD | N.A. |
| InChi | InChI=1S/C17H20N6O/c1-10(2)13-14(12-8-19-22(9-12)17(3,4)5)21-15-11(6-18)7-20-23(15)16(13)24/h7-10,21H,1-5H3 |
| InChiKey | KRXWJZIHQRIGSJ-UHFFFAOYSA-N |
| CID | 118908379 |
| Short Description | KDM5 inhibitor |
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