KDM2/7-IN-2
KDM2A/7-IN-1 is a lysine demethylase 2A (KDM2A) inhibitor with a human IC50 of 11 nM. KDM2A/7-IN-1 requires co-factor 2-oxoglutarate (2OG) for binding and occupies the H3K36me2 substrate pocket via a dimethylated lysine 36-mimicking group. KDM2A/7-IN-1 represses E2F-regulated genes, induces epithelial-mesenchymal transition, DNA repair, and mTOR pathways in specific cells, and selectively inhibits proliferation of ALT-positive cancer cell lines. KDM2A/7-IN-1 can be used for the research of ALT-positive cancers.
For research use only. We do not sell to patients.
- CAS No.: 1966932-74-0
- Formula: C25H30N2O2
- Molecular Weight:390.52
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
|
KDM7 9.6 nM (IC50) |
KDM2A 11 nM (IC50) |
KDM2B 13 nM (IC50) |
KDM2/7-IN-2 (Compound 183c) (3.5-10 μM; 1.5-4 weeks) selectively inhibits the proliferation of ALT-positive human cancer cell lines including SAOS2 in colony formation assays, while exerts weak effects on ALT-negative cell lines[1].
KDM2/7-IN-2 (11-14 days) potently inhibits the proliferation of ALT-positive SAOS2 human osteosarcoma cells in continuous growth assays, with an IC50 of 3 nM[1].
KDM2/7-IN-2 (10 μM; 3 days) induces an E2F-mediated core repressive transcriptional program in SAOS2 and SJSA1 cells, while triggering distinct adaptive responses: global downregulation of key functional pathways occurs in SAOS2 cells, whereas compensatory survival pathways are activated in SJSA1 cells, which may explain the differential sensitivity of the two cell lines to this compound[1].
KDM2/7-IN-2 (10 μM; 6 days) inhibits KDM2A activity in SJSA1 cells, increasing genome-wide H3K36me2 levels by approximately 4-fold[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1966932-74-0
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Molecular Weight 390.52
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Formula C25H30N2O2
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SMILES
CC[C@@H]1CCN(C[C@@H]1C(C2=CC3=CC=C(C(CC#N)=C3C=C2)OC)=O)C4CCC4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)