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Cat. No.: HY-187178

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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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Please store the product under the recommended conditions in the Certificate of Analysis.

KDM2/7-IN-2 Chemical Structure

CAS No.: 1966932-74-0

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
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- IC₅₀ & Target
- In Vitro
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Biological Activity

Description

IC₅₀ & Target

^[1]

KDM7

9.6 nM (IC₅₀)

KDM2A

11 nM (IC₅₀)

KDM2B

13 nM (IC₅₀)

All Histone Demethylase Isoforms :

In Vitro

Anti-cancerOthers

Anti-cancer

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].

Others

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.

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Chemical Information

CAS No. 1966932-74-0
Molecular Weight 390.52
Formula C₂₅H₃₀N₂O₂
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Mader P, et al. Structure and mechanism of inhibition of lysine demethylase 2A (KDM2A) by compound 183c. Communications chemistry. 2026 Jun 27. [Content Brief]

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How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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KDM2/7-IN-2

All Histone Demethylase Isoforms

Biological Activity

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IC50 & Target

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