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KDM2/7-IN-1 (TC-E 5002) is a selective small-molecule inhibitor of the KDM2/7 histone demethylase subfamily, exhibiting IC50 values of 0.2, 1.2, 6.8, 55, 83, >100, and >120 μM for KDM7A, KDM7B, KDM2A, KDM5A, KDM4C, KDM6A, and KDM4A, respectively. KDM2/7-IN-1 inhibits the proliferation of HeLa and KYSE-150 cancer cells in vitro, highlighting its utility in epigenetic and oncology research.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $61 | - | In Stock | |
| 5 mg | $147 | - | In Stock | |
| 10 mg | $217 | - | In Stock | |
| 25 mg | $367 | - | In Stock | |
| 50 mg | Preferential | - | In Stock |
| Description | KDM2/7-IN-1 (TC-E 5002) is a selective small-molecule inhibitor of the KDM2/7 histone demethylase subfamily, exhibiting IC50 values of 0.2, 1.2, 6.8, 55, 83, >100, and >120 μM for KDM7A, KDM7B, KDM2A, KDM5A, KDM4C, KDM6A, and KDM4A, respectively. KDM2/7-IN-1 inhibits the proliferation of HeLa and KYSE-150 cancer cells in vitro, highlighting its utility in epigenetic and oncology research. |
| Targets&IC50 | KDM7A:0.2 μM, KDM6A:>100 μM, KDM7B:1.2 μM, KDM4A:>120 μM, KDM4C:83 μM, KDM5A:55 μM, KDM2A:6.8 μM |
| In vitro | KDM2/7-IN-1 exhibits anti-proliferative activity in N2a cells with a GI50 value of 86 μM [1]. In HeLa and KYSE150 cells, KDM2/7-IN-1 significantly inhibits cell growth and is associated with elevated H3K27me2 levels [1]. After KDM2/7-IN-1 treatment, the expression of the E2F1 gene in HeLa cells markedly decreases, and the cell cycle arrests at the G0/G1 phase [1]. |
| Synonyms | TC-E 5002 |
| Molecular Weight | 285.38 |
| Formula | C15H27NO4 |
| Cas No. | 1453071-47-0 |
| Smiles | O=C(O)CCN(O)C(=O)CCCCCCCCC1CC1 |
| Relative Density. | 1.130 g/cm3 (Predicted) |
| Color | White |
| Appearance | Solid |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 24 mg/mL (84.1 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
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DMSO
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