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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 | KDM4C:83 μM, KDM7A:0.2 μM, KDM2A:6.8 μM, KDM7B:1.2 μM, KDM5A:55 μM, KDM4A:>120 μM, KDM6A:>100 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) |
| 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. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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