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KDM5-IN-1 is an effective and selective inhibitor of KDM5 with an IC50 of 15.1 nM.

| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $58 | In Stock | |
| 5 mg | $196 | In Stock | |
| 10 mg | $298 | In Stock | |
| 25 mg | $475 | In Stock | |
| 50 mg | $678 | In Stock | |
| 100 mg | $912 | In Stock | |
| 500 mg | Preferential | In Stock | |
| 1 mL x 10 mM (in DMSO) | $139 | In Stock |
| Description | KDM5-IN-1 is an effective and selective inhibitor of KDM5 with an IC50 of 15.1 nM. |
| Targets&IC50 | PC9 H3K4Me3 cells:(EC50)0.34 μM, KDM5:15.1 nM |
| In vitro | KDM5-IN-1 is significantly less potent against other KDM enzymes (1A, 2B, 3B, 4C, 5A, 6A, 7B), inhibiting KDM4C the strongest with an IC50 of 1.9 μM. KDM5-IN-1 potently inhibits KDM5B and KDM5C isoforms (IC50 of 4.7 and 65.5 nM, respectively)[1]. |
| In vivo | KDM5-IN-1(50 mg/kg; oral) shows an unbound maximal plasma concentration Cmax>15-fold over its cell EC50 in vivo[1]. |
| Molecular Weight | 324.38 |
| Formula | C17H20N6O |
| Cas No. | 1628210-26-3 |
| Smiles | CC(C)c1c([nH]c2c(cnn2c1=O)C#N)-c1cnn(c1)C(C)(C)C |
| Relative Density. | 1.28 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 30 mg/mL (92.48 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (6.17 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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