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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 | Inquiry | 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:(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. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 30 mg/mL (92.48 mM) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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