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KDM5A-IN-1 is an orally available, potent and selective inhibitor of the pan-histidine lysine demethylase 5 KDM5, inhibiting KDM5A, KDM5B, and KDM5C with IC50 values of 45 nM, 56 nM, and 55 nM, respectively.KDM5A-IN-1 inhibits PC9 H3K4Me3, and may be useful in cancer research.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $149 | In Stock | |
1 mL x 10 mM (in DMSO) | $396 | In Stock |
Description | KDM5A-IN-1 is an orally available, potent and selective inhibitor of the pan-histidine lysine demethylase 5 KDM5, inhibiting KDM5A, KDM5B, and KDM5C with IC50 values of 45 nM, 56 nM, and 55 nM, respectively.KDM5A-IN-1 inhibits PC9 H3K4Me3, and may be useful in cancer research. |
Targets&IC50 | KDM5A:45 nM, KDM5C:55 nM, KDM5B:56 nM |
In vivo | KDM5A-IN-1 (compound 50, 5 mg/kg; oral administration; female CD-1 mice) exhibits moderate clearance in mice (28 mL/min/kg), good oral bioavailability (F% 34), significantly low plasma protein binding in mice (40%), and a half-life (t1/2) of 0.4 hours[1]. |
Molecular Weight | 290.36 |
Formula | C15H22N4O2 |
Cas No. | 1905481-36-8 |
Smiles | CC(C)c1cc([nH]n1)C(=O)N1CC[C@H](C1)NC(=O)C1CC1 |
Relative Density. | 1.25 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. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 30 mg/mL (103.32 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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