Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DYRK1-IN-1 is a highly selective and ligand-efficient DYRK1A inhibitor. DYRK1-IN-1 inhibits DYRK1A phosphorylation activity with an IC 50 value of 220 nM. DYRK1-IN-1 exhibits good permeability and cellular activity without P-glycoprotein liability that can be used for the research of central nervous system penetrant DYRK1A chemical probe [1].
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
100 mg | 10-14 weeks | $ 1,450.00 | |
200 mg | 10-14 weeks | $ 1,942.00 |
Description | DYRK1-IN-1 is a highly selective and ligand-efficient DYRK1A inhibitor. DYRK1-IN-1 inhibits DYRK1A phosphorylation activity with an IC 50 value of 220 nM. DYRK1-IN-1 exhibits good permeability and cellular activity without P-glycoprotein liability that can be used for the research of central nervous system penetrant DYRK1A chemical probe [1]. |
In vitro | DYRK1-IN-1 is a potent inhibitor of DYRK1A phosphorylation, achieving inhibition with an IC 50 value of 220 nM and demonstrating an ability to inhibit tau phosphorylation at an IC 50 of 0.59 μM. This compound exhibits good permeability and cellular activity, devoid of P-glycoprotein liability. It also possesses excellent physicochemical characteristics, including high enzymatic potency, favorable aqueous solubility, outstanding kinome selectivity, and robust on-target in vitro inhibition efficacy. In HEK293 cells, DYRK1-IN-1 shows satisfactory cellular activity with an IC 50 of 434 nM, in comparison to an enzymatic IC 50 of 75 nM. |
In vivo | DYRK1-IN-1 (1 mg/kg; i.v.) has high clearance [1]. Animal Model: Sprague Dawley rats [1] Dosage: 1 mg/kg (Pharmacokinetic Analysis) Administration: I.v. Result: High clearance was observed. |
Molecular Weight | 240.26 |
Formula | C12H12N6 |
CAS No. | 2814486-79-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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DYRK1-IN-1 2814486-79-6 inhibitor inhibit