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DYRK1-IN-1 is a highly selective and ligand-efficient DYRK1A inhibitor. DYRK1-IN-1 inhibits DYRK1A phosphorylation activity with an IC50 value of 220 nM.
DYRK1-IN-1 can be used for the research of central nervous system penetrant DYRK1A chemical probe.
| Molecular Weight | 240.26 |
| Formula | C12H12N6 |
| CAS Number | 2814486-79-6 |
| Form | Solid |
| Solubility (25°C) | DMSO 20 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related DYRK Products |
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| Dyrk1A-IN-4
Dyrk1A-IN-4 is a potent and orally active DYRK1A and DYRK2 inhibitor with IC50s of 2 nM and 6 nM, respectively. |
| Woodtide
Woodtide is a substrate for the DYRK (DYRK) family of kinases whose sequence is based on that around the DYRK phosphorylation site in FKHR. |
| Aristolactam A IIIa
Aristolactam A IIIa (Sch 546909) is a DYRK1A Inhibitor. Aristolactam A IIIa inhibits platelet aggregation induced by arachidonic acid (AA), collagen and platelet-activating factor (PAF). Aristolactam A IIIa has strong cytotoxic effect on HeLa cells. |
| Dyrk1A-IN-5
Dyrk1A-IN-5 (compound 5j) is a potent and selective DYRK1A inhibitor, with an IC50 of 6 nM. Dyrk1A-IN-5 dose-dependently reduces the phosphorylation of Thr434 in SF3B1, with an IC50 of 0.5 μM. Dyrk1A-IN-5 inhibits phosphorylation of tau at Thr212, with an IC50 of 2.1 μM. Dyrk1A-IN-5 can be used for Down syndrome research. |
| GSK-626616
GSK-626616 is a potent, orally bioavailable inhibitor of DYRK3 (IC50=0.7 nM). GSK-626616 inhibits other members of the DYRK family (e.g., DYRK1A and DYRK2) with similar potency, which is a potential therapy for the treatment of anemia. |
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