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GNF2133 is a potent, selective, orally active DYRK1A inhibitor with IC50s of 0.0062 and >50 µM for DYRK1A and GSK3β, respectively. GNF2133 shows good proliferation potency and efficacy on rat and human primary β-cell. GNF2133 significantly improves glucose disposal capacity and increases insulin secretion. GNF2133 has potential for the study of type 1 diabetes.
| Molecular Weight | 434.53 |
| Formula | C24H30N6O2 |
| CAS Number | 2561414-56-8 |
| Solubility (25°C) | DMSO 4 mg/mL (ultrasonic and warming) |
| 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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| DYRK1-IN-1
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. |
| 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. |
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Products are for research use only. Not for human use. We do not sell to patients.
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