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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 |
|---|
| ID-8
Id-8 is a DYRK inhibitor that maintains the self-renewal of embryonic stem cells in long-term culture. |
| Harmine-hydrochloride
Harmine Hydrochloride (Telepathine Hydrochloride) is a DYRK inhibitor with anticancer and anti-inflammatory activities. Harmine Hydrochloride has a high affinity for 5-HT2A serotonin receptor, with a Ki value of 397 nM. |
| Harmine
Harmine is a potent and selective DYRK1A inhibitor. |
| Protein kinase inhibitors 1
Protein kinase inhibitors 1 is a novel inhibitor of HIPK2 with an IC50 of 74 nM and Kd of 9.5 nM. |
| GNF4877
GNF4877 is a potent DYRK1A and GSK3β inhibitor with IC50s of 6 nM and 16 nM, respectively, which leads to blockade of nuclear factor of activated T-cells (NFATc) nuclear export and increased β-cell proliferation (EC50 of 0.66 μM for mouse β (R7T1) cells). |
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