About 10 results found for searched term "DYRK1-IN-1" (0.13 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M7390 | TC-S 7004 | Others |
| Dyrk1B/A-IN-1 | ||
| TC-S 7004 is a potent and selective DYRK1A/B inhibitor. | ||
| M58573 | DYRK1-IN-1 | DYRK |
| 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. | ||
| M8642 | FINDY | Others |
| FINDY is a cell-permeable thioxothiazolidinone derivative that specifically targets newly synthesized cellular DYRK1A, but not DYRK1B or DYRK2, for proteasomal degradation by suppressing DYKR1A intramolecular Ser97 autophosphorylation, a necessary event for folding/maturation of newly translated DYRK1A. | ||
| M14889 | GNF4877 | DYRK |
| 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). | ||
| M21230 | GNF2133 | DYRK |
| GNF2133 is a potent, selective, orally active DYRK1A inhibitor with IC50s of 0.0062 and >50 µM for DYRK1A and GSK3β, respectively. GNF2133 has potential for the study of type 1 diabetes. | ||
| M27658 | GSK-626616 | DYRK |
| 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. | ||
| M27803 | Leucettine L41 | CDK |
| Leucettine L41 is a potent inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A), DYRK2, CDC-like kinase 1 (CLK1), and CLK3 (IC50s = 0.04, 0.035, 0.015, and 4.5 µM, respectively). Leucettine L41 prevents lipid peroxidation and the accumulation of reactive oxygen species (ROS) induced by Aβ25-35 in the hippocampus in a mouse model of Alzheimer’s disease-like toxicity. Leucettine L41 also prevents memory deficits induced by Aβ25-35 in the same model. | ||
| M28808 | Dyrk1A-IN-5 | DYRK |
| 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. | ||
| M49769 | ZDWX-25 | GSK-3 |
| ZDWX-25 is a highly potent GSK-3β and DYRK1A dual inhibitor with an IC50 value of 71 nM for GSK-3β. | ||
| M57196 | Dyrk1A-IN-4 | DYRK |
| Dyrk1A-IN-4 is a potent and orally active DYRK1A and DYRK2 inhibitor with IC50s of 2 nM and 6 nM, respectively. | ||
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