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A 1070722 is a potent glycogen synthase kinase-3 (GSK-3) inhibitor (Ki = 0.6 nM for GSK-3α and GSK-3β). Displays high selectivity (> 50-fold) for GSK-3 over a panel of other kinases tested, including CDK family members. Decreases phosphorylation of microtubule-associated protein Tau in vitro; protects rat primary cortical neurons against β amyloid and glutamate challenge. Brain penetrant.
| Molecular Weight | 362.31 |
| Formula | C17H13F3N4O2 |
| CAS Number | 1384424-80-9 |
| Form | Solid |
| Solubility (25°C) | DMSO 36.23 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] R C Marcove. The treatment of malignant bone tumors by conservative surgery
| Related GSK-3 Products |
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| CHIR-99021
CHIR-99021 (CT99021) is an aminopyrimidine derivative that inhibits GSK3α and GSK3β with IC50 values of 10 and 6.7 nM, respectively. |
| CHIR-99021 HCl
CHIR-99021 HCl (Laduviglusib; CT99021) is a hydrochloride of CHIR-99021, with IC50 of 10 nM and 6.7 nM for GSK-3α and GSK-3β, respectively. |
| SB 216763
SB 216763 is a potent and selective, cell permeable glycogen synthase kinase-3 (GSK-3) inhibitor with an IC50 value of 34 nM for GSK-3α. |
| AZD2858
AZD2858 is a potent, orally bioactive inhibitor of GSK-3 with an IC50 of 68 nM. |
| Indirubin
Indirubin is a potent cyclin-dependent kinases and GSK-3β inhibitor with IC50 of ~75 nM and 0.19 μM. |
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