| Cat. No. |
Product Name |
CAS No. |
Information |
| H9397 |
EHT 5372
|
1425945-63-6 |
EHT 5372 is a highly potent and selective inhibitor of DYRK’s family kinases with IC50s of 0.22, 0.28, 10.8, 93.2, 22.8, 88.8, 59.0, 7.44, 221 nM for DYRK1A, DYRK1B , DYRK2， DYRK3， CLK1, CLK2, CLK4, GSK-3α, GSK-3β. |
| H9247 |
2B-(SP) TFA
|
|
2B-(SP) TFA is a eIF2B-based substrate for glycogen synthase kinase-3 (GSK-3). 2B-(SP) TFA is readily phosphorylated by both the α and β isoforms of GSK-3. |
| H9246 |
2B-(SP)
|
186901-17-7 |
2B-(SP) is a eIF2B-based substrate for glycogen synthase kinase-3 (GSK-3). 2B-(SP) is readily phosphorylated by both the α and β isoforms of GSK-3. |
| H8255 |
TWS119
|
601514-19-6 |
A GSK-3β inhibitor with IC50 of 30 nM in a cell-free assay; can induce neurogenesis in murine ESCs; reduces Cdon levels and aberrant Cx43 activitiesin rat cardiomyocytes; attenuates rtPA-induced hemorrhagic transformation and activates the Wnt/β-catenin signaling pathway after acute ischemic stroke in rats. |
| H8254 |
TDZD-8
|
327036-89-5 |
A potent, selective, non-ATP competitive GSK-3β inhibitor with IC50 of 2 uM; displays no activity against PKA, CK-2, PKC, and CDK1 (IC50>100 uM); reduces the colonic inflammation induced by TNBS in vivo, also prevents 6-OHDA-induced neuronal cell death. |
| H8253 |
SB 216763
|
280744-09-4 |
SB 216763 is a potent, selective, ATP competitive and cell permeable inhibitor GSK-3 with Ki of 9 nM (GSK-3α), equally potent for GSK-3β; displays no significant activity against a panel of 24 other protein kinases; stimulates glycogen synthesis in human liver cells and induces expression of a beta-catenin-LEF/TCF regulated reporter gene in HEK293 cells, protects both central and peripheral nervous system neurones in culture from death, activates beta-catenin-mediated transcription, and enhances the survival of CLL lymphocytes; displays therapeutic properties in a mouse model of pulmonary inflammation and fibrosis. |
| H8252 |
PF-04802367
|
1962178-27-3 |
A potent, highly selective GSK-3 inhibitor with IC50 of 2.1 nM for human GSK-3β in enzyme assays; shows equal effectivity against GSK-3α and GSK-3β with IC50 of 10.0 and 9.0 nM respectively in mobility shift assays, inhibits phosphorylation of tau with an IC50 of 466 nM in a stable inducible CHO cell line over-expressing GSK-3β and substrate tau; modulates tau phosphorylation in vitro and in vivo. |
| H8251 |
MMBO
|
1005203-15-5 |
MMBO is a potent, highly selective, brain penetrant, orally active inhibitor of GSK-3 with IC50 of 37 and 53 nM for GSK-3α and GSK-3β, respectively; inhibits tau phosphorylation in primary neural cell culture and also in normal mouse brain, significantly decreases hippocampal tau phosphorylation at GSK-3 sites in transgenic mouse model of AD; suppresses tau pathology as assessed by AT8-immunoreactivity without affecting amyloid β pathology, significantly improves memory and cognitive deficits in AD models. |
| H8250 |
Methyliodobikinin
|
1186336-04-8 |
Methyliodobikinin is a potent bikinin-like inhibitor targeting GSK3/Shaggy-like kinase, shows improved cell permeability, highly potent in vivo although it had lower activity in vitro; activates brassinosteroid (BR) signalling and mimic BR action, 3.4 times more active in vivo than bikinin. |
| H8249 |
Indirubin-3|-monoxime
|
160807-49-8 |
A potent GSK3β inhibitor with IC50 of 22 nM; prevents tau phosphorylation both in vitro and in vivo; also inhibits CDKs at higher concentrations, including Cdk1/cyclin B (IC50=180 nM), Cdk2/cyclin A (IC50~500 nM), Cdk2/cyclin E (IC50=250nM), Cdk4/cyclin D1 (IC50=3.3 uM) and Cdk5/p35 (IC50=100 nM); reversibly inhibits the proliferation of many cells types, arresting cycling in the G2/M phase. |
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