gsk3α

GSK3-IN-2 is a potent GSK3 inhibitor for the treatment of diabetes and neurodegenerative diseases.

GSK3β Inhibitor XI has GSK3β inhibitory effect.

GSK3β inhibitor II is a GSK3β inhibitor. GSK3β inhibitor II exhibits the research potential of Alzheimer's disease (AD).

AChE/BACE1/GSK3β-IN-1 is an orally active, blood-brain barrier-transparent, moderately bioavailable triple inhibitor of AChE/BACE1/GSK3β. AChE/BACE1/GSK3β-IN-1 can be used to study Alzheimer's disease (AD).

GSK3 Substrate, α, β subunit, serves as a peptide substrate for Glycogen Synthase Kinase-3 (GSK-3), facilitating the measurement of GSK-3 activity [1].

CDK9/10/GSK3β-IN-1 is a kinase inhibitor (Flavopiridol analogue) that effectively inhibits HsGSK3β, HsCDK9/CyclinT, HsCDK5/p25 and HsCDK2/CyclinA with IC50 values of 59 nM, 64 nM, 1.093 μM and 1.725 μM, respectively. CDK9/10/GSK3β-IN-1 exhibited comparable or higher anti-cancer cell activity than Flavopiridol and showed high anti-proliferative activity against up to seven cancer cell lines in vitro.

GS87 is a highly specific inhibitor of GSK3 (glycogen synthase kinase 3) that induces extensive differentiation of AML cells.

(Rac)-BRD0705 is a less active racemate of BRD0705. BRD0705 is an effective and selective inhibitor of GSK3α.

R547 (Ro 4584820) is a potent ATP-competitive inhibitor of CDK1/2/4 with Ki of 2 nM/3 nM/1 nM. It is less potent to CDK7 and GSK3α/β, while inactive to other kinases. Phase 1.

AZD1080 is a selective, orally active, brain permeable GSK3 inhibitor.

(3S,4S)-Tivantinib, a potent and highly selective inhibitor of the receptor tyrosine kinase c-MET, targets GSK3α and GSK3β—two novel enzymes implicated in the pathogenesis of non-small cell lung cancer (NSCLC) [1].

(rel)-Tivantinib is a potent, highly selective inhibitor of the receptor tyrosine kinase c-MET and has additional novel targets, GSK3α and GSK3β, that are critical in the cellular mechanisms of non-small cell lung cancer (NSCLC) [1].

CAF-382 (compound B1), an analog of SNS-032, functions as a CDKL5 and pan-CDK inhibitor, exhibiting modest inhibitory activity against GSK3α/β with an affinity greater than 1.8 μM. It effectively inhibits CDKL5 and impedes the phosphorylation of the CDKL5 E2 domain [1].

BRD3731 is a selective inhibitor of GSK3β, demonstrating an IC50 value of 15 nM for GSK3β and 215 nM for GSK3α. Due to its inhibitory properties, BRD3731 holds promise for investigating various medical conditions, including post-traumatic stress disorder (PTSD), psychiatric disorders, diabetes, and neurodegenerative disorders [1].

BRD0209 is a highly selective and potent GSK3 inhibitor.

(R)-BRD3731, a GSK3 inhibitor, specifically compound example 273. It exhibits inhibitory activity with respective IC50 values of 1.05 μM for GSK3β and 6.7 μM for GSK3α.

JNJ-28583113, a TRPM2 antagonist with brain permeability, inhibits the phosphorylation of GSK3α and β subunits, thereby protecting cells from oxidative stress-induced cell death. Additionally, it suppresses cytokine release in response to pro-inflammatory stimuli in microglia [1].

SB 415286 is a potent GSK3α inhibitor with IC50/Ki of 78 nM/31 nM with equally effective inhibition of GSK-3β.

PT-65, a potent and selective GSK3 degrader, demonstrates the highest degradation capacity for GSK3α (DC50 = 28.3 nM) and GSK3β (DC50 = 34.2 nM) in SH-SY5Y cells, making it applicable for Alzheimer's disease research [1].

BIO-acetoxime (GSK-3 Inhibitor X) is a potent dual GSK3α/β inhibitor with IC50 of 10 nM, >240-fold selectivity over CDK5/p25, CDK2/cyclin A and CDK1/cyclin B.

(Sar1,Ile4,8)-Angiotensin II is a functionally selective agonist for the angiotensin II type 1 receptor (AT1R), enhancing insulin-stimulated signaling of the insulin receptor (IR) and glycogen synthesis. It boosts the insulin-induced phosphorylation of Akt and GSK3α/β [1].

CHIR98014 is a reversible, cell-permeable inhibitor of GSK3α and GSK3β (IC50s: 0.65 and 0.58 nM). Through its effects on GSK3, CHIR98014 stimulates glycogen synthase in cells (EC50: 106 nM), potentiates insulin-dependent glucose transport in isolated musc

ABC1183 is a novel diaminothiazole that inhibits GSK3α, GSK3β and CDK9. ABC1183 inhibits the growth of a numerous cancer cell lines by decreasing cell survival by inducing G2/M arrest and through altering GSK3, glycogen synthetase, β-catenin phosphorylation and MCL1 expression,and is orally active.

BRD5648 is a negative control for BRD0705, a paracrine-selective and orally potent GSK3α inhibitor with a Kd of 4.8 μM and an IC50 of 66 nM. BRD0705 is 8-fold more selective (8-fold) for GSK3α than GSK3β (IC50 515 nM).BRD0705 can be used in acute myeloid leukemia. leukemia.

BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor (IC50: 66 nM; Kd: 4.8 μM). BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC50: 515 nM).