GSK-3 Inhibitor

GSK-3β-IN-30 is a glycogen synthase kinase-3β (GSK-3β) inhibitor. GSK-3β-IN-30 stabilizes its conformation in the binding pocket by occupying the ATP-binding cleft of GSK-3β, forming hydrogen bonds with Lys183 and Ser203, and establishing π-anion interactions with Asp181 and Asp200. GSK-3β-IN-30 can be used for the research of Alzheimer's disease.

GSK3A Human Pre-designed siRNA Set A contains three designed siRNAs for GSK3A gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

AJ-4 is an orally active, blood-brain barrier-permeable GSK-3β/AChE inhibitor, with an IC₅₀ of 4.7 nM against GSK-3β and 2.97 μM against AChE. AJ-4 increases the level of phosphorylated GSK-3β and reduces the expression of Amyloid-β and phosphorylated Tau. AJ-4 improves scopolamine-induced learning and memory impairment and alleviates hippocampal neuron damage in AD mice. AJ-4 can be used for the research of Alzheimer's disease.

GSK-3β inhibitor 21 (compound 44) is an ATP-competitive GSK-3β inhibitor (IC₅₀=6.06 μM) with anti-amyloid aggregation and tau phosphorylation inhibitory activities. GSK-3β inhibitor 21 can be used in the study of Alzheimer's disease.

GSK-3β inhibitor 6 is a potent GSK-3β inhibitor with an IC₅₀ value of 24.4 μM. GSK-3β inhibitor 6 shows high hepatocyte glucose uptake (38%). GSK-3β inhibitor 6 can be used in the research of numerous diseases like diabetes, inflammation, cancer, Alzheimer's disease, and bipolar disorder.

Gsk3a Mouse Pre-designed siRNA Set A contains three designed siRNAs for Gsk3a gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

GSK3-IN-11 is a Glycogen Synthase Kinase-3 (GSK-3) inhibitor with an IC₅₀ of 5010 nM.

GSK3-IN-4 (compound 0715) is a potent GSK3 inhibitor. GSK3-IN-4 can be used for psychiatric disorder research.

GSK3β-IN-3 is an ATP-competitive GSK-3β inhibitor (IC₅₀ = 0.90 μM). GSK3β-IN-3 can reduce the phosphorylation level of tau protein in the BR5706 strain and reduce the deposition of Aβ aggregates in the CL2006 strain, and can be used to research Alzheimer's disease (AD).

GSK-3β inhibitor 16 (compound 7c) is a GSK-3β inhibitor with the IC₅₀ of 4.68 nM. GSK-3β inhibitor 16 decreases Tau hyperphosphorylated aggregate and alleviates cognitive impairments in the Scopolamin (HY-N0296)-induced model in mice.

CDK7-IN-20 is a potent, selective and irreversible CDK7 (CDK) inhibitor with an IC₅₀ value of 4 nM. CDK7-IN-20 displays >206-fold selectivity for CDK7 over CDK1, CDK2, CDK3, CDK5, CDK6, CDK9 and CDK12 . CDK7-IN-20 has the potential for autosomal dominant polycystic kidney disease (ADPKD) research.

CHIR-98023 is a potent, selective and reversible inhibitor of GSK3, with IC₅₀s of 10 nM and 6.7 nM for GSK3α and GSK3β, respectively. CHIR-98023 can improve insulin action and glucose metabolism.

MRT68921 hydrochloride is a potent NUAK1/ULK1 dual inhibitor. MRT68921 hydrochloride inhibits ULK1 and ULK2 with IC₅₀ values of 2.9 nM and 1.1 nM, respectively. MRT68921 hydrochloride can block cells autophagy and kill tumor cells by breaking the balance of oxidative stress signals. MRT68921 hydrochloride can inhibit cell proliferation and induce ROS production and apoptosis. MRT68921 hydrochloride can be used for the research of cancer, such as breast cancer.

MJ34 is a potent inhibitor of GSK-3β and GSK-3α, with the IC₅₀s of 15.4 nM and 31.5 nM, respectively. MJ34 plays an important role in cancer research

GSK3β-IN-4 is a selective, potent, orally active and brain-penetrant ATP-competitive GSK3β inhibitor with an IC₅₀ of 0.37 nM. GSK3β-IN-4 shows an IC₅₀ of 2.75 nM and SI of 7.4 for GSK3α. GSK3β-IN-4 reduces tau phosphorylation at Ser396 by inhibiting GSK3β and imoroves cognitive deficits in Alzheimer's disease models. GSK3β-IN-4 can be used for the research of Alzheimer's disease.

SkQR1 hydroxide is a mitochondrial targeted antioxidant. SkQR1 hydroxide can inhibit glycogen synthase kinase 3β (GSK3β) in the brain. SkQR1 hydroxide has a significant memory promoting effect. SkQR1 hydroxide can be used for research related to brain memory.

AChE/GSK-3β-IN-1 (compound GT15) is a potent, dual AChE/GSK-3β inhibitor with IC₅₀ values of 1.2, 149.8 and 22.4 nM for hAChE , hBChE and hGSK-3β, respectively. AChE/GSK-3β-IN-1 penetrates the blood-brain barrier (BBB). AChE/GSK-3β-IN-1 has high kinase selectivity profiles for the CMGC kinase family. AChE/GSK-3β-IN-1 occupies the ATP binding site of DYRK1A. AChE/GSK-3β-IN-1 inhibits ROS expression and reduces oxidative stress. AChE/GSK-3β-IN-1 can be used for Alzheimer’s disease research.

Multi-kinase-IN-7 is a multikinase inhibitor with IC₅₀s of 2.19, 2.95, 3.59 and 9.31 μM against EGFR, VEGFR2, TrKA and CDK2, respectively. Multi-kinase-IN-7 shows moderate and weaker activity against FAK, AKT1, GSK3β and CDK5 with IC₅₀ values of 6.3, 9.2, 11.7 and 23.4 μM, respectively. Multi-kinase-IN-7 displays broad spectrum anti­proliferative potential against NCI cancer cell lines. Multi-kinase-IN-7 induces cell cycle arrest, apoptosis and necrosis. Multi-kinase-IN-7 Inhibitor can be used for the study of breast cancer.

GSK-3β inhibitor 7 is a GSK-3β inhibitor with an IC₅₀ value of 5.25 μM. GSK-3β inhibitor 7 is inserted into the ATP-binding binding pocket of GSK-3β and forms hydrogen-bond. GSK-3β inhibitor 7 shows high hepatocyte glucose uptake (83.5%), and can be used in the research of numerous diseases like diabetes, inflammation, cancer, Alzheimer's disease, and bipolar disorder.

(Rac)-BRD0705 is a less active racemate of BRD0705. BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC₅₀ of 66 nM and a K_d of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC₅₀ of 515 nM). BRD0705 can be used for acute myeloid leukemia (AML).