GSK-3 Inhibitor

SB 216763 (Standard) is the analytical standard of SB 216763. This product is intended for research and analytical applications. SB 216763 is potent, selective and ATP-competitive GSK-3 inhibitor with IC50s of 34.3 nM for both GSK-3α and GSK-3β.

Amsacrine lactate (m-AMSA lactate) is a Topoisomerase II inhibitor. Amsacrine lactate intercalates into DNA. Amsacrine lactate induces Ca²⁺-mediated inactivation of ERK, and also downregulates AKT, promoting MCL1 downregulation mediated by GSK3β via reducing the phosphorylation level of GSK3β. Amsacrine lactate induces Apoptosis by activating Caspase-9 and Caspase-3. Amsacrine lactate blocks HERG potassium channels in the open/inactivated state. Amsacrine lactate induces chromosomal aberrations and sister chromatid exchanges, and inhibits the synthesis of RNA and DNA. Amsacrine lactate exhibits anti-leukemic activity. Amsacrine lactate causes cardiac repolarization disorders, QT interval prolongation, ventricular arrhythmias, and increases the risk of sudden cardiac death. Amsacrine lactate can be used in research related to acute myeloid leukemia, lymphoma and progressive malignancies.

TDZD-8 (Standard) is the analytical standard of TDZD-8. This product is intended for research and analytical applications. TDZD-8 is an inhibitor of GSK-3β, with an IC50 of 2 μM; TDZD-8 shows less potent activities against Cdk-1/cyclin B, CK-II, PKA, and PKC, with all IC50s of >100 μM.

MeBIO (Standard) is the analytical standard of MeBIO (HY-103221). This product is intended for research and analytical applications. MeBIO is a potent AhR (aryl hydrocarbon receptor) agonist, with IC₅₀ of 44 μM (GSK-3) and 55 μM (CDK1/cyclin B), respectively.

MRT68921 (dihydrochloride) (Standard) is the analytical standard of MRT68921 (dihydrochloride) (HY-100006A). This product is intended for research and analytical applications. MRT68921 dihydrochloride is a potent NUAK1/ULK1 dual inhibitor. MRT68921 dihydrochloride inhibits ULK1 and ULK2 with IC50 values of 2.9 nM and 1.1 nM, respectively. MRT68921 dihydrochloride can block cells autophagy and kill tumor cells by breaking the balance of oxidative stress signals. MRT68921 dihydrochloride can inhibit cell proliferation and induce ROS production and apoptosis. MRT68921 dihydrochloride can be used for the research of cancer, such as breast cancer.

Antitrypanosomal agent 31 is an antitrypanosoma agent with a pEC50 of 6.4. Antitrypanosomal agent 31 inhibits GSK-3β, CDK-2, and CDK-4 with pIC₅₀s of 5.8, 6.9, and 7.1, respectively. Antitrypanosomal agent 31 can be used for the research of human african trypanosomiasis.

(E)-Methyl 4-coumarate (Standard) is the analytical standard of (E)-Methyl 4-coumarate (HY-N2492). This product is intended for research and analytical applications. (E)-Methyl 4-coumarate (Methyl 4-hydroxycinnamate) is a phenolic compound and derivative of Cinnamic acid (HY-N0610A). (E)-Methyl 4-coumarate can be found in several plants, such as the leaves of Allium cepa and Morinda citrifolia L. (E)-Methyl 4-coumarate, when combined with Carnosic acid (HY-N0644), induces Apoptosis. (E)-Methyl 4-coumarate inhibits GSK3β activity and modulates inflammatory cytokine levels (increasing IL-10 and decreasing IL-4). (E)-Methyl 4-coumarate combined with Carnosic acid exhibits anticancer effects against acute myeloid leukemia. (E)-Methyl 4-coumarate ameliorates Plasmodium berghei NK65 infection.

5-Iodo-indirubin-3'-monoxime (Standard) is the analytical standard of 5-Iodo-indirubin-3'-monoxime (HY-111930). This product is intended for research and analytical applications. 5-Iodo-indirubin-3'-monoxime is a potent GSK-3β, CDK5/P25 and CDK1/cyclin B inhibitor, competing with ATP for binding to the catalytic site of the K_inase, with IC₅₀s of 9, 20 and 25 nM, respectively.

Cefetecol hydrate (GR69153 hydrate) is a semisynthetic β-lactam antibacterial agent and α-glucosidase inhibitor (yeast IC₅₀ = 2.1 μM; K_i = 5.78 μM) that crosses the blood-brain barrier. Cefetecol hydrate reduces blood glucose levels in Streptozotocin-induced diabetic mice. Cefetecol hydrate decreases the mRNA expression of GSK-3, PPAR-γ, and UCP-3. Cefetecol hydrate induces bacterial cell filamentation and exhibits bactericidal activity against Gram-positive and Gram-negative bacteria. Cefetecol hydrate is used in the study of diabetes and bacterial infections.

Laduviglusib (trihydrochloride) (Standard) is the analytical standard of Laduviglusib (trihydrochloride). This product is intended for research and analytical applications. Laduviglusib (CHIR-99021) trihydrochloride is a potent and selective GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. Laduviglusib trihydrochloride shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. Laduviglusib trihydrochloride is also a potent Wnt/β-catenin signaling pathway activator. Laduviglusib trihydrochloride enhances mouse and human embryonic stem cells self-renewal. Laduviglusib trihydrochloride induces autophagy.

Cazpaullone is a glycogen synthase kinase-3 (GSK-3) inhibitor. Cazpaullone can activate pancreatic beta cell protection and replication. Cazpaullone can be used for the research of diabetes.

DC-120 is an ATP-competitive AKT inhibitor, with particular activity against AKT1 (an IC₅₀ of 0.153 μM). DC-120 functionally blocks AKT kinase activity and reduces the phosphorylation levels of FOXO3a and GSK-3β. DC-120 induces cancer cell apoptosis (apoptosis) and inhibits cancer cell proliferation. DC-120 activates the mTORC1 pathway via the Ca²⁺/calmodulin (calmodulin)/hVps34 signaling pathway. DC-120 abrogates AKT-mediated inhibition of CRAF, thereby activating the MEK/ERK MAPK pathway. DC-120 exerts anti-tumor activity in a nude mouse hepatocellular carcinoma xenograft model. DC-120 can be used for hepatocellular carcinoma-related research.

TWS119 (Standard) is the analytical standard of TWS119. This product is intended for research and analytical applications. TWS119 is a specific inhibitor of GSK-3β, with an IC50 of 30 nM, and activates the wnt/β-catenin pathway.

LY2090314 (Standard) is the analytical standard of LY2090314 (HY-16294). This product is intended for research and analytical applications. LY2090314 is a potent inhibitor of glycogen synthase K_inase-3 (GSK-3) with IC₅₀ values of 1.5 nM and 0.9 nM for GSK-3α and GSK-3β, respectively.

K00546 (Standard) is the analytical standard of K00546 (HY-103647). This product is intended for research and analytical applications. K00546 is a potent CDK1 and CDK2 inhibitor with IC₅₀s of 0.6 nM and 0.5 nM for CDK1/cyclin B and CDK2/cyclin A, respectively. K00546 is also a potent CDC2-like kinase 1 (CLK1) and CLK3 inhibitor with IC₅₀s of 8.9 nM and 29.2 nM, respectively.

Protein kinase inhibitor 13 (Compound I-90) is the inhibitor for protein kinase that exhibits inhibitory effects on kinases such as PIM-1, CDK-2, GSK-3 and SRC.

GCN2/GSK3α-IN-1 is a GCN2 and GSK3α inhibitor with an IC₅₀ of less than 1 μM for both targets. GCN2/GSK3α-IN-1 can be used in cancer research.

Kuwanon G (Standard) is the analytical standard of Kuwanon G (HY-N4247). This product is intended for research and analytical applications. Kuwanon G is a flavonoid compound and an antagonist of the bombesin receptor. Kuwanon G has multiple activities such as bactericidal, anti-tumor, anti-inflammatory, antioxidant, anti-atherosclerotic, and neuroprotective effects. Kuwanon G exhibits strong antibacterial activity against oral pathogens, especially cariogenic bacteria and periodontal pathogens. Kuwanon G can induce apoptosis and inhibit proliferation, migration, and invasion of tumor cells. Kuwanon G can be used in the research of diseases such as gastric cancer and atherosclerosis.

GSK-3β inhibitor 25 (Compound 6h) exhibits a weak inhibitory activity against GSK-3β wih an IC₅₀>100 μM.

SB 415286 (Standard) is the analytical standard of SB 415286. This product is intended for research and analytical applications. SB 415286 is a potent and selective cell permeable inhibitor of GSK-3α, with an IC50 of 77.5 nM, and a Ki of 30.75 nM; SB 415286 is equally effective at inhibiting human GSK-3α and GSK-3β.