GSK-3 Inhibitor

TCS 183, a peptide, is a GSK-3β inhibitor. TCS 183 blocks GSK-3β autoinhibition and decreases the level of AMPK phosphorylation. TCS 183 can be used for neuropathological diseases, particularly Alzheimer’s disease, research.

UNC10112785 is a serine/threonine kinase inhibitor with a human GSK-3β IC₅₀ of 0.031 μM, human CDK-2 IC₅₀ of 0.016 μM, and human CDK-4 IC₅₀ of 1.99 μM. UNC10112785 can be used for the research of type 2 diabetes.

AZ12943203 (Compound 13e) is a GSK-3 PET radioligand with a K_d of 2.94  nM. AZ12943203 has a significant inhibitory potency toward GSK-3β (IC₅₀ : 4.44 nM), and can specifically bind to GSK-3-rich regions of the rodent brain. AZ12943203 can be used for neurodegenerative diseases imaging, particularly Alzheimer’s disease.

BRD1652 is a highly selective GSK3 inhibitor. BRD1652 can be used in the study of emotion-related diseases.

Indazole (Standard) is the analytical standard of Indazole. This product is intended for research and analytical applications. Indazole, also called isoindazole, a heterocyclic aromatic organic compound. Its derivatives display a broad variety of biological activities including anti-inflammatory, antibacterial, anti-HIV, antiarrhythmic, antifungal and antitumour properties. Indazole and its derivatives can be used for research of cancer, neurological disorders, cardiovascular diseases, gastrointestinal diseases.

Dihydronarwedine (Lycoraminone) is the alkaloid. Dihydronarwedine inhibits 39% activity of glycogen synthase kinase-3β (GSK-3β) at a concentration of 10 μM.

GNF7156 is a DYRK1A/GSK3B inhibitor, IC₅₀ values of 100 nM for DYRK1A and 40 nM for GSK3B. GNF7156 inhibits DYRK1A and GSK3B kinase activity and induces NFAT nuclear retention. GNF7156 stimulates beta-cell cycle entry and division and maintains insulin secretory capacity. GNF7156 can be used for the research of type 1 diabetes, and type 2 diabetes.

Multi-kinase-IN-14 is an orally active and blood-brain barrier-permeable multi-kinase inhibitor. Multi-kinase-IN-14 reduces the excessive phosphorylation of α-synuclein by inhibiting four kinases (ABL1, DYRK1A, GSK3β, and LRRK2) and stabilizing microtubules. Multi-kinase-IN-14 is applicable for research on neurodegenerative diseases such as Parkinson’s disease and Alzheimer’s disease.

TFGF-18 is a GSK-3β inhibitor (IC₅₀: 0.59 μM). TFGF-18 inhibits LPS-induced microglia activation and proinflammatory mediators release via inhibiting GSK-3β and downstream p65/NF-κB signaling. TFGF-18 inhibits neuronal apoptosis and oxidative stress, inhibits expressions of Bax, caspase3 and cleaved-caspase3 and increases the expression of Bcl-2. TFGF-18 has neuroprotection effect, inhibit neuroinflammation and attenuates cognitive impairment.

R547 (Standard) is the analytical standard of R547 (HY-10014). This product is intended for research and analytical applications. R547 is a potent, selective and orally active ATP-competitive CDK inhibitor, with Kis of 2 nM, 3 nM and 1 nM for CDK1/cyclin B, CDK2/cyclin E and CDK4/cyclin D1, respectively.

PHA-793887 hydrochloride is a CDK inhibitor (with IC₅₀ values of 8 nM for Cdk2, 60 nM for Cdk1, 62 nM for Cdk4, 138 nM for Cdk9). PHA-793887 hydrochloride inhibits purified GSK3β (IC₅₀ 79 nM). PHA-793887 hydrochloride reduces the phosphorylation level of nucleophosmin/cdc6, induces G1/G2/M phase arrest, and triggers Apoptosis by activating Caspase-3. PHA-793887 hydrochloride exhibits anticancer activity against leukemia. PHA-793887 hydrochloride can be used in research related to acute leukemia, chronic myeloid leukemia, and advanced/metastatic solid tumors.

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

Ceftriaxone (sodium hydrate) (Standard) is the analytical standard of Ceftriaxone (sodium hydrate). This product is intended for research and analytical applications. Ceftriaxone sodium hydrate (Ro 13-9904 sodium hydrate) is a broad spectrum β-lactam third-generation cephalosporin antibiotic, which has good antibacterial activity against a variety of gram-negative and positive bacteria. Ceftriaxone sodium hydrate is a covalent inhibitor of GSK3β with IC₅₀ value of 0.78 μM. Ceftriaxone sodium hydrate is an inhibitor of Aurora B. Ceftriaxone sodium hydrate has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone sodium hydrate can be used in the study of bacterial infections and meningitis.

GSK-3 inhibitor 7 (compound 22) is a glycogen synthase kinase-3 (GSK-3) inhibitor. GSK-3 inhibitor 7 can be used in nervous system research.

BIP-135 (Standard) is the analytical standard of BIP-135 (HY-111055). This product is intended for research and analytical applications. BIP-135 is a potent and selective ATP-competitive GSK-3 inhibitor, with IC₅₀s of 16 nM and 21 nM for GSK-3α and GSK-3β, respectively. BIP 135 exhibits neuroprotective effect.

2-Cyanoethylalsterpaullone (compound 7) is an Alsterpaullone (HY-108359) derivative, which exhibits potent and selective inhibitory activities against CDK1/Cyclin B and GSK-3β (GSK-3β: IC₅₀=0.8 nM; CDK1/Cyclin B: IC₅₀=0.23 nM).

IM-12 (Standard) is the analytical standard of IM-12. This product is intended for research and analytical applications. IM-12 is an inhibitor of GSK-3β, with an IC50 of 53 nM, and also enhances Wnt signalling.

CP21R7 (Standard) is the analytical standard of CP21R7 (HY-100207). This product is intended for research and analytical applications. CP21R7 is potent GSK-3β inhibitor, with an IC50 of 1.8 nM; CP21R7 also shows inhibitory activitiy against PKCα, with an IC50 of 1900 nM.

Tagtociclib hydrate (Standard) is the analytical standard of Tagtociclib hydrate (HY-137894A). This product is intended for research and analytical applications. PF-07104091 hydrate is a potent and selective CDK2/cyclin E₁ and GSK3β inhibitor, with K_is of 1.16 and 537.81 nM, respectively. PF-07104091 hydrate has anti-tumor activity for cyclin E₁-amplified cancers. (patent WO2020157652A2).

Neoandrographolide (Standard) is the analytical standard of Neoandrographolide. This product is intended for research and analytical applications. Neoandrographolide is a diterpenoid compound isolated from Andrographis paniculata. Neoandrographolide inhibits osteoclasts differentiation and bone resorption through inhibition of MAPK/NF-κB/PI3K/AKT/GSK3β/PPAR/CAMK signaling pathway. Neoandrographolide inhibits apoptosis in rat embryonic ventricular cardiomyocytes. Neoandrographolide inhibits iNOS and the generation of ROS, activates eNOS, exhibiting anti-inflammatory and hypolipidemic activity.