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GSK-3

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Cat. No. Product Name Field of Application Chemical Structure
DC81557 Sodium bromide
Sodium bromide (NSC 77384; Sanibrom 40) is a GABA-ergic system modulator that crosses the blood-brain barrier, and it effectively reduces and blocks epileptiform discharges. Sodium bromide exerts significant anticonvulsant effects by enhancing GABA-ergic inhibitory functions, such as increasing the amplitude of inhibitory postsynaptic currents and paired-pulse inhibition. Sodium bromide specifically enhances stimulation-induced extracellular alkalosis without affecting baseline pH or subsequent acidosis processes. Sodium bromide exhibits species-specific pharmacokinetic characteristics, competes with chloride ions for renal tubular reabsorption sites, and serves as a marker for extracellular fluid volume. Sodium bromide can be used in the research of epilepsy and related neurological diseases.
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DC81381 PROTAC IKKβ/NR4A1 degrader-1
PROTAC IKKβ/NR4A1 degrader-1 is a highly efficient and effective dual-PROTAC degrader targeting IKKβ and NR4A1. PROTAC IKKβ/NR4A1 degrader-1 can increase the levels of caspase 3 and cleaved caspase 3 proteins, while the necroptosis marker RIP kinase remained unchanged, indicating that it can induce apoptosis. PROTAC IKKβ/NR4A1 degrader-1 can be used for the study of Acute myeloid leukemia (AML). Red: IKKβ/NR4A1 ligand; Blue: E3 ligase CRBN ligand; Black: Linker. (Pink: Nur77/NR4A1 ligand ; Blue: Cereblon ligand ; Black: linker).
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DC80910 KRAS G12C-IN-75
KRAS G12C-IN-75 is an orally active, blood-brain barrier penetrant KRASG12C inhibitor with an IC50 of 0.53 nM. KRAS G12C-IN-75 attenuates active transport mediated by P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP). KRAS G12C-IN-75 inhibits tumor growth, regulates the expression of downstream MAPK target genes DUSP6 and SPRY4, and exhibits dose-dependent KRASG12C alkylation in KRASG12C-positive xenograft models. KRAS G12C-IN-75 can be used for research related to non-small cell lung cancer.
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DC80263 Asocainol hydrochloride
Asocainol hydrochloride (Goe 4704 hydrochloride) is an antiarrhythmic agent. Asocainol hydrochloride reduces the maximum rate of action potential rise and action potential amplitude. Asocainol hydrochloride is applicable for the research of arrhythmias.
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DC80215 Antifungal agent 143
Antifungal agent 143 is potent antifungal agent which also exihibits antibacterial activity. Antifungal agent 143 inhibits growth of Candida albicans and Aspergillus niger, Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, and Streptococcus pyogenes. Antifungal agent 143 can be used for antimicrobial research.
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DC79617 JGK-263
JGK-263 is an orally active Glycogen synthase kinase-3β (GSK-3β) inhibitor. JGK-263 exhibits neuroprotective effect and can improve motor function. JGK-263 can be used for the research of neurological disease, such as amyotrophic lateral sclerosis (ALS).
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DC79220 GSK-3β inhibitor 27
GSK-3β inhibitor 27 (Compound 1c) is a reversible and competitive GSK-3β inhibitor with an IC50 value of 2.2 μM. GSK-3β inhibitor 27 inhibits tau hyperphosphorylation, reduces Aβ protein aggregation and possesses metal chelation and neuroprotective potential. GSK-3β inhibitor 27 is promising for research of neurodegenerative diseases (such as Alzheimer’s disease).
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DC77207 GSK-3β probe-1
GSK-3β probe-1 (10c) is a GSK-3β probe (Ex = 341 nm, Em= 574nm, ɛ= 3.51 × 104L/mol·cm−1) and can be be used in the study of Alzheimer's disease.
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DC77206 2-Cyanoethylalsterpaullone
2-Cyanoethylalsterpaullone (compound 7) is an Alsterpaullone derivative and a PI3K/Akt signalling activator which promotes epithelium repair. Hydroxy celecoxib can be utilized in asthma research.
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DC1063 TWS119 Featured
TWS119 is a GSK-3β inhibitor with IC50 of 30 nM.
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DC9703 CHIR-99021 HCl Featured
CHIR-99021 HCl is a potent and selective inhibitor of glycogen synthase kinase 3 beta (GSK-3β), a key enzyme involved in regulating various cellular processes, including metabolism, cell proliferation, and differentiation. By inhibiting GSK-3β, CHIR-99021 HCl modulates downstream signaling pathways, particularly the Wnt/β-catenin pathway, leading to significant biological effects both in vitro and in vivo.
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DC1023 CHIR-99021 (CT99021) Featured
CHIR-99021 is a glycogen synthase kinase 3 beta inhibitor that has antiproliferative activity in vitro and in vivo.
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DC71176 TC-G 24 Featured
TC-G 24 (Compound 24) is a potent, selective glycogen synthase kinase-3β (GSK-3β) inhibitor with an IC50 of 17.1 nM.
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DC40570 KY19382 Featured
KY19382 is a potent and orally active dual inhibitor of CXXC5-DVL and GSK3β, with IC50s of 19 and 10 nM, respectively. KY19382 activates Wnt/β-catenin signaling through inhibitory effects on both CXXC5-DVL interaction and GSK3β activity. KY19382 can be us
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DC7680 IM-12 Featured
The GSK3β Inhibitor XIX, IM-12 is a selective GSK-3β inhibitor with IC50 of 53 nM, and also enhances canonical Wnt signalling.
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DC2067 TDZD-8 Featured
TDZD-8 is a non-ATP competitive GSK-3β inhibitor with IC50 of 2 μM.
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DC4227 SB216763 Featured
SB 216763 is a potent and selective cell permeable ATP-competitive inhibitor of GSK3α with an IC50 value of 34 nM (similar potency for GSK3β).
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DC7384 CHIR-98014 Featured
CHIR-98014 is a potent GSK-3α/β inhibitor with IC50 of 0.65 nM/0.58 nM, with the ability to distinguish GSK-3 from its closest homologs Cdc2 and ERK2.
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DC7004 AR-A014418(GSK3β Inhibitor VIII) Featured
AR-A014418 is a selective and effective GSK3β inhibitor with an IC 50 value of 104 +/- 27 nM; no significant inhibition on 26 other kinases.
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DC7663 BIO Featured
BIO (6-bromoindirubin-3'-oxime) is a specific inhibitor of GSK-3 with IC50 of 5 nM for GSK-3α/β, shows >16-fold selectivity over CDK5, also a pan-JAKinhibitor.
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DC11299 ABC 1183 Featured
ABC1183 is a potent, selective, orally active GSK3α/β and CDK9 inhibitor with IC50 of 327/657 nM and 321 nM (CDK9/cyclin T1), shows growth inhibitory activity against a broad panel of cancer cell lines; decreases cell survival through G2/M arrest and modu
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DC11827 9-ING-41 Featured
9-ING-41 is a potent glycogen synthase kinase-3 (GSK-3) inhibitor[1]. 9-ING-41 induces apoptosis and cell cycle arrest at prophase by targeting centrosomes and microtubule-bound GSK-3β. 9-ING-41 has anticancer activity[2].
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DC71240 ARN25068
ARN25068 is a sub-micromolar inhibitor of the three protein kinases, GSK-3β, FYN and DYRK1A to tackle tau hyperphosphorylation.
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DC70465 GSK3β-IN-1a
GSK3β-IN-1a is a relatively selective and potent GSK-3β inhibitor with IC50 of 64 nM; induces replication of growth-arrested R7T1 β cells in a dose-dependent manner with EC50 of 1.1 uM, likely mediates β-cell proliferation through the Wnt signaling pathway.
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DC70316 COB-187
COB-187 (COB187) is a highly potent and selective inhibitor of GSK-3 with IC50 of 22/11 nM against GSK-3α/GSK-3β.COB-187 inhibits GSK-3 phosphorylation of β-catenin and, albeit to a lesser extent, glycogen synthase.COB-187 increases the protein level of β-catenin in RAW 264.7 macrophages.COB-187 enhances β-catenin localization to the perinuclear and nuclear region in THP-1 macrophage, does not change the β-catenin mRNA level.COB-187 significantly increases the expression of the Wnt target gene cyclin D1, reduces the phosphorylation of tau in HEK293 cells transfected with tau expression vector.COB-187 inhibits only 3 kinases at >40% in a panel of 414 kinase assays, more selective relative to Tideglusib.
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DC50131 CHIR-98023
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.
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DC48703 (E/Z)-BIO-acetoxime
(E/Z)-BIO-acetoxime (GSK-3 Inhibitor X) is a potent and selective GSK-3α/β inhibitor, with an IC50 of 10 nM. (E/Z)-BIO-acetoxime shows more than 200-flod selectivity over CDK5/p25, CDK2/cyclin A and CDK1/cyclin B (IC50=2.4, 4.3, 63 μM).
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DC8263 Bikinin Featured
Bikinin is a strong activator of brassinosteroid (BR) signaling.
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DC9726 CP21 (CP21R7) Featured
CP21R7 is a potent and selective GSK-3β inhibitor.
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DC5144 1-Azakenpaullone Featured
1-Azakenpaullone is a potent and ATP-competitive GSK-3β (glycogen synthase kinase-3β) inhibitor (IC₅₀ = 18 nM).
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