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

GSK3β Inhibitor XI has GSK3β inhibitory effect.

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

GSK-3β inhibitor 8 (GSK3β Inhibitor XVIII) is a potent and selective GSK-3β inhibitor with an IC50 value of 64 nM.GSK-3β inhibitor 8 is a thienopyrimidine derivative that negatively regulates the Wnt signaling pathway and stimulates β-cell proliferation.

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.

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].

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

Ceftriaxone Sodium is a broad-spectrum β-lactam tertiary cephalosporin antibiotic with anti-inflammatory, antitumor, antibacterial, and antioxidant activities.Ceftriaxone Sodium is a covalent GSK3β and Aurora B inhibitor used in the study of sepsis and infective endocarditis.

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

3CAI is a potent and specific AKT1 and AKT2 inhibitor which showed significant inhibition of AKT in an in vitro kinase assay and suppressed expression of AKT direct downstream targets such as mTOR and GSK3β as well as induced growth inhibition and apoptosis in colon cancer cells.

Polygalacin D shows anti- proliferation, anti-inflammary, and hepatoprotective activities, it can inhibit the expression of lipopolysaccharide (LPS)-induced iNOS and COX-2 protein and mRNA without an appreciable cytotoxic effect on RAW 264.7 macrophages, and can suppress induction by LPS of pro-inflammatory cytokines such as prostaglandin E2 (PGE2).

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

Ro 31-8220 Mesylate (Bisindolylmaleimide IX mesylate) is a pan-PKC inhibitor for PKC-α/βI/βII/γ/ε (IC50: 5/24/14/27/24 nM), and also shows potent inhibition against MSK1, MAPKAP-K1b, S6K1, and GSK3β.

Cynarin (1,5-Dicaffeoylquinic acid) has neuroprotective, and antioxidant effects, it can inhibition of GSK3β as well as the modulation of Bcl-2/Bax.

Adezmapimod (SB 203580) is a p38 MAPK inhibitor (IC50=0.3-0.5 μM) that is selective and ATP-competitive. Adezmapimod possesses autophagy and mitochondrial autophagy activating activity. Adezmapimod displays more than 100-fold higher selectivity than PKB, LCK, and GSK-3β.

AR-A014418 (GSK 3β inhibitor VIII) is an ATP-competitive, and selective GSK3β inhibitor.

Biatractylolide has a neuroprotective effect on glutamate-induced injury in PC12 and SH-SY5Y cells through a mechanism of the PI3K-Akt-GSK3β-dependent pathways. The molecular mechanisms of inhibitory activities of biatractylolide on AChE are not only thro

FCPR03 is a selective inhibitor of phosphodiesterase 4 (PDE4) with IC50s of 31 nM, 47 nM, and 60 nM for PDE4B1, PDE4D7, and PDE4 catalytic domain, respectively. FCPR03 has neuroprotective, anti-inflammatory, and antidepressant-like effects.

P7C3-A20 is a derivative of P7C3 that has proneurogenic and neuroprotective activity.

BMP Agonist 1 (compound 2 b) is a small-molecule stimulator of bone morphogenic protein (BMP) signaling, crucial for the differentiation of C2C12 cells. It acts by inhibiting GSK3β and enhancing β-catenin signaling, thereby synergistically modulating Id2 and Id3 expression. This compound is employed in skeletal disease and defect research [1].

hAChE-IN-5 (compound 49) is a dual inhibitor of human acetylcholinesterase (hAChE) and human butyrylcholinesterase (hBuChE), exhibiting inhibitory potency with IC50 values of 0.17 μM for both enzymes. Additionally, it demonstrates potent glycogen synthase kinase 3 beta (GSK3β) inhibition with an IC50 of 0.21 μM. The compound is an effective inhibitor of tau protein and Aβ1-42 peptide self-aggregation. It can virtually bind the peripheral anionic site (PAS), preventing amyloid-beta (Aβ)-induced neurotoxicity. hAChE-IN-5's ability to cross the blood-brain barrier (BBB) underpins its utility in the development of multitargeted anti-Alzheimer’s agents [1].

6-Me-ATP (N6-Methyl-ATP), a N6-modified adenosine triphosphate (ATP) derivative, exhibits strong binding affinity for glycogen synthase kinase 3 (GSK3) and acts as the phosphate group donor in GSK3β-catalyzed phosphorylation of its substrate peptide [1].

hAChE-IN-6 (compound 51) is a brain-penetrant acetylcholinesterase (AChE) inhibitor exhibiting an IC50 of 0.16 μM. It also demonstrates inhibitory effects on human butyrylcholinesterase (hBuChE) and glycogen synthase kinase 3 beta (GSK3β), with IC50 values of 0.69 μM and 0.26 μM, respectively. Additionally, hAChE-IN-6 impedes the self-aggregation of tau protein and amyloid-beta 1-42 (Aβ1-42), rendering it useful for Alzheimer's disease (AD) research [1].

9-Hydroxycanthin-6-one might be the active component that contributed to the aphrodisiac effect of E. longifolia by antagonizing the smooth muscle tone of CC as well as SV probably through interfering with Ca2+ mobilization.9-Hydroxycanthin-6-one inhibits Wnt signaling through the activation of GSK3β independent of CK1α.

Presenilin 1 (349-361), an active peptide, is phosphorylated by glycogen synthase kinase-3β (GSK3β) in vitro when represented by its amino acid sequence 349–361. It is utilized for research into multiple diseases [1].

(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].

2-Methoxystypandrone displays an immunomodulatory effect in a cellular model, it blocks inflammatory responses by impairing NF-κB signaling to limit the inflammation and oxidative stress for preservation of BBB integrity. 2-Methoxystypandrone concomitant

TCS 183 can mimic the Akt phosphorylation site on GSK3β preventing conditioning of LTD.

Cu(II)GTSM, a cell-permeable copper-complex, effectively inhibits GSK3β and shows inhibitory effects against Amyloid-β oligomers (AβOs) while reducing tau phosphorylation. Additionally, Cu(II)GTSM decreases the abundance of Amyloid-β trimers. With its potential as an anticancer and antimicrobial agent, Cu(II)GTSM exhibits promising therapeutic capabilities.

Dihydronarwedine is a metabolite of Galanthamine, an inhibitor of glycogen synthase kinase 3β (GSK3β)

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].

CM-414 is a dual inhibitor of HDACs and PDE5 for the Treatment of Alzheimer’s Disease (IC50 values of 60 nM, 310 nM, 490 nM, 322 nM, and 91 nM against PDE5, HDAC1, HDAC2, HDAC3, and HDAC6, respectively). Chronic treatment of Tg2576 mice with CM-414 dimini

6-Me-ATP (N6-Methyl-ATP) trisodium, an N6-modified ATP derivative, demonstrates high binding affinity for GSK3 and effectively acts as the phosphate group donor in GSK3β-catalyzed phosphorylation of its substrate peptide [1].

LDN-193665 is a potent inhibitor of tau kinase. It acts by targeting CDK5/p25 and GSK3β.

(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.

GSK2646264 (Compound 44) is a highly effective and specific inhibitor of spleen tyrosine kinase (SYK) with a pIC50 of 7.1. In addition to targeting SYK, GSK2646264 also inhibits several other kinases, including LCK, LRRK2, GSK3β, JAK2, VEGFR2, Aurora B, and Aurora A, with pIC50 values of 5.4, 5.4, 5.3, 5, 4.5, <4.6 and <4.3, respectively. Notably, GSK2646264 demonstrates skin penetrability, reaching both the epidermis and dermis [1].

KY19382 (2H-Indol-2-one, 5,6-dichloro-3-[1,3-dihydro-3-(methoxyimino)-2H-indol-2-ylidene]-1,3-dihydro-Ky19382) is a potent and orally active dual inhibitor of CXXC5-DVL and GSK3β( IC50s of 19 and 10 nM, respectively). It activates Wnt/β-catenin signaling through inhibitory effects on both CXXC5-DVL interaction and GSK3β activity. KY19382 can be used for the research of high fat diet (HFD) induced metabolic diseases.

PKCβ inhibitor 1 (KUN79359)(KUN79359) is a potent, selective and ATP-competitive inhibitor of PKC isozymes(IC50s of 21 and 5 nM for human PKCβ1 and PKCβ2, respectively).

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

SGK1 inhibitor is an inhibitor of serum- and glucocorticoid-regulated kinase 1 (SGK1) and SGK2. It is selective for SGK1 and SGK2 over SGK3 in the presence of a high concentration of ATP. SGK1 inhibitor prevents phosphorylation of GSK3β in U2OS cells and decreases cell viability in BYL719-insensitive HCC1954 cells when used in combination with the PI3Kα inhibitor BYL719. SGK1 inhibitor reduces tumor growth in an HCC1954 mouse xenograft model when administered in combination with BYL719.

KY02111 facilitates differentiation of hPSCs to cardiomyocytes by inhibiting Wnt signaling, maybe affect downstream of GSK3β and APC.

Methyl Linoleate (Telfairic Acid methyl ester) linoleate has antioxidant activity.

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.

BX795 is an effective and selective PDK1 inhibitor (IC50: 6 nM), and its selectivity is 140- and 1600-fold for PDK1 over PKA and PKC in cell-free assays, respectively. Meanwhile, the selectivity for PDK1 is 100-fold than GSK3β.

Adezmapimod (SB 203580) hydrochloride is a selective ATP-competitive inhibitor of p38 MAPK, displaying IC50 values of 50 nM for SAPK2a/p38 and 500 nM for SAPK2b/p38β2. This compound also inhibits LCK, GSK3β, and PKBα, albeit with IC50 values 100-500 times higher than those for SAPK2a/p38. Additionally, Adezmapimod hydrochloride acts as an activator of autophagy and mitophagy [1].

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].

GSK-3β inhibitor 1 is an inhibitor of GSK-3β( IC50 of 4.9 nM) and demonstrates high antidiabetic efficacy.

Darovasertib (LXS196) is a potent, selective and orally active protein kinase C (PKC) inhibitor(IC50 values of 1.9 nM, 0.4 nM and 3.1 μM for PKCα, PKCθ and GSK3β, respectively).