gsk-3 inhibitor xiii

GSK-3 Inhibitor XIII, an ATP-competitive GSK-3 inhibitor (Ki: 24 nM), can be used to study diabetes and obesity.

JAK1/2/3 Inhibitor 1 is a potent protein kinase inhibitor.JAK1/2/3 Inhibitor 1 has antitumor activity that inhibits the growth of a variety of cancer cell lines. It inhibits the growth of cancer cells by binding to the cancer cell backbone and inhibiting the production of new proteins.

GSK-3 Inhibitor 5 (4-Cyanophenacyl bromide) is a ketone derivative that is used as an intermediate in pharmaceuticals and organic synthesis, and inhibits glycogen synthase kinase 3 (GSK-3).

GSK-3 inhibitor 3 is a selective, orally active, brain-permeable GSK-3 inhibitor that inhibits GSK-3α and GSK-3β with IC50s of 0.35 nM and 0.25 nM, respectively.GSK-3 inhibitor 3 reduces the phosphorylation level of tau protein S396 with an IC50 of 10 nM in a triple transgenic mouse model of Alzheimer's disease. GSK-3 inhibitor 3 reduced the phosphorylation level of tau protein S396 in a triple transgenic mouse model of Alzheimer's disease, with an IC50 of 10 nM.GSK-3 inhibitor 3 can be used for the study of neurological diseases.

GSK-3β inhibitor 12 is a selective GSK-3β inhibitor.GSK-3β inhibitor 12 inhibits 49.11% of 25 μM GSK-3β activity and 37.11% of 50 μM GSK-3β activity.GSK-3β inhibitor 12 can be used for the study of Parkinson's in the presence of lipopolysaccharide induction.

Rac1 Inhibitor W56 acetate(1095179-01-3 free base) is a peptide comprising residues 45-60 of the guanine nucleotide exchange factor (GEF) recognition/activation site of Rac1. Rac1 Inhibitor W56 acetate(1095179-01-3 free base) selectively inhibits Rac1 interaction with Rac1-specific GEFs TrioN, GEF-H1 and Tiam1.

GSK-3 inhibitor 4 is an orally active and brain-permeable triple inhibitor of GSK-3, CDK2 and CDK5 with inhibitory effects on GSK-3β, GSK-3α, CDK2 and CDK5, with IC50 values of 0.56 nM, 0.45 nM, 0.47 μM, 0.68 μM, respectively.GSK-3 inhibitor 4 can effectively reduce Tau protein levels. GSK-3 inhibitor 4 can effectively reduce the level of Tau protein.GSK-3 inhibitor 4 can be used in the study of Alzheimer's disease.

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.

GSK-3 inhibitor 1 is a GSK-3 inhibitor.

mTOR inhibitor-3 is a selective mTOR inhibitor (Ki= 1.5 nM). mTOR inhibitor-3 inhibits mTORC1 and mTORC2 in cellular and in vivo experiments.

RIP2 Kinase Inhibitor 3 is a potent and selective inhibitor of RIP2 with an IC50 of 1 nM.

GSK 3 Inhibitor IX (6-BIO) is a selective reversible, ATP-competitive inhibitor of GSK-3α/β and CDK1-cyclinB complex. It inhibits (GSK-3α/β)/CDK1/CDK5 activity with IC50 values of 5 nM/320 nM/83 nM, respectively.

GSK-3β inhibitor 14 (1,5-Benzothiazepin-4(5H)-one, 2,3-dihydro-2-methyl-5-(phenylmethyl)-) is a weak GSK-3β inhibitor, IC50﹥ 100μM.

WRN Inhibitor 3 (example 110), a cyclic vinyl sulfone-based compound, serves as an inhibitor of the Werner Syndrome ATP-dependent helicase enzyme (WRN). It is utilized in cancer research [1].

MAPK4 Inhibitor 3 (compound 23b) serves as a selective antagonist of MAPK4, demonstrating an inhibition constant (IC50) of 1.01 μM and effectively impeding the proliferation of cancer cells. This compound is utilized in research focused on cancer and tauopathies [1].

Aurora A Inhibitor 3 (Compound 5h) effectively inhibits Aurora-A kinase, exhibiting an IC50 of 0.78 μM, and demonstrates cytotoxicity against MCF-7 and MDA-MB-231 cell lines with GI50 values of 0.12 μM and 0.63 μM, respectively [1].

MMP-3 Inhibitor acetate is a cell-permeable and potent inhibitor of human MMP-3.

PRL-3 Inhibitor I (BR-1) is a phosphatase of regenerating liver 3 (PRL-3) inhibitor which blocks the migration and invasion of metastatic cancer cells.

Wnt pathway inhibitor 3 is a potent AC1 inhibitor with an IC50 value of 45 nM.Wnt pathway inhibitor 3 has antiproliferative activity and can be used in studies to ameliorate osteoarthritis in a mouse model of experimental osteoarthritis.

p38α inhibitor 3 is a inhibitor of the mitogen-activated protein kinase p38α that can block the effectiveness of myoblast differentiation.

Schnurri-3 inhibitor-1, a potent inhibitor of schnurri-3, is an essential regulator of bone formation in adults that can be used in osteoporosis research. Schnurri-3 inhibitor-1 can inhibit Shn3 with EF1alpha promoter in osteoblast cell line Shn3FFL (AC50 = 2.09 μM) [1].

KRAS inhibitor-3, an efficacious inhibitor of both wild-type (WT) and oncogenic KRAS mutations, exhibits high-affinity binding (K D: 0.28 μM for KRAS WT, 0.63 μM for KRAS G12C, 0.37 μM for KRAS G12D, and 0.74 μM for KRAS Q61H). Additionally, it impedes the interaction between KRAS and Raf, highlighting its potential as a targeted therapeutic agent in KRAS-mutant cancers.

Chitin Synthase Inhibitor 3 (Compound 2d) is a potent inhibitor of chitin synthase, exhibiting an IC50 value of 0.16 mM and demonstrating antifungal activity with a minimum inhibitory concentration (MIC) of 1 μg/mL against Candida albicans [1].

JNK3 Inhibitor-3 (compound 15g) is a selective, blood-brain barrier permeable, and orally active inhibitor of c-Jun N-terminal kinase 3 (JNK3) with IC50 values of 147.8 nM, 44.0 nM, and 4.1 nM against JNK1, JNK2, and JNK3, respectively. This compound has been shown to significantly enhance memory in mouse models of dementia and is utilized in Alzheimer’s disease research [1].

PI4KIII beta inhibitor 3 is a novel and high effective inhibitor of PI4KIIIβ (IC50 of 5.7 nM).

ChoKα Inhibitor-3, a sulfur-containing choline kinase inhibitor, effectively inhibits HChoK α1 with an IC50 value of 0.66 μM and possesses the capability to induce apoptosis. This compound is utilized in cancer research [1].

PI3K/mTOR Inhibitor-3 (compound 12) is an imidazoline compound with potent dual inhibitory effects on PI3K and mTOR. This compound exhibits notable anti-cancer activity [1].

Topoisomerase I/II inhibitor 3 (compound 7) is a potent dual inhibitor of topoisomerase I (Topo I) and II (Topo II) . By inhibiting PI3K /Akt/mTOR signaling pathway, Topoisomerase I/II inhibitor 3 can inhibit cell proliferation, invasion and migration, and induce apoptosis . Topoisomerase I/II inhibitor 3 has research value in liver cancer.

HIV-1 integrase inhibitor 3 is an HIV-1 integrase strand transfer (INST) inhibitor (IC50: 2.7 nM).

Glutaminyl Cyclase Inhibitor 3, a designed anti-Alzheimer’s compound, is a potent human Glutaminyl Cyclase (GC) inhibitor (IC50: 4.5 nM). It significantly reduced the brain concentrations of pyroform Aβ and total Aβ and restored cognitive functions.

KRas G12C inhibitor 3 is a compound that inhibits KRas G12C.

α-Synuclein inhibitor 3 (Compound 7g) is a potent inhibitor of α-synuclein (α -Syn) aggregation. It has potential applications in Parkinson's disease research [1].

Topoisomerase II inhibitor 3 (Compound 6 h) is an acridone derivative that acts as a Type II DNA topoisomerase (topo II) inhibitor. It specifically inhibits the topo IIα/β subtypes, with an IC50 value of 0.17 μM for topo IIα and 0.23 μM for topo IIβ. This compound elicits significant DNA damage and induces apoptosis by triggering the loss of mitochondrial membrane potential [1].

Compounds 17o (IC50: 14.0 nM, NCI-H460) and 17p (IC50: 2.9 nM, NCI-H460) with furan moieties showed potent cytotoxic effects at the nanomolar level against various human cancer cell lines.

Compound 5a, also known as DPP-4 inhibitor 3, is a powerful dipeptidyl peptidase IV (DPP-IV) inhibitor, demonstrating an IC50 value of 0.75 nM. It exhibits outstanding antioxidant and insulinotropic activity [1].

BET Bromodomain Inhibitor 3 is a BET bromodomain inhibitor with an inhibitory Ki value of >40 µM against BrdT. It is utilized in research related to contraception, cancer, and heart disease [1].

SPR inhibitor 3 is an effective sepiapterin reductase inhibitor. SPR inhibitor 3 decreases neuropathic and inflammatory pain through a reduction of BH4 levels. SPR inhibitor 3 shows a high binding affinity to human SPR in a cell-free assay (IC50=74 nM) an

GSK-3/CDK5/CDK2-IN-1 is an imidazole derivative compound that inhibits cdk5, cdk2, and GSK-3.it has demonstrated applications in cancer research and the study of neurodegenerative diseases [1].

Cathepsin K Inhibitor 3, exhibiting an IC50 value of 0.5 nM, is a highly selective inhibitor of cathepsin K, featuring a favorable pharmacokinetic profile. It holds potential for use in studies of osteoarthritis (OA).

IRAK inhibitor 3 is an interleukin-1 (IL-1) receptor-associated kinase (IRAK) modulator.

Aurora kinase inhibitor-3 (Aurora Kinase Inhibitor III) is a potent inhibitor of Aurora A kinase (IC50 = 42 nM).1 It is selective for Aurora A over BMX, BTK, IGF-1R, c-Src, TRKB, SYK, and EGFR.

GSK-3β inhibitor 7 is a GSK-3β inhibitor (IC50: 5.25 μM). GSK-3β inhibitor 7 acts by inserting into the ATP-binding binding pocket of GSK-3β and forming hydrogen bonds. GSK-3β inhibitor 7 has a high rate of glucose uptake by hepatocytes ( 83.5%) and can be used to study a variety of diseases such as cancer, diabetes, inflammation, Alzheimer's disease and bipolar disorder.

HPGDS inhibitor 3 is a powerful oral compound that selectively inhibits the hematopoietic prostaglandin D synthase (H-PGDS). With an IC50 value of 9.4 nM and EC50 of 42 nM, it demonstrates high potency in peripherally restricting H-PGDS. Moreover, HPGDS inhibitor 3 exhibits excellent selectivity with no associated central nervous system toxicity. This compound also possesses favorable pharmacokinetic properties in mouse, rat, and dog models. Additionally, HPGDS inhibitor 3 displays noteworthy anti-inflammatory activity [1].

MMP-3 Inhibitor is a peptide matrix metalloproteinase-3 (MMP-3) inhibitor with a Ki value of 95 nM.MMP-3 inhibitor has anticancer and antitumor activity.

sEH inhibitor-3 is an orally available, selective and potent inhibitor of soluble epoxide hydrolase (sEH) for the study of cancer.

Cyclophilin inhibitor 3 (compound 7c), a potent inhibitor of cyclophilin A (CypA), exhibited potent anti-HCV effects with an EC50 value of 4.2 μM.

GSK-3β inhibitor 15 (Compound 54), with an IC50 of 3.4 nM, effectively suppresses Aβ 1-42-induced phosphorylation of GSK-3β and tau protein, as well as LPS-induced iNOS expression. It demonstrates neuroprotective properties against Aβ 1-42-induced neurotoxicity, indicating its potential utility in Alzheimer's disease (AD) research [1].

Prostaglandin E2 (PGE2) inhibitor 3 is a selective inhibitor targeting microsomal prostaglandin E synthase-1 (mPGES-1; IC50 = 0.2 µM), demonstrating greater selectivity for mPGES-1 over COX-1, COX-2, 5-lipoxygenase (5-LO), and soluble epoxide hydrolase (sEH) in assays at 10 µM. This compound effectively reduces IL-1β-induced PGE2 production in A549 cells and decreases LPS-induced IL-6 and PGE2 in J774A.1 macrophages at concentrations of 10 and 1 µM, respectively. Additionally, it blocks the production of 5-LO-derived products, including leukotriene B4 (LTB4) and 5-H(p)ETE, in response to calcium ionophore A23187 alone or combined with arachidonic acid, with IC50 values of 4.9 and 5.2 µM, respectively. When administered in vivo at doses of 10 mg/kg, PGE2 inhibitor 3 effectively prevents leukocyte infiltration in a mouse model of zymosan-induced peritonitis.

Z-DEVD-FMK, a Caspase-3 Inhibitor, is an irreversible, cell-permeable inhibitor of caspase-3/CPP32 that impedes tumor cell apoptosis. In vivo studies show it offers neuroprotection in rat hippocampi post-seizures and considerably diminishes post-traumatic apoptosis, enhancing neurological recovery in rats before and after traumatic brain injury induction.

GSK-3β inhibitor 11 (compound 21) is a potent inhibitor of glycogen synthase kinase-3β (GSK-3β) with an inhibitory concentration (IC50) of 10.02 μM. This compound demonstrates potential utility in the field of neurodegenerative disease research [1].