About 30 results found for searched term "GSK-3 inhibitor 4" (0.11 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M43378 | GSK-3 inhibitor 4 | GSK-3 |
| GSK-3 inhibitor 4 is an orally active and brain-penetrant inhibitor of GSK-3, CDK2, and CDK5, with IC50 values of 0.56 nM (GSK-3β), 0.45 nM (GSK-3α), 0.47 μM, and 0.68 μM, respectively. | ||
| M1758 | Foretinib | c-Met |
| GSK089; EXEL-2880; XL880; GSK1363089 | ||
| Foretinib (XL880, GSK1363089) is a multi-targeted inhibitor of c-Met and vascular endothelial growth factor receptor 2 (VEGFR2) with IC50 value of 0.4 nM for c-MET. | ||
| M2061 | SB 216763 | GSK-3 |
| SB 216763 is a potent and selective, cell permeable glycogen synthase kinase-3 (GSK-3) inhibitor with an IC50 value of 34 nM for GSK-3α. | ||
| M2405 | AR-A014418 | GSK-3 |
| GSK-3β Inhibitor VIII | ||
| AR-A014418 is an ATP-competitive, and selective GSK3β inhibitor with IC50 and Ki of 104 nM and 38 nM, without significant inhibition on 26 other kinases tested. | ||
| M2733 | GSK2190915 | Lipoxygenase |
| AM-803, Fiboflapon | ||
| GSK2190915 (AM803), a potent FLAP inhibitor, prevents the synthesis of leukotrienes and 5-oxo-ETE, with IC50 of 76 nM for inhibition of LTB4 in human blood, provides treatment for asthma. | ||
| M2736 | GSK343 | EZH2 |
| GSK343 is a potent and selective EZH2 inhibitor with IC50 of 4 nM, showing 60 fold selectivity against EZH1, and >1000 fold selectivity against other histone methyltransferases. | ||
| M3484 | Dolutegravir | Integrase |
| GSK1349572 | ||
| Dolutegravir (GSK1349572) is a two-metal-binding HIV integrase inhibitor with IC50 of 2.7 nM, modest activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q148H. | ||
| M5269 | GSK180736A | ROCK |
| GSK180736 | ||
| GSK180736A, developed as a Rho-associated, coiled-coil-containing protein kinase inhibitor, binds to GRK2(G protein-coupled receptor kinase 2) with logIC50 pf -6.6 (logIC50 -4.0 for GRK5 and >-3 for GRK1); ≥400-fold selective for GRK2 over both GRK1 and GRK5. | ||
| M6771 | GSK2837808A | LDH |
| GSK 2837808A | ||
| GSK2837808A is a potent, selective lactate dehydrogenase A (LDHA) inhibitor with IC50s of 2.6 and 43 nM for hLDHA and hLDHB, respectively. | ||
| M6772 | GSK 319347A | IκB/IKK |
| GSK319347A | ||
| GSK319347A is a dual inhibitor of TBK1 and IKKε with IC50s of 93 nM and 469 nM, respectively. | ||
| M9146 | GSK1324726A | Epigenetic Reader Domain |
| I-BET726 | ||
| GSK1324726A (I-BET726) is a highly selective inhibitor of BET family proteins with IC50 of 41 nM, 31 nM, and 22 nM for BRD2, BRD3, and BRD4, respectively. | ||
| M9526 | GSK-J5 | Histone demethylase |
| GSK J5 | ||
| GSK-J5 is a cell-permeable, inactive control for histone demethylase JMJD3/UTX inhibitor GSK-J4. | ||
| M9871 | GSK2643943A | Deubiquitinase |
| GSK2643943A is a deubiquitylating enzyme (DUB) inhibitor targeting USP20/Ub-Rho with an IC50 of 160 nM. GSK2643943A has anti-tumor efficacy and can be used for the research of oral squamous cell carcinoma (OSCC). | ||
| M10530 | BRD0705 | GSK-3 |
| BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM. | ||
| M10637 | GSK3368715 2HCl | PRMTs |
| EPZ019997 2HCl | ||
| GSK3368715 2HCl is a novel potent, orally active, reversible type I protein arginine methyltransferases (PRMTs) inhibitor, with IC50 values of 3.1 nM, 48 nM, 1148 nM, 5.7 nM and 1.7 nM for PRMT1, PRMT3, PRMT4, PRMT6, PRMT8, respectively. | ||
| M10933 | GSK3179106 | RET |
| GSK3179106 is an orally active, selective RET kinase inhibitor for human and rat RET IC50 0.4 nM and 0.2 nM, respectively. GSK3179106 has the potential for use in irritable bowel syndrome (IBS) by reducing post-inflammatory and stress-induced visceral hypersensitivity reactions. | ||
| M13815 | GSK-3484862 | DNA Methyltransferase |
| GSK-3484862 is a non-covalent inhibitor for Dnmt1. GSK-3484862 induces DNA hypomethylation to against cancer. GSK-3484862 mediates global demethylation in murine embryonic stem cells. | ||
| M14837 | GSK-3β inhibitor 1 | GSK-3 |
| GSK-3β inhibitor 1 (compound 3a) is a glycogen synthase kinase 3β (GSK-3β) inhibitor and demonstrates high antidiabetic efficacy, with an IC50 of 4.9 nM. | ||
| M21394 | GSK3368715 3HCl | Others |
| GSK3368715 is a potent inhibitor of type I protein arginine methyltransferases (PRMT) that inhibits PRMT1, 3, 4, 6 and 8, corresponding to Kiapp values ranging from 1.5 nM to 81 nM. | ||
| M21395 | GSK3186899 | Others |
| DDD-853651 | ||
| GSK3186899 (DDD-853651) is an inhibitor of CRK12 with an EC50 value of 1.4 μM for L. donovani. | ||
| M28252 | GSK837149A | FAS |
| GSK837149A is a selective inhibitor of human Fatty Acid Synthase (FASN) targeting the KR domain. GSK837149A has reversible inhibition effect on FASN and selectivity for type I FASN (Ki=30 nM). GSK837149A is also a competitive inhibitor of NADPH and a non-competitive inhibitor of acetoacetyl-CoA. GSK837149A can be used for the research of obesity and breast cancer. | ||
| M28650 | BRD0209 | GSK-3 |
| BRD0209 is a potent, selective and dual inhibitor of GSK3α/β inhibitor (GSK3α IC50 = 19 nM; GSK3β IC50 = 5 nM). BRD0209 is also a reversible ATP-competitive inhibitor with fast-off kinetics (Ki = 4.2 nM, respectively). BRD0209 is a tricyclic pyrazolotetrahydroquinolinone compound. BRD0209 has the potential for the research of mood disorder diseases. | ||
| M28726 | GSK3368715 | Histone Methyltransferase |
| EPZ019997 | ||
| GSK3368715 (EPZ019997) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 (EPZ019997) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity. | ||
| M28814 | GSK8573 | Epigenetic Reader Domain |
| GSK8573 is an inactive control compound for GSK2801 (acetyl-lysine competitive inhibitor of BAZ2A and BAZ2B bromodomains). GSK8573 has binding activity to BRD9 with a Kd value of 1.04 μM and is inactive against BAZ2A/B and other bromodomain familiy. GSK8573 can be used as a structurally related negative control compound in biological experiments. | ||
| M29173 | GSK3494245 | Parasite |
| DDD01305143 | ||
| GSK3494245 (DDD01305143) is a potent, orally active, and selective inhibitor of the chymotrypsin-like activity of the parasite proteasome binding in a site sandwiched between the β4 and β5 subunits (IC50=0.16 μM for WT L. donovani proteasomes). GSK3494245 moderately inhibits chymotrypsin-like activity of human proteasome (IC50: purified 26S=13 µM; enriched THP-1 extracts IC50=40µM). GSK3494245 exhibits attractive biological and biosafety properties. | ||
| M29291 | GSK973 | Epigenetic Reader Domain |
| GSK973 is a highly selective, orally bioavailable inhibitor of the BD2s (second bromodomains) of the BET family, with a pIC50 of 7.8 and a pKd of 8.7 for BRD4 BD2. GSK973 displays a 1600-fold selectivity for BRD4 BD2 over BRD4 BD1. GSK973 shows good potency against BRD2 BD2, BRD3 BD2, and BRDT BD2 (pIC50=7.4~7.8; pKd=8.3~8.5). | ||
| M29789 | GSK215 | FAK |
| GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader with a pDC50 of 8.4. GSK215 is designed by a binder for the VHL E3 ligase and the FAK inhibitor VS-4718. GSK215 induces rapid and prolonged FAK degradation, giving a long-lasting effect on FAK levels and a marked pharmacokinetic/pharmacodynamics (PK/PD) disconnect. | ||
| M30050 | GSK-3 Inhibitor XIII | GSK-3 |
| GSK-3 Inhibitor XIII is a potent and ATP-competitive GSK-3 inhibitor with a Ki of 24 nM. | ||
| M30534 | GSK356278 | PDE |
| GSK356278 is a potent, selective, orally bioavailable and brain-penetrant inhibitor of phosphodiesterase 4 (PDE4), with pIC50s of 8.6, 8.8, and 8.7 for human PDE4A, PDE4B, and PDE4D, respectively. GSK356278 has anti-inflammatory activity, and exhibits anxiolytic and cognition-enhancing effects. | ||
| M49514 | GSK-3/CDK5/CDK2-IN-1 | CDK |
| GSK-3/CDK5/CDK2-IN-1, an imidazole derivative, is an inhibitor of cdk5, cdk2, and GSK-3 extracted from patent WO2002010141A1, example 9a. | ||
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