gsk-a-1

GSK-A1 is a specific inhibitor of PI4KA, also inhibited calcium-driven PRL secretion without affecting calcium signaling and Prl expression. GSK-A1 has anti-hepatitis C virus (HCV) potential.

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

MBM-55S is an effective inhibitor of Nek2 with an IC50 of 1 nM. MBM-55S indecus cell cycle arrest and apoptosis thereby inhibiting the proliferation of cancer cells. MBM-55S shows antitumor activities.

GSK 2833503A is a potent and selective TRPC6 and TRPC3 antagonist (IC50 = 3-16 nM and 21-100 nM, respectively). GSK 2833503A exhibits >63-fold selectivity over other ion channels, including other TRP channels, CaV1.2, hERG and NaV1.5. GSK 2833503A suppresses angiotensin II or endothelin-1-induced cardiac hypertrophy signaling in HEK293 cellsin vitroand in cardiomyocytes.

GSK1904529A (GSK 4529) is a specific inhibitor of IGF-1R (IC50=27 nM) and IR(IC50=25 nM) .

ARN25068 is a potent inhibitor of GSK-3β, FYN, and DYRK1A protein kinases, exerting its activity in the sub-micromolar range. This compound effectively addresses tau hyperphosphorylation [1].

GSK-364735 is a human immunodeficiency virus type 1 integrase (HIV-1 IN) inhibitor with antiviral activity and is used in the study of retroviral infections.

GSK3-IN-4 is a GSK-3 inhibitor with IC50 of 0.101-1 μM of GSK-3α and GSK-3β in Calipe Assay.

(E/Z)-GSK-3β inhibitor 1 is a glycogen synthase kinase 3β (GSK-3β) inhibitor demonstrating high antidiabetic efficacy.

GSK-2793660 is an orally active and irreversible inhibitor of Cathepsin C (CTSC). GSK-2793660 is a bioactive dipeptide that can be used for the research of bronchiectasis [1] [2].

GSK-5498A is a selective blocker of CARC (IC50, 1 μM). It inhibits mediator release from mast cells, and pro-inflammatory cytokine release from T-cells in a variety of species.

GSK 690 (Hydrochloride) is a reversible lysine-specific demethylase 1 (LSD1) inhibitor with a Kd of 9 nM and an IC50 of 37 nM.

MBM-55 is an effective inhibitor of NIMA related kinase 2 (NEK2) with an IC50 of 1 nM. MBM-55 effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis.

BIP-135 is a potent and selective ATP-competitive GSK-3 inhibitor, with IC50 values of 16 nM and 21 nM for GSK-3α and GSK-3β, respectively, and exhibits neuroprotective effects [1].

SB-265610 (GSK-CXCR2) is a nonpeptide and allosteric CXCR2 antagonist. SB-265610 blocks rat cytokine-induced neutrophil chemoattractant-1 (CINC-1)-induced calcium mobilization and neutrophil chemotaxis (IC50s: 3.7 nM and 70 nM, respectively).

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.

hAChE hBuChE GSK-3β-IN-1 (Compound 6c) is a multi-target compound designed for Alzheimer's treatment capable of crossing the blood-brain barrier. It inhibits hAChE with an IC50 of 28.88 nM, hBuChE with an IC50 of 131.90 nM, and GSK-3β with an IC50 of 51.42 nM. Additionally, it acts as an inhibitor of tau protein and Aβ protein aggregation.

Protein Kinase Inhibitor 12 (compound 1-91) is a triazole derivative and protein kinase inhibitor, particularly effective against PIM-1, CDK-2, GSK-3, and SRC mammalian protein kinases, and can be used to study diseases related to protein kinases.

Protein kinase inhibitor 13 (Compound I-90) functions as a kinase inhibitor, specifically targeting kinases such as PIM-1, CDK-2, GSK-3, and SRC.

GSK-3α/β-IN-1 is a GSK-3α/β inhibitor with IC50 values of 0.265 μM for GSK-3α and 0.255 μM for GSK-3β. It also inhibits PKA with an IC50 of 0.188 μM. GSK-3α/β-IN-1 effectively reduces cell viability in three glioblastoma (GBM) cell lines (IC50: 3-6 μM over 72 hours) without being toxic to human astrocytes, and it exhibits good metabolic stability. Additionally, it shows potential central nervous system activity in a whole human blood-brain barrier (BBB) GBM model.

GSK-3β/CK-1δ-IN-1 (8d) is a dual inhibitor of GSK-3β and CK-1δ that can cross the blood-brain barrier, with IC50 values of 0.77 μM and 0.57 μM, respectively. GSK-3β/CK-1δ-IN-1 (8d) is applicable in neuroblastoma research.

GSK-3β inhibitor 9 (Compound 9b) is a highly selective, orally bioavailable and potent GSK-3β inhibitor with the IC 50 of 35 nM. GSK-3β inhibitor 9 exhibits good pharmacokinetic profiles including favorable BBB penetration. GSK-3β inhibitor 9 is able to be used for the research of Alzheimer's disease [1].

GSK-114, a selective inhibitor of TNNI3 Interacting Kinase (TNNI3K) with IC50 of 25 nM, shows significant bias for TNNI3K over B-Raf with IC50 of 1000 nM, exceptional broad spectrum kinase selectivity and adequate oral exposure to enable its use in cellul

CHIR-99021 HCl (Laduviglusib HCl) is a highly potent and selective inhibitor of GSK-3α/β, with IC50 values of 10 nM and 6.7 nM respectively. It demonstrates remarkable selectivity for GSK-3, with over 500-fold selectivity over CDC2, ERK2, and other protein kinases. Additionally, CHIR-99021 HCl serves as a robust activator of the Wnt/β-catenin signaling pathway. Moreover, it exhibits the ability to enhance self-renewal in both mouse and human embryonic stem cells. Furthermore, CHIR-99021 HCl induces autophagy [1] [2] [3].