glycogen synthase kinase-3

CHIR-99021 (CT99021) is an activator of the Wnt/β-catenin signaling pathway and a GSK-3α/β inhibitor (IC50=10/6.7 nM) with selective and oral activity.CHIR-99021 induces cellular autophagy, which enhances self-renewal in mouse and human embryonic stem cells.

5-Iodo-indirubin-3'-monoxime is a potent inhibitor of GSK-3β, CDK5/P25, and CDK1/cyclin B, competing with ATP for binding to the catalytic site of the kinase (IC50s: 9, 20, and 25 nM).

GNF4877 is a potent inhibitor of DYRK1A and GSK3β (IC50s: 6 nM and 16 nM, respectively), resulting in the blockade of nuclear export of nuclear factor of activated T-cells (NFATc) and increased β-cell proliferation.

R547 (Ro 4584820) is a potent ATP-competitive inhibitor of CDK1/2/4 with Ki of 2 nM/3 nM/1 nM. It is less potent to CDK7 and GSK3α/β, while inactive to other kinases. Phase 1.

Cromolyn sodium (FPL-670) is a chromone complex that acts by inhibiting the release of chemical mediators from sensitized mast cells.

Tideglusib (NP031112), a non-ATP competitive inhibitor of glycogen synthase kinase 3 (GSK-3), is with anti-inflammatory and neuroprotective activities.

VP3.15 dihydrobromide is a potent, orally bioavailable, and CNS-penetrant dual inhibitor of phosphodiesterase (PDE7) and glycogen synthase kinase (GSK)3, with IC50 values of 1.59 μM and 0.88 μM, respectively.

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

GSK-3β inhibitor 10 has skin-whitening, anti-oxidizing and PPAR activities.

A 1070722 is a potent and selective GSK-3 inhibitor, exhibiting high affinity for both GSK-3α (Ki = 0.6 nM) and GSK-3β (Ki = 0.6 nM). It can penetrate the blood-brain barrier (BBB) and accumulate in brain regions, indicating potential use as a PET radiotracer for quantifying GSK-3 in the brain.

BRD0705 is a potent, orally active GSK3α inhibitor with high selectivity (IC50: 66 nM; Kd: 4.8 μM), demonstrating an 8-fold higher selectivity for GSK3α compared to GSK3β (IC50: 515 nM).

BRD5648 ((R)-BRD0705) is an inactive (R)-enantiomer of BRD0705, a GSK3α inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM, used in acute myeloid leukemia [AML] studies.

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

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

9-ING-41 is a glycogen synthase kinase-3 inhibitor.

TCS 21311 (NIBR3049) is an effective and highly selective inhibitor of JAK3 (IC50: 8 nM). TCS 21311 inhibits PKCα, PKCθ, and GSK3β (IC50s: 13, 68, and 3 nM, respectively). It displays >100-fold selectivity over JAK1, JAK2, and TYK2.

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

LY2090314, an effective GSK-3α/β inhibitor (IC50: 1.5 nM/0.9 nM), may improve the efficacy of platinum-based chemotherapy regimens. LY2090314 has been used in trials studying the treatment of Leukemia, Advanced Cancer, and Pancreatic Cancer.

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

AZD2858 is a selective GSK-3 inhibitor, inhibiting tau phosphorylation at the S396 site and activating Wnt signaling pathway.

Bikinin (Abrasin), a potent inhibitor of plant GSK-3/Shaggy-like kinase, activates BR signaling downstream of the BR receptor.

TWS119 is a GSK-3β inhibitor; capable of inducing neuronal differentiation

MeBIO is an agonist of aryl hydrocarbon receptor, with IC50 of 44 and 55 μM for GSK-3 and CDK1/CyclinB, respectively. MeBIO does not affect GSK-3β.

7-bromoindirubin-3'-oxime (7BIO) is a caspase independent nonapoptotic cell death inducer. 7BIO is an inhibitor of FLT3, DYRK1A, DYRK2, Aurora B and Aurora C kinases.