gsk3β inhibitor 3

GSK-3β inhibitor 3 is a potent, selective, and irreversible covalent inhibitor of glycogen synthase kinase 3β (GSK-3β) with an IC50 of 6.6 μM, and can be used to study acute promyelocytic leukemia.

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.

GSK3β Inhibitor XI has GSK3β inhibitory effect.

GNF4877 is a small molecule inhibitor, a potent dual-specificity kinase inhibitor targeting DYRK1A (IC50=6 nM) and GSK3β (IC50=16 nM). This compound promotes β-cell proliferation by blocking NFATc nuclear export (EC50=0.66 μM for mouse R7T1 cells) and is primarily used for research on β-cell regeneration related to diabetes.

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

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

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

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.

Akt1-IN-8 (Compound JL18) is a potent AKT1 kinase inhibitor with oral bioavailability of 41% and an IC50 value of 8.8 nM. It exhibits significant antiproliferative effects against PC-3 prostate cancer cells, with an IC50 of 3.0 μM. Akt1-IN-8 also reduces phosphorylated GSK3β levels.

GSK3β-IN-3 is an ATP-competitive GSK-3β inhibitor (IC50= 0.90 μM) that demonstrates good blood-brain barrier permeability (Pe= 10.7 x 10^-6 cm/s). It effectively reduces tau protein phosphorylation in the BR5706 strain and decreases Aβ aggregate deposition in the CL2006 strain, indicating its potential as a candidate for Alzheimer's disease (AD) research.

Ro 31-8220 formic is a potent inhibitor of protein kinase C (PKC), specifically targeting PKCα, PKCβI, PKCβII, PKCγ, PKCε, and rat brain PKC, with IC50 values of 5, 24, 14, 27, 24, and 23 nM, respectively. It also inhibits MAPKAP-K1b, MSK1, S6K1, and GSK3β, with IC50 values of 3, 8, 15, and 38 nM. Additionally, Ro 31-8220 formic suppresses the expression of MKP-1, induces c-Jun expression, and activates JNK, exhibiting these effects through mechanisms independent of PKC.

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

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.

Indirubin-3'-monoxime (Indirubin-3'-oxime) is a potent inhibitor of GSK3β (IC50: 22 nM) and also inhibits CDKs ( (IC50s: 100/180/250 nM for Cdk5/p35, Cdk1/cyclin B, Cdk2/cyclin E).

FSG67 is a glycerol 3-phosphate acyltransferase (GPAT) and glycerol-3-phosphate acyltransferase, mitochondrial (GPAM) inhibitor that attenuates hepatic regeneration following acetaminophen overdose by altering GSK3β and Wnt/β-catenin signaling.

APN/AKT-IN-1 is a potent dual inhibitor of aminopeptidase N (APN) and protein kinase B (AKT), with IC50 values of 0.21 μM for APN and 0.27 μM for AKT inhibition. The compound effectively suppresses the phosphorylation of glycogen synthase kinase 3 beta (GSK3β), an intracellular substrate of AKT [1].

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.

Ro 31-8220 is a potent inhibitor of PKC with IC50 values of 5, 24, 14, 27, 24, and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε, and rat brain PKC, respectively. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1, and GSK3β with IC50 values of 3, 8, 15, and 38 nM, respectively, without affecting MKK3, MKK4, MKK6, and MKK7.

hAChE-IN-6 (compound 51) is a brain-penetrant acetylcholinesterase (AChE) inhibitor with an IC50 of 0.16 μM. It also inhibits 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), making it useful for Alzheimer's disease (AD) research [1].

hAChE-IN-5 (compound 49) is a dual inhibitor of human acetylcholinesterase (hAChE) and human butyrylcholinesterase (hBuChE), showing IC50 values of 0.17 μM for both enzymes. It also potently inhibits glycogen synthase kinase 3 beta (GSK3β) with an IC50 of 0.21 μM. Furthermore, it effectively inhibits tau protein and Aβ1-42 peptide self-aggregation, and can bind the peripheral anionic site (PAS) to prevent amyloid-beta (Aβ)-induced neurotoxicity. hAChE-IN-5's ability to cross the blood-brain barrier (BBB) supports its potential in developing multitargeted anti-Alzheimer's agents [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.