gak

SGC-GAK-1 is a selective cyclin G-associated kinase (GAK) inhibitor (Ki: 3.1 nM).

Mps1-IN-1 is a potent, selective, and ATP-competitive inhibitor of Mps1 kinase (IC50: 367 nM).

GAK inhibitor 2 (Compound 14g) is a highly potent inhibitor of cyclin G-associated kinase (GAK) with an IC50 of 0.024 μM and exhibits remarkable antiviral activity against dengue virus (DENV) with an EC50 of 1.049 μM [1].

GAK inhibitor 49 hydrochloride is a potent, highly selective, ATP-competitive inhibitor of cyclin G-associated kinase (GAK) with a Ki of 0.54 nM and a cell IC50 of 56 nM. It can also bind to RIPK2.

GAK inhibitor 49 is a highly selective and ATP-competitive cyclin G associated kinase (GAK) inhibitor (IC50: 56 nM; Ki: 0.54 nM ).

EPHA2/A4/GAK-IN-1 (compound 55) is a potent inhibitor of EPHA2, EPHA4, and GAK, exhibiting KD values of 180.5 nM for EPHA2 and 19.2 nM for GAK, respectively. The predicted half-life of EPHA2/A4/GAK-IN-1 in microsomal stability tests measures 4.6 hours. Additionally, this compound has antiviral efficacy, capable of preventing Dengue virus infection in Huh7 hepatocytes.

SGC-GAK-1N is a negative control for SGC-GAK-1.

BMT-124110 Formate is a selective AAK1 inhibitor (IC50: 0.9 nM) with anti-injury sensory activity.BMT-124110 Formate inhibits the BMP-2-inducible protein kinase BIKE with an IC50: 17 nM.BMT-124110 Formate inhibits the cell-cycle protein G-related BMT-124110 Formate inhibits the cell cycle protein G-associated kinase GAK with an IC50:99 nM.

LP-935509 is a selective, brain-permeable, small molecule competitive inhibitor of articulin-2-associated kinase 1 (AAK1) with an IC50 of 3.3 nM and a Ki of 0.9 nM. LP-935509 is a potent inhibitor of BIKE (IC50 of 14 nM) and a moderate inhibitor of GAK (IC50 of 320±40 nM).

Garvicin KS (GarKS) is a bacteriocin composed of a 34 amino acid peptide, GakA, and two additional peptides, GakB and GakC. GakA alone has been found to reduce fibroblast viability and proliferation. When combined with GakB, GakA forms an effective duo that exhibits notable peptide stability, antimicrobial potency, and an influence on fibroblast viability and proliferation. Among the Garvicin KS peptides, GakB is the most effective against MSSA, with minimum inhibitory concentration (MIC) values ranked as GakB > GakC > GakA [1].

Garvicin KS (GarKS) is a bacteriocin comprising a 34-amino-acid peptide, GakB, along with two additional peptides, GakA and GakC. GakB specifically impairs fibroblast viability and proliferation. When combined with GakA, GarKS demonstrates enhanced peptide stability, antimicrobial activity, and notable impacts on fibroblast viability and proliferation. Regarding methicillin-sensitive Staphylococcus aureus (MSSA) inhibition, minimum inhibitory concentration (MIC) values rank the peptides in descending order of effectiveness as GakB, followed by GakC, and then GakA [1].

Garvicin KS is a 32-amino-acid peptide that, in collaboration with two other peptides, GakA and GakB, constitutes the bacteriocin GarKS. This compound impairs fibroblast viability and proliferation and exhibits antimicrobial activity against MSSA, demonstrating minimum inhibitory concentration (MIC) values ranked as GakB > GakC > GakA [1].

Nigakinone, isolated from Kumu, is an alkaloid with the pharmacological activity.

BMT-124110 is a selective AAK1 inhibitor (IC50: 0.9 nM) with antinociceptive activity. BMT-090605 inhibited BMP-2 induced protein kinase BIKE with IC50 of 17 nM. BMT-090605 inhibits cyclin G-associated kinase GAK with an IC50 of 99 nM.

Anagrelide (Xagrid) is a Platelet-reducing Agent. The mechanism of action of anagrelide is as a Phosphodiesterase 3 Inhibitor. The physiologic effect of anagrelide is by means of Decreased Platelet Production.

Eltrombopag (SB-497115-GR), an orally active thrombopoietin receptor agonist with megakaryopoiesis stimulating activity, binds to and stimulates the platelet thrombopoietin receptor (TPO-R or CD110).

Eltrombopag Olamine (Eltrombopag diethanolamine salt) is an orally active small-molecule, nonpeptide thrombopoietin receptor agonist that stimulates megakaryopoiesis. It binds to and activates the transmembrane domain of the platelet thrombopoietin receptor (TPO-R or CD110), promoting the proliferation and differentiation of megakaryocytic cells and enhancing platelet production.

Avatrombopag (YM477) is a new oral thrombopoietin (TPO) receptor agonist, activating TPO receptor and increasing megakaryocytic proliferation/differentiation and platelet production.

Mps1-IN-2 is a potent, selective, and ATP-competitive inhibitor of both Mps1 and Plk1.

TIM-098a is a selective AAK1 inhibitor with an IC50 of 0.24 µM. It does not inhibit CaMKK isoforms. By inhibiting AAK1 kinase activity, TIM-098a disrupts AAK1-regulated endocytosis.

Ro3280 (Ro5203280) is an effective, specific inhibitor of PLK1(IC50=3, Kd=0.09 nM).

SM1-71 is a potent multi-targeted acrylamide-modified TAK1 inhibitor that inhibits MKNK2, MAP2K1/2/3/4/6/7, GAK, AAK1, BMP2K, MAP3K7, MAPKAPK5, GSK3A/B, MAPK1/3, SRC, YES1, FGFR1, ZAK (MLTK), MAP3K1, LIMK1 and RSK2.SM1-71 can be used as a kinase probe with anticancer activity and inhibits the proliferation of various cancer cell lines.

Mps1-IN-1 dihydrochloride, a potent ATP-competitive inhibitor of Mps1 kinase, exhibits an IC50 of 367 nM. It effectively inhibits the activity of Mps1 mitotic kinase and disrupts spindle assembly checkpoint (SAC) function, thereby reducing the viability of both cancerous and 'normal' cells.

Megakaryocytes/platelets inducing agent being useful in treating diseases involving thrombopenia. Megakaryocytes/platelets inducing agent is an inducing agent for megakaryocytes and/or platelets from pluripotent stem cells.