gak

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

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.

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

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

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

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.

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].

Zigakibart (BION-1301) is a humanized monoclonal antibody targeting TNFSF13 with anti-inflammatory activity for the study of immunoglobulin A nephropathy (IgAN).

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.

BMT-090605 is a potent, selective AAK1 inhibitor with an IC50 of 0.6 nM, and inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC50s of 45 and 60 nM, respectively[1]. BMT-090605 also exhibits antinociceptive activity.

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).

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

PKN3-IN-1 (compound 16) inhibits PKN3 (serine threonine-protein kinase N3) and GAK (cyclin G-associated kinase) with an IC50 of 0.014 μM and a Ki of 0.0044 μM. PKN3-IN-1 is a potential tool compound for investigating the cell biology of PKN3 and its role in pancreatic and prostate cancers, as well as T-cell acute lymphoblastic leukemia.

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.

BMT-090605 hydrochloride is an effective and selective inhibitor of connexin-2 associated kinase 1 (AAK1) (IC50=0.6 nM). BMT-090605 hydrochloride inhibits BMP-2 induced protein kinase (BIKE) (IC50=45 nM) and cyclin G-related kinase GAK (IC50=60 nM). BMT-090605 hydrochloride shows anti-injury activity. BMT-090605 hydrochloride has research value in neuropathic pain.

LP-922761 hydrate is a selective, potent, orally active AAK1 inhibitor with IC50 values of 4.8 nM and 7.6 nM in enzyme and cellular assays, respectively. LP-922761 hydrate inhibits BMP-2 inducible protein kinase (BIKE) (IC50: 24 nM). 922761 hydrate has no significant effect on cellular GAK, opioids, adrenergic α2 or GABAa receptors.

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.

DB1113 (Example 24) is a bifunctional compound designed for the targeted degradation of various kinases, including ABL1, ABL2, BLK, CDK11B, CDK4, CSK, EPHA3, FER, GAK, LIMK1, MAP3K20, MAP4K1, MAP4K2, MAP4K3, MAP4K5, MAPK14, MAPK7, MAPK8, MAPK9, MAPKAPK2, MAPKAPK3, NLK, PDIK1L, PTK2B, RIPK1, RPS6KA1, RPS6KA3, SIK2, SIK3, STK35, TNK2, and ULK1. This capability positions DB1113 as a valuable tool for research into diseases or disorders associated with aberrant kinase activity [1].