aak1

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.

(Iso)-BMT-124110 Formate has an inhibitory effect on the protein serine threonine kinase AAK, and is used in the treatment of Parkinson's disease, schizophrenia, neuropathic pain, and Alzheimer's disease.

SGC-AAK1-1, a potent and selective inhibitor of AAK1 (AP2-associated kinase 1), has an IC50 of 270 nM and a Ki of 9 nM, and serves as a chemical probe.

AAK1 HDACs-IN-1 (Compound 12) is a dual inhibitor targeting AAK1 and HDACs, effectively inhibiting AAK1, HDAC1, and HDAC6, with IC50 values of 15.9, 148.6, and 5.2 nM, respectively. This compound also hinders SARS-CoV-2 infection by blocking the endocytosis of the ACE2-SARS-CoV-2 complex and the AP2M1-ACE2 interaction.

AAK1-IN-6 is an inhibitor of AP-2 associated protein kinase 1 (AAK1, IC50 = 12 nM) and exhibits antiviral activity against Dengue virus (DNEV2, EC50 = 0.24 μM) and Venezuelan equine encephalitis virus (VEEV, EC50 = 0.30 μM). AAK1-IN-6 is applicable in antiviral research.

SGC-AAK1-1N is a potent and selective inhibitor of AAK1 (AP2 associated kinase 1), with an IC50 of 1.8 μM [1].

AAK1-IN-2 (compound (S)-31) is a potent, selective, and brain-penetrant Adaptor Protein 2-Associated Kinase 1 (AAK1) inhibitor (IC50 = 5.8 nM) used in neuropathic pain research [1].

AAK1-IN-3 is a quinoline analogue that can be used in the research of neuropathic pain. AAK1-IN-3 is a brain-penetrant inhibitor of adaptor protein 2-associated kinase 1 (AAK1) (IC 50 = 11 nM) [1].

AAK1-IN-4 is a potent and specific inhibitor of adaptor protein-2-associated kinase 1 (AAK1), capable of efficiently penetrating the central nervous system and exhibiting oral bioactivity. It has demonstrated a high degree of selectivity with an AAK1 inhibitory concentration (IC50) of 4.6 nM, a Filt dissociation constant (Ki) of 0.9 nM, and a cellular IC50 of 8.6 nM. AAK1-IN-4 holds promise as a valuable tool in the investigation of neuropathic pain [1].

AAK1-IN-5 is a potent and specific inhibitor of adaptor protein-2-associated kinase 1 (AAK1), characterized by its ability to penetrate the central nervous system and its oral bioavailability. It displays high selectivity, with an AAK1 inhibitory potency (IC 50) of 1.2 nM, a binding affinity (K i) of 0.05 nM, and an inhibitory potency against cellular AAK1 activity (cell IC 50) of 0.5 nM. AAK1-IN-5 holds promise for investigating neuropathic pain in scientific research [1].

AAK1-IN-2 TFA (compound (S)-31) is a selective and potent inhibitor of AAK1 with an IC50 of 5.8 nM, capable of crossing the blood-brain barrier.

AAK1-IN-3 TFA is an adaptor protein 2-associated kinase 1 (AAK1) inhibitor (IC50: 11 nM) that crosses the blood-brain barrier and is a quinoline analogue.AAK1-IN-3 has shown potential for research in neuropathic pain.

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.

LP-922761 is a potent, selective, and orally active AAK1 inhibitor with inhibitory effects on BMP-2 induced protein kinase (BIKE).

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).

AAK1-IN-1 (example 123) is an AAK1 (adaptor associated kinase 1) inhibitor with an IC50 of 2.2 nM. AAK1-IN-1 can be used for neurodegenerative diseases research[1]. Adaptor associated kinase 1 (AAK1) is a member of the Arkl Prkl family of serine threonine kinases. AAKl mRNA exists in two splice forms termed short and long. The long form predominates and is highly expressed in brain and heart. AAKl is enriched in synaptosomal preparations and is co-localized with endocytic structures in cultured cells. AAKl modulates clatherin coated endocytosis, a process that is important in synaptic vesicle recycling and receptor-mediated endocytosis[1]. [1]. Guanglin Luo, et al. Biaryl kinase inhibitors. WO2015153720A1.

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.

RSS0680 is a protein kinase degrader that degrades a variety of kinases and can be used to study diseases caused by kinase abnormalities.

Pim1 AKK1-IN-1 (LKB1 AAK1 dual inhibitor) is a potent multi-kinase inhibitor with Kd values of 35 nM 53 nM 75 nM 380 nM for Pim1 AKK1 MST2 LKB1 respectively, and also inhibits MPSK1 and TNIK.

BMS-901715 is an effective and selective inhibitor of adapter protein-2 associated kinase 1 (AAK1; IC50: 3.3 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.

BMS-911172 is an adaptor-associated kinase 1 (AAK1 kinase) inhibitor with an IC50 of 35 nM.

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.