AAK1 Inhibitor

LP-935509 is an orally active, potent, selective, ATP-competitive and brain-penetrant inhibitor of adaptor protein-2 associated kinase 1 (AAK1) with an IC₅₀ of 3.3 nM and a K_i of 0.9 nM, respectively. LP-935509 is also a potent inhibitor of BIKE (IC₅₀=14 nM) and a modest inhibitor of GAK (IC₅₀=320 nM). LP-935509 shows antinociceptive activity. LP-935509 can be used for neuropathic pain and SARS-CoV-2 research.

FMF-06-098-1 is a multi-target kinase PROTAC degrader. FMF-06-098-1 can be used to target degradation kinases which degrades AAK1, AΒL2, AURKA, AURKB, BUBIB, CDC7, CDK1, CDK12, CDK13, CDK2, CDK4, CDk6, CDK7, CDK9, CHEK1, CSNKID, EPHA1, PER, FGFR1, GAK, IRAK4, ITK, LIMK2, MAP4K2, MAP4K3, MAPK6, MAPK7, MARK4, MELK, PKN3, PLK4, PRKAA1, PTK2, PTK6, RPS6KA4, S1K2, STK35, TNK2, UHMK1, ULK1, and WEE1.

dAurAB5 is a dual Aurora-A (DC₅₀ = 8.8 nM) and Aurora-B (DC₅₀ = 6.1 nM) PROTAC degrader. dAurAB5 induces degradation of Aurora-A and Aurora-B, reduces N-Myc levels, and decreases viability in IMR32 neuroblastoma cells. dAurAB5 downregulates the levels of AAK1, PTK2, GAK, and TTK. dAurAB5 can be used to study cancers such as neuroblastoma. (Pink: TTK ligand 2: HY-168542, Blue: Thalidomide-O-COOH: HY-103597, Black: 6-Aminocaproic acid: HY-B0236).

AAK1-IN-12 (Compound 4) is a selective, orally active AAK1 inhibitor that can cross the blood-brain barrier. AAK1-IN-12 is applicable to the research of schizophrenia, Parkinson's disease, neuropathic pain and Alzheimer's disease.

BMT-090605 hydrochloride is a potent, selective the adapter protein-2 associated kinase 1 (AAK1) inhibitor with an IC₅₀ value of 0.6 nM. BMT-090605 hydrochloride shows antinociceptive activity. BMT-090605 hydrochloride inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC₅₀ values of 45 nM and 60 nM, respectively. BMT-090605 hydrochloride can be used for the research of neuropathic pain.

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

GSK-3β inhibitor 13 (compound 47) is an orally active and potent GSK-3β inhibitor with blood-brain permeability. GSK-3β inhibitor 13 inhibits GSK-3β and GSK-3α with IC₅₀s of 0.73 nM and 0.35 nM, respectively. GSK-3β inhibitor 13 significantly decreases the phosphorylation of tau (IC₅₀=58 nM), which leads the formation of the neurofibrillary tangles associated with Alzheimer's disease.

BMT-124110 formic is a potent, selective AAK1 inhibitor, with an IC₅₀ of 0.9 nM. BMT-124110 shows antinociceptive activity. BMT-124110 formic inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC₅₀s of 17 and 99 nM, respectively.

AAK1-IN-9 (Compound 3) is an AAK1 (adaptor associated kinase 1) inhibitor with an IC₅₀ of 10.92 nM. AAK1-IN-9 can be used in the study of neurodegenerative diseases.

AAK1/HDACs-IN-1 (Compound 12) is the dual inhibitor for AAK1 and HDAC, that inhibits AAK1, HDAC1, and HDAC6 with IC₅₀s of 15.9, 148.6, and 5.2 nM, respectively. AAK1/HDACs-IN-1 inhibits SARS-CoV-2 infection, suppresses the endocytosis of ACE2-SARS-CoV-2 complex, as well as AP2M1-ACE2 interaction.

SARS-CoV-2-IN-81 (compound 12e) is a potent AAK1 inhibitor with an IC₅₀ value of 9.38 nM. SARS-CoV-2-IN-81 shows anti-viral property against SARS-CoV-2. SARS-CoV-2-IN-81 attenuates AAK1-induced phosphorylation of AP2M1 threonine 156 and disrupts the direct interaction between AP2M1 and ACE2, ultimately inhibiting SARS-CoV-2 infection.

HW161023 (compound 5) is an orally active AP2-associated protein kinase 1 (AAK1) inhibitor with IC₅₀ values of 5.4 nM and 11.9 μM aganist of AAK1and hERG, respectively. HW161023 inhibits the pain in chronic constriction injury of the sciatic nerve rat model.

AAK1-IN-10 (Compound 1-2) is an AAK1 inhibitor. AAK1-IN-10 has significant AAK1 enzyme inhibitory activity (IC₅₀: 9.62 nM). AAK1-IN-10 mainly exerts its effects by inhibiting the activity of connexin-associated kinase 1 (AAK1). AAK1-IN-10 has low cardiotoxicity (IC₅₀ = 13.7 μM). AAK1-IN-10 can be used in the study of diabetic neuropathy and postherpetic pain.

TIM-098a is a selective AAK1 inhibitor with an IC₅₀ of 0.24 µM. TIM-098a has no inhibitory activity against CaMKK isoforms. TIM-098a inhibits AAK1-regulated endocytosis by suppressing AAK1 kinase activity.

BMT-090605 is a potent, selective the adapter protein-2 associated kinase 1 (AAK1) inhibitor with an IC₅₀ value of 0.6 nM. BMT-090605 shows antinociceptive activity. BMT-090605 inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC₅₀ values of 45 nM and 60 nM, respectively. BMT-090605 can be used for the research of neuropathic pain.

BMT-090605 (hydrochloride) (Standard) is the analytical standard of BMT-090605 (hydrochloride) (HY-101290A). This product is intended for research and analytical applications. BMT-090605 hydrochloride is a potent, selective the adapter protein-2 associated kinase 1 (AAK1) inhibitor with an IC50 value of 0.6 nM. BMT-090605 hydrochloride shows antinociceptive activity. BMT-090605 hydrochloride inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC50 values of 45 nM and 60 nM, respectively. BMT-090605 hydrochloride can be used for the research of neuropathic pain.

AAK1-IN-6 (Compound 23) is an inhibitor of AP-2-associated protein kinase 1 (AAK1, IC₅₀ = 12 nM) with antiviral activity against the dengue virus (DNEV2, EC₅₀ = 0.24 μM) and Venezuelan equine encephalitis virus (VEEV, EC₅₀ = 0.30 μM). AAK1-IN-6 can be utilized in antiviral research.

AAK1-IN-7 (Compound 16) is a dual AAK1/GAK inhibitor (EC₅₀ values are 40 and 80 nM, respectively). AAK1-IN-7 inhibits the phosphorylation of AP2-µ2 subunit at T156. AAK1-IN-7 has weak antiviral activity against RNA viruses.

AAK1-IN-8 (Compound 18) is a pan-NAK inhibitor. AAK1-IN-8 inhibits AAK1 and GAK (EC₅₀ values are 50 and 190 nM, respectively). AAK1-IN-8 inhibits the phosphorylation of AP2-µ2 subunit at T156.

BMT-046091 is a selective inhibitor of adaptor-associated kinase 1 (AAK1). BMT-046091 inhibits phosphorylation of the μ2 peptide by AAK1 with an IC₅₀ value of 2.8 nM.