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Neuroscience

AAK1 (AP2 associated kinase 1)

Melanocortin Receptor

Neuropeptide Y Receptor

Serotonin Transporter

(124)

iGluR

(401)

AAK1 (AP2 associated kinase 1)

AAK1 (AP2-associated kinase 1) is a serine/threonine kinase belonging to the Numb-associated kinase (NAK) family, primarily involved in clathrin-mediated endocytosis. It regulates the efficiency of receptor binding to endocytic vesicles by phosphorylating the μ2 subunit of the AP2 complex, thereby influencing the endocytosis and recycling of various membrane proteins such as transporters and receptors. AAK1 is particularly crucial in the recycling of synaptic vesicles within neurons, being closely associated with neurotransmitter release and synaptic plasticity. Furthermore, AAK1 has been identified as participating in viral entry and signal transduction processes, positioning it as a potential therapeutic target for antiviral agents and neuropsychiatric disorder drug development.

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BMS-986176

T358561815613-42-3

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.

$175

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BMT-124110

T105721679371-59-5In house

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.

$329

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RSS0680

T746432769753-48-0

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

$399

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LP-922761

T157801454808-95-7In house

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

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SGC-AAK1-1

T128852247894-32-0

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.

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LP-935509

T157811454555-29-3

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).

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AAK1-IN-2

T608281802703-21-4

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].

$1,520

8-10 weeks

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DB0614

T746442769753-47-9

DB0614 (Example 21) is a bifunctional compound designed for the targeted degradation of kinases, effectively breaking down AAK1, AURKA, BMP2K, CAMKK1, CDK16, CML, CDK6, EIF2AK2, FER, GAK, LCK, LIMK2, MAP3KH, MAPK8, MAPK9, NEK9, PLK4, PTK2B, SIK2, STK17A, STK17B, ULK1, ULK3, and WEE1. This compound has potential applications in research on diseases or disorders caused by aberrant kinase activity [1].

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SGC-AAK1-1N

T346302242913-80-8

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

$430

35 days

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LP-922761 hydrate

T62143

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.

$1,130

1-2 weeks

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HW161023

T2068962920698-73-1

HW161023 (compound) is an orally active inhibitor of AP2 associated protein kinase 1 (AAK1), exhibiting IC50 values of 5.4 nM for AAK1 and 11.9 μM for hERG. HW161023 can suppress pain response in a rat model of chronic sciatic nerve compression injury.

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10-14 weeks

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BMS-901715

T105711699861-37-4

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

$2,980

10-14 weeks

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BMT-090605

T146911551403-51-0

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.

$2,120

8-10 weeks

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AAK1-IN-3

T608291802703-20-3

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].

$1,520

8-10 weeks

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BMS-911172

T305431644248-18-9

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

$1,620

6-8 weeks

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AAK1-IN-3 TFA

T63834

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.

$1,520

10-14 weeks

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AAK1-IN-2 TFA

T63833

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.

$1,520

10-14 weeks

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AAK1-IN-4

T614991815612-79-3

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].

$1,520

8-10 weeks

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BMT-090605 hydrochloride

T619412231664-45-0

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.

$1,810

8-10 weeks

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AAK1-IN-5

T616931815613-44-5

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].

$2,140

8-10 weeks

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