AAK1

Pim1/AKK1-IN-1 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.

LP-935509 is a potent inhibitor of the Adapter protein-2 Associated Kinase 1 (AAK1).

RSS0680 is a small noncoding RNA (sRNA) that targets the ribosome binding site (RBS) of mRNA, functioning as a PROTAC to facilitate the degradation of various protein kinases. By competitively binding to the RBS through its conserved anti-Shine-Dalgarno sequence, RSS0680 inhibits the translation initiation of target genes. Key biological activities include the degradation of kinases such as AAK1, CDK1, and MAPK6, making it a valuable tool for investigating diseases associated with dysregulated kinase activity. Additionally, RSS0680 plays a role in bacterial oxidative stress defense and can enhance resistance to heat shock and oxidative damage by modulating metabolic pathways.

FMF-06-098-1 is a multitargeted kinase PROTAC degrader designed to promote the degradation of various kinases, including AAK1, ABL2, AURKA, and WEE1, among others. This compound exhibits broad biological activity by modulating kinase levels, which can influence cellular signaling pathways and impact cancer progression. FMF-06-098-1 is valuable in research applications focused on understanding kinase function and developing therapeutic strategies targeting multiple kinases in various diseases.

SGC-AAK1-1 is a potent and selective inhibitor of AP2 associated kinase 1 (AAK1), exhibiting an IC50 of 270 nM and a Ki of 9 nM. In addition to its primary target, SGC-AAK1-1 also strongly inhibits BMP2K. This compound is valuable for research into the Wnt signaling pathway, particularly in studies related to the function and regulation of AAK1.

BMT-090605 hydrochloride is a selective inhibitor of the adapter protein-2 associated kinase 1 (AAK1), exhibiting a potent IC50 of 0.6 nM. This compound demonstrates significant antinociceptive activity, making it valuable for neuropathic pain research. Additionally, 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, supporting its role in diverse biological investigations.

BMT-090605 is a potent and selective inhibitor of adaptor protein-2 associated kinase 1 (AAK1), featuring an IC50 value of 0.6 nM. This compound exhibits significant antinociceptive activity and also demonstrates inhibitory effects on BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK), with IC50 values of 45 nM and 60 nM, respectively. BMT-090605 is a valuable tool for research into mechanisms underlying neuropathic pain.

AAK1-IN-8 is a selective inhibitor of AAK1 and GAK, demonstrating effective inhibition with EC50 values of 50 nM and 190 nM, respectively. This compound significantly hinders the phosphorylation of the AP2-µ2 subunit at threonine 156, providing insight into clathrin-mediated endocytosis. AAK1-IN-8 is utilized in research applications focused on uncovering the roles of AAK1 and GAK in cellular processes and their implications in diseases related to endocytic pathways.

AAK1-IN-6 is a potent inhibitor of AP-2-associated protein kinase 1 (AAK1) with an IC50 value of 12 nM. This compound exhibits significant antiviral activity against dengue virus (DNEV2, EC50 = 0.24 μM) and Venezuelan equine encephalitis virus (VEEV, EC50 = 0.30 μM). AAK1-IN-6 is a valuable tool for researchers investigating antiviral mechanisms and potential therapeutic strategies.

BMS-986176 is a potent and selective inhibitor of adaptor associated kinase 1 (AAK1) with an IC50 value of 2 nM. This compound is designed for effective brain penetration, making it a valuable tool in the investigation of neurodegenerative diseases. It is applicable in research focused on the modulation of AAK1 pathways and their implications in various neurological disorders.

AAK1-IN-12 is a selective inhibitor of the AP2-associated kinase 1 (AAK1) that demonstrates oral bioavailability and the ability to cross the blood-brain barrier. This compound has important implications for research into neurodegenerative disorders, including schizophrenia, Parkinson's disease, neuropathic pain, and Alzheimer's disease. AAK1-IN-12 serves as a valuable tool for investigating the therapeutic potential of AAK1 modulation in various neurological contexts.

LP-922761 is a selective inhibitor of adapter protein-2 associated kinase 1 (AAK1), demonstrating potent activity with IC50 values of 4.8 nM in enzyme assays and 7.6 nM in cellular assays. Additionally, LP-922761 inhibits BMP-2-inducible protein kinase (BIKE) at an IC50 of 24 nM. Importantly, it shows no significant activity against cyclin G-associated kinase (GAK), opioid receptors, adrenergic α2 receptors, or GABAa receptors, making it a valuable tool for studying AAK1-related signaling pathways and its role in cellular processes.

BMS-911172 is an inhibitor of adaptor-associated kinase 1 (AAK1), exhibiting an IC50 value of 35 nM. This compound is primarily used in research focused on modulating clathrin-mediated endocytosis and exploring the role of AAK1 in cellular processes. Its ability to selectively inhibit AAK1 makes it a valuable tool for investigating signaling pathways related to receptor internalization and trafficking.

BMT-124110 is a highly selective inhibitor of AAK1 (AP2-associated protein kinase 1) with an IC50 value of 0.9 nM. This compound exhibits notable antinociceptive activity, making it relevant in pain management research. Additionally, BMT-124110 inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC50 values of 17 nM and 99 nM, respectively, further supporting its utility in kinase-related studies.

SGC-AAK1-1N is a selective inhibitor of AAK1 (AP2 associated kinase 1) with an IC50 value of 1.8 μM. This compound is utilized in research to elucidate the role of AAK1 in cellular processes, particularly in clathrin-mediated endocytosis and signaling pathways. Its potency makes it a valuable tool in studies focused on understanding the therapeutic potential of AAK1 modulation in various diseases.

BMS-901715 is a highly selective inhibitor of adaptor protein-2 associated kinase 1 (AAK1) with an IC50 of 3.3 nM. This compound disrupts clathrin-mediated endocytosis, making it valuable for studying cellular processes related to membrane trafficking. BMS-901715 is particularly useful in research applications focused on viral infections and the modulation of synaptic transmission.

AAK1-IN-2 TFA is a selective and potent inhibitor of Adaptor Protein 2-Associated Kinase 1 (AAK1), demonstrating an IC50 value of 5.8 nM. This compound effectively penetrates the blood-brain barrier, making it a valuable tool for research in neuropathic pain mechanisms. AAK1-IN-2 TFA enables the investigation of AAK1's role in various neurological conditions, providing insights into potential therapeutic targets for pain management.

AAK1-IN-3 is a potent inhibitor of adaptor protein 2-associated kinase 1 (AAK1), exhibiting an IC50 of 11 nM. This quinoline analogue effectively penetrates the blood-brain barrier, making it suitable for investigating the role of AAK1 in neuropathic pain mechanisms. AAK1-IN-3 is a valuable tool for research focused on neuropharmacology and the modulation of pain pathways.

AAK1-IN-4 is a selective inhibitor of adaptor protein-2-associated kinase 1 (AAK1), demonstrating an IC50 of 4.6 nM. This orally active compound effectively penetrates the central nervous system, with a filtration Ki of 0.9 nM and a cell IC50 of 8.6 nM. AAK1-IN-4 is primarily utilized in research studies focused on neuropathic pain, offering insights into its underlying mechanisms and potential therapeutic applications.

AAK1-IN-3 TFA is a quinoline derivative that selectively inhibits adaptor protein 2-associated kinase 1 (AAK1) with an IC50 of 11 nM. This compound demonstrates significant brain penetration and is suitable for investigating neuropathic pain mechanisms. Its ability to modulate AAK1 activity makes it a valuable tool for research applications focused on pain pathways and related neurobiological processes.

HW161023 is a potent inhibitor of AP2-associated protein kinase 1 (AAK1), demonstrating an IC50 of 5.4 nM against AAK1 and a much higher IC50 of 11.9 μM against hERG. This compound has shown efficacy in alleviating pain in a chronic constriction injury model of the sciatic nerve in rats. HW161023 is valuable for research in pain mechanisms and the modulation of AAK1-related signaling pathways.

AAK1-IN-10 is a selective inhibitor of adapter-associated kinase 1 (AAK1), exhibiting potent enzyme inhibitory activity with an IC50 of 9.62 nM. This compound primarily functions by impairing the activity of AAK1, a kinase involved in various cellular processes. AAK1-IN-10 demonstrates low cardiotoxicity, with an IC50 of 13.7 μM, making it a suitable candidate for research into conditions such as diabetic neuropathy and postherpetic pain. Its distinct mechanism and safety profile facilitate investigations into therapeutic applications targeting nerve pain and associated disorders.

AAK1-IN-2 is a selective inhibitor of Adaptor Protein 2-Associated Kinase 1 (AAK1), exhibiting an IC50 of 5.8 nM. This compound demonstrates the ability to penetrate the blood-brain barrier, making it suitable for neurological research. AAK1-IN-2 is particularly relevant for studies investigating the mechanisms underlying neuropathic pain.

AAK1-IN-5 is a selective inhibitor of adaptor protein-2-associated kinase 1 (AAK1), demonstrating an IC50 of 1.2 nM and a filtrate Ki of 0.05 nM, along with a cell-based IC50 of 0.5 nM. This compound is notable for its ability to penetrate the central nervous system and is orally active, making it suitable for in vivo studies. AAK1-IN-5 is primarily used in research focused on neuropathic pain, providing a valuable tool for understanding AAK1's role in pain pathways.

PROTAC AAK1 Degrader-1 is a potent PROTAC designed to selectively degrade the AAK1 protein, a known modulator of clathrin-mediated endocytosis. This compound facilitates targeted protein degradation, thereby influencing cellular pathways critical in cancer research. Its application is valuable for studying the role of AAK1 in tumor biology and therapeutic resistance, potentially leading to innovative cancer treatment strategies.

BMT-046091 is a selective inhibitor of adaptor-associated kinase 1 (AAK1), targeting its activity to modulate cellular processes. This compound effectively inhibits the phosphorylation of the μ2 peptide by AAK1, demonstrating an IC50 value of 2.8 nM. BMT-046091 is useful in research applications studying AAK1's role in endocytic trafficking and signaling pathways, contributing to a better understanding of its implications in various diseases.