ak1

AK-1 is a sirtuin 2 (SIRT2) inhibitor (IC50:12.5 µM).that prevents hippocampal neurodegeneration in Alzheimer's disease models and induces cell cycle arrest in colon carcinoma cells.

JAK1/2/3 Inhibitor 1 is a potent protein kinase inhibitor.JAK1/2/3 Inhibitor 1 has antitumor activity that inhibits the growth of a variety of cancer cell lines. It inhibits the growth of cancer cells by binding to the cancer cell backbone and inhibiting the production of new proteins.

TAK1 MAP4K2 inhibitor 1 is a potent dual inhibitor of TGFβ-activated kinase 1 (TAK1) and MAP4K2 [IC50s: 41.1 nM and 18.2 nM].

NVS-PAK1-1 is a potent allosteric inhibitor of PAK1 with an IC 50 of 5 nM for dephosphorylated PAK1 and 6 nM for phosphorylated PAK1 as assessed. Inhibition is ATP-competitive, most likely due to indirect competition due to incompatibility of ATP binding with the DFG-out binding conformation of the allosteric compound. NVS-PAK1-1 has an IC50 of 270 nM against dephosphorylated PAK2 and 720 nM against phosphorylated PAK2 respectively [1].

AK-IN-1, a competitive inhibitor for adenosine (Ado) but not for ATP, demonstrates significant inhibition of AK activity, achieving 86%, 87%, and 89% at concentrations of 2, 4, and 10 µM, respectively. This compound shows promise for research across various disease areas, such as ischemia, inflammation, and seizures.

NVS-PAK1-1 is an effective and selective allosteric PAK1 inhibitor (IC50: 5 nM).

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-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].

PAK1-IN-1 is a selective and potent inhibitor of PAK1 (IC50: 9.8 nM). PAK1-IN-1 inhibits PAK1-associated tumour cell migration and invasion in a dose-dependent manner.

NVS PAK1 C is a negative control of NVS PAK1 1, a potent and selective PAK1 inhibitor.

JAK1 TYK2-IN-3 is a selective, potent, orally active dual inhibitor of TYK2 (IC50: 6 nM) and JAK1 (IC50: 37 nM), with selective action on JAK2 (IC50: 140 nM) and JAK3 (IC50: 362 nM). It regulates the expression of TYK2 JAK1-related genes and formation of Th1, Th2, and Th17 cells to exert anti-inflammatory activity.

AZ-Tak1 is a potent and a relatively selective inhibitor of TAK1 kinase activity, with an IC50 of 0.009 mM. AZ-Tak1 treatment decreased the level of p38 and ERK in mantle cell lymphoma cells, and induced apoptosis in a dose and time dependent manner, with an IC50 of 0.1–0.5 mM. Using the annexin-V and PI staining and FACS analysis, After 48 hours of incubation, AZ-Tak1 (0.1 mM) induced apoptosis in 28%, 34% and 86% of Mino, SP53, and Jeko cells, respectively, which was increased to 32%, 42%, and 86% when 0.5 mM concentration was used.

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

JAK1-IN-11 (compound 11) is a potent Janus kinase inhibitor with nanomolar IC50 values of 0.02 nM for JAK1 and 0.44 nM for JAK2, demonstrating high selectivity for JAK1 over JAK2 [1].

JAK1-IN-4 is a selective JAK1 inhibitor (IC50s: 85 nM, 12.8 μM and >30 μM for JAK1, JAK2, and JAK3, respectively). JAK1-IN-4 inhibits STAT3 phosphorylation in NCI-H 1975 cells (IC50, 227 nM).

TAK1-IN-3 is a novel ATP-competitive TAK1 inhibitor for the study of cancer.

LRRK2/NUAK1/TYK2-IN-1 (compound 226) exhibits inhibitory activity against LRRK2 (Wt), LRRK2 (G2019), TYK2, and NUAK1, demonstrating IC50 values below 10 nM. This compound is useful for research into autoimmune diseases.

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.

JAK1-IN-B61 is a JAK1 inhibitor.

TAK1 inhibitor is an inhibitor, which can inhibit MCF-7, A549, DU-145 and MDA MB-231, with IC50 of 0.021, 0.14, 0.064 and 0.19, respectively. TAK1 inhibitor showed good antibacterial activity with microphones ranging from 93.7 to 46.9μg/mL and from 7.8 to 5.8μg/mL.

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.

JAK1-IN-10 (compound 9), a cyano-substituted cyclic hydrazine derivative, is a potent and selective inhibitor of JAK1 [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].

DRAK1/2-IN-1 is a potent inhibitor targeting both DRAK1 and DRAK2, displaying dissociation constants (Kd) of 1 µM and 6 µM, respectively.

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].

TAK1-IN-2 is a potent and selective TAK1 inhibitor with an IC50 of greater than 2 nM [1].

EAK16-II, an amphipathic peptide, concentration-dependently inhibits the self-sorting of EAKIIH6 [1].

JAK1 TYK2-IN-1 is a dual inhibitor of TYK2 [IC50 = 29 nM] and JAK1 (IC50 = 41 nM).

JAK1-IN-8, a specific inhibitor of Janus kinase 1 (JAK1, IC50<500 nM).

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].

JAK1-IN-9 (compound 23a) is a potent, selective JAK1 inhibitor with an IC50 of 72 nM, exhibiting over 12-fold selectivity against other JAK family members [1].

BMS-911543 is a potent and selective inhibitor of JAK2 with IC50 of 1.1 nM, ~350-, 75- and 65-fold selective to JAK1, JAK3 and TYK2, respectively. Phase 1 2.

JAK-IN-23 is an orally active dual JAK STAT and NF-κB inhibitor that inhibits JAK1 (IC50: 8.9 nM), JAK2 (IC50: 15 nM), and JAK3 (IC50: 46.2 nM). It exhibits strong anti-inflammatory effects and can reduce the release of various pro-inflammatory factors. JAK-IN-23 can be used to study inflammatory bowel disease (IBD).