ak-4

AK-4 is an antidiabetic agent that functions as a mitochondrial uncoupler.

TAK-418 is a selective and orally active inhibitor of LSD1/KDM1A enzyme with an IC50 of 2.9 nM. TAK-418 unlocks abnormal epigenetic mechanisms and improves autism symptoms in models of neurodevelopmental disorders.

TAK-441 is an orally active inhibitor of Hedgehog signaling(IC50 = 4.4 nM) with potent antitumor activity. TAK-441 suppresses transcription factor Gli1 mRNA expression and tumor growth.

AK-42 is a novel potent and specific inhibitor of CLC-2, displaying unprecedented selectivity over CLC-1, the closest CLC-2 homolog, and exhibiting no off-target engagement against a panel of 61 common channels, receptors, and transporters expressed in brain tissue.

TAK-448 is an investigational oligopeptide analog of kisspeptin and a potent agonist of the GPR54 receptor. In animals, acute TAK-448 administration stimulates LH/FSH release, whereas continuous sc exposure rapidly down-regulates the pituitary-gonadal axis, with rapid reduction of T levels in a dose-dependent manner. TAK-448 has exhibited potent antitumor activity in rat androgen-dependent prostate cancer models. Therefore, TAK-448 may be useful in the treatment of PC in humans..

IRAK-4 protein kinase inhibitor 2 is a potent inhibitor of interleukin-1 receptor-associated kinase-4 (IC50 = 4 μM).

TAK-448 acetate (MVT-602 acetate) is a synthetic peptide and small molecule KISS1R agonist with antitumor activity. It inhibits the proliferation of VCaP cells and is useful in prostate cancer research.

TAK-448 (MVT-602), a potent and full KISS1R agonist with an IC50 of 460 pM and an EC50 of 632 pM, has been studied in trials for the treatment of Prostate Cancer, Low Testosterone, Prostatic Neoplasms, and Hypogonadotropic Hypogonadism.

Bamirastine inhibits ligand binding to recombinant human histamine H1 receptor (rhH1R) with an IC50 of 17.3 nM and possesses an inhibitory effect on allergic skin inflammation.

Zabedosertib (BAY 1834845) is an inhibitor of IRAK4 with immunomodulatory potential. Zabedosertib protects against acute respiratory distress syndrome, a new study suggests.

HS271 is a selective, highly potent and orally active IRAK4 inhibitor (IC50= 7.2 μM). HS271 shows excellent enzymatic and cellular activities, as well as excellent pharmacokinetic properties.

IRAK4-IN-10 (compound 75) is a potent IRAK4 inhibitor (IC50 = 1.5 nM) that can block the MyD88-dependent signaling pathway and has research potential in inflammatory diseases, autoimmune diseases, and cancer.

IRAK4-IN-8 (VI-177) is an IRAK4 inhibitor used to study diseases related to cancer and inflammation.

IRAK inhibitor 2 (IRAK-IN-2) is a potent inhibitor of interleukin 1 receptor-associated kinase 4 (IRAK-4) for the study of inflammation-related diseases.

GLPG2534 is an orally active, selective and potent IRAK4 inhibitor with anti-inflammatory activity. GLPG2534 inhibits human and mouse IRAK4 and could be used to study psoriasis and atopic dermatitis.

Azilsartan Medoxomil Potassium (TAK-491 Potassium) is an orally administered angiotensin II receptor type 1 antagonist with IC50 of 0.62 nM, which used in the treatment of adults with essential hypertension.

Azilsartan Medoxomil (TAK-491) is an orally administered angiotensin II receptor type 1 antagonist with IC50 of 0.62 nM, which used in the treatment of adults with essential hypertension.

Thalidomide 4-fluoride (E3 ligase Ligand 4) (Cereblon ligand 4) is the Thalidomide-based Cereblon ligand. Thalidomide 4-fluoride can be used in the recruitment of CRBN protein. Thalidomide 4-fluoride (Cereblon ligand 4) can be connected to the ligand for IRAK4 protein by a linker to form PROTAC IRAK4 degrader-1.

Thalidomide 5-fluoride (H-Isoindole-1,3(2H)-dione, 2-(2,6-dioxo-3-piperidinyl)-5-fluoro-) is a thalidomide-based Cereblon ligand that binds to the IRAK4 protein ligand via a linker to form PROTACIRAK4 degrader-1.

Lapaquistat acetate (TAK-475) is a squalene synthase inhibitor with potential anti-inflammatory activity. It mitigates statin-induced toxicity in human skeletal muscle cells and protects guinea pigs from simvastatin-induced myotoxicity, useful for research on hypercholesterolemia and HMG-CoA reductase deficiency.

HG-12-6 is a type II inhibitor of IRAK4, demonstrating preferential binding to unphosphorylated inactive IRAK4 (IC50: 165 nM) and modulating IRAK4 activity in autoimmunity and inflammation.

IRAK4-IN-4 (compound 15) inhibits cyclic GMP-AMP synthase (cGAS) with an IC50 of 2.1 nM.IRAK4-IN-4 is an interleukin-1 receptor–associated kinase 4 (IRAK4) inhibitor, has an IC50 of 2.8 nM.

IRAK4-IN-6 is a selective and orally efficacious inhibitor of IRAK4, demonstrating an IC50 value of 4 nM. This compound specifically targets MyD88 L265P mutant diffuse large B-cell lymphoma [1].

LCH-7749944 (GNF-PF-2356) is a potent PAK4 inhibitor with an IC50 of 14.93 μM, effectively suppressing the proliferation of human gastric cancer cells by downregulating the PAK4/c-Src/EGFR/cyclin D1 pathway and inducing apoptosis.