u-87 mg

Capmatinib (INCB28060) is an orally bioavailable inhibitor of the proto-oncogene c-Met (HGFR)with potential antineoplastic activity.

CCT128930 is a potent, ATP-competitive and selective inhibitor of Akt2 with IC50 of 6 nM, 28-fold greater selectivity for Akt2 than the closely related PKA kinase.

Perphenazine (Trilafon) is a phenothiazine derivative and a dopamine antagonist with antiemetic and antipsychotic properties.

TP-10 is a selective inhibitor of PDE10A against other PDEs with IC50 of 0.8 nM.

AA-BR-157 is a PROTAC degrader targeting metallothionein 2A (MT2A) with a DC50 of 190 nM. It downregulates DIAPH3, a protein involved in cytoskeletal and cellular movement regulation, inhibiting cell migration in MDA-MB-231 and U-87 MG cell lines. Additionally, AA-BR-157 modulates zinc homeostasis in MDA-MB-231 cells. (Pink: ligand for target protein MT2A ligand 1; Black: linker; Blue: ligand for VHL E3 ligase).

Amentoflavone (3',8''-Biapigenin), as a potent inhibitor of CYP3A4 and CYP2C9, can interact with many other medications. CYP3A4 and CYP2C9 are proteins used for drug metabolism in the body. Amentoflavone also is an inhibitor of human cathepsin B. It has antimalarial activity in trials significant affinities towards the Delta-1, kappa opioid receptors (as an antagonist) and binds to benzodiazepine receptors. Amentoflavone may be a potential lead for a new type of anti-inflammatory agents having the dual inhibitory activity of group II phospholipase A2 and cyclooxygenase. Amentoflavone and quercetin differentially exerted suppression of PGE2 biosynthesis via downregulation of COX-2/iNOS expression.