a-1062

A-1062, a resolvase-binding inhibitor, inhibits resolvase binding to the res site.

Datopotamab deruxtecan (DS-1062) is an antibody-drug conjugate (ADC) that targets tropomyosin 2 (TROP2) on the surface of trophoblast cells. Datopotamab deruxtecan exhibits antitumor activity by specifically binding to TROP2 and internalizing, releasing DXd to inhibit topoisomerase I (IC₅₀ = 0.31 μM), thereby inducing DNA damage and apoptosis. Datopotamab deruxtecan induces significant antibody-dependent cellular cytotoxicity in the presence of peripheral blood lymphocytes and inhibits tumor growth in xenograft models.

AMG-424 (XmAb968) is a human bispecific antibody (bsAb) targeting CD38 and CD3E. It effectively kills cancer cells that express CD38, stimulates T cell proliferation, and reduces cytokine release. AMG-424 exhibits antitumor activity in mouse cancer models with bone marrow invasion and induces peripheral B cell depletion in cynomolgus monkeys. It is used in studies of multiple myeloma. Recommended isotype control: half-IG G1-kappa/(scFv-heavy-lambda)-h-CH2-CH3.

UNC1062 is a highly selective tyrosine kinase inhibitor that specifically targets MERTK. This compound effectively suppresses MERTK-mediated downstream signaling, induces apoptosis in cell cultures, reduces colony formation in soft agar, and inhibits invasion of melanoma cells. Notably, UNC1062 demonstrates potent inhibition of MERTK kinase activity, with an IC50 of 1.1 nM and a Morrison Ki of 0.33 nM. It also displays specificity within the TAM family, exhibiting IC50 values of 60 nM for TYRO3 and 85 nM for AXL [1].

SR 1903 is an inverse agonist of RORγ and PPARγ (IC₅₀ = 100 nM and 209 nM, respectively) and an agonist of LXR (EC₅₀ = 154 nM). It exerts anti-inflammatory and anti-diabetic effects in mouse models of collagen-induced arthritis and diet-induced obesity.

Memogain is a pro-drug of galantamine. It is used for the treatment of Alzheimer's disease.