T6182

Tirofiban (L700462) (MK-383) is a selective palate GPIIb/IIIa antagonist which inhibits platelet aggregation with IC50 of 9 nM.

M1002 is a hypoxia-inducible factor-2 (HIF-2) agonist that enhances the affinity of HIF-2alpha and ARNT for transcriptional activation. It alters the Tyr2 conformation of the HIF-2alpha PAS-B structural domain and acts synergistically with inhibitors of the prolyl hydroxylase structural domain (PHD).

NIOCH 14 is an orally available antiviral compound that inhibits external keratovirus, poxvirus, and smallpox virus.

Ar-V7-IN-1 (compound 47) is a potent inhibitor of Ar-V7, a genetic mRNA splice variant of the androgen receptor (AR) associated with resistance to AR-targeted therapy in patients with desmoplasia-resistant prostate cancer (mCRPC).

COX-2-IN-16 (compound 2b) is a potent, selective, and orally active inhibitor of cyclooxygenase-2 (COX-2) with an IC50 value of 102 μM, effectively reducing nitric oxide (NO) production and demonstrating anti-inflammatory activity [1].

Anticancer agent 63 (compound 3h) exhibits significant cytotoxic activity against multiple cancer cell lines, including SW480, HeLa, A549, and MCF-7, with IC50 values of 4.9, 11.5, 9.4, and 3.4 μM, respectively, after 24 hours of treatment. It induces apoptosis in MCF-7 cells by down-regulating Bcl-2 expression and up-regulating IL-2 and Caspase-3 expression, and also demonstrates antioxidative properties [1].

EED ligand 1 is a highly versatile, potent, and effective inhibitor that specifically targets the EED subunit of the polycomb repressive complex 2 (PRC2) methyltransferase.

NLRP3-IN-4 is a highly efficient and orally bioavailable inhibitor of NLRP3 inflammasome, which exhibits strong anti-inflammatory properties specifically targeted towards colitis.

RJ-34, an aristolactam analogue, demonstrates strong antitumor effects across a wide range of cancer cell lines, with subnanomolar GI 50 values (GI 50 <0.1 nM) observed for A431, MES-SA, MES-SA/DX5, HCT-15, and HCT-15/CLO2 cells [1].

DNA-PK-IN-8 is a potent, selective, and orally active inhibitor of DNA-dependent protein kinase (DNA-PK) with an IC50 value of 0.8 nM, demonstrating synergistic antiproliferative effects across various cancer cell lines and significantly reducing HL-60 tumor growth when combined with Doxorubicin [1].

Carbonic anhydrase inhibitor 4 is a photoprobe that inhibits the activity of carbonic anhydrase. It specifically targets human carbonic anhydrases, including hCA I-XIV, with K i values ranging from 640-1166 nM [1].