T7968

Dazoxiben (UK-37248) is a potent inhibitor of thromboxane (TX) synthase

PSEN1-IN-2 (Compound 13K) is a potent inhibitor of PSEN1-APH1A and PSEN1-APH1B complexes, with IC50 values of 6.9 nM and 2.4 nM, respectively. This PSEN1 inhibitor is used in Alzheimer's disease research [1].

Compound 4H is a potent carbonic anhydrase inhibitor with an IC50 value of 0.033 μM [1].

QSL-304 is a DNA gyrase B inhibitor that serves as an antibacterial agent, exhibiting an IC50 of 31.23 mg/mL against Staphylococcus aureus SA-P2003 [1].

HDAC/CD13-IN-1 (Compound 12) is an inhibitor of both HDAC and CD13, with IC50 values of 0.34 μM for hCD13, 0.53 μM for porcine CD13, and 0.03, 0.06, and 0.02 μM for HDAC1, HDAC2, and HDAC3, respectively. This compound effectively suppresses proliferation and induces apoptosis in MV4-11, K562, Jeko-1, and HL60 cancer cells, with IC50 ranges of 0.25-2.04 μM, and demonstrates capabilities in hindering metastasis and invasion [1].

Compound 8 (5-HT6R antagonist 1), a 5-HT6R antagonist (K i : 5 nM), not only demonstrates inhibition of platelet aggregation and excellent metabolic stability but also reverses MK-801-induced memory impairments in rats, suggesting its utility in Alzheimer's disease (AD) research [1].

PI3Kα-IN-13 (Compound 18a), a PI3Kα inhibitor with an IC50 of 2.5 nM, effectively induces apoptosis and hampers the proliferation of various cancer cell lines, exhibiting IC50 values of 0.75 μM (MCF-7), 3.79 μM (HCT-116), 13.71 μM (MDA-MB-231), and 9.85 μM (SW620). This compound also impedes tumor cell colony formation, migration, and invasion [1].

TEAD-IN-6 (Example 11-1) is a TEAD modulator that inhibits the YAP1/TAZ-TEAD interaction and has applications in cancer research [1].

FAK-IN-11 (Compound 4l), a FAK inhibitor, specifically targets the ATP binding pocket of FAK to prevent its phosphorylation. It exhibits cytotoxic effects on MDA-MB-231 cells, achieving an IC50 value of 13.73 μM, and induces non-apoptotic cell death in these cells [1].