T7875

Emoxypine Succinate is an antioxidant.

NF-κB-IN-10 (compound E1) is an NF-κB inhibitor that mitigates heart failure symptoms by modulating the Nrf2/NF-κB signaling pathway, alleviating oxidative stress and inflammation. It suppresses LPS-induced NO production and downregulates iNOS and COX-2 expression in RAW264.7 cells, showing potential for cardiovascular disease research [1].

DG1 (Compound 8Nc), a Thymidylate Synthase (TS) inhibitor, impedes angiogenesis and alters metabolic reprogramming in NSCLC cells, while effectively suppressing the expression of CD26, ET-1, FGF-1, and EGF. Additionally, it notably inhibits cancer tissue proliferation in the A549 xenograft mouse model [1].

Compound 1b, also known as Antibacterial agent 145, targets the bacterial iron uptake pathway to exert its effects. It compromises the integrity of the bacterial cytoplasmic membrane and inhibits cellular metabolism while demonstrating minimal cytotoxicity to normal cells [1].

Aurora Kinases-IN-4 (Compound 11c) is a covalent, ATP-competitive inhibitor of aurora kinase A with an IC50 value of 1.7 nM. It inhibits cell proliferation in SJSA-1, MDA-MB-231, A549, and HeLa cell lines with IC50 values of 4.27, 1.54, 3.08, and 6.99 μM, respectively. This compound is applicable in research concerning triple-negative breast cancer (TNBC) [1].

COX-2-IN-33 (compound 5f) is a selective COX-2 inhibitor with an IC50 of 45.5 nM, demonstrating potential as an anti-inflammatory agent by effectively suppressing pro-inflammatory cytokine production in vivo while maintaining gastric safety [1].

PD-1/PD-L1-IN-31 is a potent inhibitor of PD-1/PD-L1 (IC50=2.2 nM) that enhances IFN-γ secretion and activates the immune response of peripheral blood mononuclear cells (PBMCs), leading to the inhibition of tumor cells [1].

IHMT-IDH1-053 (compound 16) is an irreversible inhibitor highly selective for the IDH1 R132H mutant, with an IC50 of 4.7 nM. It preferentially targets IDH1 mutants over wild-type IDH1 and IDH2, in both their wild-type and mutant forms. In 293T cells transfected with the IDH1 R132H mutant, IHMT-IDH1-053 reduces 2-hydroxyglutarate (2-HG) production with an IC50 of 28 nM. The compound binds to the R132H protein at an allosteric site near the NADPH binding region, forming a covalent linkage with Cys269. Additionally, IHMT-IDH1-053 inhibits the growth of both the HT1080 cell line and primary acute myeloid leukemia (AML) cells harboring IDH1 R132 mutations [1].

VEGFR2-IN-4 (compound 25) is a potent and selective VEGFR2 kinase inhibitor with a GI50 of 0.7 nM and demonstrates anti-angiogenic properties, utilized in rheumatoid arthritis research [1].