T6264

Bosentan (Benzenesulfonamide) is a sulfonamide-derived, competitive and specific endothelin receptor antagonist with a slightly higher affinity for the endothelin A receptor than endothelin B receptor. Bosentan blocks the action of endothelin 1, an extremely potent endogenous vasoconstrictor and bronchoconstrictor, by binding to endothelin A and endothelin B receptors in the endothelium and vascular smooth muscle. Bosentan decreases both pulmonary and systemic vascular resistance and is particularly used in the treatment of pulmonary arterial hypertension.

FPR2 agonist 2 is a potent FPR2 agonist with blood-brain barrier permeability that acts on h-FPR2 (EC50: 0.13 nM), inhibiting the production of pro-inflammatory cytokines, counteracting changes in mitochondrial function, and inhibiting caspase-3 activity.

EP2 receptor antagonist-1 is a reversible, potent, agonist-dependent variant of the prostaglandin EP2 receptor antagonist.EP2 receptor antagonist-1 exhibits anti-inflammatory activity.

Microtubule inhibitor 4 (compound 2) is a potent microtubule inhibitor that prevents microtubule protein polymerization and exhibits cytotoxicity in HT-29 cells (IC50: 2.1 nM).

DY-46-2 is a selective non-nucleoside DNA methyltransferase 3A (DNMT3A) inhibitor (IC50: 0.39 ± 0.23 μM) with anticancer activity for the study of cancer and tumors.

HDAC-IN-41 (Compound 7c) is an orally active, selective class I HDAC inhibitor targeting HDAC1 (IC50: 0.62 μM), HDAC2 (IC50: 1.46 μM), and HDAC3 (IC50: 0.62 μM). HDAC-IN-41 also exhibits NO-releasing activity.

HPK1-IN-14 is a potent inhibitor of HPK1. HPK1-IN-14 has potential for the study of HPK1-related diseases.

Pparδ agonist 5 is a selective, orally active PPARδ agonist with an EC50 of 0.335 μM and better selectivity than GW0742. Pparδ agonist 5 has a beneficial effect on the improvement of bone density and microarchitecture in vivo.

Aurora A inhibitor 2 (Compound 16h) is a potent Aurora A kinase inhibitor with an IC50 of 21.94 nM.

DNA-PK-IN-1, a potent inhibitor of DNA-PK, holds potential for cancer disease research.

HDAC-IN-34 (compound 27) is a potent inhibitor of HDAC, targeting HDAC1 (IC50: 0.022 μM) and HDAC6 (IC50: 0.45 μM). It can bind to DNA and induce DNA damage, exhibiting a significant anti-proliferative effect on HCT-116 cells (IC50: 1.41 μM).