T6203

Saxagliptin (BMS-477118) is a selective, reversible DPP4 inhibitor with an IC50 of 26 nM.

SIRT5 inhibitor 2 (compound 49) is a potent SIRT5 inhibitor with IC50=2.3 μM that has inhibitory activity through SIRT5-dependent deacetylation and can be used to study cancer and neurodegenerative diseases.

BRD4-BD1-IN-1 (Compound 9a) is a BRD4-BD1 inhibitor with an IC50 of 38.20 μM.

SARS-CoV-2 nsp13-IN-4 (C4 (d)) is a potent and selective small-molecule inhibitor of the nsp13 helicase. It exerts its effect by inhibiting the ssDNA+ ATPase activity of nsp13 with an IC50 of 57 μM. Characterized as an agent-like molecule (MW < 450 Da), it demonstrates potential for broad-spectrum antiviral effects in coronavirus research.

Antitumor agent-65 (Compound 5), an analogue/derivative of (-)-cleistenolide, shows potential in cancer research.

DNA-PK-IN-7 is a potent DNA-PK inhibitor (IC50= 1 nM) (WO2021104277A1, compound 5).

Sovesudil (PHP-201) is a potent, ATP-competitive, locally acting Rho kinase (ROCK) inhibitor, showing IC50 values of 3.7 nM for ROCK-I and 2.3 nM for ROCK-II, and capable of lowering intraocular pressure (IOP) without inducing hyperemia.

BNS-22 is a DNA topoisomerase II (Topo II) inhibitor with IC₅₀ values of 2.8 μM and 0.42 μM for human TopoIIα and TopoIIβ-mediated kinetoplast DNA decatenation, respectively. BNS-22 induces mitotic abnormalities and exhibits antiproliferative activity against human cancer cells.

CDK2-IN-8 is a potent CDK2 inhibitor (IC50 = 1.74 μM) that exhibits antiproliferative activity and can be used for melanoma research.

L-365260 hemihydrate is a selective, orally active non-peptide gastrin and brain cholecystokinin receptor (CCK-B) antagonist, demonstrating competitive interaction with guinea pig stomach gastrin and brain CCK receptors and exhibiting inhibition constants (Kis) of 1.9 nM and 2.0 nM, respectively.

Saxagliptin is a new oral hypoglycemic of the new dipeptidyl peptidase-4 (DPP-4) inhibitor class of drugs. Saxagliptin is a competitive DPP4 inhibitor that slows the inactivation of the incretin hormones and reducing fasting and postprandial glucose conce