potential

KDM4-IN-4 (compound 47) is a potent inhibitor of histone lysine demethylase 4 (KDM4), with a binding constant of approximately 80 μM for the KDM4A-Tudor domain. It inhibits H3K4Me3 binding to the Tudor domain in cellular contexts with an EC50 value of 105 μM, holding potential for anticancer research applications [1].

Relacorilant is a selective and orally bioavailable antagonist of glucocorticoid receptor(Ki of 7.2 nM in HepG2 TAT assay, and also shows Kis of 12, 81.2, 210 nM for rat, human and monkey glucocorticoid receptor in cell-based assay, respectively). Relacorilant has the potential for Cushing's syndrome treatment.

Tasquinimod (ABR-215050) is an oral antiangiogenic agent with potential antitumor activity. It is also an S100A9 inhibitor and binds to the HDAC4Zn2+ binding structural domain with Kd values between 10 and 30 nM.

Selvigaltin (GB1211) is a Gal-3 inhibitor with potential anticancer activity. Selvigaltin is used in the study of cirrhosis and cancer.

VVD-130037 is a small molecule activator specifically targeting Kelch-like ECH-associated protein 1 (KEAP1) with potential antitumor activity.VVD-130037 inhibits tumor growth in advanced solid tumors by degrading NRF2.

Elamipretide (MTP-131) is a mitochondria-targeted antioxidant tetrapeptide (D-Arg-dimethylTyr-Lys-Phe-NH2) that reduces toxic reactive oxygen species (ROS) production and stabilizes cardiolipin, with blood-brain-barrier permeability. It is a potential therapeutic agent in the rare disease of Barnes syndrome.

RBN-3143 is a potent inhibitor of NAD+-competitive catalytic PARP14 (IC50= 4 nM), which inhibits ADP-ribosylation mediated by PARP14 and stabilizes PARP14 in cell lines, demonstrating research potential for lung inflammation.

Dinaciclib (SCH 727965) is a selective CDK inhibitor targeting CDK1, CDK2, CDK5, and CDK9 (IC50 = 3 1 1 4 nM). It exhibits potential antitumor activity by inhibiting the incorporation of thoracic glycan (dThd) DNA.

Pevonedistat (MLN4924) is a potent and selective NEDD8 activating enzyme (NAE) inhibitor (IC50=4.7 nM) with therapeutic potential for myelodysplastic syndromes (MDS) and antitumor activity.

Rosiglitazone (BRL49653) is a PPARγ agonist, TRPC5 activator, and TRPM3 inhibitor with oral activity. Rosiglitazone is also a hypoglycemic agent and a thiazolidinedione insulin sensitizer.

D-F07 is a novel fluorescent IRE-1 RNase inhibitor and a tricyclic chromone with potential anticancer activity.

Tanzisertib (CC-930) (CC-930) is a potent inhibitor of JNK1 2 3 with IC50s of 61 7 6 nM, respectively, with potential antifibrotic activity.

Diphenyleneiodonium chloride (DPI)(DPI) is an irreversible inhibitor of iNOS and eNOS (IC50 values of 50 nM and 0.3 μM, respectively),and displays broad-spectrum bactericidal activity.

TD139 is a small molecule inhibitor of inhaled galectin-3 (Gal-3) with potential anti-fibrotic activity, commonly used in the study of idiopathic pulmonary fibrosis.

Ivosidenib (AG-120) is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1) with potential antineoplastic activity. It specifically inhibits a mutated form of IDH1 in the cytoplasm, preventing the formation of the oncometabolite 2-hydroxyglutarate (2 hG), which may induce cellular differentiation and inhibit cellular proliferation in IDH1-expressing tumor cells.

Baricitinib (INCB028050) is a JAK1 and JAK2 inhibitor (IC50=5.9 5.7 nM) with selective and oral activity. Baricitinib has potential anti-inflammatory, immunomodulatory and anti-tumor activity.

CHZ868 is a type II JAK inhibitor with potential antitumor activity that reverses the persistence of type I JAK inhibitors and can be used to study leukemia.

Sacituzumab is a humanized IgG1 monoclonal antibody utilized in the synthesis of antibody-active small-molecule couplings (naked antibody to Sacituzumab govitecan). It exhibits potential antitumor activity and is employed in tumor research.

Clozic (ICI 55897) exhibits reversible anti-proliferative effects and can be used in studies about serving as a potential anti-arthritic agent.

EMD-503982 is a potential Factor Xa and Factor VIIa inhibitor with potential anticancer and antitumor activity for the study of thromboembolic and neurological disorders.

TPN171 is potent PDE5 inhibitor with subnanomolar potency for PDE5 and good selectivity over PDE6, which has the potential for the treatment of pulmonary arterial hypertension (PAH). TPN171 was proven to exert a longer lasting effect than sildenafil in animal models, providing a foundation for a once-daily oral administration for its clinical use.

Avelumab, a fully human IgG1 anti-PD-L1 monoclonal antibody, exhibits potential antibody-dependent cell-mediated cytotoxicity.

Suramin Sodium Salt (BAY-205) is a sodium salt form of suramin, a polysulphonated naphthylurea with potential antineoplastic activity. Suramin blocks the binding of various growth factors, including insulin-like growth factor I (IGF-I), epidermal growth factor (EGF), platelet-derived growth factor (PDGF), and tumor growth factor-beta (TGF-beta), to their receptors, thereby inhibiting endothelial cell proliferation and migration. This agent also inhibits vascular endothelial growth factor (VEGF)- and basic fibroblast growth factor (bFGF)-induced angiogenesis; retroviral reverse transcriptase; uncoupling of G-proteins from receptors; topoisomerases; cellular folate transport; and steroidogenesis.

GLPG3970 GLPG3970 is a novel orally available selective dual SIK2 SIK3 inhibitor.GLPG3970 has potential anti-inflammatory activity for the study of autoimmune diseases.