kd-16

CM-579 is a dual inhibitor of G9a and DNMT( IC50:16 nM, 32 nM for G9a and DNMT). It has potent in vitro cellular activity in a wide range of cancer cells.

SNX2112 (PF 04928473) is an orally active Hsp90 inhibitor, with a Kd of 16 nM.

Thanatin acetate is a cationic peptide with antimicrobial activity, inhibiting the growth of bacteria and fungi by targeting the LptC-LptA interaction and destabilizing the LptA complex involved in lipopolysaccharide transport.

NMS-P515 is an effective, orally active, and stereospecific PARP-1 inhibitor (Kd: 16 nM and an IC50: 27 nM (in Hela cells)). It has anti-tumor activity.

SARS-CoV-2-IN-17 (Compound 16) is a highly effective inhibitor of the SARS-CoV-2 nucleocapsid protein (NPro), demonstrating potent antiviral activity with an EC50 value of 2.18 μM and binding to NPro with a low Kd value of 7.82 μM, underscoring its potency as a NPro ligand [1].

AGN 193109 is a potent antagonist of retinoic acid receptors (RARs; Kd= 2, 2, and 3 nM for RARα, β, and γ, respectively), exhibiting selectivity for RARs over retinoid X receptors (RXRs; Kd= >10,000 nM for human RXRα, β, and γ receptors). This compound effectively reverses cellular morphology changes and growth suppression induced by RAR agonists such as all-trans-RA, 13-cis-RA, and 9-cis-RA in ECE16-1 human endometrial ectocervical epithelial cells, particularly when used at a 10-fold molar excess. Furthermore, AGN 193109 downregulates the expression of cytokeratin K5-8, 13, 14, 16, 17, and 19 genes, indicating inhibition of retinoid action, specifically when co-administered with TTNPB but not as a standalone treatment. In vivo studies demonstrate teratogenic effects, including cleft palate, frontonasal dysplasia, and eye malformations in mouse fetuses following a single oral dose of 1 mg kg.

CCT241736 is an orally bioavailable dual FLT3 Aurora kinase inhibitor that also inhibits clinically relevant FLT3-resistant mutants including FLT3-ITD and FLT3, CCT241736, an advanced analog of CCT137690, is a preclinical development candidate for the treatment of human malignancies, and in particular AML in adults and children.

GPX4-IN-16 ((R)-9i) is a potent inhibitor of GPX4 with a KD value of 20.4 nM, exhibiting cytotoxic properties and anticancer activity.

Galanin (1-16), mouse, porcine, rat is a potent agonist of the hippocampal galanin receptor with a Kd of 3 nM, and it exhibits high biological activity on locus coeruleus neurons.

Galanin (1-16), mouse, porcine, rat, is a hippocampal galanin receptor agonist (Kd = 3 nM) exhibiting high biological activity on locus coeruleus neurons.

High affinity XIAP antagonist (Kd = 16 nM for the BIR3 domain of XIAP). Exhibits cytotoxicity in a wide range of cancer cell lines in vitro (EC50 = 13 nM in MDA-MB-231 cells). Also displays antitumor activity in a mouse breast cancer xenograft model. Enhances TRAIL-induced apoptosis in chronic lymphocytic leukemia (CLL) cells. Oost et al (2004) Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer. J.Med.Chem. 47 4417 PMID:15317454 |Loeder et al (2009) A novel paradigm to trigger apoptosis in chronic lymphocytic leukemia. Cancer Res. 69 8977 PMID:19920200

[Nle20] H4 peptide (16−23) is a potent inhibitor of the histone methyltransferase SETD8, exhibiting strong inhibitory activity (Kd = 0.14 μM) by competing for the substrate binding site on SETD8, thereby inhibiting its methylation of histone H4. This peptide can serve as a lead compound in anticancer therapy.

SARS-CoV-2-IN-16 (Compound 12) is a potent inhibitor of SARS-CoV-2 nucleocapsid protein (NPro) with antiviral activity (EC50 = 3.69 μM) and binds to NPro with a low Kd value of 7.82 μM, indicating its effectiveness as an NPro ligand [1].

GID4 Ligand 3 (compound 16) binds to GID4 with a Kd value of 110 μM in vitro and an IC50 value of 148.5 μM. GID4 Ligand 3 is applicable in research related to cereblon (CRBN) and Von Hippel-Lindau (VHL) [1].

LV-320 is a potent, uncompetitive ATG4B inhibitor with an IC50 of 24.5 μM and a Kd of 16 μM. LV-320 inhibits ATG4B enzymatic activity, blocks autophagic flux in cells, and is stable, non-toxic, and active in vivo. These findings suggest that LV-320 will serve as a relevant chemical tool to study the various roles of ATG4B in cancer and other contexts [1].

Pegdinetanib (BMS-844203; CT-322) is a selective inhibitor targeting VEGFR-2 (VEGFR), with dissociation constants (Kd) of 11 nM and 250 nM and half-maximal inhibitory concentrations (IC50) of 16 nM and 240 nM for human and murine VEGFR-2, respectively, and shows no affinity for VEGFR-1 or VEGFR-3, demonstrating antitumor activity [1].

CM-579 trihydrochloride, a first-in-class reversible, dual inhibitor of G9a and DNMT, exhibits potent in vitro cellular activity across a broad spectrum of cancer cells. It demonstrates inhibition with IC50 values of 16 nM for G9a and 32 nM for DNMT, respectively.

CNI103 is a potent and metabolically stable inhibitor of the cell-permeable peptide, calcineurin. It selectively inhibits the interaction between calcineurin and NFATc3 (KD=16 nM), thereby preventing the activation of NFATc3 both in vitro and in vivo. CNI103 is applicable for research in acute respiratory distress syndrome (ARDS) and other inflammatory diseases.

Haloperidol decanoate (KD 16) is a typical antipsychotic agent utilized as maintenance treatment for schizophrenia and mood disorders formulated as an ester for intramuscular injection.

CM-579 trihydrochloride is a first-in-class reversible and dual inhibitor of G9a and DNMT (IC50s: 16 nM, 32 nM) with potent in vitro cellular activity in a wide range of cancer cells.