is-145

IS-145 is a thromboxane A2 receptor antagonist.

QQN-00358 is a novel potent and selective tankyrase (TNKS) inhibitor.

CDK9-IN-7 is a highly selective and orally active CDK9 cyclin T inhibitor (IC50: 11 nM), which exhibits more potent over other CDKs (CDK4 cyclinD: 148 nM; CDK6 cyclinD: 145 nM).

MSC2360844 is a potent, orally active and selective inhibitor of PI3Kδ(IC50 of 145 nM).

Duvelisib (INK1197, IPI-145) is a selective inhibitor of phosphatidylinositol 3-kinase (PI3K) and p100δ, with effects on p110δ (IC50 value is 0.0025 μM), p110γ (IC50 value is 0.274 μM), p110β (IC50 value is 0.85 μM) and p110α (IC50 value is 1.602 μM).

Lidocaine (Alphacaine) is an amide local anesthetic with anti-inflammatory properties in vitro and in vivo. It has this functions perhaps due to an attenuation of intracellular adhesion molecule-1 (ICAM-1), pro-inflammatory cytokines, and reduction of neutrophils influx.

Lidocaine hydrochloride (Lignocaine hydrochloride) is a local anesthetic and cardiac depressant used as an antiarrhythmic agent. Its actions are more intense and its effects more prolonged than those of PROCAINE but its duration of action is shorter than that of BUPIVACAINE or PRILOCAINE.

Duvelisib R enantiomer (IPI-145 R enantiomer) is an enantiomer of Duvelisib with lower activity. Duvelisib is a PI3K inhibitor.

FAAH-IN-1 is a fatty acid amide hydrolase (FAAH) inhibitor with IC50 values of 145 nM for rat FAAH and 650 nM for human FAAH.

ML 145 is a selective and potent antagonist of human GPR35, with no significant activity against GPR35 in any of its immediate rodent homologs.ML 145 has potential anti-inflammatory activity for the study of immunoinflammation.ML 145 is a novel non-steroidal anti-inflammatory agent for the study of rheumatoid arthritis.

Mps1-IN-2 is a potent, selective, and ATP-competitive inhibitor of both Mps1 and Plk1.

GSTP1-1 inhibitor 2 (Compound 5g) is an inhibitor of hGSTP1-1 (glutathione S-transferase P1-1), exhibiting an IC50 of 12.2 μM. It demonstrates substantial cytotoxicity against the cell lines DU-145, PC3, and MCF-7, with CC50 values of 36.6, 11.9, and 17.4 μM respectively, making it relevant for research in cancer therapeutics.

E3 Ligase Ligand-linker Conjugate 145 is a combination of an E3 ubiquitin ligase ligand and a linker, utilized in the synthesis of PROTACAR Degrader-7.

Aurora A inhibitor4 (compound C9) is a potent inhibitor of Aurora A, with GI50 values of 4.26 μM in DU 145 cells and 7.08 μM in HT-29 cells.

EGFR-IN-145 (compound 7c) is an EGFR kinase inhibitor. At a concentration of 20 μM, it inhibits wild-type EGFR kinase by 52.7%.

Anticanceragent 264 (Compound 5w) is an anticancer compound that exhibits significant antiproliferative activity in tumor cell lines, with an IC50 range of 7.5-33.67 μM. It notably induces cell cycle arrest at the G2 M phase in MDA-MB-231, MIA PaCa-2, and DU-145 cell lines. This compound reduces key cell cycle proteins CDK1, CDK2, and Cyclin B1 in a dose-dependent manner and has strong binding activity with differentiation inhibitors and DNA-binding proteins. Anticanceragent 264 is useful for research in the cancer disease domain.

CYP17A1-IN-1 (Compound 14) is an inhibitor of CYP17A1 with an IC50 of 26 nM. It exhibits cytotoxicity in androgen-sensitive prostate cancer cells, specifically LNCaP, and hinders the migration of DU-145 cells.

MMP-145 is used as a protease inhibitor.

Ioforminol, also known as GE-145 and AN-113111, is a new low-osmolar dimeric radiographic contrast agent. GE-145 exhibits similar preclinical properties to other dimeric radiographic contrast media. In addition, the low osmolality enables an iso-osmolar f

Panduratin A is a natural chalcone derivative with inhibitory activity against MMP-9 in human oral epidermoid carcinoma KB cells; inhibitory activity against the NS3 protease of DENV-2 (Ki=25 μM); significant cytotoxicity against human androgen-independent prostate cancer cells PC-3 and DU-145; and also able to activate the LKB1-AMPK- PPARα δ signaling pathway and enhance the oxidative capacity of myocyte mitochondria.

Kisspeptin-54 is a peptide ligand of the orphan G protein-coupled receptor GPR54 (Kis = 1.81 and 1.45 nM for rat and human receptors, respectively).1 It is a 54 amino acid peptide encoded by the metastasis suppressor gene KISS-1. Kisspeptin-54 induces calcium mobilization in CHO-K1 cells expressing rat and human receptors (EC50s = 1.39 and 5.47 nM, respectively). It also induces arachidonic acid release in CHO cells expressing rat and human GPR54 in a concentration-dependent manner. Kisspeptin-54 (10-1,000 nM) inhibits insulin secretion from isolated mouse pancreatic β-cells in the presence of 2.8 mM, but not 11.1 mM, glucose.2 Kisspeptin-54 (1-5 nmol, i.c.v.) increases serum levels of luteinizing hormone (LH) and follicular stimulating hormone (FSH) in mice, an effect which is reversed by the gonadotropin releasing hormone (GNRH) antagonist acycline.3References1. Kotani, M., Detheux, M., Vandenbogaerde, A.L., et al. The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54. J. Biol. Chem. 276(37), 34631-34636 (2001).2. Vikman, J., and Ahrén, B. Inhibitory effect of kisspeptins on insulin secretion from isolated mouse islets. Diabetes Obes. Metab. 11(Suppl 4), 197-201 (2009).3. Gottsch, M.L., Cunningham, M.J., Smith, J.T., et al. A role for kisspeptins in the regulation of gonadotropin secretion in the mouse. Endocrinology 145(9), 4073-4077 (2004). Kisspeptin-54 is a peptide ligand of the orphan G protein-coupled receptor GPR54 (Kis = 1.81 and 1.45 nM for rat and human receptors, respectively).1 It is a 54 amino acid peptide encoded by the metastasis suppressor gene KISS-1. Kisspeptin-54 induces calcium mobilization in CHO-K1 cells expressing rat and human receptors (EC50s = 1.39 and 5.47 nM, respectively). It also induces arachidonic acid release in CHO cells expressing rat and human GPR54 in a concentration-dependent manner. Kisspeptin-54 (10-1,000 nM) inhibits insulin secretion from isolated mouse pancreatic β-cells in the presence of 2.8 mM, but not 11.1 mM, glucose.2 Kisspeptin-54 (1-5 nmol, i.c.v.) increases serum levels of luteinizing hormone (LH) and follicular stimulating hormone (FSH) in mice, an effect which is reversed by the gonadotropin releasing hormone (GNRH) antagonist acycline.3 References1. Kotani, M., Detheux, M., Vandenbogaerde, A.L., et al. The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54. J. Biol. Chem. 276(37), 34631-34636 (2001).2. Vikman, J., and Ahrén, B. Inhibitory effect of kisspeptins on insulin secretion from isolated mouse islets. Diabetes Obes. Metab. 11(Suppl 4), 197-201 (2009).3. Gottsch, M.L., Cunningham, M.J., Smith, J.T., et al. A role for kisspeptins in the regulation of gonadotropin secretion in the mouse. Endocrinology 145(9), 4073-4077 (2004).

PAR2 (1-6) amide is a synthetic peptide agonist of proteinase-activated receptor 2 (PAR2) that corresponds to residues 1-6 of the amino terminal tethered ligand sequence of human PAR2 and residues 37-42 of the full-length sequence.1It binds to NCTC 2544 cells expressing human PAR2 (Ki= 9.64 μM in a radioligand binding assay) and induces calcium mobilization in the same cells (EC50= 0.075 μM).2PAR2 (1-6) amide (100 μM) reduces colony formation of A549 lung cancer cells.1It induces superoxide production and degranulation in isolated human eosinophils when used at a concentration of 500 μM.3PAR2 (1-6) amide (5 μmol/kg) induces tear secretion in rats when used in combination with amastatin .4 1.Bohm, S.K., Kong, W., Bromme, D., et al.Molecular cloning, expression and potential functions of the human proteinase-activated receptor-2Biochem. J.314(Pt 3)1009-1016(1996) 2.Kanke, T., Ishiwata, H., Kabeya, M., et al.Binding of a highly potent protease-activated receptor-2 (PAR2) activating peptide, [3H]2-furoyl-LIGRL-NH2, to human PAR2Br. J. Pharmacol.145(2)255-263(2005) 3.Miike, S., McWilliam, A.S., and Kita, H.Trypsin induces activation and inflammatory mediator release from human eosinophils through protease-activated receptor-2J. Immunol.167(11)6615-6622(2001) 4.Nishikawa, H., Kawai, K., Tanaka, M., et al.Protease-activated receptor-2 (PAR-2)-related peptides induce tear secretion in rats: Involvement of PAR-2 and non-PAR-2 mechanismsJ. Pharmacol. Exp. Ther.312(2)324-331(2005)

Terpendole I is a fungal metabolite that has been found in A. yamanashiensis.1 It is a weak inhibitor of acyl-coenzyme A:cholesterol acyltransferase (ACAT; IC50 = 145 μM) and is active against the bacteria B. cereus and B. subtilis (MICs = 100 μg/ml for both) but not S. aureus, P. aeruginosa, or K. pneumoniae (MICs = >200 μg/ml for all) or the fungus C. albicans (MIC = 200 μg/ml).1,2 It is cytotoxic to HeLa cells with an IC50 value of 52.6 μM.3 |1. Tomoda, H., Tabata, N., Yang, D.-J., et al. Terpendoles, novel ACAT inhibitors produced by Albophoma yamanashiensis. III. Production, isolation and structure elucidation of new components. J. Antibiot. (Tokyo) 48(8), 793-804 (1995).|2. Zhao, J.-C., Wang, Y.-L., Zhang, T.-Y., et al. Indole diterpenoids from the endophytic fungus Drechmeria sp. as natural antimicrobial agents. Phytochemistry 148, 21-28 (2018).|3. Nagumo, Y., Motoyama, T., Hayashi, T., et al. Structure-activity relationships of terpendole E and its natural derivatives. ChemistrySelect 2(4), 1533-1536 (2017).

MSA-2 dimer, a selective and orally active non-nucleotide STING agonist with a dissociation constant (Kd) of 145 μM, demonstrates prolonged antitumor and immunogenic activity. It non-covalently binds to STING as a dimer, showing greater permeability compared to cyclic dinucleotide[1].