nm 283

Valopicitabine, a NS5B inhibitor, is used potentially for the treatment of HCV infection.

SR-318 is a potent and highly selective inhibitor of p38 MAPK, demonstrating IC50 values of 5 nM for p38α, 32 nM for p38β, and 6.11 μM for p38α β. It possesses both anti-cancer and anti-inflammatory activity.

Pituitary adenylate cyclase-activating peptide (PACAP) (6-27) is a PACAP receptor antagonist with IC50 values of 1,500, 600, and 300 nM, respectively, for rat PAC1, rat VPAC1, and human VPAC2 recombinant receptors expressed in CHO cells. It binds to PACAP receptors on SH-SY5Y and SK-N-MC human neuroblastoma and T47D human breast cancer cells (IC50s = 24.5, 106, and 105 nM, respectively) and inhibits cAMP accumulation induced by PACAP (1-38) (Kis = 457, 102, and 283 nM, respectively, in SH-SY5Y, SK-N-MC, and T47D cells). In vivo, in newborn pigs, PACAP (6-27) (10 μM) inhibits vasodilation of pial arterioles induced by PACAP (1-27) and PACAP (1-38) . It also inhibits PACAP (1-27)-stimulated increases in plasma insulin and glucagon levels and pancreatic venous blood flow in dogs when administered locally to the pancreas at a dose of 500 μg.

LLY-283 is a potent, selective, and oral protein arginine methyltransferase 5 (PRMT5) inhibitor, exhibiting an IC50 of 22 nM and a Kd of 6 nM for the PRMT5:MEP50 complex, and demonstrates antitumor activity.

β-Glucuronidase-IN-1 is an E. coli β-glucuronidase (β-glucuronidase) inhibitor with a potent, selective, non-competitive, and orally active IC50 and Ki value of 283 nM and 164 nM, respectively, against E. coli β-glucuronidase.

DGKα-IN-3 (example 25), with an IC50 of 283 nM, is a selective DGKα inhibitor that enhances anti-PD-1's anti-tumor activity by promoting T cell proliferation and function, highlighting its potential for cancer and immunology research applications.

9(Z),11(E)-Conjugated linoleic acid is an isomer of linoleic acid that has been found in beef and milk fat.1It binds to peroxisome proliferator-activated receptor α (PPARα; IC50= 140 nM) and activates the receptor in a reporter assay using COS-1 cells expressing mouse PPARα when used at a concentration of 100 μM.29(Z),11(E)-Conjugated linoleic acid inhibits TNF-α-inducedGLUT4expression and increases insulin-stimulated glucose transport in 3T3-L1 adipocytes.3Dietary administration of 9(Z)11(E)-conjugated linoleic acid reduces serum fasting glucose, insulin, and triglyceride levels and decreases white adipose tissue macrophage infiltration inob/obmice. It also increases body weight gain and body fat in weanling mice.4[Matreya, LLC. Catalog No. 1278] 1.Shultz, T.D., Chew, B.P., Seaman, W.R., et al.Inhibitory effect of conjugated dienoic derivatives of linoleic acid and β-carotene on the in vitro growth of human cancer cellsCancer Lett.63(2)125-133(1992) 2.Moya-Camarena, S.Y., Heuvel, J.P.V., Blanchard, S.G., et al.Conjugated linoleic acid is a potent naturally occurring ligand and activator of PPARαJ. Lipid Res.40(8)1426-1433(1999) 3.Moloney, F., Toomey, S., Noone, E., et al.Antidiabetic effects of cis-9, trans-11-conjugated linoleic acid may be mediated via anti-inflammatory effects in white adipose tissueDiabetes56(3)574-582(2007) 4.Pariza, M.W., Park, Y., and Cook, M.E.The biologically active isomers of conjugated linoleic acidProg. Lipid Res.40(4)283-298(2001)

Axl-IN-5 (compound 1) is an AXL inhibitor with an IC50 of 283 nM, demonstrating anticancer activity.

UbcH5c-IN-1 is a selective small-molecule Ubiquitin-conjugating enzyme UbcH5c inhibitor (Kd: 283 nM for E2 UbcH5c-IN-1 by covalent binding with Cys85).

Lifirafenib (Beigene-283) is a potent inhibitor of RAF family kinases and EGFR in biochemical assays with IC50 of 23, 29 and 495 nM for the recombinant BRAFV600E kinase domain, EGFR and EGFR T790M L858R mutant respectively.

Valopicitabine is an effective prodrug of the effective anti-HCV drug 2'-C-methylcytidine and can be used as a promising antiviral drug for the study of chronic HCV infection.

L 888607 is an effective and selective CRTH2 agonist (Ki: 0.8 nM).