Hydroxy-PEG4-methyl acetate is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
WRW4, a specific formyl peptide receptor-like 1 (FPRL1) antagonist, inhibits WKYMVm binding to FPRL1 with an IC50 of 0.23 μM. WRW4 specifically inhibits the increase in intracellular calcium by the FPRL1 agonists MMK-1, amyloid beta42 (Abeta42) peptide, and F peptide[1].
Acetyl dipeptide-3 aminohexanoate is a bioactive peptide with anti-aging effect and has been reported used as a cosmetic ingredient[1].
1,1-Dibromo-3,3-dichloroacetone is a halogenated ozone-chlorine and ozone chloramine disinfection byproducts (DBPs) at elevated bromide levels when chlorine or chloramine is used as a secondary disinfectant[1].
Rolofylline (KW-3902) is a potent, selective adenosine A1 receptor antagonist that is under development for the treatment of patients with acute congestive heart failure and renal impairment.Rolofylline is metabolized primarily to the pharmacologically active M1-trans and M1-cis metabolites by cytochrome P450 (CYP450)[1].Rolofylline is alleviating the presynaptic dysfunction and restores neuronal activity as well as dendritic spine levels in vitro, is an interesting candidate to combat the hypometabolism and neuronal dysfunction associated with Tau-induced neurodegenerative diseases[2].
Cyclo(Ala-Glu) is a cyclic dipeptide[1].
Pymetrozine is a feeding inhibitor of Homoptera, in preventing transmission of cauliflower mosaic caulimovirus by the aphid species Myzus persicae (Sulzer).
Paecilaminol (FKI-0550) is potent NADH-fumarate reductase inhibitor. Paecilaminol exhibits an IC50 value of 5.1 μM against Ascaris suum NADH-fumarate reductase[1].
TGR5 Receptor Agonist 3 (Compound 19) is a soft-drug G-protein-coupled bile acid receptor 1 (GPBAR1, TGR5) agonist with reduced gallbladder-filling effects (favorable gallbladder safety), with EC50s of 16.4 and 209 nM for hTGR5 and mTGR5, respectively[1].
H-Arg(Mtr)-OH is an arginine derivative[1].
Lck inhibitor 2 is a bis-anilinopyrimidine inhibitor of tyrosine kinases including LCK, BTK, LYN, SYK, and TXK. The IC50 values are 13nM, 9nM, 3nM, 26nM and 2nM for Lck, Btk, Lyn, Btk and Txk respectively IC50 Value: 13 nM(Lck) [1]Target: Src family kinaseLck inhibitor 2(Compound 9) inhibited 48 kinases with %control < 1 (33 of them tyrosine kinases, almost half of the 71 tyrosine kinases in the panel). A further 27 kinases were bound with %control < 10. Kd values for 16 kinases were determined and found to be below 100 nM. These included TXK (10 nM)[2].
Navarixin is a potent, allosteric antagonist of both CXCR1 and CXCR2, with Kd values of 41 nM for cynomolgus CXCR1 and 0.20 nM, 0.20 nM, 0.08 nM for mouse, rat and cynomolgus monkey CXCR2, respectivelly.
1,3'-Dimethylguanosine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
FK-739 (free base) is an angiotensin II type 1 (AT1) receptor antagonist used in the study of hypertension[1].
TPA023B is a potent, α2/α3 subtype-selective GABAA receptor partial agonist with Ki of 2.0 and 1.8 nM, does not affect the functioning of the α1 subtype; demonstrates anxiolytic effects in rodent and primate models of anxiety, with no significant effects in ataxia and/or myorelaxation.
TCO-OH is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].
PKR-IN-C16 is a specific protein kinase (PKR) inhibitor. PKR-IN-C16 is able to inhibit the autophosphorylation of PKR and unlock the translation blockade induced by PKR in primary neuronal cultures[1].
N-((RS)-2-Hydroxy-propyl)-Val-Leu-anilide is a biologically active peptide.
Ginsenoside Rh4 is a rare saponin obtained from Panax notoginseng. Ginsenoside Rh4 activates Bax, caspase 3, caspase 8, and caspase 9. Ginsenoside Rh4 also induces autophagy.
Przewalskinic acid A is a rare, water-soluble phenolic acid thus far only found in the Salvia przewalskii Maxim herb. Phenolic acids show potent antioxidant activities and potential effects in protecting against brain and heart damage caused by ischemia reperfusion[1].
LMP2A (426-434) is a biological active peptide. (HLA A2.1-restricted epitope from Epstein-Barr Virus latent membrane protein LMP2 (426-434).)
NTU281 is a potent transglutaminase-2 inhibitor. NTU281 can reduce the increases in serum creatinine and albuminuria in diabetic rats. NTU281 can also reduce glomerular collagen I accumulation, Hic-5 and α-SMA expression, and apoptosis. NTU281 can be used for researching glomerulosclerosis caused by diabetes[1][2].
Temporin L is a potent antimicrobial peptide and is active against Gram-negative bacteria and yeast strains. Temporin L also has antiendotoxin properties[1][2].
1-Bromodecane-d21 is the deuterium labeled 1-Bromodecane[1].
Zomepirac-d4 sodium salt is the deuterium labeled Zomepirac sodium salt. Zomepirac sodium salt (McN-2783-21-98) is a potent prostaglandin biosynthesis inhibitor. Zomepirac sodium salt is a non-steroidal anti-inflammatory drug (NSAID). Zomepirac sodium salt can cause immune-mediated liver injury[1][2].
Ivabradine is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine reduces dose-dependently heart rate without modification of blood pressure. Ivabradine shows anticonvulsant, anti-ischaemic and anti-anginal activity[1][2][3][4].
Resorcinol monoacetate is an antiseptic and a disinfectant, is a chemical intermediate for the production of many other pharmaceuticals, and can be used to treat acne, seborrheic dermatitis, eczema, psoriasis, and other skin disorders.
Triptobenzene H (Hypoglic acid) significantly increases TNF-α and IL-1β mRNA levels in macrophages, causing indirect liver damage[1].
PD 407824 is a checkpoint kinase Chk1 and WEE1 inhibitor with IC50s of 47 and 97 nM, respectively. PD 407824 is a chemical BMP sensitizer and increases the sensitivity of cells to sub-threshold amounts of BMP4[1][2].
(6E)-1,7-Bis(4-hydroxyphenyl)-6-hepten-3-one (compound7) is a nature product isolated from rhizomes of Curcuma kwangsiensis. (6E)-1,7-Bis(4-hydroxyphenyl)-6-hepten-3-one has inhibitory effect on NO production induced by LPS in macrophages with an IC50 value of 8.93 μM[1].