p 29

CGP 29030A is a new piperazine derivative with analgesic activity and significant inhibitory effect on potentially nociceptive dorsal horn neurons, which can be used to study painful disorders.

SMAP 29, a bactericidal antimicrobial peptide and a cleavage product from the C-terminus of an ovine cathelicidin prepropeptide, is effective against P. aeruginosa strain PAO1 in both low- and high-salt conditions, as demonstrated in an energy-dependent luminescence assay with half-maximal effective concentrations (EC50s) of 0.05 and 0.06 µM, respectively. Additionally, it induces hemolysis in ovine red blood cells in a concentration-dependent manner.

16-Oxolyclanitin-29-yl p-coumarate is a natural product for research related to life sciences. The catalog number is TN5971 and the CAS number is 140701-70-8.

Cgp 29287 is a primate-specific renin inhibitor. It also has a prolonged duration of action.

GluR5-subunit containing kainate receptor antagonist

Jtp 2942 is a new thyrotropin-releasing hormone analog.

Lupeol (Monogynol B) is a novel androgen receptor inhibitor with anti-inflammatory and antioxidant activity.

ZX-29 is a potent and selective inhibitor of ALK with IC50 values of 2.1 nM, 1.3 nM, and 3.9 nM for ALK, ALK [L1196M], and ALK [G1202R] mutations, respectively. It also induces protective autophagy and exhibits antitumor effects.

Keenamide A, a cytotoxic cyclic hexapeptide, exhibits significant activity towards the P-388, A-549, MEL-20, and HT-29 tumor cell lines, but was inactive against the D6 and W2 Plasmodium falciparum malarial clones.

Lys05, or Lys01 trihydrochloride, is a potent, water soluble lysosomal autophagy inhibitor. Lys05 is a previously undescribed dimeric chloroquine which more potently accumulates in the lysosome and blocks autophagy compared with HCQ. Lys05 produced more p

FD223 is a potent, selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor with a marked affinity (IC50=1 nM), demonstrating notable selectivity against other isoforms (IC50s: α=51 nM, β=29 nM, γ=37 nM). This compound effectively suppresses the proliferation of acute myeloid leukemia (AML) cell lines by inhibiting p-AKT Ser473, thereby inducing G1 phase cell cycle arrest. FD223 holds promise for leukemia research, particularly in AML[1].

N-(2-Azidoethyl)betulonamide is a pentacyclic triterpenoid, a derivative of betulonic acid , and an intermediate in the synthesis of betulonic acid derivatives within vitrocancer cell cytotoxicity.1 1.Suman, P., Patel, A., Solano, L., et al.Synthesis and cytotoxicity of Baylis-Hillman template derived betulinic acid-triazole conjugatesTetrahedron73(29)4214-4226(2017)

Gliovirin is a fungal metabolite that has been found inT. harzianumand has fungicidal, antimicrobial and anti-inflammatory activities.1It is active against the plant pathogenic fungusP. ultimum(MIC = 60 ng/ml) and the parasiteT. brucei brucei(IC50= 90 ng/ml), but has no effect on the plant pathogenic fungiR. solani,P. omnivorum,T. basicola,R. arrhizus, andV. dahliaeor the bacteriaB. thuringiensis,P. fluorescens, andX. malvacearumwhen used at concentrations up to 1,000 ng/ml.2,3Gliovirin decreases phorbol 12-myristate 13-acetate (TPA)- and ionomycin-induced increased expression of COX-2 (IC50= 1 μM) and protein levels of IL-2 in Jurkat cells (IC50= 5.2 μM).1 1.Rether, J., Serwe, A., Anke, T., et al.Inhibition of inducible tumor necrosis factor-α expression by the fungal epipolythiodiketopiperazine gliovirinBiol. Chem.388(6)627-637(2007) 2.Howell, C.R., and Stipanovic, R.D.Gliovirin, a new antibiotic from Gliocladium virens, and its role in the biological control of Pythium ultimumCan. J. Microbiol.29(3)321-324(1983) 3.Iwatsuki, M., Otoguro, K., Ishiyama, A., et al.In vitro antitrypanosomal activity of 12 low-molecular-weight antibiotics and observations of structure/activity relationshipsJ. Antibiot. (Tokyo)63(10)619-622(2010)

Flumequine-13C3is intended for use as an internal standard for the quantification of flumequine by GC- or LC-MS. Flumequine is a fluoroquinolone antibiotic.1It is active againstS. aureus, S. pyogenes, B. subtilis, E. coli, P. aeruginosa, S. faecalis, andK. pneumoniae(MICs = 1-100 μg/ml). Flumequine is also active against field isolates of B. hyodysenteriae (MICs = 6.25-200 μg/ml).2It inhibits DNA gyrase, disrupting supercoiling of bacterial DNA to block transcription and replication.3In vivo, flumequine (50 mg/kg) increases survival in rat models ofP. vulgaris-induced urinary tract infection andP. mirabilis-induced prostatitis.1Formulations containing flumequine have been used in the treatment of urinary tract infections in veterinary medicine. 1.Rohlfing, S.R., Gerster, J.R., and Kvam, D.C.Bioevaluation of the antibacterial flumequine for urinary tract useAntimicrob. Agents Chemother.10(1)20-24(1976) 2.Aller-Morán, L.M., Martínez-Lobo, F.J., Rubio, P., et al.Evaluation of the in vitro activity of flumequine against field isolates of Brachyspira hyodysenteriaeRes. Vet. Sci.10351-53(2015) 3.Smith, J.T.The mode of action of 4-quinolones and possible mechanisms of resistanceJ. Antimicrob. Chemother.18 (Suppl. D)21-29(1986)

N-p-Tosyl-Gly-Pro-Lys-pNA is a colorimetric substrate for plasmin.1,2,3Plasmin binds and hydrolyzes N-p-tosyl-Gly-Pro-Lys-pNA to releasep-nitroanilide (pNA), which can be quantified by colorimetric detection at 405 nm as a measure of plasmin activity. 1.Jespersen, J., Gram, J., and Astrup, T.The autodigestion of human plasmin follows a bimolecular mode of reaction subject to product inhibitionThromb. Res.41(3)395-404(1986) 2.Kim, S.H., and Choi, N.S.Electrophoretic analysis of protease inhibitors in fibrin zymographyAnal. Biochem.270(1)179-181(1999) 3.Chen, T., and Rael, E.D.Purification of M5, a fibrinolytic proteinase from Crotalus molossus molossus venom that attacks complementInt. J. Biochem. Cell Biol.29(5)789-799(1997)

Pal-KTTKS is a lipidated pentapeptide consisting of a fragment of the type I collagen C-terminal propeptide conjugated to palmitic acid .1 It increases collagen production in human corneal and dermal fibroblasts when used at concentrations of 0.002, 0.004, and 0.008 wt%.2 Following topical administration, pal-KTTKS (50 μg/cm2) is found in the stratum corneum, epidermis, and dermis of isolated hairless mouse skin.1 It can self-assemble into flat tapes and extended fibrillar structures.3 Pal-KTTKS has been detected in anti-wrinkle creams.4 |1. Choi, Y.L., Park, E.J., Kim, E., et al. Dermal stability and in vitro skin permeation of collagen pentapeptides (KTTKS and palmitoyl-KTTKS). Biomol. Ther. (Seoul) 22(4), 321-327 (2014).|2. Jones, R.R., Castelletto, V., Connon, C.J., et al. Collagen stimulating effect of peptide amphiphile C16-KTTKS on human fibroblasts. Mol. Pharm. 10(3), 1063-1069 (2013).|3. Castelletto, V., Hamley, I.W., Whitehouse, C., et al. Self-assembly of palmitoyl lipopeptides used in skin care products. Langmuir 29(29), 9149-9155 (2013).|4. Chirita, R.-I., Chaimbbault, P., Archambault, J.-C., et al. Development of a LC-MS/MS method to monitor palmitoyl peptides content in anti-wrinkle cosmetics. Anal. Chim. Acta 641(1-2), 95-100 (2009).

7α-Thiomethylspironolactone is a major metabolite of the synthetic steroid spironolactone.1,2 1.Jankowski, A., Skorek-Jankowska, A., and Lamparczyk, H.Simultaneous determination of spironolactone and its metabolites in human plasmaJ. Pharm. Biomed. Anal.14(8-10)1359-1365(1996) 2.Gardiner, P., Schrode, K., Quinlan, D., et al.Spironolactone metabolism: Steady-state serum levels of the sulfur-containing metabolitesJ. Clin. Pharmacol.29(4)342-347(1989)

TFM is a piscicide.1It is toxic to sea lamprey (P. marinus) with LC50values ranging from 1.97 to 2.11 and 2.05 to 2.21 mg/L for sac and swim-up fry, respectively, 1.6 to 2.45 mg/L for juveniles, and 1.6 to 1.63 mg/L for adults. It is also toxic to juvenile lake sturgeon (A. fulvescens) less than 100 mm in size but not to a variety of other fish species. TFM (50 μM) uncouples oxidative phosphorylation by 22 and 28% in isolated sea lamprey and rainbow trout (O. mykiss) liver, respectively.2Formulations containing TFM have been used as lampricides in the control of larval sea lamprey populations. 1.Boogaard, M.A., Bills, T.D., and Johnson, D.A.Acute toxicity of TFM and a TFM/niclosamide mixture to selected species of fish, including lake sturgeon (Acipenser fulvescens) and mudpuppies (Necturus maculosus), in laboratory and field exposuresJ. Great Lakes Res.29(Suppl 1)529-541(2003) 2.Birceanu, O., McClelland, G.B., Wang, Y.S., et al.The lampricide 3-trifluoromethyl-4-nitrophenol (TFM) uncouples mitochondrial oxidative phosphorylation in both sea lamprey (Petromyzon marinus) and TFM-tolerant rainbow trout (Oncorhynchus mykiss)Comp. Biochem. Physiol. C. Toxicol. Pharmacol.153(3)342-349(2011)

Zelkovamycin is a cyclic peptide antibiotic isolated from Streptomyces, known to inhibit growth of X. oryzae, P. oryzae, S. aureus, and A. laidlawii in a concentration-dependent manner at concentrations ranging from 0.01 to 300 μg ml.

Compound 29 (also known as Compound 16) is an antimalarial agent that demonstrates inhibition of the P. berghei liver stage parasite load, exhibiting an effective concentration (EC50) of 5.2 μM [1].

Antimalarial agent 33 (compound 5g) exhibits antiplasmodial activity targeting both erythrocytic and hepatic stages of Plasmodium, with an effective concentration (EC50) of 1.1 μM against the K1 strain of P. falciparum. It demonstrates improved microsomal stability with a half-life (T1 2) of 29 minutes and displays no significant cytotoxicity against primary hepatocytes [1].

1-Hydroxyrutaecarpine exhibits cytotoxicities (ED50 values < 4 microg mL) against P-388 or HT-29 cell lines in vitro.

Norsanguinarine has antifungal activity, it exhibits 100 % inhibition of A. brassicicola and C. maculans at 1000 ppm whereas. It shows significant cytotoxic activities (ED (50) values < 4 microg ml) against P-388, KB16, A549, and HT-29 cell lines.

2,3-Dihydroamentoflavone 7,4'-dimethyl ether exhibits cytotoxicity (ED50 values < 4 microg mL) against P-388 and HT-29 cell lines in vitro.