f-3

Fmoc-Tyr(3-F, tBu)-OH is a cyclic peptide compound possessing high membrane permeability and exhibiting specific binding affinity towards a target molecule.

5-Acetyl-3-chloro-10,11-dihydro-5H-dibenz[b,f]azepine is a useful organic compound for research related to life sciences. The catalog number is T67591 and the CAS number is 25961-11-9.

Ir[p-F(t-Bu)-ppy]3 is a useful organic compound for research related to life sciences and the catalog number is T64556.

H-D-Phe(3-F)-OH is a useful organic compound for research related to life sciences. The catalog number is T67306 and the CAS number is 110117-84-5.

3'-F-3'-dG(iBu)-2'-phosphoramidite is a Nucleoside Phosphoramidite.

3'-F-3'-dA(Bz)-2'-phosphoramidite is a Nucleoside Phosphoramidite; Nucleoside Derivative - Fluoro-modified nucleoside.

3-O-Methyltagitinin F is a useful organic compound for research related to life sciences and the catalog number is T126402.

Boc-Phe(3-F)-OH is an amino acid derivative and has a wide range of applications in life science related research.

Ethyl 8-hydroxy-5-methyl-6-oxo-5,6-dihydro-4H-benzo[f]imidazo[1,5-a][1,4]diazepine-3-carboxylate is a useful organic compound for research related to life sciences. The catalog number is T66942 and the CAS number is 131666-45-0.

3-Chloro-6,11-dihydro-6-methyl-5,5,11-trioxodibenzo[c,f][1,2]thiazepine is a useful organic compound for research related to life sciences. The catalog number is T65901 and the CAS number is 26638-53-9.

Fmoc-D-Phe(3-F)-OH is a useful organic compound for research related to life sciences. The catalog number is T65834 and the CAS number is 198545-72-1.

Boc-D-Phe(3-F)-OH is a useful organic compound for research related to life sciences. The catalog number is T65692 and the CAS number is 114873-11-9.

VSTx-3 is a potassium voltage-gated channel (K_V) blocker, which has also been shown to be a potent tetrodotoxin-sensitive (TTX-sensitive) sodium channel inhibitor, with particular efficacy against NaV1.8 channels, as evidenced by its half-maximal inhibitory concentration (IC_50) values of 0.19 μM for hNaV1.3, 0.43 μM for hNaV1.7, and 0.77 μM for hNaV1.8 channels.

Lodenosine is an inhibitor of RNA-directed DNA polymerase, and potentially for the treatment of HIV.

Sofosbuvir impurity F (Sofosbuvir 3',5'-Bis-(S)-phosphate) is both a diastereomer of Sofosbuvir and an impurity of Sofosbuvir which is an inhibitor of HCV RNA replication.

1. Glaucocalyxin A (Leukamenin F)-SBE-β-CD could be useful with a better solubility and sustained function in drug delivery. 2. Glaucocalyxin A activates caspase-3, decreases BAD phosphorylation, and reduces the expression of X-linked inhibitor of apoptosis protein. 3. Glaucocalyxin A inhibits Akt phosphorylation, suppresses proliferation, and promotes apoptosis in a dose-dependent manner, but not in normal glial cells. 4. Glaucocalyxin A inhibits collagen-stimulated tyrosine phosphorylation of Syk, LAT, and phospholipase Cγ2, the signaling events in collagen receptor GPⅥ pathway. 5. Glaucocalyxin A could potentially be developed as an antiplatelet and antithrombotic agent, can inhibit platelet p-selectin secretion and integrin activation by convulxin, is a GPVI selective ligand.

Pulsatilla saponin H is a natural product isolated from the Roots of Pulsatilla koreana.

Polygalasaponin F has anti-neuroinflammatory activity, can inhibit the release of inflammatory cytokines TNF-α and NO induced by lipopolysaccharides (LPS) and reduce the expression of inducible nitric oxide synthases. Polygalasaponin F can significantly i

Biotin (S)-sulfoxide is an inactive metabolite of the coenzyme biotin .1,2It has also been found inE. coliand is reduced by the biotin sulfoxide reduction system as a source of biotin.3 1.Denkel, L.A., Rhen, M., and Bange, F.-C.Biotin sulfoxide reductase contributes to oxidative stress tolerance and virulence in Salmonella enterica serovar TyphimuriumMicrobiology (Reading)159(Pt 7)1447-1458(2013) 2.Carling, R.S., and Turner, C.Methods for assessment of biotin (Vitamin B7)Laboratory assessment of vitamin status193-217(2019) 3.del Campillo-Campbell, A., Dykhuizen, D., and Clearly, P.P.Enzymic reduction of d-biotin d-sulfoxide to d-biotinMethods Enzymol.62379-385(1979)

Ginsenoside-F3 has immunoenhancing activity by regulating production and gene expression of type 1, type 2 cytokines in murine spleen cells. Ginsenoside-F3 enhances the NF-kappaB DNA binding activity induced by ConA in murine spleen cells (10 μM).

Shizukanolide F is a natural product of Chloranthus, Chloranthaceae. The catalog number is TN5008 and the CAS number is 120061-96-3. Shizukanolide F can be used as a reference standard.

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)

Pyrenocine A is a fungal metabolite that has been found inP. terrestrisand has diverse biological activities.1It inhibits the asexual spore germination of the plant pathogenic fungiF. oxysporum,F. solani,M. hiemalis, andR. stolonifer(EC50s = 14, 20, 20, and 25 μg/ml, respectively). Pyrenocine A is active againstB. subtilis,S. aureus, andE. coli(IC50s = 30, 45, and 200 μg/ml, respectively). It inhibits onion seedling elongation (EC50= 4 μg/ml). Pyrenocine A is also a phytotoxin that inhibits lettuce seed germination and rice seedling elongation.2,3 1.Sparace, S.A., Reeleder, R.D., and Khanizadeh, S.Antibiotic activity of the pyrenocinesCan. J. Microbiol.33(4)327-330(1987) 2.Sato, H., Konoma, K., and Sakamura, S.Phytotoxins produced by onion pink root fungus, Pyrenochaeta terrestrisAgric. BioI. Chem.43(11)2409-2411(1979) 3.Sato, H., Konoma, K., Sakamura, S., et al.X-Ray crystal structure of pyrenocine A, a phytotoxin from Pyrenochaeta terrestrisAgric. BioI. Chem.45(3)795-797(1981)

Taurocholic acid 3-sulfate (TCA3S) is a metabolite of the conjugated bile acid taurocholic acid .1Plasma levels of TCA3S are elevated in wild-type andSortilin 1(Sort1) knockout mice at 6 hours following bile duct ligation (BDL) and are further elevated inSort1knockout mice at 24 hours post-BDL.2 1.Lefebvre, P., Cariou, B., Lien, F., et al.Role of bile acids and bile acid receptors in metabolic regulationPhysiol. Rev.89(1)147-191(2009) 2.Li, J., Woolbright, B.L., Zhao, W., et al.Sortilin 1 loss-of-function protects against cholestatic liver injury by attenuating hepatic bile acid accumulation in bile duct ligated miceToxicol. Sci.161(1)34-47(2018)

1-Heptadecanoyl-rac-glycerol is a monoacylglycerol that contains heptadecanoic acid at the sn-1 position. It is active against the bacteria E. aerogens, E. cloacae, P. mirabilis, and S. faecalis (MIC = 78 μg/ml for all).1 1-Heptadecanoyl-rac-glycerol has been found in T. africana, I. sonorae, and wheat bran.1,2,3 |1. Kuete, V., Metuno, R., Ngameni, B., et al. Antimicrobial activity of the methanolic extracts and compounds from Treculia africana and Treculia acuminata (Moraceae). S. Afr. J. Bot. 74(1), 111-115 (2008).|2. Fernández-Galicia, E., Calada, F., Roman-Romos, R., et al. Monoglycerides and fatty acids from Ibervillea sonorae root: Isolation and hypoglycemic activity. Planta Med. 73(3), 236-240 (2007).|3. Prinsen, P., Gutiérrez, A., Faulds, C.B., et al. Comprehensive study of valuable lipophilic phytochemicals in wheat bran. J. Agric. Food Chem. 62(7), 1664-1673 (2014).

Jump to search UTS2 Identifiers Aliases UTS2, PRO1068, U-II, UCN2, UII, urotensin 2 External IDs OMIM: 604097 MGI: 1346329 HomoloGene: 4939 GeneCards: UTS2 hide Gene location (Human) Chr. Chromosome 1 (human)[1] Band 1p36.23 Start 7,843,083 bp[1] En

Bleomycin B4 (Phleomycin F), an antibiotic with antitumor properties, is utilized in cancer research [1] [2] [3].

3-Hydroxymandelic Acid is a metabolite of Phenylephrine. 3-Hydroxymandelic Acid is a metabolite of Phenylephrine, which is an α-receptor agonist.

Betamethasone 21-phosphate is a synthetic glucocorticoid.1It prevents increases in macrophage and eosinophil numbers in bronchoalveolar lavage fluid (BALF) and decreases in blood leukocyte numbers in a guinea pig model of parainfluenza-3 viral infection when administered at a dose of 8 mg/kg but does not prevent airway hyperresponsiveness after infection.2Betamethasone 21-phosphate inhibits cell infiltration into the aqueous humor in a rat model of endotoxin-induced uveitis when administered topically or subcutaneously at doses of 0.01-1% or 1 mg/kg, respectively.3It increases maximal lung pressure volume curves in fetal sheep when administered to pregnant ewes at 0.75 gestation at doses of 80 and 170 μg/kg.1Betamethasone 21-phosphate increases body weight, impairs learning and memory, increases anxiolytic behavior, and reduces hippocampal neurogenesis in CD-1 mice but reduces body weight and increases neurogenesis with no effect on anxiety in high-anxiety DBA/2 mice when administered at a dose of approximately 25 mg/kg per day in the drinking water for seven weeks.4Formulations containing betamethasone 12-phosphate and betamethasone acetate have been used in the treatment of severe allergic conditions and a variety of immune-related conditions. 1.Loehle, M., Schwab, M., Kadner, S., et al.Dose-response effects of betamethasone on maturation of the fetal sheep lungAm. J. Obstet. Gynecol.202(2)186.e181-186.e187(2010) 2.Leusink-Muis, A., Ten Broeke, R., Folkerts, G., et al.Betamethasone prevents virus-induced airway inflammation but not airway hyperresponsiveness in guinea pigsClin. Exp. Allergy29(Suppl. 2)82-85(1999) 3.Tsuji, F., Sawa, K., Kato, M., et al.The effects of betamethasone derivatives on endotoxin-induced uveitis in ratExp. Eye Res.64(1)31-36(1997) 4.Aiello, R., Crupi, R., Leo, A., et al.Long-term betamethasone 21-phosphate disodium treatment has distinct effects in CD1 and DBA/2 mice on animal behavior accompanied by opposite effects on neurogenesisBehav. Brain Res.278155-166(2015)

Quorum sensing is a regulatory process used by bacteria for controlling gene expression in response to increasing cell density.[1] This regulatory process manifests itself with a variety of phenotypes including biofilm formation and virulence factor production.[2] Coordinated gene expression is achieved by the production, release, and detection of small diffusible signal molecules called autoinducers. The N-acylated homoserine lactones (AHLs) comprise one such class of autoinducers, each of which generally consists of a fatty acid coupled with homoserine lactone (HSL). AHLs vary in acyl group length (C4-C18), in the substitution of C3 (hydrogen, hydroxyl, or oxo group) and in the presence or absence of one or more carbon-carbon double bonds in the fatty acid chain. These differences confer signal specificity through the affinity of transcriptional regulators of the LuxR family.[3] C16:1-Δ9-(L)-HSL is a long-chain AHL that functions as a quorum sensing signaling molecule in strains of S. meliloti.[4],[5],[6],[7] Regulating bacterial quorum sensing signaling can be used to inhibit pathogenesis and thus, represents a new approach to antimicrobial therapy in the treatment of infectious diseases.[8] Reference：[1]. González, J.E., and Keshavan, N.D. Messing with bacterial quorum sensing. Microbiol. Mol. Biol. Rev. 70(4), 859-875 (2006).[2]. Gould, T.A., Herman, J., Krank, J., et al. Specificity of acyl-homoserine lactone syntheses examined by mass spectrometry. J. Bacteriol. 188(2), 773-783 (2006).[3]. Penalver, C.G.N., Morin, D., Cantet, F., et al. Methylobacterium extorquens AM1 produces a novel type of acyl-homoserine lactone with a double unsaturated side chain under methylotrophic growth conditions. FEBS Lett. 580(2), 561-567 (2006).[4]. Teplitski, M., Eberhard, A., Gronquist, M.R., et al. Chemical identification of N-acyl homoserine lactone quorum-sensing signals produced by Sinorhizobium meliloti strains in defined medium. Archives of Microbiology 180, 494-497 (2003).[5]. Gao, M., Chen, H., Eberhard, A., et al. sinI- and expR-dependent quorum sensing in Sinorhizobium meliloti. Journal of Bacteriology 187(23), 7931-7944 (2005).[6]. Marketon, M.M., Glenn, S.A., Eberhard, A., et al. Quorum sensing controls exopolysaccharide production in Sinorhizobium meliloti. Journal of Bacteriology 185(1), 325-331 (2003).[7]. Marketon, M., Gronquist, M.R., Eberhard, A., et al. Characterization of the Sinorhizobium meliloti sinR/sinI locus and the production of novel N-Acyl homoserine lactones. Journal of Bacteriology 184(20), 5686-5695 (2002).[8]. Cegelski, L., Marshall, G.R., Eldridge, G.R., et al. The biology and future prospects of antivirulence therapies. Nat. Rev. Microbiol. 6(1), 17-27 (2008).

1,3,6,8-Pyrenetetrasulfonic acid is an intermediate in the synthesis of the color additive pyranine.1It has been used to stabilize intermolecular interactions for the crystallization ofL. mexicanapyruvate kinase.2 1.Jitian, S., White, S.R., Yang, H.-H.W., et al.Conventional high-performance liquid chromatography versus derivative spectrophotometry for the determination of 1,3,6-pyrenetrisulfonic acid trisodium salt and 1,3,6,8-pyrenetetrasulfonic acid tetrasodium salt in the color additive D&C Green No. 8 (Pyranine)J. Chromatogr. A1324238-241(2014) 2.Morgan, H.P., McNae, I.W., Hsin, K.-Y., et al.An improved strategy for the crystallization of Leishmania mexicana pyruvate kinaseActa Crystallogr. Sect. F Struct. Biol. Cryst. Commun.66(Pt 3)215-218(2010)

3-Acetyldeoxy nivalenol-13C17is intended for use as an internal standard for the quantification of 3-acetyldeoxy nivalenol by GC- or LC-MS. 3-Acetyldeoxy nivalenol is a mycotoxin that has been found inF. graminearum.1In vivo, 3-acetyldeoxy nivalenol (40 mg/kg) induces duodenal and splenic cell necrosis, as well as lethality (LD50= 70 mg/kg) in mice.2 1.Jiao, F., Kawakami, A., and Nakajima, T.Effects of different carbon sources on trichothecene production and Tri gene expression by Fusarium graminearum in liquid cultureFEMS Microbiol.Lett.285(2)212-219(2008) 2.Schiefer, H.B., Nicholson, S., Kasali, O.B., et al.Pathology of acute 3-acetyldeoxynivalenol toxicity in miceCan. J. Comp. Med.49(3)315-318(1985)

1. Lappaol F has antioxidant and antiaging properties, it may promote the C. elegans longevity and stress resistance through a JNK-1-DAF-16 cascade.
2. Lappaol F has potential chemosensitizing activity, it may be candidates for developing novel adju

D-DOPA is an enantiomer of the dopamine precursor L-DOPA . It can be converted to L-DOPAviasequential oxidation and transamination, which are mediated by D-amino acid oxidase (DAAO) and DOPA transaminase, respectively, in rat kidney homogenates.1It reduces the number of dopaminergic neurons in primary rat embryonic mesencephalic cultures in a concentration-dependent manner.2Intraventricular administration of D-DOPA (200 μg/animal) increases striatal dopamine levels in rats.3D-DOPA (20 mg/kg, i.p.) induces contralateral turns in a rat model of Parkinson's disease induced by 6-OHDA .4 1.Wu, M., Zhou, X.-J., Konno, R., et al.D-dopa is unidirectionally converted to L-dopa by D-amino acid oxidase, followed by dopa transaminaseClin. Exp. Pharmacol. Physiol.33(11)1042-1046(2006) 2.Ling, Z.-D., Pieri, S.C., and Carvey, P.M.Comparison of the neurotoxicity of dihydroxyphenylalanine stereoisomers in cultured dopamine neuronsClin. Neuropharmacol.19(4)360-365(1996) 3.Karoum, F., Freed, W.J., Chuang, L.-W., et al.D-dopa and L-dopa similarly elevate brain dopamine and produce turning behavior in ratsBrain Res.440(1)190-194(1988) 4.Moses, J., Siddiqui, A., and Silverman, P.B.Sodium benzoate differentially blocks circling induced by D-and L-dopa in the hemi-parkinsonian ratNeurosci. Lett.218(3)145-148(1996)

3'-Dephosphocoenzyme A is an intermediate in the biosynthesis of coenzyme A from pantothenic acid .1 It is phosphorylated by CoA synthase in humans to form CoA. 3'-Dephosphocoenzyme A can be used as a transcription initiator in the synthesis of CoA-RNA by in vitro transcription.2,3 References1. Leonardi, R., Zhang, Y.M., Rock, C.O., et al. Coenzyme A: Back in action. Prog. Lipid Res. 44(2-3), 125-153 (2005).2. Huang, F. Efficient incorporation of CoA, NAD and FAD into RNA by in vitro transcription. Nucleic Acids Res. 31(3), e8 (2003).3. Sapkota, K., and Huang, F. Efficient one-pot enzymatic synthesis of dephospho coenzyme A. Bioorg. Chem. 76, 23-27 (2018).

Elatoside F is a natural product for research related to life sciences. The catalog number is TN5998 and the CAS number is 144118-18-3.

rac-1,2-bis-Palmitoyl-3-chloropropanediol is a 3-monochloropropane-1,2-diol (3-MCPD) ester.1It has been found as a contaminant in edible olive oils, with the lowest and highest concentrations in extra virgin and olive pomace oils, respectively.rac-1,2-bis-Palmitoyl-3-chloropropanediol has also been found in cottonseed and palm oils, as well as in shortening.2It induces renal tubular necrosis and a decrease in spermatids, but no gross pathological changes, in mice.3 1.Hung, W.-C., Peng, G.-J., Tsai, W.-J., et al.Identification of 3-MCPD esters to verify the adulteration of extra virgin olive oilFood Addit. Contam. Part B Surveill.10(3)233-239(2017) 2.MacMahon, S., Begley, T.H., and Diachenko, G.W.Occurrence of 3-MCPD and glycidyl esters in edible oils in the United StatesFood Addit. Contam. Part A. Chem. Anal. Control Expo. Risk Assess.30(12)2081-2092(2013) 3.Liu, M., Gao, B.-Y., Qin, F., et al.Acute oral toxicity of 3-MCPD mono- and di-palmitic esters in Swiss mice and their cytotoxicity in NRK-52E rat kidney cellsFood Chem. Toxicol.50(10)3785-3791(2012)

T3SS-IN-3 (compound F-24) serves as an inhibitor specific to the type III secretion system (T3SS), significantly reducing the transcription of the hrpY gene while not impeding bacterial growth [1].

Quorum sensing is a regulatory system used by bacteria for controlling gene expression in response to increasing cell density.[1] This regulatory process manifests itself with a variety of phenotypes including biofilm formation and virulence factor production.[2] Coordinated gene expression is achieved by the production, release, and detection of small diffusible signal molecules called autoinducers. The N-acylated homoserine lactones (AHLs) comprise one such class of autoinducers, each of which generally consists of a fatty acid coupled with homoserine lactone (HSL). Regulation of bacterial quorum sensing signaling systems to inhibit pathogenesis represents a new approach to antimicrobial therapy in the treatment of infectious diseases.[3] AHLs vary in acyl group length (C4-C18), in the substitution of C3 (hydrogen, hydroxyl, or oxo group), and in the presence or absence of one or more carbon-carbon double bonds in the fatty acid chain. These differences confer signal specificity through the affinity of transcriptional regulators of the LuxR family.[4] C16-HSL is one of a number of lipophilic, long acyl side-chain bearing AHLs, including its monounsaturated analog C16:1-(L)-HSL, produced by the LuxI AHL synthase homolog SinI involved in quorum-sensing signaling in S. meliloti, a nitrogen-fixing bacterial symbiont of certain legumes.[5],[6] C16-HSL is the most abundant AHL produced by the proteobacterium R. capsulatus and activates genetic exchange between R. capsulatus cells.[7] N-Hexadecanoyl-L-homoserine lactone and other hydrophobic AHLs tend to localize in relatively lipophilic cellular environments of bacteria and cannot diffuse freely through the cell membrane. The long-chain N-acylhomoserine lactones may be exported from cells by efflux pumps or may be transported between communicating cells by way of extracellular outer membrane vesicles.[8],[9]Reference:[1]. González, J.E., and Keshavan, N.D. Messing with bacterial quorum sensing Microbiol. Mol. Biol. Rev. 70(4), 859-875 (2006).[2]. Gould, T.A., Herman, J., Krank, J., et al. Specificity of acyl-homoserine lactone syntheses examined by mass spectrometry Journal of Bacteriology 188(2), 773-783 (2006).[3]. Cegelski, L., Marshall, G.R., Eldridge, G.R., et al. The biology and future prospects of antivirulence therapies Nature Reviews.Microbiology 6(1), 17-27 (2008).[4]. Penalver, C.G.N., Morin, D., Cantet, F., et al. Methylobacterium extorquens AM1 produces a novel type of acyl-homoserine lactone with a double unsaturated side chain under methylotrophic growth conditions FEBS Letters 580, 561-567 (2006).[5]. Gao, M., Chen, H., Eberhard, A., et al. sinI- and expR-dependent quorum sensing in Sinorhizobium meliloti Journal of Bacteriology 187(23), 7931-7944 (2005).[6]. Teplitski, M., Eberhard, A., Gronquist, M.R., et al. Chemical identification of N-acyl homoserine lactone quorum-sensing signals produced by Sinorhizobium meliloti strains in defined medium Archives of Microbiology 180, 494-497 (2003).[7]. Schaefer, A.L., Taylor, T.A., Beatty, J.T., et al. Long-chain acyl-homoserine lactone quorum-sensing regulation of Rhodobacter capsulatus gene transfer agent production Journal of Bacteriology 184(23), 6515-6521 (2002).[8]. Pearson, J.P., Van Delden, C., and Iglewski, B.H. Active efflux and diffusion are involved in transport of Pseudomonas aeruginosa cell-to-cell signals Journal of Bacteriology 181(4), 1203-1210 (1999).[9]. Mashburn-Warren, L., and Whiteley, M. Special delivery: Vesicle trafficking in prokaryotes Molecular Microbiology 61(4), 839-846 (2006).

Ipomoeassin F, a selective and potent inhibitor of endoplasmic reticulum (ER) protein translocation, targets the Sec61 complex's pore-forming subunit (Sec61α) at the ER membrane. It inhibits the ER membrane translocation of SARS-CoV-2 proteins and blocks the ER translocation of secretory and type I transmembrane proteins (TMPs), without affecting type III TMPs [1] [2] [3].

HT-2 toxin-13C22is intended for use as an internal standard for the quantification of HT-2 toxin by GC- or LC-MS. HT-2 toxin is a type A trichothecene mycotoxin and an active, deacetylated metabolite of the trichothecene mycotoxin T-2 toxin .1,2Like T-2 toxin, HT-2 toxin inhibits protein synthesis and cell proliferation in plants.2HT-2 toxin also reduces viability of HepG2, A549, HEp-2, Caco-2, A-204, U937, Jurkat, and RPMI-8226 cancer cells with IC50values ranging from 3.1 to 23 ng/ml and human umbilical vein endothelial cells with an IC50value of 56.4 ng/ml.1It induces oxidative stress, DNA damage, and autophagy in, as well as halts the development of, cultured mouse embryos when used at a concentration of 10 nM.3HT-2 toxin has been found in cereal grains and food products.4,5 1.Nielsen, C., Casteel, M., Didier, A., et al.Trichothecene-induced cytotoxicity on human cell linesMycotoxin Res.25(2)77-84(2009) 2.Nathanail, A.V., Varga, E., Meng-Reiterer, J., et al.Metabolism of the fusarium mycotoxins T-2 toxin and HT-2 toxin in wheatJ. Agric. Food Chem.63(35)7862-7872(2015) 3.Zhang, L., Li, L., Xu, J., et al.HT-2 toxin exposure induces mitochondria dysfunction and DNA damage during mouse early embryo developmentReprod. Toxicol.85104-109(2019) 4.Langseth, W., and Rundberget, T.The occurrence of HT-2 toxin and other trichothecenes in Norwegian cerealsMycopathologia147(3)157-165(1999) 5.Al-Taher, F., Cappozzo, J., Zweigenbaum, J., et al.Detection and quantitation of mycotoxins in infant cereals in the U.S. market by LC-MS/MS using a stable isotope dilution assayFood Control72(Part A)27-35(2017)

Nemorosone is a polycyclic polyprenylated acylphloroglucinol (PPAP) originally isolated from C. rosea that has antiproliferative properties.1 Nemorosone inhibits growth of NB69, Kelly, SK-N-AS, and LAN-1 neuroblastoma cells (IC50s = 3.1-6.3 μM), including several drug-resistant clones, but not MRC-5 human embryonic fibroblasts (IC50 = >40 μM).2 It increases DNA fragmentation in LAN-1 cells in a dose-dependent manner, and decreases N-Myc protein levels and phosphorylation of ERK1/2 by MEK1/2. Nemorosone also inhibits growth of Capan-1, AsPC-1, and MIA-PaCa-2 pancreatic cancer cells (IC50s = 4.5-5.0 μM following a 72-hour treatment) but not human dermal and foreskin fibroblasts (IC50s = >35 μM).1 It induces apoptosis, abolishes the mitochondrial membrane potential, and increases cytosolic calcium concentration in pancreatic cancer cells in a dose-dependent manner. Nemorosone activates the caspase cascade in a dose-dependent manner and inhibits cell cycle progression, increasing the proportion of cells in the G0/G1 phase, in both neuroblastoma and pancreatic cancer cells.1,2 Nemorosone (50 mg/kg, i.p., per day) also reduces tumor growth in an MIA-PaCa-2 mouse xenograft model.3References1. Holtrup, F., Bauer, A., Fellenberg, K., et al. Microarray analysis of nemorosone-induced cytotoxic effects on pancreatic cancer cells reveals activation of the unfolded protein response (UPR). Br. J. Pharmacol. 162(5), 1045-1059 (2011).2. Díaz-Carballo, D., Malak, S., Bardenheuer, W., et al. Cytotoxic activity of nemorosone in neuroblastoma cells. J. Cell. Mol. Med. 12(6B), 2598-2608 (2008).3. Wold, R.J., Hilger, R.A., Hoheisel, J.D., et al. In vivo activity and pharmacokinetics of nemorosone on pancreatic cancer xenografts. PLoS One 8(9), e74555 (2013). Nemorosone is a polycyclic polyprenylated acylphloroglucinol (PPAP) originally isolated from C. rosea that has antiproliferative properties.1 Nemorosone inhibits growth of NB69, Kelly, SK-N-AS, and LAN-1 neuroblastoma cells (IC50s = 3.1-6.3 μM), including several drug-resistant clones, but not MRC-5 human embryonic fibroblasts (IC50 = >40 μM).2 It increases DNA fragmentation in LAN-1 cells in a dose-dependent manner, and decreases N-Myc protein levels and phosphorylation of ERK1/2 by MEK1/2. Nemorosone also inhibits growth of Capan-1, AsPC-1, and MIA-PaCa-2 pancreatic cancer cells (IC50s = 4.5-5.0 μM following a 72-hour treatment) but not human dermal and foreskin fibroblasts (IC50s = >35 μM).1 It induces apoptosis, abolishes the mitochondrial membrane potential, and increases cytosolic calcium concentration in pancreatic cancer cells in a dose-dependent manner. Nemorosone activates the caspase cascade in a dose-dependent manner and inhibits cell cycle progression, increasing the proportion of cells in the G0/G1 phase, in both neuroblastoma and pancreatic cancer cells.1,2 Nemorosone (50 mg/kg, i.p., per day) also reduces tumor growth in an MIA-PaCa-2 mouse xenograft model.3 References1. Holtrup, F., Bauer, A., Fellenberg, K., et al. Microarray analysis of nemorosone-induced cytotoxic effects on pancreatic cancer cells reveals activation of the unfolded protein response (UPR). Br. J. Pharmacol. 162(5), 1045-1059 (2011).2. Díaz-Carballo, D., Malak, S., Bardenheuer, W., et al. Cytotoxic activity of nemorosone in neuroblastoma cells. J. Cell. Mol. Med. 12(6B), 2598-2608 (2008).3. Wold, R.J., Hilger, R.A., Hoheisel, J.D., et al. In vivo activity and pharmacokinetics of nemorosone on pancreatic cancer xenografts. PLoS One 8(9), e74555 (2013).

6-Prenylindole is a bacterial metabolite that has been found in Streptomyces and has antifungal and antimalarial properties.1 It is active against A. brassicicola strain TP-F0423 and F. oxysporum f. sp. tulipae TU-4-2 (15 and 30 μg/disc in the paper disc assay), and also drug-resistant P. falciparum strain K1 (IC50 = 21 μg/ml).2 |1. Sasaki, T., Igarashi, Y., Ogawa, M., et al. Identification of 6-prenylindole as an antifungal metabolite of Streptomyces sp. TP-A0595 and synthesis and bioactivity of 6-substituted indoles. J. Antibiot. (Tokyo) 55(11), 1009-1012 (2002).|2. Nkunya, M.H., Makangara, J.J., and Jonker, S.A. Prenylindoles from Tanzanian Monodora and Isolona species. Nat. Prod. Res. 18(3), 253-258 (2004).

ATR-IN-20, a potent ATM/ATR inhibitor, showcases an IC50 value of 3 nM. It also exhibits inhibitory activity against mTOR with an IC50 of 18 nM, while maintaining selectivity over PI3Kα (100 nM), ATM (100 nM), and DNA-PK (662 nM). Additionally, ATR-IN-20 has an excellent pharmacokinetic profile with an oral bioavailability (F) of 30%, and demonstrates anticancer effects.

AMK is an active metabolite of the neurohormone melatonin .1,2,3,4It is formed from melatoninviathe metabolic intermediate AFMK that is then deformylated by catalase or formamidase.5,6AMK scavenges singlet oxygenin vitrowhen used at a concentration of 200 μM.1It inhibits the epinephrine- and arachidonic acid-induced production of prostaglandin E2and PGD2in ovine seminal vesicle microsomes in a concentration- and time-dependent manner, as well as LPS-induced increases in COX-2 levels in RAW 264.7 macrophages when used at a concentration of 500 μM.2,3AMK (20 mg/kg) decreases MPTP-induced increases in lipid peroxidation in the cytosol and mitochondria from substantia nigra and striatum in a mouse model of MPTP-induced Parkinson’s disease.4 1.Schaefer, M., and Hardeland, R.The melatonin metabolite N1-acetyl-5-methoxykynuramine is a potent singlet oxygen scavengerJ. Pineal Res.46(1)49-52(2009) 2.Kelly, R.W., Amato, F., and Seamark, R.F.N-acetyl-5-methoxy kynurenamine, a brain metabolite of melatonin, is a potent inhibitor of prostaglandin biosynthesisBiochem. Biophys. Res. Commun.121(1)372-379(1984) 3.Mayo, J.C., Sainz, R.M., Tan, D.-X., et al.Anti-inflammatory actions of melatonin and its metabolites, N1-acetyl-N2-formyl-5-methoxykynuramine (AFMK) and N1-acetyl-5-methoxykynuramine (AMK), in macrophagesJ. Neuroimmunol.165(1-2)139-149(2005) 4.Tapias, V., Escames, G., López, L.C., et al.Melatonin and its brain metabolite N1-acetyl-5-methoxykynuramine prevent mitochondrial nitric oxide synthase induction in parkinsonian miceJ. Neurosci. Res.87(13)3002-3010(2009) 5.Tan, D.-X., Manchester, L.C., Reiter, R.J., et al.Melatonin directly scavenges hydrogen peroxide: A potentially new metabolic pathway of melatonin biotransformationFree Radic. Biol. Med.29(11)1177-1185(2000) 6.Hirata, F., Hayaishi, O., Tokuyama, T., et al.In vitro and in vivo formation of two new metabolites of melatoninJ. Biol. Chem.249(4)1311-1313(1974)

VH032-cyclopropane-F is a VHL ligand based on VH032. It is able to utilize linkers to ligands of target proteins to yield PROTAC molecules such as PROTAC 1. PROTAC 1 is a partial degrader of SMARCA2 and SMARCA4.

Brevianamide F (Cyclo(L-Pro-L-Trp)), also known as cyclo-(L-Trp-L-Pro), belongs to a class of naturally occurring 2,5-diketopiperazines. Brevianamide F possess interesting breast cancer resistance protein inhibitory activity.

6,9-Dichloro-1,2,3,4-tetrahydroacridine is a synthetic intermediate in the synthesis of tacrine-based acetylcholinesterase (AChE) inhibitors.1It is also an intermediate in the synthesis of multifunctional tacrine hybrids that possess radical scavenging, amyloid-β aggregation inhibitory, and/or β-secretase 1 (BACE1) inhibitory activities in addition to their activity as AChE inhibitors.2,3 1.Recanatini, M., Cavalli, A., Belluti, F., et al.SAR of 9-amino-1,2,3,4-tetrahydroacridine-based acetylcholinesterase inhibitors: Synthesis, enzyme inhibitory activity, QSAR, and structure-based CoMFA of tacrine analoguesJ. Med. Chem.43(10)2007-2018(2000) 2.Digiacomo, M., Chen, Z., Wang, S., et al.Synthesis and pharmacological evaluation of multifunctional tacrine derivatives against several disease pathways of ADBioorg. Med. Chem. Lett.25(4)807-810(2015) 3.Li, S.Y., Jiang, N., Xie, S.S., et al.Design, synthesis and evaluation of novel tacrine-rhein hybrids as multifunctional agents for the treatment of Alzheimer's diseaseOrg. Biomol. Chem.12(5)801-814(2014)

6'-Sialyllactose consists of the monosaccharide N-acetylneuraminic acid linked to the galactosyl subunit of lactose at the 6 position. This connection is at the 3 position in the related compound, 3’-sialyllactose. Both are major milk oligosaccharides that avidly bind several viral strains, including strains of influenza, HIV-1, reovirus, and polyomavirus.[1],[2],[3],[4],[5],[6] These compounds can be used to differentiate and characterize the binding domains of viruses that recognize N-acetylneuraminic acid-capped cell surface receptors. They are also used as analytical reference standards for quantification in samples such as milk or colostrum. Reference：[1]. Duncan, P.I., Raymond, F., Fuerholz, A., et al. Sialic acid utilisation and synthesis in the neonatal rat revisited. PLoS One 4(12), 1-10 (2009).[2]. Sprenger, N., and Duncan, P.I. Sialic acid utilization. Adv.Nutr. 3(3), 392S-397S (2012).[3]. Iskarpatyoti, J.A., Morse, E.A., McClung, R.P., et al. Serotype-specific differences in inhibition of reovirus infectivity by human-milk glycans are determined by viral attachment protein σ1. Virology 433(2), 489-497 (2012).[4]. Neu, U., Khan, Z.M., Schuch, B., et al. Structures of B-lymphotropic polyomavirus VP1 in complex with oligosaccharide ligands. PLoS Pathogens 9(10), 1-10 (2013).[5]. Rosa Borges, A., Wieczorek, L., Johnson, B., et al. Multivalent dendrimeric compounds containing carbohydrates expressed on immune cells inhibit infection by primary isolates of HIV-1. Virology 408(1), 80-88 (2010).[6]. Wu, W., and Air, G.M. Binding of influenza viruses to sialic acids: Reassortant viruses with A/NWS/33 hemagglutinin bind to α2,8-linked sialic acid. Virology 325(2), 340-350 (2004).

SMER3 is an inhibitor of the Skp1-Cullin-F-box (SCF)(Met30) ubiquitin ligase, a member of the SCF E3-ligase family, which regulates diverse cellular processes including transcription, cell-cycle control and immune response.