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Results for "lc-2" in TargetMol Product Catalog
  • Isotope products
    38
    TargetMol | Activity
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    31
    TargetMol | inventory
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    3
    TargetMol | natural
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    TargetMol | Activity
LC 2 Epimer
T412152502156-12-7
Negative control for LC 2.
  • $1,440
35 days
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TargetMol | Inhibitor Sale
LC-2
T362562502156-03-6
LC-2 (PROTAC KRASG12C Degrader-LC-2) is a novel von Hippel-Lindau-based PROTAC degrader of endogenous KRAS G12C with a DC50 between 0.25 and 0.76 μM.LC-2 is a PROTAC that covalently binds KRAS G12C with MRTX849 and recruits the E3 ligase, VH, to induce a rapid and sustained degradation of KRAS G12C. LC-2 inhibits MAPK signaling in pure and heterozygous KRAS G12C cell lines.
  • $263
In Stock
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LC kinetic stabilizer-2
T722862495750-20-2
LC Kinetic Stabilizer-2 is a powerful stabilizer for amyloidogenic immunoglobulin light chains (LC), demonstrating significant efficacy with an EC50 of 24 nM.
  • $1,520
6-8 weeks
Size
QTY
2-deoxy-D-Glucose-13C6
T35683201612-55-7
2-deoxy-D-Glucose-13C6is intended for use as an internal standard for the quantification of 2-deoxy-D-glucose by GC- or LC-MS. 2-deoxy-D-Glucose is a glucose antimetabolite and an inhibitor of glycolysis.1,2It inhibits hexokinase, the enzyme that converts glucose to glucose-6-phosphate, as well as phosphoglucose isomerase, the enzyme that converts glucose-6-phosphate to fructose-6-phosphate.32-deoxy-D-Glucose (16 mM) induces apoptosis in SK-BR-3 cells, as well as inhibits the growth of 143B osteosarcoma cells cultured under hypoxic conditions when used at a concentration of 2 mg/ml.4,5In vivo, 2-deoxy-D-glucose (500 mg/kg) reduces tumor growth in 143B osteosarcoma and MV522 non-small cell lung cancer mouse xenograft models when used alone or in combination with doxorubicin or paclitaxel .6 1.Kang, H.T., and Hwang, E.S.2-Deoxyglucose: An anticancer and antiviral therapeutic, but not any more a low glucose mimeticLife Sci.78(12)1392-1399(2006) 2.Aft, R.L., Zhang, F.W., and Gius, D.Evaluation of 2-deoxy-D-glucose as a chemotherapeutic agent: Mechanism of cell deathBr. J. Cancer87(7)805-812(2002) 3.Ralser, M., Wamelink, M.M., Struys, E.A., et al.A catabolic block does not sufficiently explain how 2-deoxy-D-glucose inhibits cell growthProc. Natl. Acad. Sci. USA105(46)17807-17811(2008) 4.Liu, H., Savaraj, N., Priebe, W., et al.Hypoxia increases tumor cell sensitivity to glycolytic inhibitors: A strategy for solid tumor therapy (Model C)Biochem. Pharmacol.64(12)1745-1751(2002) 5.Zhang, X.D., Deslandes, E., Villedieu, M., et al.Effect of 2-deoxy-D-glucose on various malignant cell lines in vitroAnticancer Res.26(5A)3561-3566(2006) 6.Maschek, G., Savaraj, N., Priebe, W., et al.2-deoxy-D-glucose increases the efficacy of adriamycin and paclitaxel in human osteosarcoma and non-small cell lung cancers in vivoCancer Res.64(1)31-34(2004)
  • $88
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NHC-diphosphate triammonium
T36881
NHC-triphosphate triammonium is an active phosphorylated intracellular metabolite of β-d-N4-Hydroxycytidine (NHC) as a triphosphate form[1]. NHC-triphosphate triammonium is a weak alternative substrate for the viral polymerase and can be incorporated into HCV replicon RNA[1][2]. In an intracellular metabolism assay, HCV replicon cells are treated with 10 μM 3H-labeled NHC, and intracellular nucleotide levels are determined after 1, 2 and 8 hours incubations. NHC is rapidly convered into the mono-, di-, and triphosphate forms, and NHC-TP reaches up to 71.12 pM after 8 hours[1].NHC-triphosphate triammonium (NHC-TP) (5-40 μM) absence leads to full-length polymerization products, it can be a weak alternative substrate. In addition, incorporation of NHC-TP instead of CTP increases the molecular weight of the polymerization product by 16 (one extra oxygen) for each event and an obvious electrophoretic shift is observed in cell-free HCV NS5B polymerization reactions[1].Huh-7 cells are incubated with (10-50 μM; 4 h) NHC or a McGuigan phosphoramidate prodrug of NHC. Intracellular levels of the parental compounds and phosphorylated metabolites are measured using LC-MS/MS. Small amounts of NHC-monophosphate (MP) and NHC-diphosphate (DP) can be observed, while NHC-triphosphate triammonium remains the most abundant metabolite[2].NHC-triphosphate triammonium (NHC-TP) metabolite may directly target the viral polymerase and behave as a nonobligate chain terminator. It plays a prominent role in inhibiting early negative-strand RNA synthesis, either through chain termination or mutagenesis, which may in turn interfere with correct replicase complex formation. [1]. Stuyver LJ,et al. Ribonucleoside analogue that blocks replication of bovine viral diarrhea and hepatitis C viruses in culture.Antimicrob Agents Chemother. 2003 Jan;47(1):244-54. [2]. Maryam Ehteshami, et al. Characterization of β-d- N4-Hydroxycytidine as a Novel Inhibitor of Chikungunya Virus.
  • $315
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O-Des[2-aminoethyl]-O-carboxymethyl dehydroamlodipine
T35602113994-45-9
O-Des[2-aminoethyl]-O-carboxymethyl dehydroamlodipine is a major metabolite of the calcium channel inhibitor amlodipine .1 1.Taguchi, R., Naito, T., Sato, H., et al.Validated LC-MS/MS method for the simultaneous determination of amlodipine and its major metabolites in human plasma of hypertensive patientsTher. Drug Monit.39(6)625-631(2017)
  • $296
35 days
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QTY
TargetMol | Inhibitor Sale
Palonosetron N-oxide
T37246813425-83-1
Palonosetron N-oxide is a metabolite of the serotonin (5-HT) receptor subtype 5-HT3antagonist palonosetron .1It is also a potential impurity in palonosetron preparations.2Palonosetron N-oxide is a degradation product formed by exposure to oxidative stress. 1.Stoltz, R.A., Cyong, J.-C., Shah, A., et al.Pharmacokinetic and safety evaluation of palonosetron, a 5-hydroxytryptamine-3 receptor antagonist, in U.S. and Japanese healthy subjectsJ. Clin. Pharmacol.44(5)520-531(2004) 2.Vishnu Murthy, M., Srinivas, K., Kumar, R., et al.Development and validation of a stability-indicating LC method for determining palonosetron hydrochloride, its related compounds and degradation products using naphthalethyl stationary phaseJ. Pharm. Biomed. Anal.56(2)429-435(2011)
  • $243
35 days
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CAY10404
T8656340267-36-9
CAY10404 (3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-T) is a potent and highly selective inhibitor of COX-2 and COX-1. It is also a potent inhibitor of PKB/Akt and MAPK signalling pathways and induces apoptosis in NSC-LC cells, with analgesic, anti-inflammatory and anti-cancer activities.
  • $34
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Lysophosphatidylcholine 18:2
T3679122252-07-9
1-Linoleoyl-2-hydroxy-sn-glycero-3-PC (LGPC) is a lysophospholipid containing linoleic acid at thesn-1 position that has been found in mouse heart, lung, liver, spleen, kidney, plasma, and serum.1Serum levels of LGPC decrease with increasing insulin resistance and dysglycemia in humans.2 1.Okudaira, M., Inoue, A., Shuto, A., et al.Separation and quantification of 2-acyl-1-lysophospholipids and 1-acyl-2-lysophospholipids in biological samples by LC-MS/MSJ. Lipid Res.55(10)2178-2192(2014) 2.Gall, W.E., Beebe, K., Lawton, K.A., et al.α-Hydroxybutyrate is an early biomarker of insulin resistance and glucose intolerance in a nondiabetic populationPLoS One5(5)e10883(2010)
  • $293
35 days
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Ribavirin-13C5
T382971646818-35-0
Ribavirin-13C5is intended for use as an internal standard for the quantification of ribavirin by GC- or LC-MS. Ribavirin is an antiviral guanosine nucleoside analog.1,2Upon entry into cells, ribavirin is metabolized to an active triphosphate form that induces viral RNA chain termination and inhibits viral polymerases. It reduces replication in a panel of seven RNA and four DNA viruses in Vero cells (EC50s = 2-95 μg/ml).3Ribavirin also reduces replication of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) in Vero cells (EC50= 109.5 μM).4Aerosol administration of ribavirin (30 mg/kg) reduces mortality in a mouse model of influenza A infection.5Formulations containing ribavirin have been used in the treatment of respiratory syncytial virus (RSV), hepatitis C virus (HCV), and viral hemorrhagic fevers. 1.Gilbert, B.E., and Knight, V.Biochemistry and clinical applications of ribavirinAntimicrob. Agents Chemother.30(2)201-205(1986) 2.Gordon, C.J., Tchesnokov, E.P., Woolner, E., et al.Remdesivir is a direct-acting antiviral that inhibits RNA-dependent RNA polymerase from severe acute respiratory syndrome coronavirus 2 with high potencyJ. Biol. Chem.295(20)6785-6797(2020) 3.Kirsi, J.J., North, J.A., McKernan, P.A., et al.Broad-spectrum antiviral activity of 2-β-D-ribofuranosylselenazole-4-carboxamide, a new antiviral agentAntimicrob. Agents Chemother.24(3)353-361(1983) 4.Wang, M., Cao, R., Zhang, L., et al.Remdesivir and chloroquine effectively inhibit the recently emerged novel coronavirus (2019-nCoV) in vitroCell Res.30(3)269-271(2020) 5.Wilson, S.Z., Knight, V., Wyde, P.R., et al.Amantadine and ribavirin aerosol treatment of influenza A and B infection in miceAntimicrob. Agents Chemother.17(4)642-648(1980)
  • $786
35 days
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QTY
TargetMol | Inhibitor Sale
WF-47-JS03
T63573
WF-47-JS03 is a selective and potent inhibitor of RET kinase that crosses the blood-brain barrier and is more than 500-fold more selective for the kinase insertion domain receptor (KDR).WF-47-JS03 acts on Ba/F3 cells transfected with KIF5B-RET (IC50: 1.7 nM) and LC-2/ad lung cancer cells transfected with CCDC6-RET (IC50: 5.3 nM). cells (IC50: 5.3 nM).
  • $1,400
10-14 weeks
Size
QTY
Palmitic acid-1-13C
T3578957677-53-9
Palmitic acid-13C is intended for use as an internal standard for the quantification of palmitic acid by GC- or LC-MS. Palmitic acid is a 16-carbon saturated fatty acid. It comprises approximately 25% of human total plasma lipids.1 It increases protein levels of COX-2 in RAW 264.7 cells when used at a concentration of 75 μM.2 Palmitic acid is involved in the acylation of proteins to anchor membrane-bound proteins to the lipid bilayer.2,3,4,5,6 |1. Santos, M.J., López-Jurado, M., Llopis, J., et al. Influence of dietary supplementation with fish oil on plasma fatty acid composition in coronary heart disease patients. Ann. Nutr. Metab. 39(1), 52-62 (1995).|2. Lee, J.Y., Sohn, K.H., Rhee, S.H., et al. Saturated fatty acids, but not unsaturated fatty acids, induced the expression of cyclooxygenase-2 mediated through toll-like receptor 4. J. Biol. Chem. 276(20), 16683-16689 (2001).|3. Dietzen, D.J., Hastings, W.R., and Lublin, D.M. Caveolin is palmitoylated on multiple cysteine residues. Palmitoylation is not necessary for localization of caveolin to caveolae. J. Biol. Chem. 270(12), 6838-6842 (1995).|4. Robinson, L.J., and Michel, T. Mutagenesis of palmitoylation sites in endothelial nitric oxide synthase identifies a novel motif for dual acylation and subcellular targeting. Proc. Nat. Acad. Sci. USA 92(25), 11776-11780 (1995).|5. Topinka, J.R., and Bredt, D.S. N-terminal palmitoylation of PSD-95 regulates association with cell membranes and interaction with K+ channel Kv1.4. Neuron 20(1), 125-134 (1998).|6. Miggin, S.M., Lawler, O.A., and Kinsella, B.T. Palmitoylation of the human prostacyclin receptor. Functional implications of palmitoylation and isoprenylation. J. Biol. Chem. 278(9), 6947-6958 (2003).
  • $36
7-10 days
Size
QTY
MRTX849 ethoxypropanoic acid
T401902561529-98-2
MRTX849 ethoxypropanoic acid is a compound that contains a ligand for KRAS G12C and a PROTAC linker. It is commonly employed in the synthesis of PROTAC LC-2, which is a highly effective and innovative PROTAC. LC-2 has been proven to degrade endogenous KRAS G12C with remarkable potency, exhibiting DC50 values ranging from 0.25 to 0.76 μM.
  • $1,520
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Palmitic acid-13C
T35791287100-87-2
Palmitic acid-13C is intended for use as an internal standard for the quantification of palmitic acid by GC- or LC-MS. Palmitic acid-13C contains 13C at the C2 position and has been used in the study of free fatty acid incorporation into phospholipid fatty acids in soil microbes.1 Palmitic acid is a 16-carbon saturated fatty acid. It comprises approximately 25% of human total plasma lipids.2 It increases protein levels of COX-2 in RAW 264.7 cells when used at a concentration of 75 μM.3 Palmitic acid is involved in the acylation of proteins to anchor membrane-bound proteins to the lipid bilayer.3,4,5,6,7 |1. Dippold, M.A., and Kuzyakov, Y. Direct incorporation of fatty acids into microbial phospholipids in soils: Position-specific labeling tells the story. Geochim. Cosmochim. Acta 174(1), 211-221 (2016).|2. Santos, M.J., López-Jurado, M., Llopis, J., et al. Influence of dietary supplementation with fish oil on plasma fatty acid composition in coronary heart disease patients. Ann. Nutr. Metab. 39(1), 52-62 (1995).|3. Lee, J.Y., Sohn, K.H., Rhee, S.H., et al. Saturated fatty acids, but not unsaturated fatty acids, induced the expression of cyclooxygenase-2 mediated through toll-like receptor 4. J. Biol. Chem. 276(20), 16683-16689 (2001).|4. Dietzen, D.J., Hastings, W.R., and Lublin, D.M. Caveolin is palmitoylated on multiple cysteine residues. Palmitoylation is not necessary for localization of caveolin to caveolae. J. Biol. Chem. 270(12), 6838-6842 (1995).|5. Robinson, L.J., and Michel, T. Mutagenesis of palmitoylation sites in endothelial nitric oxide synthase identifies a novel motif for dual acylation and subcellular targeting. Proc. Nat. Acad. Sci. USA 92(25), 11776-11780 (1995).|6. Topinka, J.R., and Bredt, D.S. N-terminal palmitoylation of PSD-95 regulates association with cell membranes and interaction with K+ channel Kv1.4. Neuron 20(1), 125-134 (1998).|7. Miggin, S.M., Lawler, O.A., and Kinsella, B.T. Palmitoylation of the human prostacyclin receptor. Functional implications of palmitoylation and isoprenylation. J. Biol. Chem. 278(9), 6947-6958 (2003).
    7-10 days
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    1-1(Z)-Hexadecenyl-2-Palmitoyl-d9-sn-glycero-3-PE
    T850832738509-20-9
    1-1(Z)-Hexadecenyl-2-palmitoyl-d9-sn-glycero-3-PE serves as an internal standard for quantitating 1-1(Z)-hexadecenyl-2-palmitoyl-sn-glycero-3-PE, which is a plasmalogen incorporating 1(Z)-hexadecanoic acid and palmitic acid at the sn-1 and sn-2 positions respectively, in analyses performed using GC- or LC-MS.
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    1,2-Dioleoyl-3-Lauroyl-rac-glycerol-13C3
    T850762692624-36-3
    1,2-Dioleoyl-3-lauroyl-rac-glycerol-13C3 is designed as an internal standard for the quantification of 1,2-dioleoyl-3-lauroyl-rac-glycerol, employable with GC- or LC-MS techniques. This compound is a type of triacylglycerol featuring oleic acid at the sn-1 and sn-2 positions, and lauric acid at the sn-3 position, and has been identified in date seed oil and the fat body of male B. lapidarius bumblebees.
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    DL-Tyrosine-13C9,15N
    T36384202407-26-9
    L-Tyrosine-13C9,15N is intended for use as an internal standard for the quantification of L-tyrosine by GC- or LC-MS. L-Tyrosine is a non-essential amino acid.1It is produced by hydroxylation of phenylalanine by phenylalanine hydroxylase but can also be obtained from dietary sources or degradation of endogenous proteins, resulting in L-tyrosine release.1,2L-Tyrosine is a precursor in the biosynthesis of catecholamine neurotransmitters, melanins, and thyroid hormones.3Plasma, skeletal muscle, and erythrocyte levels of L-tyrosine are decreased in patients with chronic kidney disease.1 1.Kopple, J.D.Phenylalanine and tyrosine metabolism in chronic kidney failureJ. Nutr.137(6 Suppl 1)1586S-1590S(2007) 2.Webster, D., and Wildgoose, J.Tyrosine supplementation for phenylketonuriaCochrane DB Syst. Rev.2013(6)CD001507(2013) 3.Slominski, A., and Paus, R.Towards defining receptors for L-tyrosine and L-DOPAMol. Cell Endocrinol.99(2)C7-C11(1994)
      35 days
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      Pal-KTTKS (acetate)
      T36929
      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).
      • $383
      35 days
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      RET-IN-11
      T63583
      RET-IN-11 is a potent and selective RET inhibitor that acts on RET (IC50: 6.20 nM) and RETV804M (IC50: 18.68 nM).RET-IN-11 induces apoptosis.RET-IN-11 exhibits anti-proliferative and migratory effects in LC-2/ad cells. RET-IN-11 showed anti-proliferative and migratory effects in LC-2/ad cells.
      • $1,520
      10-14 weeks
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      QTY
      1,2,3-Tripentadecanoyl Glycerol
      T851157370-46-9
      1,2,3-Tripentadecanoyl glycerol, a triacylglycerol featuring pentadecanoic acid at the sn-1, sn-2, and sn-3 positions, occurs in various grapes. It serves as a standard in LC-MS for detecting triacylglycerols in human plasma.
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      1-Palmitoyl-d9-2-Palmitoyl-sn-glycerol
      T852201872379-48-0
      1-Palmitoyl-d9-2-palmitoyl-sn-glycerol serves as an internal standard for quantifying 1,2-dipalmitoyl-sn-glycerol using GC or LC-MS techniques. This diacylglycerol, featuring palmitic acid at both the sn-1 and sn-2 positions, stimulates protein kinase C (PKC) activity by 15% at a 25 μM concentration. Additionally, 1,2-dipalmitoyl-sn-glycerol encourages rapid growth in Frankia, a genus of Gram-positive bacteria.
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      1-Arachidonoyl-d8-rac-glycerol
      T852862692624-29-4
      1-Arachidonoyl-d8-rac-glycerol (1-AG-d8) serves as an internal standard for 1-AG quantification via GC or LC-MS. As a weak CB1 receptor agonist, 1-AG exhibits potential pharmacological effects. Notably, 1-AG, an isomer of 2-AG, is more stable, avoiding the rapid in vitro and in vivo isomerization that diminishes 2-AG's cannabinergic efficacy due to conversion to 1-AG (also known as 1(3)-AG), a common impurity in synthetic 2-AG formulations.
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      MRTX849 acid
      T401892561529-96-0
      MRTX849 acid, a derivative of MRTX849, is employed in the synthesis of PROTAC LC-2. LC-2, a potent and pioneering PROTAC, exhibits the ability to efficiently degrade endogenous KRAS G12C with DC50 values ranging between 0.25 and 0.76 μM.
      • $1,520
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      1-Palmitoyl-d9-2-Palmitoyl-sn-glycero-3-PE
      T850892747990-85-6
      1-Palmitoyl-d9-2-palmitoyl-sn-glycero-3-PE serves as an internal standard for the quantification of 1,2-dipalmitoyl-sn-glycero-3-PE (1,2-DPPE) using GC- or LC-MS. 1,2-DPPE, a prevalent PE (phospholipid), contains C16:0 fatty acids at the sn-1 and sn-2 positions and is essential in the inner plasma membrane leaflet. This compound forms a condensed lipid monolayer with cholesterol through tight hydrogen bonding between 1,2-DPPE headgroups, enhancing membrane fluidity to support transport and signaling.
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      Dehydrocorydaline
      T5S235830045-16-0
      1. Dehydrocorydaline (13-Methylpalmatine) exerts anti-metastatic potential via suppression of MMPs and Bcl-2 signaling in NSC-LC cells. 2. Dehydrocorydaline stimulates p38 MAPK activation, which can enhance heterodimerization of MyoD and E proteins, thus resulting in MyoD activation and myoblast differentiation. 3. Dehydrocorydaline shows antiplatelet effects, it inhibits thrombin-induced platelet aggregation in a low dose ( IC50= 34.914 ug/mL). 4. Dehydrocorydaline has anti-inflammatory and antinociceptive effects. 5. Dehydrocorydaline inhibits MCF-7 cell proliferation by inducing apoptosis mediated by regulating Bax/Bcl-2, activating caspases as well as cleaving PARP.
      • $52
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      eIF4A3-IN-18
      T729441402931-84-3
      eIF4A3-IN-18, a silvestrol analogue, disrupts the formation of the eIF4F translation complex, exhibiting EC 50 values of 0.8, 35, and 2 nM for myc-LUC, tub-LUC, and the growth inhibition of MBA-MB-231 cells, respectively. Additionally, it demonstrates cytotoxicity towards RMPI-8226 cells with an LC 50 of 0.06 nM. This compound is utilized in researching human cancer pathogenesis [1].
      • $2,120
      8-10 weeks
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      N-desmethyl Rosuvastatin (sodium salt hydrate)
      T35718
      N-desmethyl Rosuvastatin is an active metabolite of the HMG-CoA reductase inhibitor rosuvastatin .1,2N-desmethyl Rosuvastatin is formed when rosuvastatin undergoes demethylation, primarily by the cytochrome P450 (CYP) isoform CYP2C9 and to a lesser extent by CYP2C19 and CYP3A4.1 1.Macwan, J.S., Ionita, I.A., and Akhlaghi, F.A simple assay for the simultaneous determination of rosuvastatin acid, rosuvastatin-5S-lactone, and N-desmethyl rosuvastatin in human plasma using liquid chromatography-tandem mass spectrometry (LC-MS/MS)Anal. Bioanal. Chem.402(3)1217-1227(2012) 2.Bai, X., Wang, X.P., He, G.D., et al.Simultaneous determination of rosuvastatin, rosuvastatin-5 S-lactone, and N-desmethyl rosuvastatin in human plasma by UPLC-MS/MS and its application to clinical studyDrug Res. (Stuttg.)68(6)328-334(2018)
      • $725
      35 days
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      Olsalazine-13C6
      T36660
      Olsalazine-13C6is intended for use as an internal standard for the quantification of olsalazine by GC- or LC-MS. Olsalazine is an orally bioavailable prodrug form of the anti-inflammatory agent 5-aminosalicylic acid that is cleaved by bacterial azo reductases in the gut to generate active 5-ASA.1In vitro, olsalazine increases ion transport in isolated rabbit distal ileum when applied to the luminal side (ED50= 0.3 mM) and stimulates fluid transport in rat jejunum when used at a concentration of 5 mM.2,3Olsalazine (150 mg/kg for 8 days) improves stool consistency and decreases occult and gross bleeding as well as myeloperoxidase (MPO) activity and leukotriene B4levels in colon tissue in a mouse model of acute colitis induced by dextran sulfate .4Olsalazine also inhibits bovine xanthine oxidasein vitro(IC50= 3.4 mg/L) and lowers serum uric acid levels in a mouse model of hyperuricemia induced by oxonic acid when administered at a dose of 20 mg/kg.5Formulations containing olsalazine have been used in the treatment of inflammatory bowel disease (IBD) and ulcerative colitis. 1.Nugent, S.G., Kumar, D., Rampton, D.S., et al.Intestinal luminal pH in inflammatory bowel disease: Possible determinants and implications for therapy with aminosalicylates and other drugsGut48(4)571-577(2001) 2.Pamukcu, R., Hanauer, S.B., and Chang, E.B.Effect of disodium azodisalicylate on electrolyte transport in rabbit ileum and colon in vitro. Comparison with sulfasalazine and 5-aminosalicylic acidGastroenterology95(4)975-981(1988) 3.Mohsen, A.Q.M., Mulvey, D., Priddle, J.D., et al.Effects of olsalazine in the jejunum of the ratGut28(3)346-352(1987) 4.Murthy, S., Murthy, N.S., Coppola, D., et al.The efficacy of BAY y 1015 in dextran sulfate model of mouse colitisInflamm. Res.46(6)224-233(1997) 5.Niu, Y., Li, H., Gao, L., et al.Old drug, new indication: Olsalazine sodium reduced serum uric acid levels in mice via inhibiting xanthine oxidoreductase activityJ. Pharmacol. Sci.135(3)114-120(2017)
      • $1,590
      35 days
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      Adenosylhomocysteinase
      T747649025-54-1
      Adenosylhomocysteinase (SAHH; AHCY), a highly conserved enzyme, reversibly catalyzes S-adenosylhomocysteine (SAH) into adenosine and L-homocysteine. Its level in serum exosomes serves as a prognostic biomarker for HBV-LC patients [1] [2].
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      Tectochrysin
      T3S1775520-28-5
      1. Tectochrysin (Techtochrysine) has antioxidant effect. 2. Tectochrysin is promising inhibitors for the reversal of ABCG2-mediated drug transport. 3. Tectochrysin leads to apoptotic cell death in NSC-LC cells through activation of DR3 and Fas expression via inhibition of STAT3 phosphorylation.
      • $48
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      1-Palmitoyl-d9-2-hydroxy-sn-glycero-3-PA
      T849952830282-77-2
      1-Palmitoyl-d9-2-hydroxy-sn-glycero-3-PA (1-palmitoyl-d9LPA) serves as an internal standard for the quantification of 1-palmitoyl LPA using GC- or LC-MS. This compound, an analog of LPA with palmitic acid at the sn-1 position, activates reporter gene expression in PC12 cells fitted with human lysophosphatidic acid receptor 4 (LPA4) at 0.01 to 10 µM concentrations. Additionally, 1-palmitoyl LPA prompts aggregation in isolated human platelets within the 12-300 µM range, a process reversible by prostaglandin E1 (PGE1), theophylline, or EDTA. It also interacts with calcium and magnesium to boost the efficacy of ampicillin, piperacillin, and ceftazidime against P. aeruginosa strains from cystic fibrosis patients.
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