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Results for "

a 121

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  • Inhibitors & Agonists
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A 121
T2640368072-84-4
A 121 is a non-polyene antifungal antibiotic. It is active against a number of filamentous fungi including some plant and human pathogens.
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AT-121 hydrochloride
T395292099681-71-5In house
AT-121 hydrochloride is a dual agonist of nociception and mu opioid receptor with Ki values of 3.67 and 16.49 nM, respectively.AT-121 hydrochloride is a safe, non-addictive, pain relieving compound with anti-injury and analgesic activity. AT-121 hydrochloride is a safe, non-addictive, pain relieving compound with anti-injury and analgesic activity.
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AT-121
T376102099681-31-7In house
AT-121 is a dual μ-opioid and neuropeptide receptor partial agonist (Kis 16.49 and 3.67 nM, respectively). It stimulates [35S]GTPγS binding to cell membranes expressing either μ-opioid receptors or neuropeptide receptors (EC50s of 19.6 and 34.7 nM, respectively.) AT-121 (0.003-0.03 mg kg) reduced capsaicin-induced thermal anisocoria in a dose-dependent manner, but did not increase scratching activity in rhesus monkeys. In rhesus monkey drug self-administration tests, AT-121 at doses of 0.3 to 10 μg kg per injection lacked reinforcing effects (a potential marker of abuse) and did not reduce the reinforcing effects of food pellets.AT-121 (0.01 or 0.03 mg kg) did not induce hyperalgesia, a marker of tolerance, in rhesus monkeys.AT-121 is a safe non-addictive pain reliever with anti-injury and analgesic effects.
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6-8weeks
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TargetMol | Inhibitor Sale
MB-07729
MB07729, MB 07729
T11955882755-95-5In house
MB-07729 is a potent non-competitive inhibitor of fructose-1,6-bisphosphate with IC50 values of 189, 121 and 31 nM in rat, monkey and human, respectively, for the study of diabetes.
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6-8 weeks
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TargetMol | Inhibitor Sale
PP121
T24151092788-83-4
PP-121 is a multi-targeted inhibitor of PDGFR (IC50: 2 nM), Hck (IC50: 8 nM), mTOR (IC50: 10 nM), VEGFR2(IC50: 12 nM), Src (IC50: 14 nM) and Abl (IC50: 18 nM) , also inhibits DNA-PK (IC50: 60 nM).
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TargetMol | Citations Cited
IGF-1R inhibitor-2
T385021116236-15-7
IGF-1R inhibitor-2 (example 121) is a compound that inhibits the insulin-like growth factor-1 receptor (IGF-1R), potentially reversing the transformed phenotype of tumor cells and increasing their susceptibility to apoptosis.
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AMK (hydrochloride)
T361761215711-91-3
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)
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NS2 (114-121), Influenza
NS2 (114-121), Influenza
T39292184763-32-4
NS2 (114-121), Influenza, is a fragment derived from the nonstructural protein 2 (NS2) of the influenza virus, serving as an epitope for influenza research and useful for studying CD8+ cytotoxic T lymphocyte (CTL) responses in antiviral immunity.
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RC 121
RC121,IM 4-28,RC-121,P-Cttlvc-T
T3427299660-13-6
RC 121 is a highly potent somatostatin (SRIF) analog.
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Malathion-d7
TMIJ-0456352438-94-9
Malathion-d7 is a deuterated compound of Malathion. Malathion has a CAS number of 121-75-5. Malathion is an organophosphate parasympathomimetic which binds irreversibly to cholinesterase, is an insecticide of relatively low human toxicity.
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20 days
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8(S),9(R)-EET
8S(9R)-Epoxyeicosatrienoic Acid, 8S(9R)-epoxy-all-cis-5,11,14-Eicosatrienoic Acid, 8S(9R)-epoxy-5(Z),11(Z),14(Z)-ETrE, 8S(9R)-EpETrE
T88387123931-39-5
8(S),9(R)-EET, an eicosanoid derived from Arachidonic acid (AA) through cytochrome P450 pathways, dilates canine epicardial arterioles in a concentration-dependent manner, exhibiting an EC 50 value of 121 nM.
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10-14 weeks
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Tpl2 Kinase Inhibitor (hydrochloride)
T35536
Tpl2 kinase inhibitor is an inhibitor of tumor progression locus 2 (Tpl2; IC50= 0.05 μM).1It is selective for Tpl2 over MEK, p38 MAPK, Src, MK2, and PKC (IC50s = >40, 180, >400, 110, and >400 μM, respectively). Tpl2 kinase inhibitor inhibits LPS-induced TNF-α production in isolated human monocytes and whole blood (IC50s = 0.7 and 8.5 μM, respectively). It enhances differentiation induced by calcitriol in HL-60 and U937 leukemia cells when used at a concentration of 5 μM.2Tpl2 kinase inhibitor (5 μM) inhibits the proliferation of KG-1a leukemia cells.3 1.Garvin, L.K., Green, N., Hu, Y., et al.Inhibition of Tpl2 kinase and TNF-α production with 1,7-naphthyridine-3-carbonitriles: Synthesis and structure-activity relationshipsBioor. Med. Chem. Lett.15(23)5288-5292(2005) 2.Wang, X., and Studzinski, G.P.Expression of MAP3 kinase COT1 is up-regulated by 1,25-dihydroxyvitamin D3 in parallel with activated c-jun during differentiation of human myeloid leukemia cellsJ. Steroid. Biochem. Mol. Biol.121(1-2)395-398(2010) 3.Wang, X., Gocek, E., Novik, V., et al.Inhibition of Cot1/Tlp2 oncogene in AML cells reduces ERK5 activation and up-regulates p27Kip1 concomitant with enhancement of differentiation and cell cycle arrest induced by silibinin and 1,25-dihydroxyvitamin D3Cell Cycle9(22)4542-4551(2010)
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Becocalcidiol
QRX-101, QRX101, DP-006, DP006, COL-121, COL121
T30310524067-21-8
Becocalcidiol(QRX-101, DP-006, COL-121) is a potential vitamin D analog for the treatment of psoriasis.
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Roccellic Acid
T3640929838-46-8
Roccellic acid is a lichen secondary metabolite that has been found in R. montagnei and has antibacterial and anticancer activities.1,2 It is active against the bacteria S. gordonii and P. gingivalis (MIC = 46.9 μg/ml for both).1 Roccellic acid (100 μg/ml) inhibits proliferation of MDA-MB-231, MCF-7, and DLD-1 cancer cells by 65.3, 75.8, and 87.9%, respectively.2 |1. Sweidan, A., Chollet-Krugler, M., Sauvager, A., et al. Antibacterial activities of natural lichen compounds against Streptococcus gordonii and Porphyromonas gingivalis. Fitoterapia 121, 164-169 (2017).|2. Mishra, T., Shukla, S., Meena, S., et al. Isolation and identification of cytotoxic compounds from a fruticose lichen Roccella montagnei, and it's in silico docking study against CDK-10. Rev. Bras. Farmacogn. 27(6), 724-728 (2017).
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Seribantumab
SAR-256212, SAR256212, MM-121, MM121
T767911334296-12-6
Seribantumab (MM 121) is a humanized monoclonal antibody targeting HER3, inhibiting NRG1-induced growth in MCF-7 cells and patient-derived breast and lung cancer cells harboring NRG1 fusions or amplifications. It also induces apoptosis in MDA-MB-175-VII and LUAD-0061AS3 cells.
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7-10 days
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Anticancer agent 121
T792032924532-47-6
Anticancer agent 121, a human lactate dehydrogenase A (hLDHA) inhibitor, exhibits potent anticancer activities, suitable for use in anticancer research [1].
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8-10 weeks
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D3R/MOR antagonist 2
T78779
Compound 121, a D3R MOR antagonist with K i values of 361 nM and 85.2 nM for D3R and MOR respectively, has the potential for analgesic effects through MOR partial agonism and may reduce opioid-misuse liability through D3R antagonism [1].
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Cephaeline dihydrochloride
(-)-Cephaeline dihydrochloride, NSC 32944
TQ01095853-29-2
(-)-Cephaeline (dihydrochloride) is an enantiomer of Cephaeline. Cephaeline is a selective CYP2D6 inhibitor (IC50: 121 μM).
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1-2 weeks
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SKA-121
T168911820708-73-3
SKA-121 is a selective KCa3.1 activator (EC50s: 109 nM and 4.4 μM for KCa3.1 and KCa2.3, respectively).
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7-10 days
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Ethyl-d5 Vanillin
TMID-00121335401-74-5
Ethyl-d5 Vanillin is a deuterated compound of Ethyl Vanillin. Ethyl Vanillin has a CAS number of 121-32-4. Ethylvanillin is a flavorant used in the production of chocolate. It is about three times as potent as vanillin.
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7-10 days
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CMS-121
CMS121
T149911353224-53-9
CMS-121, a quinolone derivative, is an orally active acetyl-CoA carboxylase 1 (ACC1) inhibitor. CMS-121 protects HT22 cells against ischemia and oxidative damage (EC50: 7 nM and 200 nM). CMS-121 shows strong neuroprotective, antioxidative, anti-inflammatory, and renoprotective activities.
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Reversin 121
T72921174630-04-7
Reversin 121, a P-glycoprotein inhibitor, enhances MDR1's ATPase activity and counteracts P-glycoprotein-mediated multidrug resistance, making it useful in cancer research.
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6-8 weeks
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4-Amino-6-chlorobenzene-1,3-disulfonamide
T65709121-30-2
4-Amino-6-chlorobenzene-1,3-disulfonamide is a useful organic compound for research related to life sciences. The catalog number is T65709 and the CAS number is 121-30-2.
    7-10 days
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    BCI-121
    T5322432529-82-3
    BCI-121 is a substrate-competitive SMYD3 inhibitor that inhibits the proliferation of the cancer cell.
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