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S-Methylisothiourea sulfate is a potent, selective and competitive inhibitor of inducible nitric oxide synthase (iNOS). S-Methylisothiourea sulfate exerts beneficial effects in rodent models of septic shock.IC50 & Target: iNOSIn Vitro: S-Methylisothiourea sulfate is a competitive inhibitor of iNOS activity at the L-arginine site.S-Methylisothiourea sulfate prevents the NO-mediated cytotoxic effect of LPS in cultured macrophages.S-Methylisothiourea sulfate […]
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S18-000003 is a potent, selective and orally active inhibitor of retinoic acid receptor-related orphan receptor-gamma-t (RORγt), with an IC50 of 10 μM). S18-000003 can be used for the research of psoriasis with low risk of thymic aberrations[2].In Vitro: S18-000003 inhibits human and mouse RORγt-dependent transactivation, with IC50s of 0.029 and 0.34 μM respectively in cell-based […]
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S2157, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2157 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2157 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2157 efficiently pass through the blood-brain barrier and can almost […]
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S3QEL-2, a suppressor of superoxide production from mitochondrial complex III, potently and selectively suppresses site IIIQo superoxide production (IC50=1.7 μM). S3QEL-2 does not affect oxidative phosphorylation, and normal electron flux. S3QEL-2 inhibits HIF-1α accumulation.In Vitro: S3QELs-2 protects against ROS-induced, JNK-mediated cell stress in pancreatic β-cells and S3QEL-2 strongly mitigates the oxidative stress-induced apoptosis that limits […]
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S516 (Compound 22) is an active metabolite of CKD-516 and a potent tubulin polymerization inhibitor with an IC50 of 4.29 μM. S516 has marked antitumor activity.IC50 & Target: IC50: 4.29 μM (tubulin polymerization)In Vitro: S516 has potent cytotoxicity with IC50s of 4.8 nM, 42.8 nM and 24.9 nM for HL-60, HCT116 and HCT15 cells, respectively.S516 […]
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S65487 (VOB560) sulfate, a potent and selective Bcl-2 inhibitor, is a prodrug of S55746. S65487 sulfate is also active on BCL-2 mutations, such as G101V and D103Y. S65487 sulfate has poor affinity with MCL-1, BFL-1 and BCL-XL. S65487 sulfate induces apoptosis and has anticaner activities[2].In Vitro: S65487 binds to the BH3 hydrophobic groove of BCL-2. […]
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S961 acetate is an high-affinity and selective insulin receptor (IR) antagonist with IC50s of 0.048, 0.027, and 630 nM for HIR-A, HIR-B, and human insulin-like growth factor I receptor (HIGF-IR) in SPA-assay, respectively.In Vitro: S961 also shows high-affinity to Rat IR and Pig IR with IC50s of 0.056 nM and 0.084 nM in PEG-assay, respectively.
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S961 TFA is an high-affinity and selective insulin receptor (IR) antagonist with IC50s of 0.048, 0.027, and 630 nM for HIR-A, HIR-B, and human insulin-like growth factor I receptor (HIGF-IR) in SPA-assay, respectively.In Vitro: S961 also shows high-affinity to Rat IR and Pig IR with IC50s of 0.056 nM and 0.084 nM in PEG-assay, respectively.
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VERU-111 (ABI-231) is a potent and orally active α and β tubulin inhibitor, which displays strong antiproliferative activity, with an average IC50 of 5.2 nM against panels of melanoma and prostate cancer cell lines. VERU-111 (ABI-231) suppresses tumor growth and metastatic phenotypes of cervical cancer cells via targeting HPV E6 and E7, and has potential […]
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Saccharin sodium hydrate is an orally active, non-caloric artificial sweeteners (NAS). Saccharin sodium hydrate has bacteriostatic and microbiome-modulating properties.In Vitro: In vitro, Saccharin sodium hydrate (0.5, 2.5, 5 mM) inhibits bacterial growth in a species-dependent manner.In Vivo: In vivo, Saccharin sodium hydrate (oral; 5 mg/kg; twice a day) intake reduces fecal bacterial load and alters […]
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Saccharin is an orally active, non-caloric artificial sweeteners (NAS). Saccharin has bacteriostatic and microbiome-modulating properties.In Vitro: In vitro, saccharin (0.5, 2.5, 5 mM) inhibits bacterial growth in a species-dependent manner.In Vivo: In vivo, saccharin (oral; 5 mg/kg; twice a day) intake reduces fecal bacterial load and alters microbiome composition, while the intestinal barrier is not […]
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Saccharopine (L-Saccharopine), a lysine degradation intermediate, is a mitochondrial toxin. Lysine and α-ketoglutarate are converted into Saccharopine by the lysine-ketoglutarate reductase. Saccharopine is then oxidized to α-aminoapidate semialdehyde and glutamate by the saccharopine dehydrogenase. Saccharopine impairs development by disrupting mitochondrial homeostasis[2].In Vitro:Saccharopine accumulation leads to mitochondrial damage and functional loss which is induced by saccharopine […]
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Sacituzumab govitecan (IMMU-132) is an antibody-drug conjugate (ADC) targeting Trop-2 for delivery of SN-38. Sacituzumab govitecan shows anticancer activity.In Vivo: Sacituzumab govitecan (IMMU-132) (17.5 mg/kg; twice weekly for 4 weeks) results in significant anti-tumor effects in mice bearing human gastric cancer xenografts.
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Sacituzumab is a humanized IgG1 monoclonal antibody for anti-trophoblast cell-surface antigen 2 (anti-Trop-2). Sacituzumab has?the?potential?for metastatic triple-negative breast cancer research.
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Sacubitril (AHU-377) is a potent and orally active NEP (neprilysin) inhibitor with an IC50 of 5 nM. Sacubitril is a component of the heart failure medicine LCZ696. Sacubitril can be used for the research of heart failure, hypertension and COVID-19[2].IC50 & Target: IC50: 5 nM (NEP)In Vitro: Sacubitril (AHU-377) is a single molecule that is […]
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Safranin (Safranin T) is an important and classical phenazinium dye. Safranin has been extensively used in the academic field as a spectroscopic probe and indicator. Safranin possesses a planar structure and cationic charge. It can readily intercalate into biological macromolecules, including DNA and proteins. Safranin can be used as a redox indicator in the determination […]
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SAG dihydrochloride is a potent Smoothened (Smo) receptor agonist (EC50=3 nM; Kd=59 nM). SAG dihydrochloride activates the Hedgehog signaling pathway and counteracts Cyclopamine (HY-17024) inhibition of Smo[2].IC50 & Target: EC50: 3 nM (Smo)In Vitro: SAG (0.1 nM-100 μM; 30 h) induces firefly luciferase expression in Shh-LIGHT2 cells with an EC50 of 3 nM and then […]
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SAH-d4 (SAH (S-Adenosylhomocysteine)-d4) is the deuterium labeled SAH. SAH (S-Adenosylhomocysteine) is an amino acid derivative and a modulartor in several metabolic pathways. It is an intermediate in the synthesis of cysteine and adenosine. SAH is an inhibitor for METTL3-METTL14 heterodimer complex (METTL3-14) with an IC50 of 0.9 μM[2].In Vitro: Stable heavy isotopes of hydrogen, carbon, […]
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SAHM1, a peptide mimetic of a dominant negative form of mastermind-like (MAML), inhibits canonical Notch transcription complex formation. SAHM1 can be used for the research of allergic airway inflammation in mice[2].IC50 & Target: Notch
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SAICAR is an intermediate of de novo purine nucleotide biosynthesis, activates pyruvate kinase isoform M2 (PKM2) in an isozyme-selective manner, with an EC50 of 0.3 mM. SAICAR stimulates PKM2 and promotes cancer cell survival in glucose-limited conditions[2].In Vitro: SAICAR accumulation induces nuclear localization of PKM2. PKM2-SAICAR phosphorylates and activates Erk1/2, which in turn sensitizes PKM2 […]
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Sakuranetin is a cherry flavonoid phytoalexin, shows strong antifungal activity. Sakuranetin has anti-inflammatory and antioxidative activities. Sakuranetin ameliorates LPS-induced acute lung injury[2].
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Salcaprozate sodium (SNAC), an oral absorption promoter, and has the potential as a delivery agent for oral forms of heparin and insulin. Salcaprozate sodium could increase passive transcellular permeation across small intestinal epithelia based on increased lipophilicity arising from non-covalent macromolecule complexation[2].In Vitro: SNAC (12.5-400 μg/mL; 24 h) has no toxicity to Caco-2 cells, and […]
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Salvianolic acid Y is a phenolic acid with the same planar structure as Salvianolic acid B. Salvianolic acid Y rescues cell injury by H2O2.In Vitro: Salvianolic acid Y has protection activityon hydrogen peroxide (H2O2)-induced cell lesion. The protection rates of Salvianolic acid Y is 54.2% in rat pheochromocytoma line PC12.
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Samatasvir (IDX71) is a potent, orally active NS5A inhibitor of HCV replication. Samatasvir is effective and selective against infectious HCV and replicons, with EC50s falling within a tight range of 2 to 24 pM in genotype 1 through 5 replicons.In Vitro: Samatasvir (IDX719) retains full activity in the presence of HIV and hepatitis B virus […]
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Samelisant (SUVN-G3031) is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant can be used for the research of sleep-related disorders.In Vitro: Samelisant displays inverse agonist […]
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SANT-1, a potent Smo antagonist, inhibits Hedgehog signaling. SANT-1 shows IC50s of 20 nM and 30 nM in Shh-LIGHT2 and SmoA1-LIGHT2 assay, respectively.IC50 & Target: IC50: 20 nM (Shh signaling), 30 nM (SmoA1)In Vitro: SANT-1 is a potent Smo antagonist, binds directly to Smo, and inhibits Hedgehog signaling, with IC50s of 20 nM and 30 […]
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Sapienic acid sodium is a fatty acid commonly found on the skin and in mucosa. Sapienic acid sodium has variable antimicrobial activities against Gram-positive and Gram-negative bacteria found on the skin and in the oral cavity. Sapienic acid sodium is active against Streptococcus sanguinis, Streptococcus mitis and Fusobacterium nucleatum with MBC values of 31.3 μg/mL, […]
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Saralasin ([Sar1,Ala8] Angiotensin II) TFA is an octapeptide analog of angiotensin II. Saralasin TFA is a competitive angiotensin II receptor antagonist with a Ki value of 0.32 nM for 74% of the binding sites, and has partial agonist activity as well. Saralasin TFA can be used for the research of renovascular hypertension, renin-dependent (angiotensinogenic) hypertension.IC50 […]
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Sarizotan (EMD 128130) is an orally active serotonin 5-HT1A receptor and dopamine receptor agonist. Sarizotan (EMD 128130) exhibits IC50 values of 6.5 nM (rat 5-HT1A), 0.1 nM (human 5-HT1A), 15.1 nM (rat D2), 17 nM (human D2), 6.8 nM (human D3) and 2.4 nM (human D4.2), respectively.In Vitro: Sarizotan concentration-dependently inhibits the electrically-induced contractions with […]
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Sarolaner (PF-6450567) is an orally active and broad-spectrum ectoparasiticide. Sarolaner is an isoxazoline compound which shows efficacy against fleas and ticks on dogs, with a LC80 value of 0.3 μg/mL against C. felis and a LC100 value of 0.003 μg/mL against O. turicata.IC50 & Target: LC80: 0.3μg/mL (C. felis)LC100: 0.003 μg/mL (O. turicata)IC50: 135 nM […]
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