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Sepimostat (FUT-187 free base) exhibits neuroprotective activity via NR2B N-methyl-D-aspartate receptor antagonism at the Ifenprodil-binding site of the NR2B subunit. Sepimostat inhibits the Ifenprodil binding with a Ki value of 27.7?μM.In Vivo: Sepimostat (1 to 100 nmol/eye, intravitreal injection) exhibits significant neuroprotective effect.
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Seselin is an anticancer, antinociceptive, anti-inflammatory and antifungal agent. Seselin is orally active[2].In Vitro:Seselin shows cytotoxic effects with ED50 of 8.66 and 9.94 μg/mL against P-388 and HT-29 cells, respectively.Seselin (5-20 μM; 0.5-24 h) inhibits cytokine output from macrophages stimulated by LPS and IFN-γ dose- and time-dependently.Seselin (5-20 μM; 12 h) inhibits the expression of […]
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SETDB1-TTD-IN-1 is a potent, selective and endogenous binder competitive inhibitor of SET domain bifurcated protein 1 tandem tudor domain (SETDB1-TTD), with a Kd of 88 nM. SETDB1-TTD-IN-1 can be used for the research of biological functions and disease associations of SETDB1-TTD.IC50 & Target: Kd: 88 nM (SETDB1-TTD)In Vitro: SETDB1-TTD-IN-1 shows some activity for 53BP1 and […]
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Sevelamer hydrochloride is an orally active and phosphate binding agent used for research of hyperphosphatemia with chronic kidney disease. Sevelamer hydrochloride consists of polyallylamine that is crosslinked with epichlorohydrin[2].In Vitro:Sevelamer hydrochloride (15 mg/mL; pH=6 or 8) decreases serum levels of gut-derived uremic toxins (such as IAA) or limits the elevation of gut-derived uremic toxins (initial […]
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Seviteronel R enantiomer (VT-464 R enantiomer) is the R enantiomer of Seviteronel (VT-464), which is a potent CYP17 lyase inhibitor(h-Lyase IC50=69 nM); Seviteronel (VT-464) R enantiomer’s activity is unknown.
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SG3199-Val-Ala-PAB is an intermediate of Tesirine synthesis. Tesirine is a drug-linker conjugate for ADC which can be used for the research of several cancers.In Vitro: SG3199-Val-Ala-PAB is an intermediate in in the synthesis of Tesirine, an antibody-drug conjugate pyrrolobenzodiazepine dimer payload.
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SGC-SMARCA-BRDVIII is a potent and selective inhibitor of SMARCA2/4 and PB1(5), with Kds of 35 nM, 36 nM, and 13 nM, respectively. SGC-SMARCA-BRDVIII also inhibits PB1(2) and PB1(3), with Kds of 3.7 and 2.0 μM, respectively. SGC-SMARCA-BRDVIII can block adipogenesis of 3T3-L1 murine fibroblasts[2].IC50 & Target: Kd: 35 nM (SMARCA2), 36 nM (SMARCA4), 13 nM […]
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SGI-1776 free base is an inhibitor of Pim kinases, with IC50s of 7 nM, 363 nM, and 69 nM for Pim-1, -2 and -3, respectively.IC50 & Target:Ki: 7 nM (Pim-1), 363 nM (Pim-2), 69 nM (Pim-3)In Vitro:SGI-1776 free base (2.5, 5 μM) inhibits Pim-1 protein expression and Pim-1 kinase activity in SACC cells. SGI-1776 free […]
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SGK1-IN-1 is a highly active and selective inhibitor of SGK-1, with an IC50 of 1 nM.IC50 & Target: IC50: 1 nM (SGK-1)[2].In Vitro: SGK1-IN-1 (14n) shows an acceptable SGK isoform selectivity with a good activity on hSGK2 and a moderate activity on the hSGK3, with IC50s of 1, 41 nM at 10 μM and 50 […]
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Shanzhiside methy lester is isolated from lamiophlomis rotata. Shanzhiside methyl ester is a small molecule glucagon-like peptide-1 (GLP-1) receptor agonist and has the ability to induce anti-allodynic tolerance.IC50 & Target:IC50: GLP-1 receptorIn Vivo: Shanzhiside methyl ester exerts dose-dependent and long-lasting (>4 h) anti-allodynic effects in spinal nerve injury-induced neuropathic rats, with a maximal inhibition of […]
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Shield-1 (Shld1) is a specific, cell-permeant and high-affinity ligand of FK506-binding protein-12 (FKBP), and reverses the instability by binding to mutated FKBP (mtFKBP), allowing conditional expression of mtFKBP-fused proteins. Shield-1 can stabilize proteins tagged with a mutated FKBP12-derived destabilization domain (DD)[2].In Vitro: Shield-1 (0.1 nM-1 μM) responses characterization of destabilizing domains.Shield-1 (1 μM; 24 h) […]
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SHP2-IN-6 hydrochloride is a potent SHP2 inhibitor with an IC50 of 25.8 nM. SHP2-IN-6 hydrochloride is extracted from patent WO2017211303A1, compound 7.In Vitro: SHP2-IN-6 inhibits the proliferation of KYSE-520 cells with an IC50 of 2.17 μM.
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SIA Crosslinker is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).In Vitro: ADCs are comprised of an antibody to which is attached an ADC cytotoxin through an ADC linker.
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Sialyl-Lewis X (sLeX) is a sialylated fucosylated tetrasaccharide, an endogenous antigen. Sialyl-Lewis X is a high-affinity ligand for selectins (E-, P-, and L-selectin). Sialyl-Lewis X binds to ELAM-1 and CD62 and has the ability?to inhibits CD62-mediated neutrophil recruitment to sites of inflammation[2].In Vitro: Sialyl-Lewis X is a high-affinity ligand of CD62, Antibodies [mAb CSLEX (IgM; […]
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SIB-1553A is an orally bioavailable nicotinic acetylcholine receptors (nAChRs) agonist, with selectivity for β4 subunit-containing nAChRs. SIB-1553A is also a selective neuronal nAChR ligand. SIB-1553A is a cognitive enhancer, and has therapeutic potential for the symptomatic treatment of Alzheimer’s disease and other cognitive disorders[2].In Vitro: SIB-1553A displaces the binding of [H]nicotine (NIC) to the rat […]
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Sibeprenlimab (VIS649) is a humanized IgG2 monoclonal antibody. Sibeprenlimab can inhibit APRIL. Sibeprenlimab can be used for the research of IgA nephropathy (IgAN).
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Sibiricaxanthone B is a xanthone isolated from Polygala tenuifolia.In Vivo: Sibiricaxanthone B, tenuifolin, sibiricose A5, sibiricose A6, tenuifoliside A, ginsenoside Re and ginsenoside Rb1 are oral administered after Kai-Xin-San, The results indicated that Sibiricaxanthone B shows no significant differences in pharmacokinetic parameters in normal and AD rats.
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SIC5-6 is a potent Separase inhibitor. Separase, a large cysteine protease, involves in chromosome segregation during mitosis and meiosis, DNA damage repair, centrosome disengagement and duplication, spindle stabilization and elongation. Separase is highly overexpressed in many solid cancers, serves as an attractive chemotherapeutic target.IC50 & Target:SeparaseIn Vitro:SIC5-6 (30 μM, 100 μM) increases the activity of […]
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SID 26681509 quarterhydrate is a potent, reversible, competitive, and selective inhibitor of human cathepsin L with an IC50 of 56 nM. SID 26681509 quarterhydrate inhibits in vitro propagation of malaria parasite Plasmodium falciparum and inhibits Leishmania major with IC50s of 15.4 μM and 12.5 μM, respectively. SID 26681509 quarterhydrate shows no inhibitory activity against cathepsin […]
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Sifalimumab (MEDI-545) is an anti-IFNα monoclonal antibody. Sifalimumab suppresses the abnormal immune activity by binding to multiple interferon-alpha (IFNα) subtypes. Sifalimumab can be used in systemic lupus erythematosus (SLE) research[2].In Vitro: Sifalimumab (3-36 μg/well; 72 h) attenuates lymphocyte cytotoxicity co-cultured with U-87MG[2].In Vivo: Sifalimumab (subcutaneous injection; 30 mg/kg and 3 μg/g) treatment shows therapeutic effect […]
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Sigma?1 receptor antagonist 1 (compound 137) is a potent and selective sigma-1 receptor (σ1R) antagonist, with a high binding affinity to σ1R receptor (Ki = 1.06 nM). Sigma?1 receptor antagonist 1 exhibits antineuropathic pain activity and acts as a promising agent for the treatment of neuropathic pain.IC50 & Target: Ki: 1.06 nM (σ1R)In Vitro: Sigma?1 […]
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Sigma-1 receptor antagonist 3 (compound135) is a potent and selective Sigma-1 (σ1) receptor antagonist with a Ki of 1.14 nM. Sigma-1 receptor antagonist 3 inhibits Human Ether-a-go-go-Related Gene (hERG) with an IC50 of 1.54 μM. Sigma-1 receptor antagonist 3 has the potential for the neuropathic pain.IC50 & Target: IC50: 1.54μM (hERG). Ki : 1.14 nM […]
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Sigma-LIGAND-1 hydrochloride is a selective sigma receptor ligand with an IC50s of 16 nM, 19 nM at the DTG site and the PPP site, respectively. Sigma-LIGAND-1 hydrochloride has a Ki of 4000 nM at the dopamine D2 receptor.IC50 & Target: IC50: 16 nM (DTG site of sigma receptor), 19 nM (PPP site of sigma receptor)Ki: […]
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Sildenafil-d3 is deuterium labeled Sildenafil-d3. Sildenafil (UK-92480) is a potent phosphodiesterase type 5 (PDE5) inhibitor with an IC50 of 5.22 nM.
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Siltuximab is an anti-IL-6 (interleukin-6) monoclonal antibody, and shows antitumor activity. Siltuximab can be used in Multicentric Castleman’s Disease (MCD) and COVID-19 research[2].In Vivo:Siltuximab (intraperitoneal injection; 10 mg/kg; 3 times per week) inhibits the growth of lung cancer cells in xenograft mouse model.Siltuximab (intraperitoneal injection; 20 mg/kg; twice per week; 6 w) inhibits the growth […]
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Silver sulfadiazine (AgSD), a sulfonamide antibiotic, effects a dual inhibitory action on bacterial growth by its sulfa moiety (SD-SDZ) that prevents bacterial folate absorption and subsequent DNA synthesis. The silver that is released from Silver sulfadiazine binds and disrupts the DNA structure, precluding bacterial DNA replication.In Vitro: Silver sulfadiazine (AgSD) is a topical antibiotic used […]
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Silybin is a flavonolignan isolated from milk thistle (Silybum marianum) seeds. Silybin induces apoptosis and exhibits hepatoprotective, antioxidant, anti-inflammatory, anti-cancer activity[2].In Vitro: Silybin (0-200 mM; for 72 hours) has growth inhibition in a time- and dose-dependent manner. Silybin (68 μM; for 72 hours) induces apoptosis and increases the cells in G1-phase of ~22%. Silybin (68 […]
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Simazine is a triazine herbicide widely used in agriculture, pot-plant and tree production. Simazine is phytotoxicity and not highly toxic to soil microflora and algae.
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Simethicone is an orally active defoamer. Simethicone reduces the surface tension of air bubbles in the gastrointestinal tract, causing them to be expelled by vomiting, exhalation or absorption into the bloodstream. Simethicone has potential applications in flatulence and colic.In Vivo:Simethicone (200 mg/kg; p.o.; single dose) has gastrointestinal regulation function in rats[2].Simethicone (20 mg/kg; p.o.; single […]
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Sinapaldehyde exhibits moderate antibacterial against Methicillin resistant S. aureus (MRSA) and E. coli with MIC values of 128 and 128 μg/mL.
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Sinbaglustat (OGT2378) is a dual inhibitor of glucosylceramide synthase (GCS) and non-lysosomal glucosyl ceramidase (GBA2). Sinbaglustat is an orally available N-alkyl iminosugar that crosses the blood-brain barrier. Sinbaglustat can be used for the research of central neurodegenerative diseases associated with lysosomal dysfunctions[2].In Vitro: Sinbaglustat (OGT2378; 20 μM) reduces the synthesis of glucosylceramide and ganglioside by […]
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Sinefungin is a potent inhibitor of virion mRNA(guanine-7-)-methyltransferase, mRNA(nucleoside-2′-)-methyltransferase, and viral multiplication. Sinefungin, a SET7/9 inhibitor, ameliorates renal fibrosis by inhibiting H3K4 methylation[2].In Vitro: Sinefungin (0.5 or 1.0 μg/mL, 60 minutes) ameliorates the TGF-β1-induced increase of α-SMA and inhibits the upregulation of histone H3K4 monomethylation in renal epithelial cells and renal fibroblast cells[2].In Vivo: Sinefungin […]
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