Schisandrin B(Wuweizisu-B) is a dibenzocyclooctadiene derivative isolated from Fructus Schisandrae, has been shown to produce antioxidant effect on rodent liver and heart.IC50 value:Target: in vitro: Schisandrin B exhibits anti-inflammatory activity through modulation of the redox-sensitive transcription factors Nrf2 and NF-κB. SB inhibited mitogen-induced proliferation and cytokine secretion by lymphocytes [1]. Sch B can protect neuronal cells against oxidative challenge, presumably by functioning as a hormetic agent to sustain cellular redox homeostasis and mitoenergetic capacity in neuronal cells [2]. Sch B exerted significant neuroprotective effects against microglial-mediated inflammatory injury in microglia-neuron co-cultures. Sch B significantly downregulated pro-inflammatory cytokines, including nitrite oxide (NO), tumor necrosis factor (TNF)-α, prostaglandin E(2) (PGE(2)), interleukin (IL)-1β and IL-6 [3]. Sch B could inhibit TGF-β induced EMT of 4T1 cells and of primary human breast cancer cells [4].in vivo: Similar anti-inflammatory effects of SB on lymphocyte proliferation and cytokine secretion were also observed in vivo [1]. Treatment with Sch B in CsA-treated mice significantly suppressed the elevation of blood urea nitrogen (BUN) and serum creatinine levels and attenuated the histopathological changes. Additionally, Sch B also decreased renal MDA levels and increased GSH levels in CsA-treated mice [5].
Edobacomab (E5) is a mouse anti-endotoxin monoclonal IgM antibody. Edobacomab ca be uesd for the research of sepsis caused by Gram-negative bacterial infections[1].
Fazamorexant (YZJ-1139) is a potent orexin receptor antagonist. Fazamorexant can be used for insomnia research[1][2].
CDK6/PIM1-IN-1 is a potent and balanced dual CDK6/PIM1 inhibitor with IC50 values of 39 and 88 nM, respectively. CDK6/PIM1-IN-1 inhibits CDK4 (IC50=3.6 nM). CDK6/PIM1-IN-1 significantly inhibits acute myeloid leukemia (AML) cell proliferation, arrest cell cycle at the G1 phase, and promote cell apoptosis. CDK6/PIM1-IN-1 exhibits potent anti-AML activity[1].
Tubulin/MMP-IN-2 is dual inhibitor of tubulin and matrix metalloproteinases. Tubulin/MMP-IN-2 can strongly inhibit tubulin polymerization and induces cell Apoptosis. Tubulin/MMP-IN-2 has inhibitory activities against MMP-2, MMP-3 and MMP-9 with IC50 values of 24.95 μM, 31.60 μM and 22.37 μM, respectively. Tubulin/MMP-IN-2 can be used for the research of cancer[1].
2-NP-AMOZ is a 2-nitrophenyl derivative of AMOZ (a metabolite of antibiotic Furaltadone), can be used to detect protein bound AMOZ[1][2].
Molindone ((±)-Molindone), an indole derivative, is a potent dopamine D2 and D5 receptor antagonist. Molindone ((±)-Molindone) can be used for the research of schizophrenia and severe mental illness[1][2].
Kallikrein-IN-1 (Formula A) is a Kallikrein inhibitor[1].
Pentaglycine (Tetraglycylglycine) is a bridge containing five glycine molecules. Pentaglycine can form highly cross-linked peptidoglycan. Glucose reduced expression of pentaglycine. Pentaglycine is cleaved by lysostaphin, and occurs in the cell envelope of staphylococci[1].
Pretomanid-d4 (PA-824-d4) is the deuterium labeled Pretomanid. Pretomanid (PA-824) is an antibiotic used for the research of multi-drug-resistant tuberculosis affecting the lungs. Pretomanid exhibits a sub-micromolar MIC against M. tuberculosis (MTB). The MIC values of PA-824 against a panel of MTB pan-sensitive and Rifampin mono-resistant clinical isolates range from 0.015 to 0.25 µg/mL[1][2].
(Rac)-Telmesteine is a protease inhibitor and is thus a suitable enzyme stabilizer extracted from patent WO 2017220302 A1, compound II-1. (Rac)-Telmesteine can be used as an enzyme stabilizer in protease-containing detergents and cleaning agents[1].
BAY-Y 3118 is a new chlorofluoroquinolone with antimicrobial activity.
Aspartame is an artificial, non-saccharide sweetener used as a sugar substitute in some foods and beverages.Target: OthersAspartame is a flavoring agent sweeter than sugar. Aspartame is a methyl ester of a dipeptide used as a synthetic nonnutritive sweetener. Epidemiological studies on aspartame include several case-control studies and one well-conducted prospective epidemiological study with a large cohort, in which the consumption of aspartame was measured. The studies provide no evidence to support an association between aspartame and cancer in any tissue. The weight of existing evidence is that aspartame is safe at current levels of consumption as a nonnutritive sweetener [1]. aspartame is safe, and there are no unresolved questions regarding its safety under conditions of intended use [2]. excessive aspartame ingestion might be involved in the pathogenesis of certain mental disorders (DSM-IV-TR 2000) and also in compromised learning and emotional functioning [3].
INH1 is a small molecule targeting the Hec1/Nek2 mitotic pathway suppresses tumor cell growth in culture and in animal.IC50 value: 10-21 uM (GI50 in human breast cancer cell lines) [1]Target: Hec1 inhibitorTreating cells with INH1 triggered reduction of kinetochore-bound Hec1 as well as global Nek2 protein level, consequently leading to metaphase chromosome misalignment, spindle aberrancy, and eventual cell death. INH1 effectively inhibited the proliferation of multiple human breast cancer cell lines in culture (GI(50), 10-21 micromol/L). Furthermore, treatment with INH1 retarded tumor growth in a nude mouse model bearing xenografts derived from the human breast cancer line MDA-MB-468, with no apparent side effects. This study suggests that the Hec1/Nek2 pathway may serve as a novel mitotic target for cancer intervention by small compounds.
Oseltamivir acid hydrochloride is an active metabolite of the antiviral agent Oseltamivir (HY-13317) ethylester. Oseltamivir acid hydrochloride belongs to baseline toxicants in toxicity ratio analysis[1].
Gevokizumab is a potent anti-IL-1β antibody, negatively modulates IL-1β signaling through an allosteric mechanism. Gevokizumab selectively decreases the binding affinity of IL-1β for the IL-1 receptor type I (IL-1RI) signaling receptor instead of IL-1 counter-regulatory decoy receptor (IL-1 receptor type II)[1][2].
HS-1793 is a resveratrol analogue with antitumor activities in a variety of cancer cell lines[1]. HS-1793 induces cell apoptosis[2].
TK4b is a Janus kinase (JAK) inhibitor with the IC50 values of 19.40 nM and 18.42 nM for JAK2 and JAK3, respectively. TK4b can be used in lymphoid-derived diseases and leukemia cancer research[1].
HO-PEG24-OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Galanin-Like Peptide (porcine) is a 60 amino acid neuropeptide that was first isolated from the porcine hypothalamus. Galanin-Like Peptide (porcine) has a high affinity for the GALR2 receptor (IC50 of 0.24 nM) and a lower affinity for the GALR1 receptor (IC50 of 4.3 nM)[1].
Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2 is a biological active peptide. (Protease activated receptor 1 (PAR-1) belongs to a subfamily of G-protein coupled receptors and is known to mediate the cellular effects of thrombin. This peptide is a PAR-1 selective agonist displaying a high level of specificity to PAR-1 over PAR-2. The specificity of peptide was evaluated in cell-based calcium signaling assay using HEK293 cells. PAR-1 selective agonists can be used to study PAR-1 activation in vivo. In addition to its varied cellular effects of thrombin, PAR-1 has also been shown to coordinate with PAR-4 and regulate thrombin-induced hepatocellular carcinoma harboring thrombin formation within the tumor environment classified as 'coagulation type'.)
Beraprost sodium, a prostacyclin analog, is a stable and orally active prodrug of PGI2. Beraprost sodium is a potent vasodilator, has the potential for pulmonary arterial hypertension treatment through expanding renal vessels, improving microcirculation[1].
FR183998 free base is a potent Na+/H+-exchange inhibitor, with IC50s of 0.3 nM, 3.1 nM and 6.5 nM by measurement of pHi change in rat lymphocytes, rat and human platelets, respectively.
4-Methylumbelliferyl-N-acetyl-α-D-glucosaminide is a fluorogenic substrate for detecting α-N-acetylglucosaminidase[1].
Taltobulin intermediate-1 is an intermediate in the synthesis of Taltobulin (HY-15584). Taltobulin is a common toxin component in ADC preparation (ADC Cytotoxin), and it is also a powerful tubulin (Microtubule/Tubulin) inhibitor. Taltobulin disrupts tubulin polymerization, induces mitotic arrest, and induces apoptosis[1].
CRBN ligand-9 (Compound 4d) is a CRBN ligand (Ki: 8.9 μM). CRBN ligand-9 can be used for synthesis of PROTACs[1][2].
Iα52 is a naturally processed peptide encompassed the residues 52-68 of the murine I-Eα chain and may contribute to selection of immature T cells[1].
Ezetimibe (SCH 58235) is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator. Ezetimibe (SCH 58235) is a potent cholesterol absorption inhibitor.
Dansyl-Tyr-Val-Gly TFA is a substrate of peptidylglycine monooxygenase (PHM). Peptidylglycine monooxygenase is an essential enzyme for the posttranslational amidation of neuroendocrine peptides[1].
DNA topoisomerase II inhibitor 1 (compound 8ed) is a potent DNA topoisomerase II inhibitor. DNA topoisomerase II inhibitor 1 shows anti-proliferative activity. DNA topoisomerase II inhibitor 1 induces apoptosis and cell cycle arrest at sub G1 phase[1].