Batimastat sodium salt is a potent broad spectrum MMP inhibitor with IC50 of 3, 4, 4, 6, and 20 nM for MMP-1, MMP-2, MMP-9, MMP-7 and MMP-3, respectively.
AZD-7762 is a potent ATP-competitive checkpoint kinase (Chk) inhibitor in with an IC50 of 5 nM for Chk1.
Calcimycin (A-23187) hemimagnesium is an antibiotic and a unique divalent cation ionophore (like calcium and magnesium). Calcimycin hemimagnesium induces Ca2+-dependent cell death by increasing intracellular calcium concentration. Calcimycin hemimagnesium inhibits the growth of Gram-positive bacteria and some fungi. Calcimycin hemimagnesium also inhibits the activity of ATPase and uncouples oxidative phosphorylation of mammalian cells. Calcimycin hemimagnesium induces apoptosis[1][2][3][4].
Onartuzumab (MetMAb) is a unique, humanized and affinity-matured monovalent (one-armed) monoclonal antibody against the MET receptor. Onartuzumab potently inhibits HGF binding and receptor phosphorylation and signaling. Onartuzumab has antibody-like pharmacokinetics and antitumor activity[1].
FIN56 is a specific inducer of ferroptosis.
Embelin is a cell-permeable benzoquinone compound that exhibits antitumor properties. Specifically antagonizes XIAP-mediated inhibition of caspase-9 activation by directly targeting the Smac and caspase-9 binding domain BIR3 (IC50 = 4.1 uM in a competitive binding assay with Smac peptide).IC50 value: 4.1 uM [1]Target: XIAPin vitro: Embelin induced activation of caspase-9 and embelin-induced apoptosis was prevented by caspase inhibitors [2]. Treatment with subtoxic doses of Embelin broadly sensitized malignant glioma cells to TRAIL-mediated apoptosis. Notably, human astrocytes were not significantly affected by the combined treatment consisting of Embelin and TRAIL. Combined treatment with Embelin and TRAIL augmented the activation of initiator caspases-8/-9 and effector caspases-3/-7, respectively [3]. in vivo: Embelin inhibited topical edema in the mouse ear, leading to substantial reductions in skin thickness and tissue weight, inflammatory cytokine production, neutrophil-mediated myeloperoxidase activity, and various histopathological indicators. Furthermore, embelin was effective at reducing inflammatory damage induced by chronic TPA exposure [4]. Embelin (10, 30 or 50mg/kg body weight) was administrated daily per oral route for 7days. Embelin significantly attenuated DSS-induced DAI scores and tissue MPO accumulation, which implied that it suppressed weight loss, diarrhea, gross bleeding, and the infiltrations of immune cells. Embelin administration also effectively and dose-dependently prevented shortening of colon length and enlargement of spleen size [5].
TIC10 isomer is the isomer of TIC10. TIC10 isomer does not possess the reported biological activity of inducing TRIAL expression.
Syncytial Virus Inhibitor-1 is a potent, orally bioavailable respiratory syncytial virus (RSV) fusion inhibitor with EC50s of 0.002 μM, 0.004 μM, and 0.002 μM for RSV Long, RSV A2, and RSV B strains, respectively[1].
VU6004909 is a mGlu5 receptor positive allosteric modulator (pEC50: 7.59). VU6004909 shows antipsychotic-like effects. VU6004909 can reverse MK801-induced cortical hyperactivity and cognitive deficits[1][2].
Cupressuflavone is a natural product that can be found in Cupressus macrocarpa. Cupressuflavone exhibits anti-inflammatory and antiulcerogenic activities. Cupressuflavone also show protective effects against CCl4-induced hepato- and nephrotoxicity in mice[1][2][3].
3-Acetoxy-11-ursen-28,13-olide (11,12-dehydroursolic lactone acetate) is a reduction product of 11-ketoursolic acid[1].
TET 830 modified/T-helper epitope from tetanus toxoid is a modified T-helper epitope from tetanus toxoid. TET 830 modified/T-helper epitope from tetanus toxoid induces T-cells responses and is used as a helper peptide in vaccinations[1].
β-Cyclocitral, a volatile oxidized derivative of β-carotene, is a grazer defence signal unique to the Cyanobacterium Microcystis. β-Cyclocitral, one of the predominant volatile terpenoid compounds, can upregulate the expression of defence genes to enhance excess light (EL) acclimation. β-Cyclocitral is a powerful repellent[1][2][3].
DGAT1-IN-3 is a potent, selective and orally bioavailable inhibitor of DGAT-1, with the IC50s of 38 nM for human DGAT-1 and 120 nM for rat DGAT-1. DGAT1-IN-3 could be used to research of obesity, dyslipidemia, and metabolic syndrome[1][2].
AMP-Deoxynojirimycin (AMP-DNM) is a potent ceramide glucosyltransferase and GCase 2 inhibitor. AMP-Deoxynojirimycin also is a GlcCer biosynthesis inhibitor[1][2].
ACV1 (Vc1.1), an α-Conotoxin, is a selective α9α10 nAChR antagonist with an IC50 of 19 nM. ACV1 is ~100-fold less potent on human α9α10 vs. rat nAChRs[1].
Levamisole Hcl is an anthelmintic and immunomodulator belonging to a class of synthetic imidazothiazole derivatives.IC50 value: Target: Levamisole suppresses the production of white blood cells, resulting in neutropenia and agranulocytosis. With the increasing use of levamisole as an adulterant, a number of these complications have been reported among cocaine users [1] [2]. Levamisole reversibly and noncompetitively inhibits most isoforms of alkaline phosphatase (e.g., human liver, bone, kidney, and spleen) except the intestinal and placental isoform [3]. It is thus used as an inhibitor along with substrate to reduce background alkaline phosphatase activity in biomedical assays involving detection signal amplification by intestinal alkaline phosphatase, for example in in situ hybridization or Western blot protocols. It is used to immobilize the nematode C. elegans on glass slides for imaging.
Glycerol is a clear, colourless, viscous, sweet-tasting liquid. Glycerol is used in sample preparation and gel formation for polyacrylamide gel electrophoresis.
Clovoxamine (DU23811) (Compound 35) has binding affinity for serotonin transporter (SERT) (Ki: 61 nM). Clovoxamine is a 5-HT and norepinephrine reuptake (NE) re-uptake inhibitor. Clovoxamine is an antidepressant[1][2][3].
Tyroserleutide (YSL), isolated from the degradation products of porcine spleen[1], is a small molecular tripeptide which inhibits tumor growth both in vitro and in vivo[2].
Btk inhibitor 2 is a Bruton's tyrosine kinase (BTK) inhibitor extracted from patent US 20170224688 A1.
STING agonist-9 (Compound 45) is a potent STING agonist with an EC50 of 1.2 nM and 32.82 μM against h-STING and m-STING, respectively. STING agonist-9 shows antitumor activity[1].
Darbufelone is a dual inhibitor of cellular PGF2α and LTB4 production. Darbufelone potently inhibits PGHS-2 (IC50= 0.19 μM) but is much less potent with PGHS-1 (IC50=20 μM).
(R)-Equol is an agonist of both ERα and ERβ with Kis of 27.4 and 15.4 nM, respectively.
Fmoc-D-Bip(4,4’)-OH is an alanine derivative[1].
COX/5-LO-IN-1 is an inhibitor of cylooxygenase and 5-lipoxygenase, used for the research of inflammatory and allergic disease states.
2-Desoxypleniradin-L-α-arabinopyranoside, 2-acetate is an active compound. 2-Desoxypleniradin-L-α-arabinopyranoside, 2-acetate can be isolated from Helenium amarum[1].
FLT3-IN-4 is a potent and orally effective Fms-like tyrosine receptor kinase 3 (FLT3; IC50=7 nM) inhibitor for treating acute myelogenous leukemia[1].
2,2-Dimethyl-8-prenylchromene 6-carboxylic acid (compound 2) is a natural product that can be found in Piper aduncum[1].
(24S)-Cycloartane-3β,24,25-triol, a cycloartane, has antitubercular activity against Mycobacterium tuberculosis H37Rv (MIC: 32 μg/mL). (24S)-Cycloartane-3β,24,25-triol can be isolated from the flowers of Chrysanthemum morifolium[1].