Pyrrolnitrin is an antibiotic isolated from Pseudomonas pyrrocinia. Pyrrolnitrin shows a broad spectrum of antibiotic activity against fungi, yeast and gram-positive bacteria[1].
Tetramethylammonium iodide is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Lixudebart is a humanized immunoglobulin G1-kappa, anti-CLDN1 monoclonal antibody[1].
Clopidogrel thiolactone is a P2Y12 receptor inhibitor, is a potent antiplatelet agent.Target: P2Y12Clopidogrel thiolactone is the metabolic intermediate resulting from the first oxidative activation of clopidogrel.
TAK-593 is a potent VEGFR and PDGFR family inhibitor with IC50s of 3.2, 0.95, 1.1, 4.3 and 13 nM for VEGFR1, VEGFR2, VEGFR3, PDFGRα and PDFGRβ, respectively.
Cathepsin G substrate is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
PF-9366 is a human methionine adenosyltransferase 2A (Mat2A) inhibitor, with an IC50 of 420 nM and a Kd of 170 nM.
trans,trans-2,4-Nonadienal is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
3,5-Di-O-benzoyl-2-deoxy-2-fluoro-5-trifluoromethyl-arabinouridine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Boc-N-Me-Tyr-OH.DCHA is a tyrosine derivative[1].
T338C Src-IN-1 is a potent mutant-Src T338C inhibitor; exhibited the most potent inhibition of T338C(IC50=111 nM) relative to WT c-Src (10-fold increase).
Qingyangshengenin B, a C-21 steroidal glycoside isolated from Qingyangshen. Qingyangshengenin B protects against Aβ toxicity, which decreases Aβ deposition by decreasing the expression of Aβ at the mRNA level. Qingyangshengenin B has antiepileptic activity[1][2][3].
Tetrahydroalstonine, a indole alkaloid isolated from the fruits of Rhazya stricta, is a selective alpha 2-adrenoceptor antagonist[1][2].
Tanshinone I is an inhibitor of type IIA human recombinant sPLA2 (IC50=11 μM) and rabbit recombinant cPLA2 (IC50=82 μM).
GNE-149 is an orally bioavailable full antagonist of estrogen receptor α (ERα; IC50=0.053 nM). GNE-149 is a selective estrogen receptor degrader (SERD). GNE-149 can be used for the research of breast cancer[1].
TIK-301 (PD-6735) is a chlorinated melatonin derivative and a potent, high-affinity and orally active melatonin MT1 and MT2 receptors agonist with Kis of 0.081 nM and 0.042 nM, respectively. TIK-301 is also a 5-HT2B/5-HT2C receptors antagonist with antidepressant action. TIK-301 has the potential for sleep disorders and other circadian rhythm disorders treatment[1][2][3].
N-Acetyl-D-glucosamine-13C,15N is the 13C and 15N labeled N-Acetyl-D-glucosamine. N-Acetyl-D-Glucosamine (N-Acetyl-2-amino-2-deoxy-D-glucose) is a monosaccharide derivative of gluc[1][2].
Inosine oxime (6-Hydroxyadenosine) is an endogenous metabolite in the course of cell metabolism by cytochrome P450, by oxidative stress or by deviating nucleotide biosynthesis. Inosine oxime has toxic and mutagenic for procaryotic and eucaryotic cells[1][2].
Linopristin is a kind of type B streptogramin antibiotics. Linopristin, together with type A, Flopristin, to form the streptogramin combination NXL 103. Linopristin exhibit synergistic antimicrobial activity against certain pathogenic bacteria with Flopristin. The preference ratio of Linopristin/Flopristin is 30:70 (w/w) or 70 μM Linopristin +120 μM Flopristin[1].
S-(2-Carboxypropyl)-L-cysteine (β-Isobuteine) is a urine metabolite, a metabolic marker of leigh-like syndrome[1].
TGR5 Receptor Agonist, a potent TGR5(GPCR19) agonist, showed improved potency in the U2-OS cell assay (pEC50 = 6.8) and in melanophore cells (pEC50 = 7.5).IC50 value: 6.8 (pEC50, U2-OS cell assay); 7.5(pEC50, melanophore cell) [1]Target: TGR5TGR5 Receptor Agonist was profiled against more than 100 in-house and external 7TM, ion channel, enzyme, transporter, and nuclear hormone receptor selectivity assays, including FXR, another bile acid receptor, and showed significant response only in secretion of the pro-inflammatory cytokine TNFalpha (pIC50 = 6.8) in human primary monocytes following stimulation with LPS (lipopolysaccharide). In addition, TGR5 Receptor Agonist has good physicochemical properties and no measurable activity against three of the common cytochrome P450 (CYP450) isoforms (1A2, 2C9, and 2D6) or hERG dofetilide binding (pIC50 <4.3). In rat pharmacokinetic (PK) studies, however, TGR5 Receptor Agonist showed high in vivo clearance (Cl = 85 mL/min/kg) and intrinsic clearance (Clint = 48 mL/min/g) which provided a reasonable explanation for the observed poor exposure. Because the TGR5 receptor is expressed in the GI tract at levels that increase corresponding with L-cell population density, we believe that agonists such as 6 and 7 possessing poor systemic exposure are good tool compounds for directly targeting the TGR5 receptor in the GI tract via local administration (vide infra) rather than systemic exposure. Our hypothesis was that for this receptor, systemic exposure was not necessary to achieve the desired effect of stimulating GLP-1 secretion in vivo [1].
L-Methionine-DL-sulfoximine (MSX) is an inhibitor of glutamine synthetase. L-Methionine-DL-sulfoximine is also a potent convulsant which metabolically and morphologically primarily affects astroglia.
Bazedoxifene is a selective estrogen receptor modulator (SERM) currently in development for osteoporosis prevention and treatment.IC50 value:Target: estrogen receptor modulatorPreclinical and clinical studies with bazedoxifene demonstrate more tissue selectivity than other SERMs. In particular, bazedoxifene has minimal if any agonist activity in the uterus and is able to antagonize effects of estrogen on the uterus. Animal studies and early clinical studies suggest effects in the bone similar to other SERMs with prevention of postmenopausal bone loss.
VRX0466617, a selective Chk2 inhibitor, inhibits the phosphorylation of Chk2 Ser 19 and Ser33-35. VRX0466617 can be used in the study of cancer[1].
3-Methylfuran-d3 is a deuterium labeled compound.
3,3'-Bis(3-sulfopropyl)-5,5'-diphenyl-9-ethyloxacarbocyanine betaine sodium is a photographic sensitizer in the green spectral region[1].
Alsterpaullone (9-Nitropaullone;NSC 705701) is a potent cyclin-dependent kinases (CDK) inhibitor, with IC50s of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also competes with ATP for binding to glycogen synthase kinase-3 alpha/beta (GSK-3alpha/GSK-3beta) with an IC50 of 4 nM, with antitumor activity and potential for the treatment of neurodegenerative and proliferative disorders[1].
Leucocrystal violet-d6 is the deuterium labeled Leucocrystal violet[1]. Leucocrystal violet is a triphenylmethane dye which can be used to detect antimony in environmental and biological samples using spectrophotometric techniques[2][3].
Icatibant acetate (HOE-140 acetate) is a potent and specific peptide antagonist of bradykinin B2 receptor with IC50 and Ki of 1.07 nM and 0.798 nM respectively[1][2][3].
GSK3-IN-1 (compound 11) is a GSK-3 inhibitor with an IC50 value of 12 μM. GSK3-IN-1 can be used in the research of diabetes[1].