KY1022 is a ras destabilizer. KY1022 targets the Wnt/ß-catenin pathway and inhibits development of metastatic colorectal cancer.
Ethyl 2-((2-((tert-butoxycarbonyl)amino)ethyl)amino)acetate hydrochloride is a Glycine (HY-Y0966) derivative[1].
HPV16-E711-20 epitope is a well-known HLA-A*0201-restricted human cytotoxic T lymphocyte (CTL) epitope of the HPV16 E7 protein that shows high-affinity binding to HLA-A2 in vitro. HPV16 CTL epitopes may be good candidates for the development of an effective peptide-based antitumor vaccine[1].
Follicle-stimulating hormone is a heterodimer glycoprotein expressed by gonadotropin in the anterior pituitary gland. Follicle-stimulating hormone affects the fertility and reproductive efficiency of animals[1][2].
Furagin, nitrofurantoin analog, is an anti-bacterial agent. Furagin is 2-substituted 5-nitrofuran, chemically and structurally similar to well-known antibacterial compound nitrofurantoin.IC50 Value: Target: Antibacterialin vitro: The furagin concentrations in serum remain several hours above the MIC concentrations of many pathogenic bacteria. Despite the high concentrations in serum, the urine levels of furagin were generally lower than those of nitrofurantoin. The 24 hr recoveries in urine were 8--13% for furagin and about 36% for nitrofurantoin [1].in vivo: A time-independent increase in SCE frequency was found in lymphocytes of children treated with furagin. Total CA frequency did not differ significantly between groups of children with various duration of furagin treatment [2]. Women were randomised into two groups receiving either ciprofloxacin 250mg twice a day for 3 days (n=13) or furagin 100mg three times a day for 7 days (n=14). Median lengths of follow-up were 4 days and 5 days in the ciprofloxacin and furagin groups, respectively [3].
OTS-964 is a potent TOPK inhibitor (IC50=28 nM), which inhibits TOPK kinase activity with high affinity and selectivity.
NH2-PEG5-C6-Cl hydrochloride is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
LH-RH (4-10) is a heptapeptide, one of major degradation products of luteinising-hormone releasing hormone (LHRH) via pituitary and hypothalamus. LH-RH (4-10) produced in macrophages and type II pneumocytes[1].
VCH-916 is a novel nonnucleoside HCV NS5B polymerase inhibitor.IC50 Value: Target: HCVVCH-916 is a novel allosteric inhibitor of HCV NS5B polymerase. The RNA-dependent RNA polymerase (NS5B) of HCV is one of the attractive validated targets for development of new drugs to block HCV infection. VCH-916 is currently being evaluated for safety/tolerability, pharmacokinetics and anti-viral efficacy in chronically infected HCV patient.
Triacetin is an artificial chemical compound, is the triester of glycerol and acetic acid, and is the second simplest fat after triformin.
Br-PEG3-OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
BMS-536924 is an ATP-competitive IGF-1R/IR inhibitor with IC50 of 100 nM/73 nM.IC50 value: 100 nM (IGF-1R); 73 nM (IR) [1]Target: IGF-1R; IRin vitro: BMS-536924 also inhibits FAK and Lck with IC50 of 150 nM and 341 nM, respectively. BMS-536924 inhibits cellular proliferation and disrupts Akt and MAPK phosphorylation [1]. BMS-536924 inhibits IGF-I-stimulated IGF-1R signaling in MCF10A cells and blocks constitutive IGF-1R activity in CD8-IGF-1R-MCF10A. Preincubation of MCF10A cells with 1 μM BMS-536924 completely blocks the ability of IGF-I to stimulate IGF-1R phosphorylation. IGF-I stimulation results in increased phosphorylation of ERK1/2, GSK3β, and Akt. BMS-536924 inhibits this ligand-induced phosphorylation. Treatment of the CD8-IGF-1R-MCF10A cells with BMS-536924 results in a dose-dependent inhibition of phosphorylation with partial inhibition at 0.01 μM and 0.1 μM, but complete receptor inhibition at a concentration of 1 μM. Maximal inhibition of phosphorylated IGF-1R is observed as early as 10 minutes following incubation. BMS-536924 retains its ability to inhibit IGF-1R phosphorylation for up to 48 hours. Addition of BMS-536924 time-dependently inhibits Akt phosphorylation starting at 1 hour. By 48 hours, Akt activation is completely blocked [2]. in vivo: Oral administration of BMS-536924 at 100-300 mpk strongly inhibits IGR-1R Sal tumor model. Efficacy is also observed in the nonengineered Colo205 human colon carcinoma mode. Oral administration of 3 on a once a day schedule (100-300 mpk) or a twice a day schedule (50, 100 mpk) demonstrates antitumor activity in this tumor model. Oral glucose tolerance test (OGTT) shows 100 mpk (b.i.d.) causes a significant elevation in glucose levels after glucose challenge. The pharmacokinetic parameters of BMS-536924, administered orally in poly(ethylene glycol) 400 and water (80:20 v/v), are determined in mouse, rat, dog, and monkey. Good bioavailability is evident in all species. Significant nonlinear pharmacokinetics is observed in rodents at increasing p.o. dose [1]. Oral administration of 70 mg/kg BMS-536924 significantly inhibits tumor growth (TGBC-1TKB cells) inoculated in nude mice. BMS-536924 up regulates apoptosis in xenografts tumors. The treatment doesn't have adverse effects on the body weight of mice or the glucose levels at the time of death, suggesting tolerable toxicity [3].
ABP688 is a high affinity human mGluR5 antagonist with anKi of 1.7 nM. Radioisotope-labeled ABP688 can be used as a PET tracer for clinical imaging of the mGlu5 receptor[1].
E3 Ligase Ligand-Linker Conjugates 21 is a synthesized compound that incorporates an E3 ligase ligand and a linker used in PROTAC technology.
SBI-115 is a TGR5 (GPCR19) antagonist. SBI-115 decreases hepatic cystogenesis with polycystic liver diseases via inhibitingTGR5[1].
MD13 is a macrophage migration inhibitory factor (MIF)-directed PROTAC with a Ki of 71 nM. MD13 can be used for cancer research[1].
Epothilone E is a related compound of epothilone, which inhibits microtubule protein function and blocks cell division, and has anti-tumor activity[1].
L-Canavanine sulfate is a selective inhibitor of inducible NO synthase.
5,5'-Dimethyl BAPTA tetrapotassium is a water-soluble, extracellular membrane metal chelator with relative selectivity for calcium ions[1].
AZ-PFKFB3-67 is potent and selective PFKFB3 kinase inhibitor, with IC50s of 11, 159 and 1130 nM for PFKFB3, PFKFB2 and PFKFB1 respectively[1].
Vosoritide (BMN 111) is a modified recombinant CNP (C-type natriuretic peptide) analogue, binds to NPR-B (natriuretic peptide receptor type B) and reduces the activity of FGFR3 (fibroblast growth factor receptor 3). Vosoritide can be used in achondroplasia and dwarfism research[1][2][3].
Isobyakangelicol is a coumarin that can be found in the roots of Angelica dahurica. Isobyakangelicol inhibits the growth of HeLa and HepG2 cells, with IC50s of 70.04 μM and 17.97 μM[1].
Silychristin is an abundant flavonolignan present in the fruits of Silybum marianum, with antioxidant properties. Silychristin is a potent inhibitor of the thyroid hormone transporter MCT8, and elicits a strong inhibition of T3 uptake with an IC50 of 110 nM[1][2].
Bis-PEG10-acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].
Thiamethoxam-d3 is the deuterium labeled Thiamethoxam[1]. Thiamethoxam is a broad spectrum neonicotinoid insecticide[2][3].
ASP6537 is a potent and selective rhCOX-1 inhibitor with an IC50 of 0.703 nM. ASP6537 has the potential for cardiovascular disease research[1].
Pipazethate (SKF 70230A), a pyridobenzothiazine derivative, is a potent GABA antagonist. Pipazethate has antitussive activity. Pipazethate can be used in research in cough supressant[1].
TRPV antagonist 1 is a transient receptor potential vanilloid (TRPV) antagonist, with an IC50 of < 250 nM.
ST 1535 is a potent and orally active A2A adenosine receptor antagonist. ST 1535 shows antiparkinsonian activity and antitremorigenic effects. ST 1535 has the potential for the research of Parkinson’s disease[1][2].
Mycophenolic acid glucuronide is a metabolite of the immunosuppressant mycophenolic acid (MPA). Mycophenolic acid glucuronide shows anti-tumor activity and can be used in adenocarcinoma research[1][2][3].