I-191 NEW
Price | $82 | $118 | $198 |
Package | 1mg | 2mg | 5mg |
Min. Order: | |
Supply Ability: | 10g |
Update Time: | 2024-11-19 |
Product Details
Product Name: I-191 | CAS No.: 1690172-25-8 |
Purity: 99.80% | Supply Ability: 10g |
Release date: 2024/11/19 |
Product Introduction
Bioactivity
Name | I-191 |
Description | I-191 is a potent antagonist of protease-activated receptor 2 (PAR2), inhibits multiple signaling functions in human cancer cells. |
In vitro | At nanomolar concentrations, I-191 inhibited PAR2 binding of and activation by structurally distinct PAR2 agonists (trypsin, peptide, nonpeptide) in a concentration-dependent manner in cells of the human colon adenocarcinoma grade II cell line (HT29).?I-191 potently attenuated multiple PAR2-mediated intracellular signaling pathways leading to Ca2+ release, extracellular signal-regulated kinase 1/2 (ERK1/2) phosphorylation, Ras homologue gene family, member A (RhoA) activation, and inhibition of forskolin-induced cAMP accumulation.?The mechanism of action of I-191 was investigated using binding and calcium mobilization studies in HT29 cells where I-191 was shown to be noncompetitive and a negative allosteric modulator of the agonist 2f-LIGRL-NH2 The compound alone did not activate these PAR2-mediated pathways, even at high micromolar concentrations, indicating no bias in these signaling properties.?I-191 also potently inhibited PAR2-mediated downstream functional responses, including expression and secretion of inflammatory cytokines and cell apoptosis and migration, in human colon adenocarcinoma grade II cell line (HT29) and human breast adenocarcinoma cells (MDA-MB-231).?I-191 is a potent PAR2 antagonist that inhibits multiple PAR2-induced signaling pathways and functional responses.?I-191 may be a valuable tool for characterizing PAR2 functions in cancer and in other cellular, physiological, and disease settings. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 8.33 mg/mL (19.67 mM) |
Keywords | I-191 | Inhibitor | I191 | inhibit | I 191 | Protease Activated Receptor (PAR) | Thrombin receptors |
Inhibitors Related | FSLLRY-NH2 TFA(245329-02-6 free base) | LRGILS-NH2 acetate | Protease-Activated Receptor-1, PAR-1 Agonist acetate | PAR-2 Activating Peptide acetate | Atopaxar | Vorapaxar sulfate | Trypsin | Vorapaxar | AY 77 | PAR-2-IN-1 | AC-55541 | VKGILS-NH2 Acetate |
Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Inhibitor Library | NO PAINS Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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