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Postion:Product Catalog >Biochemical Engineering>Inhibitors>Nuclear transcription factor (NF-κB)>IκB / IKK inhibitors>LY2409881 trihydrochloride
LY2409881 trihydrochloride
  • LY2409881 trihydrochloride

LY2409881 trihydrochloride NEW

Price $45 $64 $98
Package 1mg 2mg 5mg
Min. Order:
Supply Ability: 10g
Update Time: 2024-11-19

Product Details

Product Name: LY2409881 trihydrochloride CAS No.: 946518-60-1
Purity: ≥95% Supply Ability: 10g
Release date: 2024/11/19

Product Introduction

Bioactivity

NameLY2409881 trihydrochloride
DescriptionLY2409881 trihydrochloride is a novel specific inhibitor of IKK2 (IC50: 30 nM); IC50 for IKK1 and other common kinases is at least one log higher.
Cell ResearchCytotoxicity is evaluated using the CellTiter-Glo Reagent according to the manufacturer's manual. Experiments are carried out in 96-well plates, with each treatment in triplicate. Samples are taken at typically 24, 48, and 72 hours after treatment. Cytotoxicity is expressed by the decreasing percentage of live cells in each treatment relative to the untreated control from the same experiment. IC50 for each cell line is calculated using the CalcuSyn Version 2.0 software.(Only for Reference)
Kinase AssayCYP3A activity is assessed using the probe reactions, midazolam-1′-hydroxylation and testosterone 6β-hydroxylation. For reversible inhibition, incubations (37°C, 10 min) are composed of (final concentrations): potassium phosphate buffer (100 mM, pH 7.4), β-NADPH (1 mM), magnesium chloride (5 mM), microsomal protein (0.025 mg/mL), probe substrate (1 μM midazolam or 25 μM testosterone), LCL161 (0, 0.5, 1, 5, 10, 25, 50, or 100 μM) and organic solvent (0.2% acetonitrile for midazolam, 0.2% methanol for testosterone). After a 3-minute preincubation, the reactions are initiated by addition of β-NADPH and terminated by addition of acetonitrile (two volumes). Reactions are previously shown to be linear with respect to time and protein concentration (results not shown) with midazolam and testosterone turnover of 8.7±1.3% (n=3) and 2.6±0.20%, respectively. Formation of 1′-hydroxymidazolam and 6β-hydroxytestosterone is determined by LC-MS/MS as described below[3].
In vitroLY240988 was moderately toxic to ovarian cancer SKOV3 cell line. In diffuse large B-cell lymphoma cells, LY2409881 inhibited activated NF-?B, concentration- and time-dependently inhibiting cell growth and causing apoptosis. In SUDHL2 cells, LY2409881 inhibited cell growth synergistically with cyclophosphamide and adriamycin, but had no synergistic effect on LY1 cells. In SUDHL22 and LY1 cells, histone deacetylase inhibitor romidepsin synergized with LY2409881 to inhibit cell growth.
In vivoLY240988 was moderately toxic to ovarian cancer SKOV3 cell line. In diffuse large B-cell lymphoma cells, LY2409881 inhibited activated NF-?B, concentration- and time-dependently inhibiting cell growth and causing apoptosis. In SUDHL2 cells, LY2409881 inhibited cell growth synergistically with cyclophosphamide and adriamycin, but had no synergistic effect on LY1 cells. In SUDHL22 and LY1 cells, histone deacetylase inhibitor romidepsin synergized with LY2409881 to inhibit cell growth.
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility InformationDMSO : 16 mg/mL (26.9 mM)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : < 1 mg/mL (insoluble or slightly soluble)
KeywordsLY 2409881 | LY2409881 trihydrochloride | LY-2409881 Trihydrochloride | LY2409881 Trihydrochloride | Inhibitor | IκB kinase | Apoptosis | IKK | LY-2409881 | inhibit | I kappa B kinase | LY-2409881 trihydrochloride | LY 2409881 Trihydrochloride
Inhibitors RelatedStavudine | 5-Fluorouracil | Acetylcysteine | Kaempferol | Myricetin | Sodium 4-phenylbutyrate | L-Ascorbic acid | Dextran sulfate sodium salt (MW 4500-5500) | Metronidazole | Sorafenib | Tributyrin | Lidocaine hydrochloride
Related Compound LibrariesBioactive Compound Library | Kinase Inhibitor Library | Anti-Ovarian Cancer Compound Library | Anti-Breast Cancer Compound Library | Pyroptosis Compound Library | Inhibitor Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library | Anti-Liver 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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