PS-1145 NEW
Price | $42 | $84 | $157 |
Package | 1mg | 5mg | 10mg |
Min. Order: | |
Supply Ability: | 10g |
Update Time: | 2024-11-19 |
Product Details
Product Name: PS-1145 | CAS No.: 431898-65-6 |
Purity: 99.63% | Supply Ability: 10g |
Release date: 2024/11/19 |
Product Introduction
Bioactivity
Name | PS-1145 |
Description | PS-1145 (IKK Inhibitor X) is a specific IKK inhibitor with IC50 of 88 nM. |
Cell Research | The inhibitory effect of PS-1145 on MM growth is assessed by measuring MTT dye absorbance of the cells. Cells from 48-h cultures are pulsed with 10 μL of 5 mg/ml MTT to each well for the last 4 h of 48-h cultures, followed by 100 μl of isopropanol containing 0.04N HCl. Absorbance is measured at 570 nm using a spectrophotometer. (Only for Reference) |
Kinase Assay | Kinase assay: PS-1145 are dissolved in DMSO and stored at ?20?°C until use. Ki value of PS-1145 against the IKK complex is determined by measuring Km ,?ATP against varying fixed concentration of the inhibitor. Briefly, partially purified IKK complex obtained from unstimulated HeLa S3 cells are pre-activated using the catalytic domain of MEKK1 expressed in sf9. Kinase activity is assessed using a biotinylated IκBα peptide (250 μM, RHDSGLDSMKD,Km ,peptide = 30 μM,K m ,?ATP = 10 μM) and phospho-[Ser32]-phosphoantibodies in an ELISA format with appropriate standard curve for quantification. For PS-1145 Ki measurement, the activated IKK complex is first preincubated in varying fixed concentration of the inhibitor (0.1–1 μM) at 25 °C for 1 h. Then apparentK m measurement for MgATP is performed at each discrete inhibitor concentration. |
In vitro | Administering 50 mg/kg of PS-1145 intravenously in male Wistar rats with DMBA-induced skin tumors resulted in the upregulation of p53 and activation of caspases, coupled with the downregulation of NF-κB and VEGF factors, thereby enhancing apoptosis in tumor cells. |
In vivo | PS-1145 inhibits the proliferation of primary human CD4(+) T cells and impedes the activation of NF-κB and AP-1 transcription factors through the cooperative engagement of CD3 and CD28 co-receptors. Additionally, PS-1145 blocks TNFalpha-induced NF-kappaB activation by inhibiting the phosphorylation of IkappaBalpha and disrupting the protective effect of IL-6 on Dex-induced apoptosis. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 50 mg/mL (154.92 mM), Sonication is recommended. H2O : < 1 mg/mL (insoluble or slightly soluble) Ethanol : 2 mg/mL (6.19 mM), Heating is recommended. |
Keywords | I kappa B kinase | PS1145 | inhibit | Apoptosis | IKK | PS 1145 | PS-1145 | IκB kinase | Inhibitor |
Inhibitors Related | Stavudine | 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 Libraries | Apoptosis Compound Library | Bioactive Compound Library | Anti-Neurodegenerative Disease Compound Library | Kinase Inhibitor Library | Inhibitor Library | Anti-Prostate Cancer Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library | Anti-Cancer Active 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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