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PS-1145

Catalog No. T3094 CAS 431898-65-6

Synonyms: IKK Inhibitor X

PS-1145 (IKK Inhibitor X) is a specific IKK inhibitor with IC50 of 88 nM.

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PS-1145, CAS 431898-65-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 42.00
2 mg	In stock	$ 58.00
5 mg	In stock	$ 84.00
10 mg	In stock	$ 157.00
25 mg	In stock	$ 297.00
50 mg	In stock	$ 585.00
100 mg	In stock	$ 836.00
500 mg	In stock	$ 1,720.00
1 mL * 10 mM (in DMSO)	In stock	$ 93.00

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Purity: 99.63%

Purity: 97.06%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	PS-1145 (IKK Inhibitor X) is a specific IKK inhibitor with IC50 of 88 nM.
Targets&IC50	IKKϵ:88 nM
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.
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.
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)

Synonyms	IKK Inhibitor X
Molecular Weight	322.75
Formula	C17H11ClN4O
CAS No.	431898-65-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 60 mg/mL (185.9 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 2 mg/mL(6.19 mM), Heating is recommended.

References and Literature

1. Hideshima T, et al. J Biol Chem. 2002, 277(19), 16639-16647. 2. Lupino E, et al. J Immunol. 2012, 188(6), 2545-2555. 3. Rajmani RS, et al. Cell Biol Int. 2015, 39(11), 1317-1328.

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library Inhibitor Library Anti-Cancer Active Compound Library Anti-Neurodegenerative Disease Compound Library HIF-1 Signaling Pathway Compound Library Bioactive Compounds Library Max Anti-Aging Compound Library Anti-Cancer Compound Library Anti-Prostate Cancer Compound Library Immunology/Inflammation Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

PS-1145 431898-65-6 Apoptosis NF-Κb IκB/IKK I kappa B kinase PS1145 inhibit IKK PS 1145 IKK Inhibitor X IκB kinase Inhibitor inhibitor

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