Home NF-κB IκB/IKK inhibitor PS-1145

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PS-1145 IκB/IKK inhibitor

Cat.No.S7691

PS-1145 is a specific IKK inhibitor with IC50 of 88 nM.
PS-1145 IκB/IKK inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 322.75

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Quality Control

Batch: S769101 DMSO]64 mg/mL]false]Ethanol]2 mg/mL]false]Water]Insoluble]false Purity: 99.82%
99.82

Solubility

In vitro
Batch:

DMSO : 64 mg/mL (198.29 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 322.75 Formula

C17H11ClN4O

 Storage (From the date of receipt)
CAS No. 431898-65-6 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles C1=CC(=CN=C1)C(=O)NC2=CC(=CC3=C2NC4=C3C=CN=C4)Cl

Mechanism of Action

Targets/IC50/Ki
IKK
88 nM
In vitro

PS-1145 blocks TNFalpha-induced NF-kappaB activation through inhibition of IkappaBalpha phosphorylation, and blocks the protective effect of IL-6 against Dex-induced apotosis. This compound also inhibits paracrine MM cell growth and IL-6 secretion in BMSCs triggered by MM cell adherence. In human primary CD4(+) T cells, it abrogates cell proliferation and impairs the activation of NF-κB and AP-1 transcription factors by engagement of CD3 and CD28 coreceptor.

Kinase Assay
Kinase assay
PS-1145 are dissolved in DMSO and stored at −20 °C until use. Ki value of this compound 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 this compound 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 vivo

In male Wistar rats with 7,12-dimethylbenz[α]anthracene-induced skin tumor, PS-1145 (50 mg/kg, i.v.) enhances tumor cell apoptosis by up-regulating p53, activating caspases and down regulating NF-κB and VEGF factor, and thus induces the tumor progression.

References

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