Home NF-κB IκB/IKK inhibitor PS-1145 For research use only.

PS-1145

PS-1145 is a specific IKK inhibitor with IC50 of 88 nM.

PS-1145 Chemical Structure

PS-1145 Chemical Structure

CAS No. 431898-65-6

Purity & Quality Control

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

PS-1145 Related Products

Signaling Pathway

IκB/IKK Signaling Pathways

IκB/IKK Signaling Pathway

Biological Activity

Description PS-1145 is a specific IKK inhibitor with IC50 of 88 nM.
Targets
IKK [1]
88 nM
In vitro
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. PS-1145 also inhibits paracrine MM cell growth and IL-6 secretion in BMSCs triggered by MM cell adherence. [1] In human primary CD4(+) T cells, PS-1145 abrogates cell proliferation and impairs the activation of NF-κB and AP-1 transcription factors by engagement of CD3 and CD28 coreceptor. [2]
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 Cell lines MM.1S, U266, and RPMI8226 cell lines
Concentrations ~50 μM
Incubation Time 48 h
Method

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.
In Vivo
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. [3]
Animal Research Animal Models Male Wistar rats with 7,12-dimethylbenz[α]anthracene-induced skin tumor
Dosages ~50 mg/kg
Administration i.v.

Chemical Information & Solubility

Molecular Weight 322.75 Formula

C17H11ClN4O
CAS No. 431898-65-6 SDF Download PS-1145 SDF
Smiles C1=CC(=CN=C1)C(=O)NC2=CC(=CC3=C2NC4=C3C=CN=C4)Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 64 mg/mL ( (198.29 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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