PS-1145

Catalog No.S7691 Batch:S769101

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Technical Data

Formula

C17H11ClN4O
Molecular Weight 322.75 CAS No. 431898-65-6
Solubility (25°C)* In vitro DMSO 64 mg/mL (198.29 mM)
Ethanol 2 mg/mL (6.19 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
1.07mg/ml Taking the 1 mL working solution as an example, add 50 μL of 21.3 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to make it clear. Volume up to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description PS-1145 is a specific IKK inhibitor with IC50 of 88 nM.
Targets
IKK [1]
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. 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]
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]

Protocol (from reference)

Kinase Assay:

[1]
  • 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 Assay:

[1]
  • 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.
Animal Study:

[3]
  • Animal Models

    Male Wistar rats with 7,12-dimethylbenz[α]anthracene-induced skin tumor

  • Dosages

    ~50 mg/kg

  • Administration

    i.v.

Customer Product Validation

Data from [Data independently produced by , , Redox Biol, 2017, 562-576]

Data from [Data independently produced by , , J Biol Chem, 2018, 293(19):7268-7280]

Selleck's PS-1145 has been cited by 4 publications

Identifying enhancers of innate immune signaling as broad-spectrum antivirals active against emerging viruses [ Cell Chem Biol, 2022, 29(7):1113-1125.e6] PubMed: 35728599
TRAF-interacting protein with forkhead-associated domain (TIFA) transduces DNA damage-induced activation of NF-κB [Fu J J Biol Chem, 2018, 293(19):7268-7280] PubMed: 29581234
Sensitization of melanoma cells to alkylating agent-induced DNA damage and cell death via orchestrating oxidative stress and IKKβ inhibition. [Tse AK, et al. Redox Biol, 2017, 562-576] PubMed: 28107677
Pathogenic role of B-cell receptor signaling and canonical NF-κB activation in mantle cell lymphoma. [ Blood, 2016, 128(1):82-92] PubMed: 27127301

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.