PKC-theta inhibitor

Catalog No.S6577 Batch:S657702

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Technical Data

Formula

C20H25F3N6O3
Molecular Weight 454.45 CAS No. 736048-65-0
Solubility (25°C)* In vitro DMSO 91 mg/mL (200.24 mM)
Ethanol 5 mg/mL (11.0 mM)
Water Insoluble
* <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.)

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Biological Activity

Description PKC-theta inhibitor (compound 20) inhibits PKC-θ with an IC50 of 18 nM.
Targets
PKCθ [1]
18 nM
In vitro

PKC-theta inhibitor (compound 20) inhibits PKC-θ.
In vivo

Compound 20 is a potent inhibitor of Protein Kinase C θ (PKC-θ). It improves muscle performance in the mdx mice model of Duchenne muscular dystrophy.

Protocol (from reference)

Cell Assay:

[3]
  • Cell lines

    MN9D cells

  • Concentrations

    5 μM

  • Incubation Time

    24 h

  • Method

    PKCθ inhibitor was dissolved in DMSO at 5 mM and diluted to the working concentration (5 μM) and cells were incubated with PKCθ inhibitor was 24 h.
Animal Study:

[3]
  • Animal Models

    C57BL/6 mice

  • Dosages

    10 mg/kg

  • Administration

    i.p.

Selleck's PKC-theta inhibitor has been cited by 5 publications

Hyperprogression of cutaneous T cell lymphoma after anti-PD-1 treatment [ JCI Insight, 2023, 8(4)e164793] PubMed: 36649072
Black Ginseng Extract Exerts Potentially Anti-Asthmatic Activity by Inhibiting the Protein Kinase Cθ-Mediated IL-4/STAT6 Signaling Pathway [ Int J Mol Sci, 2023, 24(15)11970] PubMed: 37569348
Cooperation of Striatin 3 and MAP4K4 promotes growth and tissue invasion [ Commun Biol, 2022, 5(1):795] PubMed: 35941177
4,4'-Dimethoxychalcone regulates redox homeostasis by targeting riboflavin metabolism in Parkinson's disease therapy [ Free Radic Biol Med, 2021, 174:40-56] PubMed: 34332078
The MAP4K4-STRIPAK complex promotes growth and tissue invasion in medulloblastoma [ bioRxiv, 2021, 10.1101/2021.05.07.442906] PubMed: None

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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.