IC261

Catalog No.S8237 Batch:S823701

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Technical Data

Formula

C18H17NO4
Molecular Weight 311.33 CAS No. 186611-52-9
Solubility (25°C)* In vitro DMSO 62 mg/mL (199.14 mM)
Water Insoluble
Ethanol 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 IC261 (SU-5607) is a novel inhibitor of CK1. The IC50 of IC261 for CK1 is 16 μM and for Cdk5 is 4.5 mM.
Targets
CK1 [4]
16 μM
In vitro IC261 leads to a p53-dependent arrest of the cells with a DNA content of 4 N. It can produce effects on cell cycle progression that are indistinguishable from an established spindle poison and are dependent on the p53 status of the cells[1].
In vivo Intrathecal injection of a CK1 inhibitor IC261 attenuates neuropathic pain behaviors. CK1 inhibitors are found to be effective in reducing spinal excitatory response elicited by the presynaptic electrical stimulation only in neuropathic mice[2]. Targeting CK1 isoforms by IC261 influences both pancreatic tumour cell growth and apoptosis sensitivity in vitro and the growth of induced tumours in vivo[3].

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    MEFs

  • Concentrations

    1 μM

  • Incubation Time

    12 h, 24 h, 48 h

  • Method

    Cultures of MEFs of di€erent genotypes (p53+/+, p53+/-, p53-/-) are treated with the inhibitor IC261 in the low micromolar range (1 μM). After 12, 24, 48 hours exposure, the effects of IC261 on cell cycle distribution are measured by flow cytometry.
Animal Study:

[2]
  • Animal Models

    Male C57BL/6J mice

  • Dosages

    0.1-1 nmol

  • Administration

    intrathecal administration

Selleck's IC261 has been cited by 7 publications

Elevated FBXW10 drives hepatocellular carcinoma tumorigenesis via AR-VRK2 phosphorylation-dependent GAPDH ubiquitination in male transgenic mice [ Cell Rep, 2023, 42(7):112812] PubMed: 37450367
Distinct properties of adipose stem cell subpopulations determine fat depot-specific characteristics [ Cell Metab, 2022, S1550-4131(21)00542-8] PubMed: 35021043
Establishment and characterization of immortalized sweat gland myoepithelial cells [ Sci Rep, 2022, 12(1):7] PubMed: 34997030
Phosphorylation of β-catenin Ser60 by polo-like kinase 1 drives the completion of cytokinesis [ EMBO Rep, 2021, e51503] PubMed: 34585824
The GSK-3β-FBXL21 Axis Contributes to Circadian TCAP Degradation and Skeletal Muscle Function [ Cell Rep, 2020, 32(11):108140] PubMed: 32937135
Aurora kinase A promotes hepatitis B virus replication and expression. [ Antiviral Res, 2019, 170:104572] PubMed: 31376425
PP5 (PPP5C) is a phosphatase of Dvl2 [ Sci Rep, 2018, 8(1):2715] PubMed: 29426949

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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.