Home Metabolism Casein Kinase inhibitor IC261

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IC261 Casein Kinase inhibitor

Cat.No.S8237

IC261 (SU-5607) is a novel inhibitor of CK1. The IC50 of this compound for CK1 is 16 μM and for Cdk5 is 4.5 mM.
IC261 Casein Kinase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 311.33

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Quality Control

Batch: S823701 DMSO]62 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.75%
99.75

Solubility

In vitro
Batch:

DMSO : 62 mg/mL (199.14 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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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 311.33 Formula

C18H17NO4

 Storage (From the date of receipt)
CAS No. 186611-52-9 Download SDF Storage of Stock Solutions

Synonyms SU-5607 Smiles COC1=CC(=C(C(=C1)OC)C=C2C3=CC=CC=C3NC2=O)OC

Mechanism of Action

Targets/IC50/Ki
CK1
16 μM
In vitro
IC261 leads to a p53-dependent arrest of the cells with a DNA content of 4 N. This compound 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.
In vivo
Intrathecal injection of a CK1 inhibitor IC261 attenuates neuropathic pain behaviors. This compound is found to be effective in reducing spinal excitatory response elicited by the presynaptic electrical stimulation only in neuropathic mice. Targeting CK1 isoforms by this chemical influences both pancreatic tumour cell growth and apoptosis sensitivity in vitro and the growth of induced tumours in vivo.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/11572969/

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