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Chemical Structure| 186611-52-9 Chemical Structure| 186611-52-9

Structure of IC261
CAS No.: 186611-52-9

Chemical Structure| 186611-52-9

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IC261 is an ATP-competitive inhibitor of CK1 with IC50s about 1 μM for CK1δ and CK1ε, 16 μM for CK1α.

Synonyms: SU5607

4.5 *For Research Use Only !

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Product Citations

Product Citations

Yuan, Feifei ; Li, Donghe ; Guo, Mengzhou ; Fang, Tingting ; Sun, Jialei ; Qi, Feng , et al.

Abstract: Hepatocellular carcinoma (HCC) is one of the most deadly cancers worldwide that responds poorly to existing therapies. The Casein kinase 1 (CK1) isoforms CK1δ and CK1ε are reported to be highly expressed in several tumor types, and both genetic and pharmacological inhibition of CK1δ/ε activity has deleterious effects on tumor cell growth. IC261, an CK1δ/ε selectively inhibitor, shows anti-tumor effect against pancreatic tumor and glioblastoma, but its role in HCC remains poorly characterized. In our research, IC261 displayed time- and dose-dependent inhibition of HCC cell proliferation, and induced G2/M arrest and cell apoptosis in vitro. However, the anti-tumor effects of IC261 was independent of CK1δ/ε. Additionally, IC261 was verified to induce centrosome fragmentation during mitosis independent of CK1δ status, and intraperitoneal injection of IC261 to HCCLM3 xenograft models inhibited tumor growth. Taken together, our data indicated that IC261 has therapeutic potential for HCC.

Keywords: IC261 ; Casein kinase 1 d/ε ; Hepatocellular carcinoma ; Cell cycle ; Centrosome fragmentation

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Product Details of IC261

CAS No. :186611-52-9
Formula : C18H17NO4
M.W : 311.33
SMILES Code : O=C1NC2=C(C=CC=C2)/C1=C\C3=C(OC)C=C(OC)C=C3OC
Synonyms :
SU5607
MDL No. :MFCD00118156
InChI Key :JBJYTZXCZDNOJW-JLHYYAGUSA-N
Pubchem ID :5288600

Safety of IC261

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of IC261

DNA
Hedgehog

Isoform Comparison

Biological Activity

Target
  • CK1

    CK1, IC50:16 μM

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.21mL

0.64mL

0.32mL

16.06mL

3.21mL

1.61mL

32.12mL

6.42mL

3.21mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1

References

 

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