CCT020312

Catalog No.E1030

For research use only.

CCT020312 is a selective PERK (EIF2AK3) activator with an EC50 of 5.1 μM. CCT020312 can be used for the selective activation of EIF2A-mediated translation control.

CCT020312 Chemical Structure

CAS No. 324759-76-4

Purity & Quality Control

Choose Selective PERK Inhibitors

Biological Activity

Description

CCT020312 is a selective PERK (EIF2AK3) activator with an EC50 of 5.1 μM. CCT020312 can be used for the selective activation of EIF2A-mediated translation control.

Targets
PERK [1]
()
5.1 μM(EC50)
In vitro

CCT020312 treatment effectively inhibits cell proliferation. Treatment of HT29 cells and HCT116 cells with CCT020312 shows inhibition of pRB phosphorylation at comparable concentrations with half-maximal reduction of pRB phosphorylation. CCT020312 acts selectively to instigate proliferation inhibition through an EIF2A phosphorylation-associated translation inhibition.[1]

In vivo

CCT020312 suppresses tumor growth and reduces the protein levels of CDK4 and CDK6 in MDA-MB-453 xenograft mice. CCT020312 increases the levels of p-eIF2α, ATF4, and CHOP, and decreases the levels of p-AKT and p-mTOR. Thus, CCT020312, a selective eIF2α/PERK activator, inhibits TNBC viability and proliferation by activating the PERK/eIF2α/ATF4/CHOP pathway and inactivating the AKT/mTOR pathway in vivo.[2]

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: HT29 cells
  • Concentrations: 7 µM
  • Incubation Time: 24 h
  • Method:

    HT29 cells seeded in 96-well plates are exposed to 7 µM CCT020312 for 24 hours. Ser608 pRB phosphorylation was quantified using the cell-based immunoassay for the detection of pRB-P-Ser608 as employed for the primary screen.

  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(153.75 mM)
Ethanol 100 mg/mL
(153.75 mM)
Water 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.

Chemical Information

Molecular Weight 650.40
Formula

C31H30Br2N4O2

CAS No. 324759-76-4
Storage 3 years -20°C powder
2 years -80°C in solvent

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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