Home Cell Cycle PERK activator CCT020312 For research use only.

CCT020312

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

CCT020312 Chemical Structure

CAS: 324759-76-4

Selleck's CCT020312 has been cited by 2 publications

Purity & Quality Control

Batch: Purity: 99.74%
99.74

CCT020312 Related Products

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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
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]
Cell Research 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.
In Vivo
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]

Chemical Information & Solubility

Molecular Weight 650.40 Formula

C31H30Br2N4O2
CAS No. 324759-76-4 SDF --
Smiles CCN(CC)CCC(=O)N1N=C(CC1C2=CC=C(Br)C=C2)C3=C(C4=CC=CC=C4)C5=C(NC3=O)C=CC(=C5)Br
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (153.75 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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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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.

Handling Instructions

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