CCT020312

Catalog No.E1030 Batch:E103001

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Technical Data

Formula

C31H30Br2N4O2
Molecular Weight 650.40 CAS No. 324759-76-4
Solubility (25°C)* In vitro DMSO 100 mg/mL (153.75 mM)
Ethanol 100 mg/mL (153.75 mM)
Water 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

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 Assay:

[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.

Selleck's CCT020312 has been cited by 2 publications

Acute Endoplasmic Reticulum Stress Suppresses Hepatic Gluconeogenesis by Stimulating MAPK Phosphatase 3 Degradation [ Int J Mol Sci, 2023, 24(21)15561] PubMed: 37958545
Ginsenoside Rg1 regulates autophagy and endoplasmic reticulum stress via the AMPK/mTOR and PERK/ATF4/CHOP pathways to alleviate alcohol‑induced myocardial injury [ Int J Mol Med, 2023, 52(1)56] PubMed: 37232350

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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.