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CCT020312

Chemical Structure : CCT020312

CAS No.: 324759-76-4

CCT020312 (CCT-020312;CCT 020312)

Catalog No.: PC-35976Not For Human Use, Lab Use Only.

CCT020312 (CCT-020312) is a small molecule PERK activator, inhibits pRB phosphorylation in HT29 colon carcinoma cells with EC50 of 5.1 uM.

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Biological Activity

CCT020312 (CCT-020312) is a small molecule PERK activator, inhibits pRB phosphorylation in HT29 colon carcinoma cells with EC50 of 5.1 uM.
CCT020312 shows no effect on the activity on CDK4/cyclin D or CDK1/cyclin B, effectively inhibits cell proliferation of HT29 colon carcinoma cells with IC50 of 3.1 uM (96 h).
CCT020312 elicits EIF2A phosphorylation in cells, does not induce full ER stress signalling; also reduced tau phosphorylation, tau conformational change and 4-repeat tau isoforms, and increased cell viability in cultured human neurons.
CCT020312  significantly improved memory and locomotor function, reduced tau pathology, and prevented dendritic spine and motoneuron loss in P301S tau mice.

Physicochemical Properties

M.Wt 650.415
Formula C31H30Br2N4O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

6-Bromo-3-[5-(4-bromo-phenyl)-1-(3-diethylamino-propionyl)-4,5-dihydro-1H-pyrazol-3-yl]-4-phenyl-1H-quinolin-2-one

References

1. Stockwell SR, et al. PLoS One. 2012;7(1):e28568. doi: 10.1371/journal.pone.0028568.

2. Bruch J, et al. EMBO Mol Med. 2017 Mar;9(3):371-384.

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