CCT020312

Product NameCCT020312
CAS324759-76-4
MFC31H30Br2N4O2
MW650.4
EINECS
MOL File324759-76-4.mol

Chemical Properties

Density	1.48±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	DMSO: soluble
form	A solid
pka	9.43±0.70(Predicted)
color	Light yellow to yellow
SMILES	O=C1C(C2=NN(C(CCN(CC)CC)=O)C(C3=CC=C(Br)C=C3)C2)=C(C4=CC=CC=C4)C5=CC(Br)=CC=C5N1

Safety Information

WGK Germany	WGK 2
Storage Class	11 - Combustible Solids

Usage And Synthesis

Uses

CCT020312 is a selective EIF2AK3/PERK activator. CCT020312 elicits EIF2A phosphorylation in cells.

Biological Activity

CCT020312 is a selective activator of EIF2AK3/PERK. It induces phosphorylation of EIF2A in cells.

in vitro

CCT020312 treatment effectively inhibits cell proliferation (as measured at 96 hours) even if treatment is for 2 hours only with subsequent compound washout, indicating that CCT020312 is capable of eliciting durable rather than transient cytostasis.

in vivo

Treatment of 15-week-old wildtype mice with the PERK activator CCT020312 (1-5 mg/kg; i.p.; once daily for 3 days) leads to increased levels of phosphorylated PERK and NRF2 in brain homogenates^[2].
P301S transgenic mice treated with CCT020312 (2 mg/kg; i.p.; once daily for 6 weeks) performes significantly better in Morris water maze^[2].

Animal Model:	9-week-old P301S tau transgenic mice^[2]
Dosage:	2 mg/kg
Administration:	Intraperitoneal injection; once daily for 6 weeks
Result:	P301S transgenic mice treated with CCT020312 performed significantly better in Morris water maze.

target

EIF2AK3/PERK.

References

[1] Stockwell SR, et al.Mechanism-based screen for G1/S checkpoint activators identifies a selective activator of EIF2AK3/PERK signalling. PLoS One. 2012;7(1):e28568. DOI:10.1371/journal.pone.0028568
[2] Bruch J, et al. PERK activation mitigates tau pathology in vitro and in vivo. EMBO Mol Med. 2017 Mar;9(3):371-384. DOI:10.15252/emmm.201606664