| Identification | Back Directory | [Name]
CCT020312 | [CAS]
324759-76-4 | [Synonyms]
CCT020312
2(1H)-Quinolinone, 6-bromo-3-[5-(4-bromophenyl)-1-[3-(diethylamino)-1-oxopropyl]-4,5-dihydro-1H-pyrazol-3-yl]-4-phenyl- | [Molecular Formula]
C31H30Br2N4O2 | [MOL File]
324759-76-4.mol | [Molecular Weight]
650.4 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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.
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Store at -20°C | [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 |
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| Company Name: |
BOC Sciences
|
| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
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