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[CAS NO. 324759-76-4] CCT020312
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-119240 |
| Brand: | MCE |
| CAS: | 324759-76-4 |
Overview
| MDL | - |
|---|---|
| Molecular Weight | 650.40 |
| Molecular Formula | C31H30Br2N4O2 |
| SMILES | O=C1NC2=C(C(C3=CC=CC=C3)=C1C4=NN(C(C4)C5=CC=C(C=C5)Br)C(CCN(CC)CC)=O)C=C(C=C2)Br |
11 Publications Citing Use of MCE
- [1]Cell Metab. 2021 Mar 2;33(3):598-614.e7.
- [2]Cell Death Dis. 2020 Oct 13;11(10):847.
- [3]Cell Biol Toxicol. 2022 Jan 14.
- [4]Front Cell Dev Biol. 04 August 2021.
- [5]Oxid Med Cell Longev. 05 Aug 2022.
- [6]Int J Mol Sci. 2022 Dec 29;24(1):544.
- [7]Front Pharmacol. 2020 May 19;11:737.
- [8]J Transl Med. 2023 Feb 6;21(1):89.
- [9]Mediat Inflamm. 21 Aug 2021.
- [10]Biochem Biophys Res Commun. 557 (2021) 316-322.
- [11]Research Square Print. December 29th, 2022.
Summary
CCT020312 is a selective EIF2AK3/PERK activator. CCT020312 elicits EIF2A phosphorylation in cells.
In Vitro
Treatment of HT29 cells with CCT020312 for 24 hours reveals a concentration-dependent loss of P-S608-pRB signal, with a linear response between 1.8 and 6.1 μM
[1]
.
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
[1]
.
Treatment of HT29 cells with 10 μM CCT020312 for 24 hours reduces the amount of the G1/S cyclins D1, D2, E and A as well as the CDK catalytic subunit CDK2 and increased the level of the CDK inhibitor p27KIP1 present in such cells
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| 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. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 100 mg/mL ( 153.75 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.5375 mL | 7.6876 mL | 15.3752 mL |
| 5 mM | 0.3075 mL | 1.5375 mL | 3.0750 mL |
| 10 mM | 0.1538 mL | 0.7688 mL | 1.5375 mL |
References
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