| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg | |||
| Other Sizes |
| Targets |
EIF2AK3[1]. PERK[2].
CCT020312 targets eukaryotic elongation factor 2 kinase (eEF2K). eEF2K is a kinase that phosphorylates eEF2 on threonine 56, inhibiting its activity and thus reducing protein synthesis. By inhibiting eEF2K, CCT020312 prevents the phosphorylation of eEF2, maintaining protein synthesis. This can affect cell growth, survival, and response to stress. |
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| ln Vitro |
Upon subjecting HT29 cells to CCT020312 for a whole day, a concentration-dependent decrease in P-S608-pRB signal was observed, exhibiting a linear response ranging from 1.8 to 6.1 μM [1]. Even while CCT020312 treatment only lasted for two hours and the substance was later removed, it successfully suppressed cell proliferation (measured at 96 hours), suggesting that CCT020312 is capable of eliciting long-lasting rather than temporary cellular inhibition [1]. After subjecting HT29 cells to a 24-hour treatment of 10 μM CCT020312, the amount of G1/S cyclins D1, D2, E, and A as well as the CDK catalytic subunit CDK2 were reduced. Conversely, the levels of the CDK inhibitor p27KIP1 were elevated in these cells [1].
CCT020312 is a small-molecule inhibitor of eEF2K. It inhibits eEF2K activity, preventing the phosphorylation of eEF2. This maintains protein synthesis and has been shown to affect cell growth and survival in cellular models. CCT020312 is used as a research tool to study eEF2K function. |
| ln Vivo |
Upon administering the PERK activator CCT020312 (1–5 mg/kg; intraperitoneally; once daily for three days) to 15-week-old wild-type mice, brain homogenates demonstrated elevated levels of phosphorylated PERK and NRF2 [2]. In the Morris water maze, P301S transgenic mice given CCT020312 (2 mg/kg; i.p.; once daily for 6 weeks) fared far better [2].
Specific in vivo activity data for CCT020312 is not extensively detailed in the available literature. As a research compound, its in vivo effects are primarily studied in the context of eEF2K inhibition and its impact on protein synthesis, cell growth, and cancer. Further studies are needed to fully characterize its in vivo efficacy and pharmacokinetic properties. |
| Enzyme Assay |
CCT020312's activity as an eEF2K inhibitor is assessed using in vitro kinase assays that measure its ability to inhibit eEF2K-mediated phosphorylation of eEF2. IC50 values are determined from dose-response curves. Selectivity profiling against other kinases is performed to evaluate its specificity.
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| Cell Assay |
Cellular assays for CCT020312 involve treating cells with the compound and measuring eEF2 phosphorylation and protein synthesis. eEF2 phosphorylation is assessed by Western blot analysis using phospho-specific antibodies. Protein synthesis is measured using puromycin incorporation or other assays. Cell proliferation and viability are also assessed.
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| Animal Protocol |
Animal/Disease Models: 9weeks old P301S tau transgenic mice[2]
Doses: 2 mg/kg Route of Administration: intraperitoneal (ip)injection; one time/day for 6 weeks Experimental Results: P301S transgenic mice treated with CCT020312 performed Dramatically better in Morris water maze. In vivo animal model protocols for CCT020312 would involve its administration to animal models to study the role of eEF2K in various diseases. The compound's effects on protein synthesis, cell growth, and disease phenotypes would be assessed. |
| ADME/Pharmacokinetics |
Specific pharmacokinetic data for CCT020312 is not extensively detailed in the available literature. As a small molecule inhibitor, its pharmacokinetic properties would need to be evaluated in preclinical studies.
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| Toxicity/Toxicokinetics |
The toxicological profile of CCT020312 has not been extensively characterized. As a research compound, it is intended for research use only and not for human consumption. Standard safety assessments would be required for clinical development.
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| References | |
| Additional Infomation |
CCT020312 (CAS# 324759-76-4) is a research compound used to study eEF2K function in protein synthesis, cell growth, and cancer. It is a small-molecule inhibitor of eEF2K. It is not approved for clinical use and is supplied as a research chemical.
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| Molecular Formula |
C31H30BR2N4O2
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|---|---|
| Molecular Weight |
650.403505802155
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| Exact Mass |
648.073
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| CAS # |
324759-76-4
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| PubChem CID |
3108148
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| Appearance |
Light yellow to yellow solid powder
|
| LogP |
5.6
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
39
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| Complexity |
950
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| Defined Atom Stereocenter Count |
0
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| SMILES |
BrC1C=CC(=CC=1)C1CC(C2C(NC3C=CC(=CC=3C=2C2C=CC=CC=2)Br)=O)=NN1C(CCN(CC)CC)=O
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| InChi Key |
OAXDKXMGESZLKV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C31H30Br2N4O2/c1-3-36(4-2)17-16-28(38)37-27(20-10-12-22(32)13-11-20)19-26(35-37)30-29(21-8-6-5-7-9-21)24-18-23(33)14-15-25(24)34-31(30)39/h5-15,18,27H,3-4,16-17,19H2,1-2H3,(H,34,39)
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| Chemical Name |
6-bromo-3-[3-(4-bromophenyl)-2-[3-(diethylamino)propanoyl]-3,4-dihydropyrazol-5-yl]-4-phenyl-1H-quinolin-2-one
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| Synonyms |
CCT 020312 CCT-020312 CCT020312
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~153.75 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.20 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.08 mg/mL (3.20 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.20 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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