CS640
Based on 1 Customer Validation
CS640 (Compound 19) is a chemical probe and a calmodulin-dependent kinase inhibitor. CS640 inhibits CaMK1D, CaMK1B, CaMK1A, CaMK1G, MEK5, RIPK4, mLK3 and PIP5K1, with IC50 values of 8, 3, 1, 1, 25 nM, 5.69, 2.75 and 11.2 μM, respectively. CS640 blocks Aβ-induced hyperphosphorylation of tau protein at the Thr181 site, but fails to protect primary mouse cortical neurons from Aβ-induced toxic damage. CS640 is applicable to research related to Alzheimer's disease.
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- Purity: 99.48%
- CAS No.: 2388506-83-8
- 화학식: C21H31N7O
- 분자량:397.52
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보관:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MDA-MB-231 | IC50 |
0.011 μM
Compound: 19
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Inhibition of HA-tagged CAMK1D (unknown origin) expressed in human MDA-MB-231 cells assessed as reduction in CAMK1D autophosphorylation measured after 4 hrs by Western blot analysis
Inhibition of HA-tagged CAMK1D (unknown origin) expressed in human MDA-MB-231 cells assessed as reduction in CAMK1D autophosphorylation measured after 4 hrs by Western blot analysis
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[PMID: 32433887] |
CS640 (1 nM-10 μM; 24 h) shows no significant neurotoxicity in mouse primary cortical neurons at concentrations up to 1 μM, but is highly toxic at 10 μM[2].
CS640 (10 nM-1 μM; 24 h) does not consistently rescue mouse primary cortical neurons from Aβ1-42-induced toxicity at concentrations up to 1 μM[2].
CS640 (1 μM; 12 h) reverses Aβ1-42-induced hyperphosphorylation of tau at Thr181 in mouse primary cortical neurons, reducing phosphorylated tau levels to near control levels[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Bioavailability | AUC0-∞ | Cmax | T1/2 | CL | Vss |
|---|---|---|---|---|---|---|---|---|
| Mice[1] | 2 mg/kg | i.v. | / | 2454 ng·h/mL | 503 ng/mL | 8.3 h | 13.7 mL/min/kg | 7.46 L/kg |
| Mice[1] | 10 mg/kg | p.o. | 44 % | 5408 ng·h/mL | 387 ng/mL | 5.9 h | / | / |
| Mice[1] | 20 mg/kg | p.o. | 118 % | 28923 ng·h/mL | 2015 ng/mL | 5.9 h | / | / |
| Mice[1] | 40 mg/kg | p.o. | 100 % | 49220 ng·h/mL | 3792 ng/mL | 6.2 h | / | / |
| Rat[1] | 2 mg/kg | i.v. | / | 913 ng·h/mL | 391 ng/mL | 7.7 h | 36.5 mL/min/kg | 18.5 L/kg |
| Rat[1] | 10 mg/kg | p.o. | 67.5 % | 3058 ng·h/mL | 199 ng/mL | 7.0 h | / | / |
Chemical Information
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CAS No. 2388506-83-8
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Appearance Solid
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분자량 397.52
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화학식 C21H31N7O
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Color White to light yellow
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SMILES
NC(C1=CN=C(N2C[C@H](CCC2)N)N=C1NC3=CC(C(C)C)=NC(C(C)C)=C3)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 5 mg/mL (12.58 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Fromont C, et al. Discovery of Highly Selective Inhibitors of Calmodulin-Dependent Kinases That Restore Insulin Sensitivity in the Diet-Induced Obesity in Vivo Mouse Model. J Med Chem. 2020;63(13):6784-6801. [Content Brief]
[2]. Grant P, et al. Effects of Specific Inhibitors for CaMK1D on a Primary Neuron Model for Alzheimer's Disease. Molecules. 2021;26(24):7669. Published 2021 Dec 18. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5156 mL | 12.5780 mL | 25.1560 mL | 62.8899 mL |
| 5 mM | 0.5031 mL | 2.5156 mL | 5.0312 mL | 12.5780 mL | |
| 10 mM | 0.2516 mL | 1.2578 mL | 2.5156 mL | 6.2890 mL |
CS640 Related Classifications
HY-148907 Related Classifications
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