A-893 |
| Catalog No.GC30503 |
A-893 est un inhibiteur cellulaire actif de la méthyltransférase SMYD2, avec une IC50 de 2,8 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1868232-32-9
Sample solution is provided at 25 µL, 10mM.
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A-893 is a cell-active inhibitor of Methyltransferase SMYD2, with an IC50 of 2.8 nM.
The ratio of p53K370me1 to overall p53 levels is reduced, as expected, by treatment with either A-893 or AZ505. While this unexpectedly depicts a more robust response with AZ505, further dissection of the data provides clarity into the origin of this. While overall p53 levels are unaffected by A-893, a surprising >3-fold increase is observed with AZ505. Analysis of p53K370me1 levels reveals that inhibitor A-893 exhibited 42% reduction in the methyl mark, while AZ-505 is slightly less effective at 28% reduction[1].
[1]. Sweis RF, et al. Discovery of A-893, A New Cell-Active Benzoxazinone Inhibitor of Lysine Methyltransferase SMYD2. ACS Med Chem Lett. 2015 Apr 29;6(6):695-700.
Cell experiment: | Human A549 lung carcinoma cells are chosen due to their high SMYD2 expression levels and wild-type p53 status. After 18 h of treatment with 10 μM of compound (e.g. A-893), changes in p53K370me1 are measured along with changes to overall p53 levels[1]. |
References: [1]. Sweis RF, et al. Discovery of A-893, A New Cell-Active Benzoxazinone Inhibitor of Lysine Methyltransferase SMYD2. ACS Med Chem Lett. 2015 Apr 29;6(6):695-700. | |
| Cas No. | 1868232-32-9 | SDF | |
| Canonical SMILES | O=C(CCNCCC1=CC(Cl)=C(Cl)C=C1)N(C2CCCCC2)CCNC[C@H](O)C3=CC=CC(N4)=C3OCC4=O | ||
| Formula | C29H38Cl2N4O4 | M.Wt | 577.54 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7315 mL | 8.6574 mL | 17.3148 mL |
| 5 mM | 0.3463 mL | 1.7315 mL | 3.463 mL |
| 10 mM | 0.1731 mL | 0.8657 mL | 1.7315 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 18 reference(s) in Google Scholar.)
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