AMZ30
Based on 1 publication(s) in Google Scholar
AMZ30 is selective protein phosphatase methylesterase-1(PME-1) inhibitor with IC50s of 600 nM and 3.5 µM in human cell lysates and in HEK 293T cells, respectively. AMZ30 shows >100-fold selectivity relative to other serine hydrolases. AMZ30 reduces the demethylated form of PP2A in living cells. AMZ30 attenuates muscle cell differentiation. AMZ30 increases the resistance of U87MG and U251MG glioblastoma cells to t-BHP-induced oxidative stress. AMZ30can be used for the study of glioblastoma.
For research use only. We do not sell to patients.
- Purity: 99.10%
- CAS No.: 1313613-09-0
- Formula: C19H12FN3O6S2
- Molecular Weight:461.44
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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Publications Citing Use of MedChemExpress (MCE) AMZ30
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Customer Validation & Images
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Biological Activity
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Cell Line
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Type | Value | Description | References |
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| HEK-293T | IC50 |
3.5 μM
Compound: 28, AMZ30
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Inhibition of PME1 binding to FP-rhodamine in HEK293T cells after 1 hr by fluorescence polarization activity-based protein profiling assay
Inhibition of PME1 binding to FP-rhodamine in HEK293T cells after 1 hr by fluorescence polarization activity-based protein profiling assay
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[PMID: 21639134] |
| HEK-293T | IC50 |
600 nM
Compound: 28, AMZ30
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Inhibition of PME1 binding to FP-rhodamine in human HEK293T cells after 45 mins by fluorescence polarization activity-based protein profiling assay
Inhibition of PME1 binding to FP-rhodamine in human HEK293T cells after 45 mins by fluorescence polarization activity-based protein profiling assay
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[PMID: 21639134] |
AMZ30 (50 μM, 24 h) treatment of C2C12 cells significantly inhibits the expression of muscle cell differentiation markers myosin heavy chain (MyHC) and myogenin during differentiation, while moderately but significantly increasing the level of the PP2A catalytic subunit[1].
AMZ30 (10-40 μM, 24 h) treatment of C2C12 cells transfected with the AP-1 reporter gene significantly reduces AP-1 reporter gene activity[1].
AMZ30 (50 μM, 24 h) mediates inhibition of Ppme1 and attenuates MAP kinase signaling in C2C12 cells[1].
AMZ30 (20 μM, 1 h pretreatment) increases the resistance of U87MG and U251MG glioblastoma cells to t-BHP-induced oxidative stress[2].
AMZ30 (20 μM, 1 h pretreatment) abolishes the sensitizing effect of PME-1 overexpression in U87MG cells and eliminates the increased sensitivity of U251MG shGFP cells to t-BHP-induced oxidative stress[2].
AMZ30 (20 μM, 1 h) significantly reduces the demethylated form of PP2A and increases the methylated form in HEK 293T cells stably overexpressing PME-1[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:C2C12 cells
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Concentration:50 μM
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Incubation Time:24 h
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Result:Inhibited the expression of muscle cell differentiation markers myosin heavy chain (MyHC) and myogenin.
Increased the level of the PP2A catalytic subunit.
Reduced the phosphorylation levels of ERK1/2 and p38.
Increased c-Jun protein level without a significant change in the ratio of phosphorylated c-Jun to total c-Jun.
Reduced the phosphorylation status of Akt.
Chemical Information
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CAS No. 1313613-09-0
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Appearance Solid
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Molecular Weight 461.44
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Formula C19H12FN3O6S2
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SMILES
O=S(C1=CC([N+]([O-])=O)=CC=C1)(N2C(/C=C(S(=O)(C3=CC=C(F)C=C3)=O)\C#N)=CC=C2)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Front Aging Neurosci
Leucine Carboxyl Methyltransferase Downregulation and Protein Phosphatase Methylesterase Upregulation Contribute Toward the Inhibition of Protein Phosphatase 2A by α-Synuclein. [Abstract]2018 Jun 8:10:173. PMID: 29950985
AMZ30 purchased from MedChemExpress. Usage Cited in: Front Aging Neurosci. 2018 Jun 8:10:173. [Abstract]
Immunoblotting and quantifications of deMe-PP2A, total-PP2A, p-α-syn, α-syn, and Flag-LCMT-1 in vector, α-syn, α-syn+LCMT-1, α-syn+AMZ30, α-syn+PP2Ac, and α-syn+siPME-1 group. β-tubulin is used as a loading control.
Solvent & Solubility
DMSO : 100 mg/mL (216.71 mM; Need ultrasonic; 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (283 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[1]. Labuzan SA, et al. Inhibition of protein phosphatase methylesterase 1 dysregulates MAP kinase signaling and attenuates muscle cell differentiation. Gene. 2020 May 20;739:144515. [Content Brief]
[2]. Guffens L, et al. PME-1 sensitizes glioblastoma cells to oxidative stress-induced cell death by attenuating PP2A-B55α-mediated inactivation of MAPKAPK2-RIPK1 signaling. Cell Death Discov. 2023 Jul 27;9(1):265. [Content Brief]
[3]. Bachovchin DA, et al. Discovery and optimization of sulfonyl acrylonitriles as selective, covalent inhibitors of protein phosphatase methylesterase-1. J Med Chem. 2011 Jul 28;54(14):5229-36. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1671 mL | 10.8356 mL | 21.6713 mL | 54.1782 mL |
| 5 mM | 0.4334 mL | 2.1671 mL | 4.3343 mL | 10.8356 mL | |
| 10 mM | 0.2167 mL | 1.0836 mL | 2.1671 mL | 5.4178 mL | |
| 15 mM | 0.1445 mL | 0.7224 mL | 1.4448 mL | 3.6119 mL | |
| 20 mM | 0.1084 mL | 0.5418 mL | 1.0836 mL | 2.7089 mL | |
| 25 mM | 0.0867 mL | 0.4334 mL | 0.8669 mL | 2.1671 mL | |
| 30 mM | 0.0722 mL | 0.3612 mL | 0.7224 mL | 1.8059 mL | |
| 40 mM | 0.0542 mL | 0.2709 mL | 0.5418 mL | 1.3545 mL | |
| 50 mM | 0.0433 mL | 0.2167 mL | 0.4334 mL | 1.0836 mL | |
| 60 mM | 0.0361 mL | 0.1806 mL | 0.3612 mL | 0.9030 mL | |
| 80 mM | 0.0271 mL | 0.1354 mL | 0.2709 mL | 0.6772 mL | |
| 100 mM | 0.0217 mL | 0.1084 mL | 0.2167 mL | 0.5418 mL |
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