[CAS NO. 1073529-41-5] ABL127
PRODUCTS SPECIFICATIONS [1073529-41-5]
DESCRIPTION [1073529-41-5]
Overview
| MDL | MFCD28053514 |
|---|---|
| Molecular Weight | 332.35 |
| Molecular Formula | C17H20N2O5 |
| SMILES | O=C(N1N(C(OC)=O)[C@@](C2=CC=CC=C2)(C3CCCC3)C1=O)OC |
Summary
ABL127 is a selective and covalent inhibitor of protein methylesterase 1 ( PME-1 ) with IC 50 s of 6.4 nM and 4.2 nM in HEK293T and MDA-MB-231 cells, respectively.
IC50 & Target
IC50: 6.4 nM (PME-1 in HEK293T), 4.2 nM (PME-1 in MDA-MB-231) [1]
In Vitro
Three described PME-1 inhibitors are tested in this assay and a thermal shift with 100 μM ABL127 is detected. Using 25 or 50 μM ABL127 also shows a shift in protein melting temperature. It is found that treatment of Ishikawa cells with ABL127 and AMZ-30 significantly decreases cell proliferation similarly to depletion of PME-1 with shRNA. It is also found that treatment of ECC-1 cells with ABL127 or AMZ-30 affects cell invasion in a dose-dependent manner. The treatment of EC cells with ABL127 leads to a significant ~45 % increase in protein phosphatase 2A (PP2A) activity, while treatment with AMZ-30 leads to a modest ~10 % increase in PP2A activity [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
No significant decrease in tumor burden can be assessed in these pilot studies [1] . Gel-based profiles indicate that brain PME-1 is inactivated by ABL127, but overlapping serine hydrolase activities preclude a confident assessment of the extent of inactivation [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Oil
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Pure form | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 100 mg/mL ( 300.89 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.0089 mL | 15.0444 mL | 30.0888 mL |
| 5 mM | 0.6018 mL | 3.0089 mL | 6.0178 mL |
| 10 mM | 0.3009 mL | 1.5044 mL | 3.0089 mL |
References
- [1] Pusey M, et al. Inhibition of protein methylesterase 1 decreased cancerous phenotypes in endometrial adenocarcinoma cell lines and xenograft tumor models. Tumour Biol. 2016 Sep;37(9):11835-11842.
- [2] Bachovchin DA, et al. Academic cross-fertilization by public screening yields a remarkable class of protein phosphatase methylesterase-1 inhibitors. Proc Natl Acad Sci U S A. 2011 Apr 26;108(17):6811-6.
