A covalent inhibitor of PME-1
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AMZ30

Item No. 42052

Technical Information
Formal Name
(2E)-2-[(4-fluorophenyl)sulfonyl]-3-[1-[(3-nitrophenyl)sulfonyl]-1H-pyrrol-2-yl]-2-propenenitrile
CAS Number
1313613-09-0
Synonyms
  • ML-136
Molecular Formula
C19H12FN3O6S2
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMSO: Sparingly soluble: 1-10 mg/ml
SMILES
O=S(C1=CC([N+]([O-])=O)=CC=C1)(N2C=CC=C2/C=C(S(C3=CC=C(F)C=C3)(=O)=O)\C#N)=O
InChi Code
InChI=1S/C19H12FN3O6S2/c20-14-6-8-17(9-7-14)30(26,27)19(13-21)11-15-4-2-10-22(15)31(28,29)18-5-1-3-16(12-18)23(24)25/h1-12H/b19-11+
InChi Key
GUCUORSUHTZMBW-YBFXNURJSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    AMZ30 is a covalent inhibitor of protein phosphatase methylesterase 1 (PME-1; IC50 = 0.6 µM).1 It reduces the levels of methylated protein phosphatase 2A (PP2A) in HEK293T cells stably overexpressing PME-1 when used at a concentration 20 µM. AMZ30 (210 µM) inhibits decreases in viability induced tert-butyl hydroperoxide (t-BHP) in U87MG and U-251MG glioblastoma cells.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Bachovchin, D.A., Zuhl, A.M., Speers, A.E., et alDiscovery and optimization of sulfonyl acrylonitriles as selective, covalent inhibitors of protein phosphatase methylesterase-1. J. Med. Chem. 54(14), 5229-5236 (2011).

    2. Guffens, L., Derua, R., and Janssens, V. PME-1 sensitizes glioblastoma cells to oxidative stress-induced cell death by attenuating PP2A-B55α-mediated inactivation of MAPKAPK2-RIPK1 signaling. Cell Death Discov. 9(1), 265 (2023).