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ABL127 | ABL127 : Covalent Inhibitor of PPME1
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (1 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
PPME1
  • IC50:4.2 nM
  • INH:500 nM
  • IC50:11.1 nM
  • IC50:6.4 nM
Covalent Inhibitor
100 nM, up to 10 uM

Selectivity

In Cell Selectivity Assessment
Potency Assay Off-Target:
Combined mass spec LC revealed complete and selective in situ inhibition of PME-1 by ABL127 with no ...

Potency
Cellular
In Vitro

PPME1

Mode of Action: Covalent Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1073/pnas.1015248108

In Vivo Validations

Mouse
Dose: 50 mg/Kg
Route of delivery: Intraperitoneal

DOI Reference: 10.1073/pnas.1015248108

Negative Control Compounds

CANSAR1531928
Notes: ent-ABL127 (R-enantiomer) IC50 450 nM in vitro

Chemical Information

Molecular Formula C17H20N2O5
SMILEs COC(=O)N1C(=O)[C@@](c2ccccc2)(C2CCCC2)N1C(=O)OC
InChI InChI=1S/C17H20N2O5/c1-23-15(21)18-14(20)17(13-10-6-7-11-13,19(18)16(22)24-2)12-8-4-3-5-9-12/h3-5,8-9,13H,6-7,10-11H2,1-2H3/t17-/m1/s1
Molecular weight 332.14 Da
AlogP 2.6641000000000012
HBond acceptors 7
HBond donors --
Atoms 44

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Expert Reviews

by SERP
(on 18 Nov 2023 )
Cellular Use Rating
In Model Organisms
ABL127 is a highly potent PME1 inhibitor (apparent IC50 ~10 nM in cells). Treatment with ABL127 affords a partial decrease in PPME1 methylation. ~100 nM recommended dose for cell based studies, with off...
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