IMP-1088

Inhibitor of NMT1, NMT2

Structure

Information

Protein target names: NMT1, NMT2

Mechanism of action: Inhibitor

In Vitro Validations

Uniprot ID: P30419
Target Class: Other post-translational modification
Target SubClass: Acyltransferase
Potency: IC 50
Potency Value: < 1 nM
Potency Assay: Fluorogenic detection of the CoASH (NMT inhibition assay)
PDB ID for probe-target interaction (3D structure): 5MU6
Structure-activity relationship: yes
Target aliases:
Glycylpeptide N-tetradecanoyltransferase 1, NMT, N ...

DOI Reference: 10.1016/j.chembiol.2019.03.006

Uniprot ID: P30419
Target Class: Other post-translational modification
Target SubClass: Acyltransferase
Potency: Kd
Potency Value: 0.210 nM
Potency Assay: SPR
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Glycylpeptide N-tetradecanoyltransferase 1, NMT, N ...

DOI Reference: 10.1016/j.chembiol.2019.03.006

In Cell Validations

In Vivo Data

No in Vivo Validations

I have extra information to add

SERP ratings and comments


SERP Ratings

In Cell Rating

Comments:

The cited reference (10.1016/j.chembiol.2019.03.006)  is an excellent comparative study of the 5 cmpds that have been used as NMT probes and shows clearly and conclusively that only IMP-1088 and IMP-366 ( DDD85646 ) are suitable to use as orthogonal probes in vitro and in cells for the human NMT1 and NMT2 targets.  Of these two, IMP-1088 is clearly the more potent probe cmpd.

(last updated: 18 Jun 2021 )

SERP Ratings

In Cell Rating
In Model Organisms

Comments:

Proteomic data suggest that this compound has high specificity for NMT1 and NMT2, but genetic evidence for target specificity is still awaited. There is no information on its usefulness in animal models.

(last updated: 30 Jun 2021 )

SERP Ratings

In Cell Rating

Comments:

There is no selectivity data indicating that this compound inhibits the intended target(s) without inhibiting other acyltransferases.  Looking at the chemical structure, I would anticipate activity on other target classes outside of the acyltransferases. In addition, there is no negative control compound that would raise the comfort level of using this compound as a chemical probe.

(last updated: 7 Jul 2021 )