IMP-1088

Inhibitor of NMT1, NMT2

Structure

SERP Rating

In Cells

(3 ratings)

In Model Organisms

(1 ratings)

note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars.

Information

NMT1
NMT2

Inhibitor

Probe Availability:

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

SERP 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

SERP 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

SERP 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 )