ABT-100

Inhibitor of FNTB

Structure

Information

  • FNTB
  • Inhibitor
  • 10-1000 nM

In Vitro Validations

Uniprot ID: P49356
Target Class: Other post-translational modification
Target SubClass: Transferase
Potency: IC50
Potency Value: 0.05 nM
Potency Assay: Scintillation proximity assay
PDB ID for probe-target interaction (3D structure): --
Structure-activity relationship: yes see DOI:10.1097/00001813-200511000-00004
Target aliases:
Protein farnesyltransferase subunit beta, FNTB, FN ...

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

>100 000-fold selective for FNTB over the closely related enzyme PGGT1B (GGTase I)

Probe Selectivity in Cell:

No activity in panel of 75 off-targets @10 µM; closest hit: phencyclidine PCP receptor IC50 = 3 μM

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SERP ratings and comments


SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

ABT-100 has been investigated as a novel farnesyltransferase inhibitor in vitro and in vivo. ABT-100 is a highly potent (IC50 = 0.05 nmol/L) inhibitor of the farnesyltransferase and displays >100,000-fold selectivity relative to geranylgeranyltransferase I.

(last updated: 4 Jun 2020 )

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

ABT-100 appears to be a potent and selective probe compound for the investigation of FNTB  biology.  Selectivity against the closest related target appears good, though there are little data in the peer-reviewed literature to describe off-target selectivity claims or the SAR relationships. The presence of an inactive tool compound (ABT-108) for use as control is claimed though again, the identity or properties of this claimed derivative are not clearly reported in the literature for verification. However, independent validation is available for these factors via the SGC at https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/ABT-100. This additional data, alongside an accompanying data package from the originators at Abbvie, significantly enhances the probe’s value and helps support its recommendation as a credible tool molecule. 

(last updated: 24 Nov 2020 )

Portal Comments

In a 2023 study, Hu et al. evaluated ABT-100 in live-cell assays for Phospholipidosis induction, cautioning about adverse effects at concentrations near 1 uM. (DOI: 10.1016/j.chembiol.2023.09.003)

(last updated: 7 Nov 2023)