ABT-100

Protein target name:

FNTB

Mechanism of action:

Inhibitor

Recommended Concentration for use in cells:

10-1000 nM

Probe Availability

MedChemExpress

Probe Information

Target and Probe Information

Target Details

Target class:

FPTB

Probe Details

Chemical Probes Portal ID:

CPP1838

Probe alias:

ABT100, ABT-409100

PubChem CID:

6451154

ChEMBL ID:

CHEMBL4586794

SMILES string:

N#CC1=CC(C2=CC=C(OC(F)(F)F)C=C2)=C(OC[C@](O)(C3=CC=C(C#N)C=C3)C4=CN=CN4C)C=C1

InChi Key:

HEUVRFNVTLGKMZ-SANMLTNESA-N

Control compound:

ABT-108

Validation in Cells and Model Organisms

In vitro validation

On target activity

Potency:

IC50

0.05 nM

Potency assay:

Scintillation proximity assay

Structure-activity relationship:

yes see DOI:10.1097/00001813-200511000-00004

Off target activity

Probe Selectivity in Vitro:

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

In cell validation

On target activity in cells

Potency in cells:

EC50

0.73 nM

Potency assay (cells):

Ras and Rap 1A processing assay

Off target activity in cells

Probe Selectivity in Cell:

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

In vivo validation

Organism:

RatDog

Dose:

5 mg/kg (Rat)2.5 mg/kg (Dog)up to 25 mg/kg (PO)

Route of delivery:

OralIntravenous

Plasma half life:

2.3 h (Rat)6.8 h (Dog)

Systemic clearance:

1.2 (Rat) and 0.34 (Dog) l/h/kg

Fraction of probe bound to plasma protein:

15.1 %30.7 %35.1 %

Cmax:

0.08 ug/ml0.74 ug/ml

Primary Reference

Reference (doi):

10.1158/1078-0432.CCR-04-2041 10.1158/1078-0432.CCR-04-2386 10.1016/j.healun.2004.06.006 10.1126/science.1124875 10.1097/00001813-200511000-00004

Reference (PMID):

15837760 15930366 16143263 16484451 16222147

External Resources

Available data:

SGC additional analysis

Under Review

This probe is in the process of SAB review. Please continue to check back for new reviews and commentary.

Part of the Donated Chemical Probes initiative from SGC.

SAB Rating

Rating for use in Cells

2 review(s)

Rating for use in Model Organisms

2 review(s)

SAB Members

SAB 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.

Jun 4 2020 - 3:37pm

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.

Aug 4 2021 - 10:00pm

ABT-100

Probe Availability

Probe Information

Target Details

FPTB

Probe Details

In vitro validation

In cell validation

In vivo validation

Primary Reference

External Resources

Supporting Organizations

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ABT-100

Probe Availability

Probe Information

Target Details

FPTB

Probe Details

In vitro validation

In cell validation

In vivo validation

Primary Reference

External Resources

Supporting Organizations

Interested in supporting the portal?