Eleutherobin

Protein target name:

Tubulin

Mechanism of action:

Stabilization of microtubules

Recommended Concentration for use in cells:

5 uM

Probe Information

Target and Probe Information

Target Details

Target class:

Structural protein

Subclass:

Cytoskeleton

Probe Details

Chemical Probes Portal ID:

CPP1630

PubChem CID:

6918335

ChEMBL ID:

CHEMBL504387

SMILES string:

CC1=CC[C@@H]([C@@H]/2[C@H]1C[C@@H]([C@@]3(C=C[C@@](O3)(/C(=C2)/CO[C@H]4[C@H]([C@@H]([C@@H](CO4)O)O)OC(=O)C)OC)C)OC(=O)/C=C/C5=CN(C=N5)C)C(C)C

InChi Key:

XOPYFXBZMVTEJF-PDACKIITSA-N

Validation in Cells and Model Organisms

In vitro validation

On target activity

Potency:

EC50

6.2 uM

Potency assay:

In vitro calf brain tubulin polymerization assays,

Structure-activity relationship:

Yes, pharmacore reported (PMID: 10200249); see also PMID: 10412947.

In cell validation

On target activity in cells

Potency in cells:

IC50

2 uM

Potency assay (cells):

Displacement of 3H-taxol

Target engagement assay (cells):

Yes, displacement of taxol

Toxicity

Cytoxicity assay:

Yes

Notes on cytotoxicity:

In XTT assays, Eleutherobin was cytotoxic to HCT116 cells (IC50=10.7 uM); overexpression of P-glycoprotein efflux pump renders cells resistant. Cytotoxicity is due to an on-target induction of mitotic arrest.

Primary Reference

Reference (doi):

Cancer Res 10.1073/pnas.96.8.4256 10.1021/bi983023n Cancer Chemother Pharmacol

Reference (PMID):

9515790 10200249 10220336 10412947

Eleutherobin

Probe Information

Target Details

Probe Details

In vitro validation

In cell validation

Toxicity

Primary Reference

Supporting Organizations

Interested in supporting the portal?

Search form

Eleutherobin

Probe Information

Target Details

Probe Details

In vitro validation

In cell validation

Toxicity

Primary Reference

Supporting Organizations

Interested in supporting the portal?