Chemical Probes logo

Luminespib

Inhibitor of HSP90AA1, HSP90AB1

Structure

Information

  • HSP90AA1
  • HSP90AB1
  • Inhibitor

In Vitro Validations

Uniprot ID: P07900
Target Class: Other post-translational modification
Target SubClass: Chaperone
Potency: IC50
Potency Value: 7.8 nM
Potency Assay: Fluorescence polarisation (FP) competitive binding assay
PDB ID for probe-target interaction (3D structure): 2VCI,  2UWD,  2BSM
Structure-activity relationship: yes, see details here https://doi.org/10.1021/jm701018h
Target aliases:
Heat shock protein HSP 90-alpha, HSPCA, HSPC1, HSP ...

DOI Reference: 10.1158/1078-0432.CCR-05-0518

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency end-point : IC50 GRP94 535 nM, TRAP-1 85 nM
Potency assay (off target): Fluorescence polarisation (FP) competitive binding assay
Probe Selectivity in Vitro:
At 10 uM there is no inhibition of human HSP72 ATPase or decatenation activity of human topoisomerase II and little or no activity against a range of 13 kinases. In a screen of 14 additional enzymes and 67 receptors, NVP-AUY922 exhibited >50% inhibitory activity at 10 uM against only 6 receptors and 1 enzyme; further profiling showed NVP-AUY922 to be >50-fold selective for HSP90.
I have extra information to add

SERP ratings and comments

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

AUY922 targets members of the heat shock protein 90 (Hsp90) family. This molecule binds to the N-terminal nucleotide-binding sites of Hsp90s. It is worth noting that there are other possible binding sites and mechanisms for inhibiting this target (e.g. targeting the C-terminal dimerization domain) and the pharmacology associated with these mechanisms may not be equivalent. 

(last updated: 3 Jul 2020 )

SERP Ratings

In Cell Rating
In Model Organisms

(last updated: 5 Sept 2020 )

SERP Ratings

In Cell Rating
In Model Organisms

(last updated: 10 Nov 2020 )