Luminespib

Inhibitor of HSP90AA1, HSP90AB1

Structure

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Information

Protein target names: HSP90AA1, HSP90AB1

Mechanism of action: Inhibitor

Primary References:

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Probe Availability:

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

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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 )