BIIB021

Inhibitor of HSP90AA1, HSP90AB1

Structure

Information

  • HSP90AA1
  • HSP90AB1
  • Inhibitor
  • 400-1000 nM

In Vitro Validations

Uniprot ID: P07900
Target Class: Other post-translational modification
Target SubClass: Chaperone
Potency: Ki
Potency Value: 1.7 ± 0.4 nM
Potency Assay: fluorescence polarization competition assay
PDB ID for probe-target interaction (3D structure): 3O6O
Structure-activity relationship: yes
Target aliases:
Heat shock protein HSP 90-alpha, HSPCA, HSPC1, HSP ...

DOI Reference: 10.1021/jm050752; 10.1158/0008-5472

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Tested for selectivity against protein kinases and ATPases, with no significant inhibition detected at 10 uM

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SERP ratings and comments


SERP Ratings

In Cell Rating
In Model Organisms

(last updated: 9 Dec 2021 )

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

BII021 is a N-terminal HSP90 inhibitor and its worth to note that C-terminal HSP90 inhibitors also reported.

(last updated: 27 Mar 2022 )