BIIB021

Inhibitor of HSP90AA1, HSP90AB1

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(2 ratings)

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Probe BIIB021 is in the process of SERP review.

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Information

HSP90AA1
HSP90AB1

Inhibitor

400-1000 nM

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Probe Availability:

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 )