SGC-SMARCA-BRDVIII

Inhibitor of SMARCA2, SMARCA4, PBRM1

Structure

SERP Rating

In Cells

(3 ratings)

In Model Organisms

(0 ratings)

note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars.

Information

SMARCA2
SMARCA4
PBRM1

Inhibitor

up to 10 uM
Reviewer recommended concentration: 500-1000 nM

Additional Data

SGC Chemical Probe Collection

Probe Availability:

MCULE

In Vitro Validations

Uniprot ID: P51531

Target Class: Epigenetic

Target SubClass: Bromodomain

Potency: Kd

Potency Value: 35 nM

Potency Assay: ITC

PDB ID for probe-target interaction (3D structure): --

Structure-activity relationship: yes

Target aliases:

Probable global transcription activator SNF2L2, SN ...

DOI Reference: 10.1021/acs.jmedchem.0c01242

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency end-point : KD PB1(2) 3655 nM, PB1(3) 1963 nM

Probe Selectivity in Vitro:

Selectivity of the SGC-SMARCA-BRDVIII probe within the bromodomain families was confirmed by an in-house thermal shift panel containing 25 bromodomains. Outside Target Family: No activity was also observed on 85 protein kinases screened in an in-house DSF panel.

Probe Selectivity in Cell:

SGC-SMARCA-BRDVIII is non-toxic and does not influence cell growth at a dose of 10 µM as indicated in the NCI-60 human tumor cell lines screen, and can therefore ideally be used in cell differentiation assays.

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SERP ratings and comments

SERP Ratings

In Cell Rating

(last updated: 29 Mar 2021 )

SERP Ratings

In Cell Rating

SERP Comments:

SGC-SMARCA-BRDVIII and control compound SGC-BRDVIII-NC comprise high quality small molecules for the evaluation of the inhibition of SMARCA2/4 and PBRM1.

(last updated: 30 Mar 2021 )

SERP+ Ratings

In Cell Rating

SERP+ Comments:

No direct target engagement data is available even though the functions has been tested in different cell lines.

(last updated: 22 Mar 2023 )