SGC-SMARCA-BRDVIII

Inhibitor of SMARCA2, SMARCA4, PBRM1

Structure

Information

  • SMARCA2
  • SMARCA4
  • PBRM1
  • Inhibitor
  • up to 10 uM
  • Reviewer recommended concentration: 500-1000 nM

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 )