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FHT 1015

Catalog #: 7644 Datasheet
Catalog # Availability Size / Price Qty
7644/2
FHT 1015 | CAS No. 2368903-18-6 | Bromodomain Inhibitors
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Description: Potent and selective SMARCA4/2 inhibitor

Chemical Name: (S)-1-(Methylsulfonyl)-N-[4-(methylthio)-1-oxo-1-[[4-[3-(pyridin-4-yl)phenyl]thiazol-2-yl]amino]butan-2-yl]-1H-pyrrole-3-carboxamide

Purity: ≥95%

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Biological Activity

FHT 1015 is a potent and selective allosteric inhibitor of SMARCA4/SMARCA2 ATPase (also known as BRG1/BRM respectively) of the BAF (BRG/Brahma-associated factors) complex, with IC50s of ≤ 10 nM. Exhibits selectivity for SMARCA4/SMARCA2 over related CHD4 (IC50 of > 400 μM). Mutations in I1143 on SMARCA4 and I1173 on SMARCA2 render these proteins resistant to inhibition by FHT 1015. The compound induces lineage-specific changes in chromatin accessibility in different cancer cell lines, preventing binding of cancer-associated transcription factors, SOX10 and MITF transcription factors.

Technical Data

M.Wt:
555.69
Formula:
C25H25N5O4S3
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥95%
Storage:
Store at -20°C
CAS No:
2368903-18-6

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
Sold under license from Foghorn Therapeutics Inc.

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