FHT 1015

Tocris Bioscience | Catalog # 7644

Potent and selective SMARCA4/2 inhibitor
Tocris Bioscience
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Key Product Details

Description

Potent and selective SMARCA4/2 inhibitor

Product Description

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.

Licensing Information

Sold under license from Foghorn Therapeutics Inc.

Product Specifications for FHT 1015

Molecular Weight

555.69

Formula

C25H25N5O4S3

Storage

Store at -20°C

Purity

≥95% (HPLC)

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

CAS Number

2368903-18-6

PubChem ID

139371523

InChI Key

FAYSHZVDWADZMD-NRFANRHFSA-N

SMILES

CSCC[C@@H](C(NC1=NC(C2=CC(C3=CC=NC=C3)=CC=C2)=CS1)=O)NC(C4=CN(S(C)(=O)=O)C=C4)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

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Solubility

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 55.57 100

Preparing Stock Solutions for FHT 1015

The following data is based on the product molecular weight 555.69.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.80 mL 9.00 mL 18.00 mL
5 mM 0.36 mL 1.80 mL 3.60 mL
10 mM 0.18 mL 0.90 mL 1.80 mL
50 mM 0.04 mL 0.18 mL 0.36 mL

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Background References

References are publications that support the biological activity of the product.

  • Centore Discovery of novel BAF inhibitors for the treatment of transcription factor-driven cancers. Cancer Res.

Product Documents for FHT 1015

Certificate of Analysis

To download a Certificate of Analysis, please enter a lot or batch number in the search box below.

Product Specific Notices for FHT 1015

For research use only

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