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Submit ReviewFHT 1015
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% (HPLC)
Biological Activity for FHT 1015
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.
Technical Data for FHT 1015
| M. Wt | 555.69 |
| Formula | C25H25N5O4S3 |
| Storage | Store at -20°C |
| Purity | ≥95% (HPLC) |
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for FHT 1015
| 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 will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.8 mL | 9 mL | 18 mL |
| 5 mM | 0.36 mL | 1.8 mL | 3.6 mL |
| 10 mM | 0.18 mL | 0.9 mL | 1.8 mL |
| 50 mM | 0.04 mL | 0.18 mL | 0.36 mL |
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Product Datasheets for FHT 1015
References for FHT 1015
References are publications that support the biological activity of the product.
Centore et al (2021) Discovery of novel BAF inhibitors for the treatment of transcription factor-driven cancers. Cancer Res. 81
If you know of a relevant reference for FHT 1015, please let us know.
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Keywords: FHT 1015, FHT 1015 supplier, FHT1015, inhibitor, inhibits, smarca, SMARCA4, brg, BRG1, SMARCA2, BRM, SWItch, SWI, SNF, BRG, Brahma, associated, factors, disrupts, BAF, SOX10-MITF, Chromatin, Remodeling, Complexes, Bromodomains, Other, ATPases, 7644, Tocris Bioscience
Citations for FHT 1015
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