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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.
Sold under license from Foghorn Therapeutics Inc.
Technical Data for FHT 1015
|Storage||Store at -20°C|
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|
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|
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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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Epigenetics Scientific Review
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.
Epigenetics in Cancer Poster
This poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.
Rheumatoid Arthritis Poster
Rheumatoid arthritis (RA) is a chronic destructive inflammatory autoimmune disease that results from a breakdown in immune tolerance, for reasons that are as yet unknown. This poster summarizes the pathology of RA and the inflammatory processes involved, as well as describing some of the epigenetic modifications associated with the disease and the potential for targeting these changes in the discovery of new treatments.