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Submit ReviewFHT 1015
说明： Potent and selective SMARCA4/2 inhibitor
化学名： (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
纯度： ≥95% (HPLC)
生物活性 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.
许可信息
Sold under license from Foghorn Therapeutics Inc.
技术数据 for FHT 1015
| 分子量 | 555.69 |
| 公式 | C25H25N5O4S3 |
| 储存 | Store at -20°C |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for FHT 1015
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 55.57 | 100 |
制备储备液 for FHT 1015
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for FHT 1015
参考文献 for FHT 1015
参考文献是支持产品生物活性的出版物。
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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关键词: 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
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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