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首页-小分子抑制剂&激动剂-Epigenetics-Bromodomain-FHT-1015
FHT-1015

Chemical Structure : FHT-1015

CAS No.: 2368903-18-6

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FHT-1015 (FHT1015)

货号: PC-20342Not For Human Use, Lab Use Only.

FHT-1015 (FHT1015) is a potent, selective inhibitor of SMARCA4 and SMARCA2 (BRG1 and BRM) with IC50 of 4 and 5 nM respectively, the ATPase component of the BAF complex.

规格 价格 库存 数量
10 mg ￥1380 In stock
25 mg ￥2480 In stock
50 mg ￥3980 In stock
100 mg ￥5880 In stock
250 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

FHT-1015 (FHT1015) is a potent, selective inhibitor of SMARCA4 and SMARCA2 (BRG1 and BRM) with IC50 of 4 and 5 nM respectively, the ATPase component of the BAF complex.
FHT-1015 displays no activity against the closely related ATPase CHD4 (IC50>400 uM).
SMARCA4 I1143M mutation confers resistance to FHT-1015.
FHT-1015 elicits lineage-specific effects on chromatin accessibility in treated cancer cells, causes reduced occupancy of master diseaseassociated transcription factors in 92-1 UM cells.
FHT-1015 affects the proliferation of many cancer cell types, and elicits rapid effects on UM, hematological cancer, and other cell lines inhibits the master transcription factor, SOX10, and its downstream transcriptional program, impacting cell survival and lineage specification.
FHT-1015 elicits tumor regression, demonstrating therapeutic utility in UM and perhaps other transcription factor-driven cancers.

物理化学性质&存储条件

分子量 555.69
分子式 C25H25N5O4S3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(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

参考文献

1. Elena Battistello, et al. Mol Cell. 2023 Mar 15;S1097-2765(23)00153-3.

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