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- 详细信息
- 技术资料
- 保存条件:
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 英文名:
FHD-286
- 库存:
货期:1-2天
- 供应商:
MedChemExpress LLC
- 规格:
10 mM * 1 mL/1 mg/5 mg/10 mg
| 规格: | 10 mM * 1 mL | 产品价格: | ¥4580.0 |
|---|---|---|---|
| 规格: | 1 mg | 产品价格: | ¥1800.0 |
| 规格: | 5 mg | 产品价格: | ¥3700.0 |
| 规格: | 10 mg | 产品价格: | ¥5400.0 |
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FHD-286
CAS No. : 2671128-05-3
MCE 国际站:FHD-286
产品活性:FHD-286 是一种选择性具有口服活性的 SMARCA4/SMARCA2 ATP 酶 (BRG1 和 BRM) 抑制剂。FHD-286 在急性髓系白血病等 BAF 相关疾病的研究中具有潜力。
研究领域:Epigenetics
作用靶点:Epigenetic Reader Domain
In Vitro: FHD-286 (10 to 100 nM) for 7 days induces differentiation followed by loss of viability of AML cell lines and PD AML cells with MLL rearrangement (r), mutant (mt) NPM1 and chromosome 3q26 lesions (with EVI1 overexpression). Treatment with FHD-286 causes whole-genome, concordant, up- or down-regulations in ATAC-Seq peaks and RNA-Seq-determined mRNA expressions of specific loci, associated with significant reduction in the gene-sets of targets of MYC, mTORC1, E2F, Interferon-gamma, IL6-JAK-STAT3, as well as of inflammatory response and oxidative phosphorylation genes. QPCR analyses determined significant reduction in mRNA expression of MYC, SPI1 and BCL2 genes. Mass spectrometry on AML cell lysates treated with FHD-286 showed log2 fold-reductions in c-Myc, SPI1, MEF2C, KMT2C and CDK4 (in MOLM13) and in EVI1, c-Myb, CDK6 and c-Myc (in AML191) cells.
In Vivo: FHD-286 (1.5 mg/kg; oral administration; for 10 days) increases in IFNγ and Th1-type chemokine CXCL10 levels.
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