计算溶液所需的质量、体积或浓度。
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
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文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
FX1 是一种选择性的BCL6 BTB抑制剂，IC50为35 μM。在所检测的50多种激酶中，FX1 具有高选择性，10 μM的FX1 不能显著地抑制这些激酶。FX1 可诱导凋亡。
Information
FX1 FX1 is a selective BCL6 BTB inhibitor with an IC50 value of 35 μM in reporter assays. FX1 shows great selectivity against a panel of 50 different kinases. 10 μM FX1 fails to significantly inhibit of any of these kinases. FX1 induces apoptosis .
In vitro
FX1 disrupted formation of the BCL6 repression complex, reactivated BCL6 target genes, and mimicked the phenotype of mice engineered to express BCL6 with corepressor binding site mutations. FX1 suppressed ABC-DLBCL cells in vitro and in vivo, as well as primary human ABC-DLBCL specimens ex vivo. FX1 is specific to BCL6 and binds with a greater affinity than the natural BCL6 ligand SMRT. FX1 almost invariantly induced significant derepression of these genes(BCL6 target genes CASP8, CD69, CXCR4, CDKN1A, and DUSP5) as compared with vehicle in 2 independent DLBCL cell lines. FX1 was more than 100-fold more powerful than the previous generation of BCL6 inhibitors represented by 79-6, and 300-fold more potent than the recently reported binding of the antibiotics rifamycin and rifabutin (KD ~1 mM).
In vivo
Low doses of FX1 induce regression of established tumors in mice bearing DLBCL xenografts. The half-life is estimated to be approximately 12 hours for FX1 in SCID mice. No signs of toxicity, inflammation, or infection are evident from H&E-stained sections of lung, gastrointestinal tract, heart, kidney, liver, spleen, and bone marrow of the fixed organs from mice treated with FX1 compared with vehicle. Peripheral blood counts and serum chemistry in FX1-treated mice are also examined and they remain within normal parameters. FX1 causes profound and significant suppression of DLBCLs in DLBCL xenografts, and indeed not only prevented growth of the xenografts but in addition causes these tumors to shrink from their initial volume. The maximal effect is already achieved by the lower 25 mg/kg dose. TUNEL and Ki-67 staining shows that FX1 also induced more apoptosis and growth arrest than 79-6, respectively.
Cell Data
cell lines：GFP-LC3 HeLa cells
Concentrations：50 μM
Incubation Time：30 min
Powder Purity:≥99%
规格
英文别名
3-Thiazolidinepropanoic acid, 5-(5-chloro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)-4-oxo-2-thioxo-, (5Z)-
规格或纯度
10mM in DMSO
英文名称
FX1
生化机理
FX1 是一种选择性 BCL6 BTB 抑制剂，在报告实验中的 IC50 值为 35 μM。FX1 对 50 种不同的激酶具有很高的选择性。10 μM 的 FX1 无法显著抑制其中任何一种激酶。FX1 可诱导细胞凋亡。
储存条件
-80℃储存
运输条件
特低温运输
名称和识别符
分子类型
小分子
Isomeric SMILES
C1=CC2=NC(=O)C(=C2C=C1Cl)C3=C(N(C(=S)S3)CCC(=O)O)O
PubChem CID
分子量
368.82
技术文档
高级数据
安全和危险性（GHS）
象形图
信号词
Warning
危险声明
H302: 吞食有害
预防措施声明
P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。
RIDADR
NONHforallmodesoftransport
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| 批号(Lot Number) | 证书类型 | 货号 |
|---|---|---|
 F2419504 |
分析证书 | F408269 |
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