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说明： High affinity and selective HIF-2α inhibitor
化学名： N-(3-Chloro-5-fluorophenyl)-4-nitro-2,1,3-benzoxadiazol-5-amine
纯度： ≥99% (HPLC)
生物活性 for TC-S 7009
TC-S 7009 is a high affinity and selective HIF-2α inhibitor (Kd = 81 nM). Binds to the HIF-2α PAS-B domain; disrupts HIF-2α-ARNT heterodimerization. Exhibits >60-fold selectivity for HIF-2α over HIF-1α. Decreases HIF-2α DNA-binding and attenuates expression of HIF-2α target genes in vitro.
化合物库 for TC-S 7009
TC-S 7009 is also offered as part of the Tocriscreen Epigenetics Library. 了解 Tocris 化合物库的更多信息。
技术数据 for TC-S 7009
| 分子量 | 308.65 |
| 公式 | C12H6ClFN4O3 |
| 储存 | Store at RT |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 1422955-31-4 |
| PubChem ID | 70697712 |
| InChI Key | CDQUJZKBRAFWNG-UHFFFAOYSA-N |
| Smiles | ClC1=CC(F)=CC(NC3=C([N+]([O-])=O)C2=NON=C2C=C3)=C1 |
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 TC-S 7009
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 30.86 | 100 |
制备储备液 for TC-S 7009
以下数据基于产品分子量 308.65。 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 | 3.24 mL | 16.2 mL | 32.4 mL |
| 5 mM | 0.65 mL | 3.24 mL | 6.48 mL |
| 10 mM | 0.32 mL | 1.62 mL | 3.24 mL |
| 50 mM | 0.06 mL | 0.32 mL | 0.65 mL |
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产品说明书 for TC-S 7009
参考文献 for TC-S 7009
参考文献是支持产品生物活性的出版物。
Scheuermann et al (2013) Allosteric inhibition of hypoxia inducible factor-2 with small molecules. Nat.Chem.Biol. 9 271 PMID: 23434853
Rogers et al (2013) Development of inhibitors of the PAS-B domain of the HIF-2α transcription factor. J.Med.Chem. 56 1739 PMID: 23363003
Wu et al (2019) Bidirectional modulation of HIF-2 activity through chemical ligands. Nat.Chem.Biol. 15 367 PMID: 30804532
If you know of a relevant reference for TC-S 7009, please let us know.
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关键词: TC-S 7009, TC-S 7009 supplier, TC-S7009, high, affinity, inhibits, inhibitors, HIF2α, HIF2a, HIF2alpha, PASB, hypoxia-inducible, factors, OX3, 0X3, Hypoxia, Inducible, Factors, 5243, Tocris Bioscience
2 篇 TC-S 7009 的引用文献
引用文献是使用了 Tocris 产品的出版物。 TC-S 7009 的部分引用包括：
Kyoung Min et al (2020) A system-level approach identifies HIF-2α as a critical regulator of chondrosarcoma progression. Nat Commun 11 5023 PMID: 33024108
Sasagawa et al (2018) HIF-2α, but not HIF-1α, mediates hypoxia-induced up-regulation of Flt-1 gene expression in placental trophoblasts. Sci Rep 8 17375 PMID: 30478339
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