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Submit ReviewCHR 2797 is an aminopeptidase inhibitor (IC50 values are 100, 150, 220, > 1000, > 5000, > 10000 and > 30000 nM for LAP, PuSA, aminopeptidase N, aminopeptidase B, PILSAP, LTA4 hydrolase and MetAP2, respectively). Potently inhibits tumor cell proliferation in a variety of tumor cell lines in vitro and in vivo. Also inhibits neprilysin (IC50 = 900 nM). Exhibits antinociceptive activity and enhances the efficacy of Morphine (Cat. No. 5158) in the hot-plate and tail-flick assays, via an action on the peripheral nervous system.
CHR 2797 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 406.48 |
公式 | C21H30N2O6 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 238750-77-1 |
PubChem ID | 15547703 |
InChI Key | FWFGIHPGRQZWIW-SQNIBIBYSA-N |
Smiles | O=C([C@H]([C@]2=CC=CC=C2)NC([C@@H]([C@@H](C(NO)=O)O)CC(C)C)=O)OC1CCCC1 |
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 40.65 | 100 | |
ethanol | 20.32 | 50 |
以下数据基于产品分子量 406.48。 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 | 2.46 mL | 12.3 mL | 24.6 mL |
5 mM | 0.49 mL | 2.46 mL | 4.92 mL |
10 mM | 0.25 mL | 1.23 mL | 2.46 mL |
50 mM | 0.05 mL | 0.25 mL | 0.49 mL |
参考文献是支持产品生物活性的出版物。
Krige et al (2008) CHR-2797: an anitproliferative aminopeptidase inhibitor that leads to amino acid deprivation in human leukemic cells. Cancer Res. 68 6669 PMID: 18701491
Moore et al (2009) Aminopeptidase inhibition as a targeted treatment strategy in myeloma. Mol.Cancer Ther. 8 762 PMID: 19372548
Singh et al (2019) Discovery of anticancer clinical candidate, Tosedostat, as an analgesic agent. ACS Chem.Neurosci. 10 4007 PMID: 31415151
If you know of a relevant reference for CHR 2797, please let us know.
关键词: CHR 2797, CHR 2797 supplier, aminopeptidases, inhibitors, inhibits, proteases, proteinases, CHR2797, neprilysin, neutral, endopeptidase, NEP, Tosedostat, Aminopeptidases, 3595, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 CHR 2797 的部分引用包括:
Yogin et al (2022) Cancer genes disfavoring T cell immunity identified via integrated systems approach. Cell Rep 40 111153 PMID: 35926468
Justin R et al (2022) M24B aminopeptidase inhibitors selectively activate the CARD8 inflammasome. Nat Chem Biol 18 565-574 PMID: 35165443
Orth-He et al (2023) Protein folding stress potentiates NLRP1 and CARD8 inflammasome activation. Cell Rep 42 111965 PMID: 36649711
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