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Submit Review142D6 is a potent pan-IAP inhibitor (IC50 values are 21, 21 and 43 nM for cIAP1, cIAP2 and XIAP respectively). 142D6 covalently targets Lys residues in the BIR3 domain of the inhibitor of the apoptosis protein (IAP) family. In vitro, 142D6 reduces viability of cultured breast cancer MDA-MB-231 cells (EC50 values are 44 and 61 nM in cell viability and apoptosis assays, respectively). 142D6 is chemically stable in buffer and plasma and is orally bioavailable.
Sold under patent license from The Regents of the University of California
分子量 | 552.66 |
公式 | C26H37FN4O6S |
储存 | Store at -20°C |
纯度 | ≥95% (HPLC) |
CAS Number | 2410953-19-2 |
InChI Key | YVERFLKIJOIKPE-HXGJMTJLSA-N |
Smiles | O=C([C@H]1N(CCC1)C([C@H](C2CCCCC2)NC([C@H](C)NC)=O)=O)N[C@H]3C4=CC=CC(OS(F)(=O)=O)=C4CC3 |
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 | 55.27 | 100 |
以下数据基于产品分子量 552.66。 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 | 1.81 mL | 9.05 mL | 18.09 mL |
5 mM | 0.36 mL | 1.81 mL | 3.62 mL |
10 mM | 0.18 mL | 0.9 mL | 1.81 mL |
50 mM | 0.04 mL | 0.18 mL | 0.36 mL |
参考文献是支持产品生物活性的出版物。
Baggio et al (2019) Aryl-fluorosulfate-based lysine covalent pan-inhibitors of apoptosis protein (IAP) antagonists with cellular efficacy. J.Med.Chem. 62 9188 PMID: 31550155
Udompholkul et al (2023) Characterization of a potent and orally bioavailable Lys-covalent inhibitor of apoptosis protein (IAP) antagonist. J.Med.Chem. 66 8159 PMID: 37262387
If you know of a relevant reference for 142D6, please let us know.
关键词: 142D6, 142D6 supplier, XIAP, cIAP1, cIAP2, BIR3, domain, antagonist, potent, antagonism, inhibitors, inhibits, inhibitor, of, apoptosis, IAP, breast, cancer, Inhibitor, Apoptosis, (IAP), 8018, Tocris Bioscience
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There are two currently recognized forms of programmed cell death: apoptosis and necroptosis. This poster summarizes the signaling pathways involved in apoptosis, necroptosis and cell survival following death receptor activation, and highlights the influence of the molecular switch, cFLIP, on cell fate.