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Submit ReviewSEN 177 is a potent glutaminyl cyclase (QPCT) inhibitor (IC50 = 53 nM). SEN 177 reduces aggregation of mutant huntingtin (mHTT) through inhibition of QPCT and reduces Q80 aggregates in vitro. Inhibition of QPCT also reduces aggregate formation in in vivo models of Huntington's disease. SEN 177 potently inhibits QPCT-like protein (IC50 = 13 nM) and disrupts binding of SIRP-α to CD47. The compound increases antibody-dependent cellular phagocytosis and cytotoxicity in cancer cell lines.
分子量 | 338.39 |
公式 | C18H19FN6 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 2117405-13-5 |
PubChem ID | 91618245 |
InChI Key | AJIAMIPUWJQSPR-UHFFFAOYSA-N |
Smiles | FC=1N=CC(=CC1)C2=CC=CN=C2N3CCC(C4=NN=CN4C)CC3 |
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 | 6.77 | 20 | |
ethanol | 6.77 | 20 |
以下数据基于产品分子量 338.39。 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 |
---|---|---|---|
0.2 mM | 14.78 mL | 73.88 mL | 147.76 mL |
1 mM | 2.96 mL | 14.78 mL | 29.55 mL |
2 mM | 1.48 mL | 7.39 mL | 14.78 mL |
10 mM | 0.3 mL | 1.48 mL | 2.96 mL |
参考文献是支持产品生物活性的出版物。
Jimenez-Sanchez et al (2015) siRNA screen identifies QPCT as a druggable target for Huntington's disease. Nat.Chem.Biol. 11 347 PMID: 25848931
Logtenberg et al (2019) Glutaminyl cyclase is an enzymatic modifier of the CD47- SIRPα axis and a target for cancer immunotherapy. Nat.Med. 25 612 PMID: 30833751
If you know of a relevant reference for SEN 177, please let us know.
关键词: SEN 177, SEN 177 supplier, SEN177, QPCT, glutaminyl, cyclase, inhibitors, potent, huntingtin, mHTT, Huntingtons, aggregates, CD47, SIRPa, SIRPalpha, Other, Transferases, Immune, Checkpoints, 6979, Tocris Bioscience
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