MedChemExpress LLC (MCE)

MedChemExpress - Model SEN177 - 2117405-13-5

SEN177 is an orally effect glutamine cyclase (QC) inhibitor. The Ki of SEN177 for human glutamine cyclase (hQC) is 20 nM, and the IC50 is 13 nM. SEN177 interferes with the interaction between CD47 and SIRRPα, and has anti-tumor activity. SEN177 reduces aggregation and apoptosis caused by HTT mutation in Huntington model, and can be used in the study of neurodegenerative diseases[1][2][3].

SEN177

MCE China：SEN177

Brand：MedChemExpress (MCE)

Cat. No.HY-136780

CAS：2117405-13-5

Purity：97.10%

Storage：Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month

Shipping：Room temperature in continental US; may vary elsewhere.

Description：SEN177 is an orally effect glutamine cyclase (QC) inhibitor. The Ki of SEN177 for human glutamine cyclase (hQC) is 20 nM, and the IC50 is 13 nM. SEN177 interferes with the interaction between CD47 and SIRRPα, and has anti-tumor activity. SEN177 reduces aggregation and apoptosis caused by HTT mutation in Huntington model, and can be used in the study of neurodegenerative diseases.

In Vitro：SEN177 (0-50 μM; 0-96 h) effectively blocks the interaction between CD47 and SIRRPα in breast cancer cell line MDA-MB-468[2]. SEN177 (10 μM; 3 days) significantly enhances the ability of EGFR antibody to induce ADCP in esophageal squamous cell carcinoma (Kyse-30) and breast cancer cell line (MDA-MB-468)[2]. SEN177 (50 μM; 24 h) decreases mutant HTT aggregate ratio and apoptosis in HeLa cells expressing HTT (Q74)[3].

In Vivo：SEN177 (50 μM; Oral administration; Change every two days) has a protective effect in the Huntington Drosophila model[3].

References：

[1]. Cecilia Pozzi, et al. The structure of the human glutaminyl cyclase-SEN177 complex indicates routes for developing new potent inhibitors as possible agents for the treatment of neurological disorders. J Biol Inorg Chem. 2018 Dec;23(8):1219-1226. [Content Brief]

[2]. Baumann N, et al. Enhancement of epidermal growth factor receptor antibody tumor immunotherapy by glutaminyl cyclase inhibition to interfere with CD47/signal regulatory protein alpha interactions. Cancer Sci. 2021 Aug;112(8):3029-3040. [Content Brief]

[3]. Maria Jimenez-Sanchez, et al. siRNA screen identifies QPCT as a druggable target for Huntington's disease. Nat Chem Biol. 2015 May;11(5):347-354. [Content Brief]

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