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Description: Potent glutaminyl cyclase inhibitor; disrupts binding of SIRP-α to CD47
Chemical Name: 6'-Fluoro-2-[4-(4-methyl-4H-1,2,4-triazol-3-yl)-1-piperidinyl]-3,3'-bipyridine
Purity: ≥98% (HPLC)
Biological Activity for SEN 177
SEN 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.
Technical Data for SEN 177
| M. Wt | 338.39 |
| Formula | C18H19FN6 |
| Storage | Store at -20°C |
| Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for SEN 177
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 6.77 | 20 | |
| ethanol | 6.77 | 20 |
Preparing Stock Solutions for SEN 177
The following data is based on the product molecular weight 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.
| Concentration / Solvent Volume / Mass | 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 |
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Product Datasheets for SEN 177
References for SEN 177
References are publications that support the biological activity of the product.
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
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Keywords: 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
Citations for SEN 177
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