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SPI-1477

Chemical Structure : SPI-1477

CAS No.: 1030179-06-6

SPI-1477 (SPI-77)

Catalog No.: PC-21805Not For Human Use, Lab Use Only.

SPI-1477 (SPI-77) is a small molecule Spt5-Pol II complex inhibitor (SPI), selectively lowers mutant huntingtin gene (Htt) mRNA level with IC50 of 0.1 nM, without affecting WT Htt.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

SPI-1477 (SPI-77) is a small molecule Spt5-Pol II complex inhibitor (SPI), selectively lowers mutant huntingtin gene (Htt) mRNA level with IC50 of 0.1 nM, without affecting WT Htt.
SPI-1477 lowers mutant Htt protein levels in huntington's disease (HD) cells.
SPI-1477 selectively inhibits the expression of the mutant Htt gene without affecting the expression of the normal gene or other Spt5 activities.
SPI-1477 0.5 mM (0.6 µg/day) selectively reduces mutant Htt in mutant BACHD mice.
SPI-1477 attenuates HD-related behavioral phenotypes in BACHD mice, shows significant improvements in motor coordination, anxiety symptoms, and when administered to early-stage BACHD mice, slows down the progressive deterioration of the disease.

Physicochemical Properties

M.Wt 441.34
Formula C18H14Cl2N2O3S2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4,5-dichloro-2-(4-((2-(methylthio)benzyl)sulfonyl)phenyl)pyridazin-3(2H)-one

References

1. Bahat A, et al. EMBO Mol Med. 2024 Feb 19. doi: 10.1038/s44321-023-00020-y.

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