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BIO-2007817

Chemical Structure : BIO-2007817

CAS No.:

BIO-2007817 (BIO 2007817)

Catalog No.: PC-72861Not For Human Use, Lab Use Only.

BIO-2007817 is a small-molecule positive allosteric modulator of Parkin E3 ligase with EC50 of 0.17 uM (TR-FRET).

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Biological Activity

BIO-2007817 is a small-molecule positive allosteric modulator of Parkin E3 ligase with EC50 of 0.17 uM (TR-FRET).
BIO-2007817 stimulated Parkin autoubiquitination as measured by Western blots in a concentration-dependent manner, was also able to induce the appearance of monoubiquitinated forms of Miro1.
BIO-2007817 induced the appearance of slower-migrating Parkin species in a concentration-dependent manner with maximal efficacy at 20 uM in Parkin autoubiquitination assay.
BIO-2007817 does not affect the rate of Parkin translocation to mitochondria nor the number of mitochondria within lysosomes.

Physicochemical Properties

M.Wt 552.679
Formula C32H36N6O3
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

(S)-1-((R)-6-isopropyl-3-(4-(1,2,3,4-tetrahydroquinoline-1-carbonyl)phenyl)-6,7-dihydropyrazolo[1,5-a]pyrazin-5(4H)-yl)-2-methoxy-2-(1-methyl-1H-pyrazol-4-yl)ethan-1-one

References

1. Shlevkov E, et al. iScience. 2021 Dec 18;25(1):103650.
2. Sauvé V, et al. Nat Commun. 2024 Sep 19;15(1):7707.

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