Aster inhibitor AI-3d

Chemical Structure : Aster inhibitor AI-3d

Catalog No.: PC-21334Not For Human Use, Lab Use Only.

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Biological Activity

Aster inhibitor AI-3d is a potent, selective small molecule inhibitor of Aster proteins (encoded by the Gramd1a-c genes) with IC50 of 0.11 μM, 0.06 μM and 0.71 uM for Aster-A, Aster-B, and Aster-C, respectively.
AI-3d (10 uM) blocks cholesterol transfer by Asters, does not cause lysosomal cholesterol accumulation and not inhibit SREBP2 processing.
AI-3d is an Aster-selective inhibitor that blocks nonvesicular plasma membrane (PM) to endoplasmic reticulum (ER) cholesterol transport.
AI-3d inhibits both human and murine Asters. reduces intestinal cholesterol uptake.
AI-3d increased SREBP-2 target gene expression in human enteroids and differentiated Caco-2 cells, reduces dietary cholesterol absorption into the circulation in vivo.

Physicochemical Properties

M.Wt	429.69
Formula	C28H47NO2
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	2-((3S,8S,9S,10R,13S,14S,17S)-10,13-dimethyl-3-(2-(pyrrolidin-1-yl)ethoxy)-2,3,4,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl)propan-2-ol

References

1. Xu Xiao, et al. Proc. Natl. Acad. Sci. U.S.A. 118, e2024149118 (2021).

2. Ferrari A, et al. Science. 2023 Nov 10;382(6671):eadf0966.