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Hh signaling inhibitor Q29

Chemical Structure : Hh signaling inhibitor Q29

CAS No.:

Hh signaling inhibitor Q29 (SMO-CRD inhibitor C29)

Catalog No.: PC-22759Not For Human Use, Lab Use Only.

Hh signaling inhibitor Q29 is a small molecule inhibitor of hedgehog pathway with IC50 of 1.33 uM in Gli-luciferase assay, binds to the cysteine-rich domain (CRD) of smoothened (SMO) and blocks its cholesterylation.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

Hh signaling inhibitor Q29 is a small molecule inhibitor of hedgehog pathway with IC50 of 1.33 uM in Gli-luciferase assay, binds to the cysteine-rich domain (CRD) of smoothened (SMO) and blocks its cholesterylation.
Q29 dose dependently decreases the protein and mRNA levels of endogenous Gli1 in NIH 3T3 cells.
Q29 inhibits Gli-luciferase activities stimulated by cholesterol or 20(S)-OHC (IC50 of 3.13 uM for cholesterol and 2.02 uM for 20(S)-OHC, suppresses ciliary accumulation of SMO induced by Shh-N.
Q29 inhibits SMO through acting on the CRD, does not bind to SMO-7TM.
Q29 dose dependently decreases cholesterylation of SMO in both wild-type (WT) and Ptch1 KO cells.
Q29 (1-10 uM) dose dependently inhibits the growth of medulloblastoma cells isolated from Ptch1+/−P53−/− mice in vitro.
Q29 (90 mg/kg twice daily) inhibits the growth of Ptch1+/−P53−/− medulloblastoma allograft tumor in vivo, exhibits a synergistic inhibitory effect with vismodegib.

Physicochemical Properties

M.Wt 389.62
Formula C25H43NO2
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

N-butyl-3-((4aS,4bR,7S,8aR,10aR)-7-hydroxy-2,4b,8,8-tetramethyl-3,4,4a,4b,5,6,7,8,8a,9,10,10a-dodecahydrophenanthren-1-yl)propanamide

References

1. Liu YB, et al. Cell Chem Biol. 2024 Jul 18;31(7):1264-1276.e7.

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