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LXH-3-71

Chemical Structure : LXH-3-71

CAS No.: 2251753-65-6

LXH-3-71

Catalog No.: PC-23184Not For Human Use, Lab Use Only.

LXH-3-71 is a potent mlecular glue triggers degradation of 3-phosphoglycerate dehydrogenase (PHGDH), covalently binds to Cys281 of PHGDH, triggers significant and selective degradation of PHGDH both in vitro and in vivo.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

LXH-3-71 is a potent mlecular glue triggers degradation of 3-phosphoglycerate dehydrogenase (PHGDH), covalently binds to Cys281 of PHGDH, triggers significant and selective degradation of PHGDH both in vitro and in vivo.
LXH-3-71 modulates the stemness of colorectal cancer cells (CRCs) both in vitro and in vivo.
LXH-3-71 inhibits the growth of both colorectal cancer cells and colorectal cancer stem cells in vitro.
LXH-3-71 remarkably inhibits the growth and metathesis of mCRCs in vivo.
LXH-3-71 substantially induces the formation of a dynamic complex between PHGDH and DDB1-CUL4 ubiquitin ligase, consequently facilitating the efficient cellular proteasomal degradation of PHGDH.

Physicochemical Properties

M.Wt 657.94
Formula C41H59N3O4
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

(4aS,6aS,6bR,8aR,12aR,12bR,14bS)-N-(2-(3-(4-methoxyphenyl)ureido)ethyl)-2,2,6a,6b,9,9,12a-heptamethyl-11-methylene-10-oxo-1,3,4,5,6,6a,6b,7,8,8a,9,10,11,12,12a,12b,13,14b-octadecahydropicene-4a(2H)-carboxamide

References

1. Ziqi Huang, et al. Acta Pharm Sin B. 2024 Sep;14(9):4001-4013.

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