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LW-216

Chemical Structure : LW-216

CAS No.: 2146090-18-6

LW-216 (LW216)

Catalog No.: PC-22430Not For Human Use, Lab Use Only.

LW-216 is a novel specific small molecule thioredoxin reductase 1 (TrxR1, TXNRD1) inhibitor directly binds TrxR1 (KD of 8.8 uM in MST assays) and persistently promotes TrxR1 ubiquitination, inhibits TrxR1 expression.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

LW-216 is a novel specific small molecule thioredoxin reductase 1 (TrxR1, TXNRD1) inhibitor directly binds TrxR1 (KD of 8.8 uM in MST assays) and persistently promotes TrxR1 ubiquitination, inhibits TrxR1 expression.
LW-216 concentration-dependently reduces TrxR1 expression in both NCI-H460 and A549 cells, while TrxR2 expression remaines unaffected.
LW-216 promotes TrxR1 ubiquitination by binding at R371 and G442 sites.
LW-216 induces mitochondrial-mediated apoptosis in non-small cell lung cancer cells.
LW-216 triggers ROS-dependent apoptosis which can be reversed by TrxR1 expression.
LW-216 (8 mg/kg) inhibited tumor growth of NCI-H460 cells in xenograft mice model, with minimal impact on the body weight of the animals.

Physicochemical Properties

M.Wt 485.58
Formula C30H31NO5
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

5-Hydroxy-2-phenyl-7-(phenylmethoxy)-8-[4-(1-pyrrolidinyl)butoxy]-4H-1-benzopyran-4-one

References

1. Wang R, et al. Neoplasia. 2024 Jul;53:101004.

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