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.
Bulk size, bulk discount!
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
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.
Contact Us
sales@probechem.com
