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Chemical Structure : LW-216
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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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.
| M.Wt | 485.58 | |
| Formula | C30H31NO5 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Wang R, et al. Neoplasia. 2024 Jul;53:101004.
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