LW-216 | TrxR1 inhibitor | Probechem Biochemicals

Chemical Structure : LW-216

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LW-216 (LW216)

货号: PC-22430Not For Human Use, Lab Use Only.

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25 mg		Get quote
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100 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	485.58
分子式	C30H31NO5
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
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

参考文献

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

LW-216 (LW216)

生物&药学活性

物理化学性质&存储条件

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LW-216 (LW216)

生物&药学活性

物理化学性质&存储条件

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