GSK_WRN4 | WRN helicase inhibitor | Probechem Biochemicals

Chemical Structure : GSK_WRN4

加入收藏

GSK_WRN4 (WRNi, GSK-WRN4)

货号: PC-22110Not For Human Use, Lab Use Only.

GSK_WRN4 (WRNi, GSK-WRN4) is a potent and highly selective WRN helicase covalent inhibitor with biochemical pIC50 of 7.6, covalently targets WRN Cys727 residue.

规格	价格	库存	数量
25 mg		Get quote
50 mg		Get quote
100 mg		Get quote
250 mg		Get quote

获取报价单

* 请选择数量再加入购物车

or Bulk Inquiry

大包装，大折扣！

E-mail: sales@probechem.com

Tech Support: tech@probechem.com

生物&药学活性

GSK_WRN4 (WRNi, GSK-WRN4) is a potent and highly selective WRN helicase covalent inhibitor with biochemical pIC50 of 7.6, covalently targets WRN Cys727 residue.
GSK_WRN4 displays exceptional specificity for WRN over other RecQ helicases (RecQ5, RecQ1, BLM), significantly modifies WRN Cys727 in Jurkat cells demonstrating the remarkable specificity.
GSK_WRN4 selectively inhibits microsatellite-unstable (MSI) cell growth in vitro and phenocopies genetic inactivation, induces cytotoxic chromosomal instability and DNA damage in MSI cancer cells, by selectively degrading WRN and concurrently upregulating DNA damage response markers such as p-ATM, p-KAP1, p21, and γ-H2AX.
GSK_WRN4 (100 mpk, 300 mpk, p.o.) exerts potent anti-tumor activity in patient-derived xenograft (PDX) model from patient with treatment-refractory MSI CRC, inducing hallmarks of WRN-inhibition-mediated DNA damage.
GSK_WRN4 induces DNA damage specifically in MSI-H, but not other tissues, demonstrating that the in vivo tumor growth inhibition by GSK_WRN4 at 300 mpk is due to WRN helicase inhibition rather than off-target toxicity.

物理化学性质&存储条件

分子量	336.41
分子式	C16H20N2O4S
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	(R)-6-cyclohexyl-N-(1,1-dioxido-2,3-dihydrothiophen-3-yl)-2-oxo-1,2-dihydropyridine-3-carboxamide

参考文献

1. Picco G, et al. Cancer Discov. 2024 Apr 9. doi: 10.1158/2159-8290.CD-24-0052.

GSK_WRN4 (WRNi, GSK-WRN4)

生物&药学活性

物理化学性质&存储条件

参考文献

Bulk Inquiry

* Indicates a Required FieldYour information is safe with us.

询单

GSK_WRN4 (WRNi, GSK-WRN4)

生物&药学活性

物理化学性质&存储条件

参考文献

Bulk Inquiry

* Indicates a Required FieldYour information is safe with us.

询单

Get Quotation Now

* Indicates a Required FieldYour information is safe with us.