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首页-抗体药物偶连体和PROTACs-PROTAC-YZ-836P
YZ-836P

Chemical Structure : YZ-836P

CAS No.:

YZ-836P

货号: PC-23554Not For Human Use, Lab Use Only.

YZ-836P is a CRBN-recruiting PRMT5 PROTAC degrader, exerts cytotoxic effects in TNBC, promotes the ubiquitination and degradation of PRMT5 in a CRBN-dependent manner, downregulates key downstream target protein KLF5 in TNBC.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

YZ-836P is a CRBN-recruiting PRMT5 PROTAC degrader, exerts cytotoxic effects in TNBC, promotes the ubiquitination and degradation of PRMT5 in a CRBN-dependent manner, downregulates key downstream target protein KLF5 in TNBC.
YZ-836P dramatically decreases the protein levels of PRMT5 and KLF5. YZ-836P inhibits the growth of TNBC with IC50 of 2.1 µM and 1.0 µM for HCC1806 and HCC1937 cells, respectively.
YZ-836P induces nuclear fragmentation, cellular shrinkage, and cell separation from neighboring cells, inhibits DNA synthesis of HCC1806 and HCC1937 cells in a concentration-dependent manner.
YZ-836P induces cell cycle arrest and promotes apoptosis in TNBC, via the PRMT5-KLF5 pathway.
YZ-836P interacts with and degrades PRMT5 via the ubiquitin-proteasome system.
YZ-836P inhibits growth of TNBC patient-derived organoids and xenograft tumors in vivo.

物理化学性质&存储条件

分子量 836.01
分子式 C45H57N9O7
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

N-((S)-3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)-6-((1-(10-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)amino)decanoyl)piperidin-4-yl)amino)pyrimidine-4-carboxamide

参考文献

1. Yaxun Guo, et al. J Exp Clin Cancer Res. 2024 Nov 30;43(1):314.

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