Chemical Structure : 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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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.
分子量 | 836.01 | |
分子式 | C45H57N9O7 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Yaxun Guo, et al. J Exp Clin Cancer Res. 2024 Nov 30;43(1):314.
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