Chemical Structure : YZ-836P
CAS No.:
YZ-836P
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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836.01
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Formula
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C45H57N9O7
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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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
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References
1. Yaxun Guo, et al. J Exp Clin Cancer Res. 2024 Nov 30;43(1):314.
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