Chemical Structure : PRMT4 PROTAC C199
CAS No.:
PRMT4 PROTAC C199
Catalog No.: PC-24916Not For Human Use, Lab Use Only.
PRMT4 PROTAC C199 is a potent, selective PROTAC degrader targeting PRMT4 with DC50 of 106 nM and Dmax=93.1% in NCI-H929 cells, showes high selectivity for PRMT4 over other PRMTs.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
PRMT4 PROTAC C199 is a potent, selective PROTAC degrader targeting PRMT4 with DC50 of 106 nM and Dmax=93.1% in NCI-H929 cells, showes high selectivity for PRMT4 over other PRMTs.
C199 reduced PRMT4 protein levels in NCI-H929 cells through a VHL E3 ligase- and proteasome-dependent mechanism.
C199 (0.03-0.5 uM) reduced arginine methylation levels in NCI-H929 cells.
PRMT4 PROTAC C199 inhibited cell proliferation with GI50 values of 0.089 μM and 0.145 μM for NCI-H929 and RPMI-8226, respectively.
PRMT4 PROTAC C199 (80 mg/kg, i.p.) exhibited antitumor efficacy against the NCI-H929 xenograft model in vivo.
Physicochemical Properties
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M.Wt
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1236.07
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Formula
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C67H95ClN10O8S
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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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(2S,4R)-1-((S)-2-(17-(2-(2-(2-chloro-5-((R)-2-hydroxy-3-(methylamino)propoxy)phenyl)-6-(3,5-dimethylisoxazol-4-yl)-5-methylpyrimidin-4-yl)-2,7-diazaspiro[3.5]nonan-7-yl)-17-oxoheptadecanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide
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References
1. Yong Ju, et al. J Med Chem. 2025 Jun 18. doi: 10.1021/acs.jmedchem.5c01022.
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