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.
Bulk size, bulk discount!
Welcome credit card payment!
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
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
|
M.Wt
|
1236.07
|
|
Formula
|
C67H95ClN10O8S
|
|
Appearance
|
Solid
|
|
CAS No.
|
|
|
Storage
|
- Solide Powder
-
-20°C 12 Months; 4°C 6 Months
|
- In Solvent
-
-80°C 6 Months; -20°C 6 Months
|
|
Shipping
|
|
|
Solubility
|
10 mM in DMSO
|
|
Chemical Name/SMILES
|
(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
|
References
1. Yong Ju, et al. J Med Chem. 2025 Jun 18. doi: 10.1021/acs.jmedchem.5c01022.
Contact Us
sales@probechem.com
