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首页-抗体药物偶连体和PROTACs-PROTAC-PRMT1 PROTAC 1
PRMT1 PROTAC 1

Chemical Structure : PRMT1 PROTAC 1

CAS No.: 3126018-46-7

PRMT1 PROTAC 1

货号: PC-28660Not For Human Use, Lab Use Only.

PRMT1 PROTAC 1 (Compound 4) is potent, first-in-class, selective PRMT1 PROTAC degrader with DC50 of 0.77 uM, Dmax of 84.83% in MCF-7 cells, exhibits highly potent PRMT1 degradation with DC50 of 0.65 7M and a Dmax of 93.03% in A2058 cells.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

PRMT1 PROTAC 1 (Compound 4) is potent, first-in-class, selective PRMT1 PROTAC degrader with DC50 of 0.77 uM, Dmax of 84.83% in MCF-7 cells, exhibits highly potent PRMT1 degradation with DC50 of 0.65 7M and a Dmax of 93.03% in A2058 cells.
PRMT1 PROTAC 1 triggers dose- and time-dependent degradation of the PRMT1 protein.
PRMT1 PROTAC 1 reduces PRMT1 protein levels in MCF-7 cells through a proteasome-dependent and CRBN E3 ligase mechanism.
PRMT1 PROTAC 1 decreases global aDMA levels and asymmetric dimethylation of arginine 3 on histone H4 (H4R3me2a) levels in MCF-7 cells.
PRMT1 PROTAC 1 effectively inhibits colony formation at low concentrations, with activity against A2058 cells observed at 1.25 μM.

物理化学性质&存储条件

分子量 752.96
分子式 C43H56N6O6
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-(12-((2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)­amino)­dodecyl)-4-(2-((methyl­(2-(methylamino)­ethyl)­amino)­methyl)­phenoxy)­benzamide

参考文献

1. Guo S, et al. J Med Chem. 2026 Mar 26;69(6):6775-6789.

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