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C7280948
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
C7280948图片
CAS NO:587850-67-7
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
10mg电议
50mg电议

产品介绍
C7280948 是一种选择性和有效的蛋白质甲基转移酶 1 (PRMT1) 抑制剂,IC50 值为 12.75 μM。
Cas No.587850-67-7
化学名4-amino-N-phenethylbenzenesulfonamide
Canonical SMILESNC1=CC=C(S(NCCC2=CC=CC=C2)(=O)=O)C=C1
分子式C14H16N2O2S
分子量276.35
溶解度≥ 13.9mg/mL in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

C7280948 is a novel PRMT1 inhibitor with IC50 value of 12.75 μM [1].

Protein arginine methyltransferase 1 (PRMT1) is a histone methyltransferase specific for histone H4. PRMT1 catalyzes the transfer of the methyl group from SAM to the guanidine nitrogen atoms of arginine residues to produce monomethyl arginines (MMA) and asymmetric dimethyl arginines (ADMA) [2].

C7280948 is a novel PRMT1 inhibitor. C7280948 interacts with aromatic residues at the hPRMT1 substrate binding pocket (Tyr 147 and Tyr 160) [1]. C7280948 inhibited hPRMT1 with IC50 value of 26.7 μM [3].

References:
[1].  Heinke R, Spannhoff A, Meier R, et al. Virtual screening and biological characterization of novel histone arginine methyltransferase PRMT1 inhibitors. ChemMedChem, 2009, 4(1): 69-77.
[2].  Itoh Y, Suzuki T, Miyata N. Small-molecular modulators of cancer-associated epigenetic mechanisms. Mol Biosyst, 2013, 9(5): 873-896.
[3].  Bissinger EM, Heinke R, Spannhoff A, et al. Acyl derivatives of p-aminosulfonamides and dapsone as new inhibitors of the arginine methyltransferase hPRMT1. Bioorg Med Chem, 2011, 19(12): 3717-3731.