|TC-E 5003 PRMT1 inhibitor, potent|
Sample solution is provided at 25 µL, 10mM.
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|Cas No.||17328-16-4||SDF||Download SDF|
|Solubility||Soluble in DMSO > 10 mM||Storage||Store at -20°C|
|Physical Appearance||Off-white solid||Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|
TC-E 5003 is a selective inhibitor of PRMT1 with IC50 value of 1.5 μM .
PRMT1 is a member of the protein arginine N-methyltransferase (PRMT) family and plays a pivotal role in many biological processes by post-translational modification of target proteins. It has been reported that PRMT1 abnormal expression was observed in many types of cancer and its inhibitors was regarded as promising target in clinic .
TC-E 5003 is a potent PRMT1 inhibitor. When tested with breast cancer cell line MCF7a or prostate cancer cell line LNCaP, TC-E treatment induced cell apoptosis and inhibited cell proliferation by functioning on PRMT1. And it also reported that TC-E treatment attenuated androgen-induced gene expression in LNCaP cells .
. Bissinger, E.M., et al., Acyl derivatives of p-aminosulfonamides and dapsone as new inhibitors of the arginine methyltransferase hPRMT1. Bioorg Med Chem, 2011. 19(12): p. 3717-31.
. Avasarala, S., et al., PRMT1 is a Novel Regulator of Epithelial-Mesenchymal-Transition in Non-Small Cell Lung Cancer. J Biol Chem, 2015.