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TC-E 5003 PRMT1 inhibitor, potent

Catalog No.B7750
Size Price Stock Qty
50mg
$72.00
In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

TC-E 5003

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Chemical Properties

Cas No. 17328-16-4 SDF Download SDF
Chemical Name N,N'-(sulfonylbis(4,1-phenylene))bis(2-chloroacetamide)
Canonical SMILES ClCC(NC1=CC=C(C=C1)S(=O)(C(C=C2)=CC=C2NC(CCl)=O)=O)=O
Formula C16H14Cl2N2O4S M.Wt 401.26
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.

Background

TC-E 5003 is a selective inhibitor of PRMT1 with IC50 value of 1.5 μM [1].
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 [2].
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 [1].
References:
[1].    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.
[2].    Avasarala, S., et al., PRMT1 is a Novel Regulator of Epithelial-Mesenchymal-Transition in Non-Small Cell Lung Cancer. J Biol Chem, 2015.