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.
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Product Documents
Purity:>95.00%Appearance:A solid
Chemical Properties
CAS No.
17328-16-4
Synonyms
NSC 30176
Chemical Name
N,N'-(sulfonylbis(4,1-phenylene))bis(2-chloroacetamide)
SMILES
ClCC(NC1=CC=C(C=C1)S(=O)(C(C=C2)=CC=C2NC(CCl)=O)=O)=O
Molecular Formula
C16H14Cl2N2O4S
Molecular Weight
401.26
Solubility
DMF: 30 mg/ml,DMSO: 30 mg/ml
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.
CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility
g/mol
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