TC-E 5003 是一种选择性 PRMT1 抑制剂，对 hPRMT1 的 IC50 为 1.5 μM。
| Cas No. | 17328-16-4 |
| 别名 | N,N'-[磺酰基二(4,1-亚苯基)]二(2-氯乙酰胺) |
| 化学名 | 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 |
| 分子式 | C16H14Cl2N2O4S |
| 分子量 | 401.26 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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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