TC-E 5003

PRMT1 inhibitor, potent CAS# 17328-16-4

TC-E 5003

Catalog No. BCC8008----Order now to get a substantial discount!

Product Name & Size Price Stock
TC-E 5003: 5mg $12 In Stock
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Chemical structure

TC-E 5003

3D structure

Chemical Properties of TC-E 5003

Cas No. 17328-16-4 SDF Download SDF
PubChem ID 87052 Appearance Powder
Formula C16H14Cl2N2O4S M.Wt 401.26
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 50 mM in DMSO
Chemical Name 2-chloro-N-[4-[4-[(2-chloroacetyl)amino]phenyl]sulfonylphenyl]acetamide
SMILES C1=CC(=CC=C1NC(=O)CCl)S(=O)(=O)C2=CC=C(C=C2)NC(=O)CCl
Standard InChIKey SHRCVZJKZJGIHQ-UHFFFAOYSA-N
Standard InChI InChI=1S/C16H14Cl2N2O4S/c17-9-15(21)19-11-1-5-13(6-2-11)25(23,24)14-7-3-12(4-8-14)20-16(22)10-18/h1-8H,9-10H2,(H,19,21)(H,20,22)
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.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of TC-E 5003

DescriptionSelective protein arginine methyltransferase 1 (PRMT1) inhibitor (IC50 = 1.5 μM); exhibits no inhibitory activity against CARM1 and Set7/9 methyltransferases. Inhibits growth of MCF7a breast cancer cells and LNCaP prostate cancer cells. Attenuates androgen-induced gene expression in LNCaP cells.

TC-E 5003 Dilution Calculator

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TC-E 5003 Molarity Calculator

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Preparing Stock Solutions of TC-E 5003

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.4921 mL 12.4607 mL 24.9215 mL 49.843 mL 62.3037 mL
5 mM 0.4984 mL 2.4921 mL 4.9843 mL 9.9686 mL 12.4607 mL
10 mM 0.2492 mL 1.2461 mL 2.4921 mL 4.9843 mL 6.2304 mL
50 mM 0.0498 mL 0.2492 mL 0.4984 mL 0.9969 mL 1.2461 mL
100 mM 0.0249 mL 0.1246 mL 0.2492 mL 0.4984 mL 0.623 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on TC-E 5003

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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References on TC-E 5003

Protein arginine methyltransferase expression and activity during myogenesis.[Pubmed:29208765]

Biosci Rep. 2018 Jan 10;38(1). pii: BSR20171533.

Despite the emerging importance of protein arginine methyltransferases (PRMTs) in regulating skeletal muscle plasticity, PRMT biology during muscle development is complex and not completely understood. Therefore, our purpose was to investigate PRMT1, -4, and -5 expression and function in skeletal muscle cells during the phenotypic remodeling elicited by myogenesis. C2C12 muscle cell maturation, assessed during the myoblast (MB) stage, and during days 1, 3, 5, and 7 of differentiation, was employed as an in vitro model of myogenesis. We observed PRMT-specific patterns of expression and activity during myogenesis. PRMT4 and -5 gene expression was unchanged, while PRMT1 mRNA and protein content were significantly induced. Cellular monomethylarginines (MMAs) and symmetric dimethylarginines (SDMAs), indicative of global and type II PRMT activities, respectively, remained steady during development, while type I PRMT activity indicator asymmetric dimethylarginines (ADMAs) increased through myogenesis. Histone 4 arginine 3 (H4R3) and H3R17 contents were elevated coincident with the myonuclear accumulation of PRMT1 and -4. Collectively, this suggests that PRMTs are methyl donors throughout myogenesis and demonstrate specificity for their protein targets. Cells were then treated with TC-E 5003 (TC-E), a selective inhibitor of PRMT1 in order to specifically examine the enzymes role during myogenic differentiation. TC-E treated cells exhibited decrements in muscle differentiation, which were consistent with attenuated mitochondrial biogenesis and respiratory function. In summary, the present study increases our understanding of PRMT1, -4, and -5 biology during the plasticity of skeletal muscle development. Our results provide evidence for a role of PRMT1, via a mitochondrially mediated mechanism, in driving the muscle differentiation program.

Acyl derivatives of p-aminosulfonamides and dapsone as new inhibitors of the arginine methyltransferase hPRMT1.[Pubmed:21440447]

Bioorg Med Chem. 2011 Jun 15;19(12):3717-31.

Arginine methylation is an epigenetic modification that receives increasing interest as it plays an important role in several diseases. This is especially true for hormone-dependent cancer, seeing that histone methylation by arginine methyltransferase I (PRMT1) is involved in the activation of sexual hormone receptors. Therefore, PRMT inhibitors are potential drugs and interesting tools for cell biology. A dapsone derivative called allantodapsone previously identified by our group served as a lead structure for inhibitor synthesis. Acylated derivatives of p-aminobenzenesulfonamides and the antilepra drug dapsone were identified as new inhibitors of PRMT1 by in vitro testing. The bis-chloroacetyl amide of dapsone selectively inhibited human PRMT1 in the low micromolar region and was selective for PRMT1 as compared to the arginine methyltransferase CARM1 and the lysine methyltransferase Set7/9. It showed anticancer activity on MCF7a and LNCaP cells and blocked androgen dependent transcription specifically in a reporter gene system. Likewise, a transcriptional block was also demonstrated in LNCaP cells using quantitative RT-PCR on the mRNA of androgen dependent genes.

Description

Selective PRMT1 inhibitor

Keywords:

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