C-7280948 (C7280948) is a selective PRMT1 (protein arginine methyltransferase) inhibitor with anticancer activity. It inhibits PRMT1 with IC50 value of 12.75 μM. C-7280948 is 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. 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.

Physicochemical Properties

Molecular Formula	C14H16N2O2S
Molecular Weight	276.35
Exact Mass	276.093
CAS #	587850-67-7
Related CAS #	587850-67-7
PubChem CID	833539
Appearance	White to off-white solid powder
Density	1.3±0.1 g/cm3
Boiling Point	481.1±55.0 °C at 760 mmHg
Flash Point	244.8±31.5 °C
Vapour Pressure	0.0±1.2 mmHg at 25°C
Index of Refraction	1.617
LogP	2.18
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	4
Rotatable Bond Count	5
Heavy Atom Count	19
Complexity	350
Defined Atom Stereocenter Count	0
InChi Key	BYWZPUPRVIECEC-UHFFFAOYSA-N
InChi Code	InChI=1S/C14H16N2O2S/c15-13-6-8-14(9-7-13)19(17,18)16-11-10-12-4-2-1-3-5-12/h1-9,16H,10-11,15H2
Chemical Name	4-amino-N-(2-phenylethyl)benzenesulfonamide
Synonyms	C-7280948; C 7280948; C7280948
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

ln Vitro	Compound 6a in this article is C-7280948, which has an IC50 value of 12.75 μM against hPRMT1. Arginine methyltransferases in particular are frequently referred to as protein methyltransferases (PRMTs) because they also target substrates that are not histone proteins. As a result of its association with the activation of androgen and estrogen receptors, the subtype PRMT1 may offer a novel therapeutic approach for hormone-dependent cancer.
ln Vivo
Animal Protocol
References	[1]. Acyl derivatives of p-aminosulfonamides and dapsone as new inhibitors of the arginine methyltransferase hPRMT1. Bioorg Med Chem. 2011 Jun 15;19(12):3717-3731.

Solubility Data

Solubility (In Vitro)

DMSO:≥ 38 mg/mL Water:<1 mg/mL Ethanol:

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (9.05 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (9.05 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	3.6186 mL	18.0930 mL	36.1860 mL
	5 mM	0.7237 mL	3.6186 mL	7.2372 mL
	10 mM	0.3619 mL	1.8093 mL	3.6186 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.