N,N'-[Sulfonylbis(1,4-phenylene)]bis(chloroacetamide)
N,N'-[Sulfonylbis(1,4-phenylene)]bis(chloroacetamide) Basic information
- Product Name:
- N,N'-[Sulfonylbis(1,4-phenylene)]bis(chloroacetamide)
- Synonyms:
-
- 4',4'''-Sulfonylbis(α-chloroacetanilide)
- Bis[4-(chloroacetylamino)phenyl] sulfone
- N,N'-[Sulfonylbis(1,4-phenylene)]bis(chloroacetamide)
- TC-E 5003
- N,N'-[Sulfonylbis(4,1-phenylene)]bis(2-chloroacetamide)
- TC-E 5003 (NSC-30176)
- 1-phenylene)bis(2-chloroacetamide)
- N'-(Sulfonyldi-4
- CAS:
- 17328-16-4
- MF:
- C16H14Cl2N2O4S
- MW:
- 401.26
- Mol File:
- 17328-16-4.mol
N,N'-[Sulfonylbis(1,4-phenylene)]bis(chloroacetamide) Chemical Properties
- Melting point:
- 191-192 °C
- Boiling point:
- 704.2±60.0 °C(Predicted)
- Density
- 1.504±0.06 g/cm3(Predicted)
- storage temp.
- -20°C (des.)
- solubility
- Soluble in DMSO (up to 50 mg/ml).
- pka
- 11.56±0.70(Predicted)
- form
- solid
- color
- Brown
- Stability:
- Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month.
N,N'-[Sulfonylbis(1,4-phenylene)]bis(chloroacetamide) Usage And Synthesis
Description
TC-E 5003 is an inhibitor of protein arginine methyltransferase 1 (PRMT1; IC50 = 1.5 μM for human PRMT1 in a methylation assay). It is selective for PRMT1 over PRMT4/CARM1 and SET7/9 methyltransferases, with less than 5% inhibition at a concentration of 50 μM for SET7/9. TC-E 5003 inhibits growth of MCF-7a breast cancer and LNCaP prostate cancer cells (GI50s = 1.97 and 4.49 μM, respectively) and decreases androgen-dependent gene transcription in vitro. TC-E 5003 (80 mg/kg) also has antimalarial properties and eradicates P. berghei in mice.
Uses
NSC 30176 is a inhibitor of human PRMT1, it is selective for PRMT1 over the arginine methyltransferase CARM1 and the lysine methyltransferase Set7/9.
References
1) Bissinger?et al. (2011),?Acyl derivatives of p-aminosulfonamides and dapsone as new inhibitors of the arginine methytransferase hPRMT1; Bioorg. Med. Chem.,?19?3717
N,N'-[Sulfonylbis(1,4-phenylene)]bis(chloroacetamide)Supplier
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