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HomeProduct name listN,N'-[Sulfonylbis(1,4-phenylene)]bis(chloroacetamide)

N,N'-[Sulfonylbis(1,4-phenylene)]bis(chloroacetamide)

N,N'-[Sulfonylbis(1,4-phenylene)]bis(chloroacetamide) Structural

What is N,N'-[Sulfonylbis(1,4-phenylene)]bis(chloroacetamide)?

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.

The Uses of N,N'-[Sulfonylbis(1,4-phenylene)]bis(chloroacetamide)

NSC 30176 is a inhibitor of human PRMT1, it is selective for PRMT1 over the arginine methyltransferase CARM1 and the lysine methyltransferase Set7/9.

What are the applications of Application

TC-E 5003 is a selective PRMT1 inhibitor

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

Properties of N,N'-[Sulfonylbis(1,4-phenylene)]bis(chloroacetamide)

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.

Safety information for N,N'-[Sulfonylbis(1,4-phenylene)]bis(chloroacetamide)

Computed Descriptors for N,N'-[Sulfonylbis(1,4-phenylene)]bis(chloroacetamide)

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