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.

in vivo

IC 50

PRMT1

References

[1] ELISABETH-MARIA BISSINGER . Acyl derivatives of p-aminosulfonamides and dapsone as new inhibitors of the arginine methyltransferase hPRMT1[J]. Bioorganic & Medicinal Chemistry, 2011, 19 12: Pages 3717-3731. DOI:10.1016/j.bmc.2011.02.032

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