A PRMT1 inhibitor (IC50 = 1.5 µM); selective over CARM1/PRMT4 and SET7/9 methyltransferases (50s = 1.97 and 4.49 µM

TC-E 5003 – 100 mg

Brand:
Cayman
CAS:
17328-16-4
Storage:
-20
UN-No:
Non-Hazardous - /

TC-E 5003 is an inhibitor of protein arginine methyltransferase 1 (PRMT1; IC50 = 1.5 µM for human PRMT1 in a methylation assay).{38415} 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.{38416}  

 

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Description

A PRMT1 inhibitor (IC50 = 1.5 µM); selective over CARM1/PRMT4 and SET7/9 methyltransferases (50s = 1.97 and 4.49 µM, respectively); decreases androgen-dependent gene transcription in vitro; eradicates P. berghei in mice

Formal name: N,N’-(sulfonyldi-4,1-phenylene)bis[2-chloro]-acetamide

Synonyms:  NSC 30176

Molecular weight: 401.3

CAS: 17328-16-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Methyltransferases||Research Area|Epigenetics, Transcription, & Translation|Writers|Histone Methylation||Research Area|Immunology & Inflammation||Research Area|Infectious Disease|Parasitic Diseases|Malaria

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