CARM1-IN-1 (hydrochloride)

CARM1-IN-1 (compound 7g) hydrochloride is a highly potent and selective inhibitor of CARM1 (IC50=8.6 μM, CARM1/PABP1), with low inhibitory activity against PRMT1 and SET7 (IC50 >667 μM) . CARM1-IN-1 hydrochloride inhibits the methylation activity of CARM1 and the methylation levels of different substrates, such as PABP1, CA150, SmB, and H3. CARM1-IN-1 hydrochloride also inhibits the promoter activity of prostate-specific antigen (PSA) without significant cytotoxicity[1].

Product Specifications

CAS Number

[2070018-31-2]

UNSPSC

12352005

Target

Histone Methyltransferase

Type

Reference compound

Related Pathways

Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/CARM1-IN-1-hydrochloride.html

Purity

95.13

Solubility

DMSO : 250 mg/mL (ultrasonic)

Smiles

[H]Cl.O=C1/C(CN(CC2=CC=CC=C2)C/C1=C\C3=CC=C(O)C(Br)=C3)=C/C4=CC=C(O)C(Br)=C4

Molecular Formula

C26H22Br2ClNO3

Molecular Weight

591.72

References & Citations

[1]Cheng D, et al. Novel 3,5-bis (bromohydroxybenzylidene) piperidin-4-ones as coactivator-associated arginine methyltransferase 1 inhibitors: enzyme selectivity and cellular activity. J Med Chem. 2011 Jul 14;54 (13) :4928-32.