| Identification | Back Directory | [Name]
CARM1-IN-1 | [CAS]
1020399-49-8 | [Synonyms]
CARM1-IN-1
CARM1-IN-7g
CARM1 inhibitor 1
PRMT4/CARM1 Inhibitor
4-Piperidinone, 3,5-bis[(3-bromo-4-hydroxyphenyl)methylene]-1-(phenylmethyl)- | [Molecular Formula]
C26H21Br2NO3 | [MOL File]
1020399-49-8.mol | [Molecular Weight]
555.26 |
| Chemical Properties | Back Directory | [Boiling point ]
659.8±55.0 °C(Predicted) | [density ]
1.647±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 30 mg/ml; DMSO: 30 mg/ml; DMSO:PBS(pH 7.2) (1:4): 0.2 mg/mL; Ethanol: 0.25 mg/mL | [form ]
A crystalline solid | [pka]
7.77±0.35(Predicted) | [color ]
Yellow to orange | [InChIKey]
KNMFTTWVELIVCC-CLVAPQHMSA-N | [SMILES]
O=C(/C(CN(CC1=CC=CC=C1)C/2)=C/C3=CC=C(O)C(Br)=C3)C2=C\C4=CC(Br)=C(O)C=C4 |
| Hazard Information | Back Directory | [Uses]
CARM1-IN-1 (compound 7g) 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 inhibits the methylation activity of CARM1 and the methylation levels of different substrates, such as PABP1, CA150, SmB, and H3. CARM1-IN-1 also inhibits the promoter activity of prostate-specific antigen (PSA) without significant cytotoxicity[1]. | [Biological Activity]
Cell permeable: yes''Primary Target
PRMT4''Reversible: yes''Secondary Target
SET7''Target IC50: CARM1-mediated methylation over PRMT1 and SET7 (IC60 = 7.163 and 943 μM, | [IC 50]
PRMT4 | [References]
[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. DOI:10.1021/jm200453n |
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| Company Name: |
BOC Sciences
|
| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
| Company Name: |
Musechem
|
| Tel: |
+1-800-259-7612 |
| Website: |
www.musechem.com |
|