CARM1-IN-4
CARM1-IN-4 (compound 11f) is a potent CARM1 inhibitor with IC50s of 9 nM and 56 nM for CARM1 and PRMT1, respectively. CARM1-IN-4 displays significant anti-proliferative effects on colorectal cancer cell lines. CARM1-IN-4 effectively inhibits the methyltransferase activity of CARM1 and prevents methylation of downstream proteins. CARM1-IN-4 induces apoptosis and shows antitumor activity.
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- CAS No.: 2878481-07-1
- Formule: C24H42N2O4
- Masse moléculaire:422.60
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Voir tous les produits spécifiques à Isoform Histone Methyltransferase
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Activité biologique
|
CARM1 9 nM (IC50) |
PRMT1 56 nM (IC50) |
PRMT6 30 nM (IC50) |
PRMT8 31 nM (IC50) |
PRMT3 2637 nM (IC50) |
PRMT5 >100,000 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
3.13 μM
Compound: 11f
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Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth by CCK-8 assay
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth by CCK-8 assay
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[PMID: 38460270] |
CARM1-IN-4 (compound 11f) exhibits significant anti-proliferative activity in the HCT116 cell lines (IC50=3.13 μM)[1].
CARM1-IN-4 (0.625-5 μM; 72 h) causes a dose-dependent induction of apoptosis in HCT116 cell[1].
CARM1-IN-4 (0.625-10 μM; 48 h) effectively inhibits the methyltransferase activity of CARM1, influencing the levels of asymmetric demethylation on CARM1 substrates within a cellular environment[1].
CARM1-IN-4 exhibits a relatively high mitochondrial stability, with an extended half-life in mouse mitochondria (T1/2=217 min)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116 cells
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Concentration:0.625, 1.25, 2.5, 5 μM
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Incubation Time:72 h
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Result:Illustrated a noticeable increase in the overall percentages of both early and late apoptotic cells.
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Cell Line:HCT116 cells
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Concentration:0.625, 1.25, 2.5, 5, 10 μM
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Incubation Time:48 h
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Result:Caused dose-dependent reductions in global asymmetric dimethylarginine (aDMA) and asymmetric dimethyl-PABP1 levels in HCT116 cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:6 to 8-week-old female BALB/c nude mice bearing subcutaneous HCT116 xenograft[1]
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Dosage:10, 25 mg/kg
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Administration:Intraperitoneal injection; daily; for 12 days
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Result:Showed evident inhibitory effect.
Chemical Information
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CAS No. 2878481-07-1
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Masse moléculaire 422.60
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Formule C24H42N2O4
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SMILES
CN(C[C@@H](O)CNC)CC1=CC=CC=C1OC2CCC(COCC)(COCC)CC2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CARM1-IN-4 Related Classifications
HY-161334 Related Classifications
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