CARM1-IN-6
Based on 1 Customer Validation
CARM1-IN-6 is a potent CARM1 inhibitor that inhibits CARM1 enzymatic activity with an IC50 of 12.3 μM and a Kd of 0.6785 μM. CARM1-IN-6 suppresses oncogenic estrogen/ERα-target gene expression, activates type I interferon (IFN) and IFN-induced genes (ISGs), induces cell cycle arrest, and inhibits breast cancer cell proliferation both in vitro and in vivo. CARM1-IN-6 can be used for the research of breast cancer.
For research use only. We do not sell to patients.
- Purity: 99.59%
- CAS No.: 1269199-96-3
- Formula: C23H29N5O
- Molecular Weight:391.51
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Epigenetics Compound Library
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Immunology/Inflammation Compound Library
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Immunopotentiator Compound Library
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Anti-Ovarian Cancer Compound Library
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Multi-Target Compound Library
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Bioactive Compound Library Max
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MCE Bioactive Compound Library
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Bioactive Compound Library
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Methylation Compound Library
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High-Throughput Bioactive Compound Library
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All Histone Methyltransferase Isoforms
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Biological Activity
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CARM1 12.3 μM (IC50) |
CARM1 0.6785 μM (Kd) |
ERα |
CARM1-IN-6 (compound iCARM1) (2.5-10 µM; 4 days) represses estrogen-induced genes and activates type I IFN/ISGs in breast cancer cells (MCF7 and MDA-MB-231) in a dose-dependent and CARM1-dependent manner[1].
CARM1-IN-6 (0.098-100 µM; 7 days) inhibits cell proliferation of breast cancer cells with EC50 values of 1.797 (MCF7), 4.74 (T47D), 2.13 (BT474), 3.75 (MDA-MB-231), 2.02 (MDA-MB-468), 2.83 (HCC1806), and 1.97 μM (HCC1937), respectively
[1].
CARM1-IN-6 (2.5 µM, 1-4 days) synergizes with Tamoxifen (HY-13757A) to inhibit MCF7 cell growth, and synergizes with Etoposide (HY-13629) to inhibit both MCF7 and 4T1 cell growth[1].
CARM1-IN-6 (2.5-10 µM) induces G0-G1 cell cycle arrest in MCF7 cells in a dose-dependent manner[1].
CARM1-IN-6 (2.5 µM, 3 days) downregulates key estrogen/ERα-induced oncogenes, such as CCND1, c-Myc, and TFF1, in MCF7 cells[1].
CARM1-IN-6 (2.5-10 µM, 10 days) suppresses colony formation in MCF7 and MDA-MB-231 cells in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Wild-type and CARM1-knockout MCF7 cells, MDA-MB-231 cells
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Concentration:0.25, 5, 10 μM
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Incubation Time:4 days
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Result:Inhibited estrogen-induced genes, such as CCND1, c-Myc, N-myc, TFF1, GREB1, NRIP1, FOXC1, and PGR in MCF7 and MDA-MB-231 cells in a dose-dependent manner.
showed no repression effect in CARM1-knockout MCF7 cells.
Induced 158 genes overlapping with CARM1 knockdown, including type I IFN and ISGs (IFNα, ISG15, CCL5, IFIT1, DDX58) in a dose-dependent and CARM1-dependent manner in MCF7 and MDA-MB-231 cells.
Activated the transcription of type I IFN and ISGs, including ISG15, CCL5, IFIT1, and DDX58 in MCF7 and MDA-MB-231 cells in a dose- and CARM1-dependent manner.
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Cell Line:MCF7, T47D, BT474, MDA-MB-231, MDA-MB-468, HCC1806, and HCC1937 cells
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Concentration:0.098, 0.195, 0.391, 0.781, 1.563, 2.5, 3.125, 5, 6.25, 10, 12.5, 25, 50, 100 μM
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Incubation Time:7 days
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Result:Inhibited growth of ERα-positive cells (MCF7, T47D, and BT474 cells) and TNBC cells (MDA-MB-231, MDA-MB-468, HCC1806, and HCC1937 cells).
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Cell Line:MCF7, 4T1 cells
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Concentration:2.5 μM
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Incubation Time:1, 2, 3, 4 days
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Result:Showed synergistic inhibition of MCF7 cell growth with Tamoxifen (5 μM).
Showed synergistic inhibition of MCF7 and 4T1 cell growth with Etoposide (10 μM).
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Cell Line:MCF7, MDA-MB-231 cells
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Concentration:2.5, 5, 10 μM
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Incubation Time:10 days
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Result:Suppressed colony formation in MCF7 and MDA-MB-231 cells in a dose-dependent manner.
CARM1-IN-6 (25 and 50 mg/kg; i.p.; daily for 11 days) effectively suppresses tumor growth in MDA-MB-231 cells-derived mouse xenografts[1].
CARM1-IN-6 (25 and 50 mg/kg; i.p.; daily for 14 days) potently suppresses tumor growth and enhances antitumor immunity in a syngeneic 4T-1 mouse model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/C nude\r\nmice (4-6 weeks old) subcutaneously implanted with MCF7 cells[1]
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Dosage:25, 50 mg/kg
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Administration:i.p.; every other day for 4 weeks
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Result:Inhibited MCF7 xenograft growth with significant reduction in tumor size and weight.
Did not induce notable alterations in body weight or the morphology of organs, including the heart, liver, spleen, lungs, and kidneys.
Reduced expression of oncogenic estrogen/ERα-target genes (CCND1, c-Myc, N-myc, TFF1, GREB1, NRIP1, FOXC1, PGR).
Significant induced expression of type I IFN and ISGs (IFNα, ISG15, CCL5, IFIT1, DDX58).
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Animal Model:Female BALB/C nude mice (4-6 weeks old) subcutaneously implanted with MDA-MB-231 cells[1]
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Dosage:25, 50 mg/kg
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Administration:i.p.; daily for 11 days
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Result:Inhibited MDA-MB-231 xenograft growth with significant reduction in tumor size and weight.
Exhibited no significant impact on body weight and organ morphology.
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Animal Model:Female BALB/c wild-type mice (4-6 weeks old) subcutaneously implanted with 4T-1 cells[1]
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Dosage:25, 50 mg/kg
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Administration:i.p.; daily for 14 days
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Result:Inhibited 4T-1 allograft growth with significant reduction in tumor size and weight.
Caused no significant changes in the body weight and organ morphology.
Significantly decreased the expression of representative oncogenic estrogen/ERα-target genes including Ccnd1, C-myc, N-myc, Tff1, Greb1, Nrip1, Foxc1, and Pgr.
Significantly increased the expression of Ifnα and ISGs including Isg15, Ccl5, Ifit1, and Ddx58.
Induced the expression of Cd8a and infiltration of CD8+ T cells.
Chemical Information
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CAS No. 1269199-96-3
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Appearance Solid
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Molecular Weight 391.51
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Formula C23H29N5O
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Color White to off-white
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SMILES
CN(C)CCN(CC1)CCN1C2=NC=C(C(C3=CC=C(C)C=C3)=N2)C4=COC=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (255.42 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.39 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.39 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5542 mL | 12.7711 mL | 25.5421 mL | 63.8553 mL |
| 5 mM | 0.5108 mL | 2.5542 mL | 5.1084 mL | 12.7711 mL | |
| 10 mM | 0.2554 mL | 1.2771 mL | 2.5542 mL | 6.3855 mL | |
| 15 mM | 0.1703 mL | 0.8514 mL | 1.7028 mL | 4.2570 mL | |
| 20 mM | 0.1277 mL | 0.6386 mL | 1.2771 mL | 3.1928 mL | |
| 25 mM | 0.1022 mL | 0.5108 mL | 1.0217 mL | 2.5542 mL | |
| 30 mM | 0.0851 mL | 0.4257 mL | 0.8514 mL | 2.1285 mL | |
| 40 mM | 0.0639 mL | 0.3193 mL | 0.6386 mL | 1.5964 mL | |
| 50 mM | 0.0511 mL | 0.2554 mL | 0.5108 mL | 1.2771 mL | |
| 60 mM | 0.0426 mL | 0.2129 mL | 0.4257 mL | 1.0643 mL | |
| 80 mM | 0.0319 mL | 0.1596 mL | 0.3193 mL | 0.7982 mL | |
| 100 mM | 0.0255 mL | 0.1277 mL | 0.2554 mL | 0.6386 mL |
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