CARM1-IN-1
Based on 4 publication(s) in Google Scholar
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.
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- Pureté : 95.0%
- CAS No.: 1020399-49-8
- Formule: C26H21Br2NO3
- Masse moléculaire:555.26
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) CARM1-IN-1
MoreVoir tous les produits spécifiques à Isoform Histone Methyltransferase
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Activité biologique
Description
IC50 & Target
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PRMT4 |
In Vitro
CARM1-IN-1 (compound 7g) (100 μM; 90 min) inhibits CARM1-mediated methylation of different substrates (PABP1, CA150, SmB, and H3), such as Flag-PABP1 methylation, without inhibitory activity against HKMTs[1].
CARM1-IN-1 (compound 7g) (8 μM; 42-44 h) inhibits PSA promoter activity in luciferase assay in LNCaP cells, without affecting cell viability[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:PCR LNCa cells
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Concentration:1 μM, 2 μM, 4 μM, 6 μM, 8 μM
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Incubation Time:42-48 h
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Result:Showed a significant dose-dependent reduction of the PSA promoter activity, at concentration that did not affect cell viability.
Chemical Information
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CAS No. 1020399-49-8
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Appearance Solid
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Masse moléculaire 555.26
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Formule C26H21Br2NO3
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Color Yellow to orange
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SMILES
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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Sci Bull (Beijing)
TRIM28 protects CARM1 from proteasome-mediated degradation to prevent colorectal cancer metastasis. [Abstract]2019 Jul 30;64(14):986-997. PMID: 36659810 -
Theriogenology
Unveiling the effects of regulating endogenous growth factors and apoptosis via DGCR8 on yak blastocyst formation. [Abstract]2026 Feb 1:251:117750. PMID: 41240745 -
Theriogenology
Paraspeckles / CARM1 mediates the regulation of OEVs on cell differentiation during in vitro embryonic development of yak. [Abstract]2024 Jul 15:223:74-88. PMID: 38692037 -
Solvant et solubilité
In Vitro:
DMSO : ≥ 35 mg/mL (63.03 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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 (4.50 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 (4.50 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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.
In Vivo Dissolution Calculator
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.
Protocole
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Dual Luciferin reporter gene assay
Luciferin reporter gene assay is a reporting system to detect the activity of Firefly Luciferase using luciferin as a substrate, which is often used in the research of miRNA target gene verification and promoter transcriptive activity regulation. Dual luciferase usually refers to Firefly luciferase and Renilla luciferase.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Mammalian live/dead viability and cytotoxicity staining
Live/dead viability and cytotoxicity staining assays are based on the simultaneous detection of intracellular esterase activity in metabolically active (viable) cells and membrane integrity loss in non-viable cells. In commonly used dual-staining approaches, membrane-permeant fluorogenic substrates are converted by intracellular esterases into fluorescent products in live cells, while impermeant DNA-binding dyes selectively enter cells with compromised plasma membranes and label nucleic acids in dead or dying cells, enabling discrimination between viable and non-viable populations by fluorescence microscopy or flow cytometry.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Pureté et documentation
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Fiche technique (278 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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Instruction de manipulation (2659 KB)
Références
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.8010 mL | 9.0048 mL | 18.0096 mL | 45.0240 mL |
| 5 mM | 0.3602 mL | 1.8010 mL | 3.6019 mL | 9.0048 mL | |
| 10 mM | 0.1801 mL | 0.9005 mL | 1.8010 mL | 4.5024 mL | |
| 15 mM | 0.1201 mL | 0.6003 mL | 1.2006 mL | 3.0016 mL | |
| 20 mM | 0.0900 mL | 0.4502 mL | 0.9005 mL | 2.2512 mL | |
| 25 mM | 0.0720 mL | 0.3602 mL | 0.7204 mL | 1.8010 mL | |
| 30 mM | 0.0600 mL | 0.3002 mL | 0.6003 mL | 1.5008 mL | |
| 40 mM | 0.0450 mL | 0.2251 mL | 0.4502 mL | 1.1256 mL | |
| 50 mM | 0.0360 mL | 0.1801 mL | 0.3602 mL | 0.9005 mL | |
| 60 mM | 0.0300 mL | 0.1501 mL | 0.3002 mL | 0.7504 mL |
CARM1-IN-1 Related Classifications
HY-12759 Related Classifications
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