| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg | |||
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| Targets |
CARM1-IN-7G selectively targets CARM1, an enzyme that methylates arginine residues on histone and non-histone proteins. It has an IC50 of 8.6 µM for CARM1 and shows weak activity against other methyltransferases like PRMT1 and SET7 (IC50 > 600 µM).
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|---|---|
| ln Vitro |
In vitro, CARM1-IN-7G inhibits CARM1-mediated methylation of various substrates, including PABP1, CA150, SmB, and histone H3, at single-digit micromolar levels. It significantly and dose-dependently reduces prostate-specific antigen (PSA) promoter activity in human prostate cancer LNCaP cells without affecting cell viability.
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| ln Vivo |
In vivo data for CARM1-IN-7G is not extensively reported. As a selective inhibitor, it is primarily used as a research tool to study the biological functions of CARM1 in cells. Its in vivo effects would be related to the role of CARM1 in various diseases, including cancer.
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| Enzyme Assay |
The in vitro assay for CARM1-IN-7G measures its ability to inhibit CARM1-mediated methylation. This is typically performed using a radioactive or antibody-based assay where the enzyme is incubated with a substrate and the inhibitor, and the incorporation of methyl groups is quantified.
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| Cell Assay |
In vitro cell-based assays are performed in cancer cell lines like LNCaP. Cells are treated with the inhibitor, and the methylation of CARM1 substrates is assessed by Western blotting. The effect on gene expression, such as the reduction of PSA promoter activity, is also measured.
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| Animal Protocol |
In vivo studies with CARM1-IN-7G would involve administering the compound to tumor-bearing mice in a xenograft model to assess its effect on tumor growth. Endpoints would include tumor volume and analysis of CARM1 target methylation and downstream signaling in the tumor tissue.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of CARM1-IN-7G are not detailed in the literature. As a research compound, its primary use is in vitro, and its in vivo PK properties would need to be determined for any therapeutic development.
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| Toxicity/Toxicokinetics |
Toxicological data for CARM1-IN-7G is not available. As a research compound, it is not intended for human use. Its safety profile would need to be established in preclinical studies if it were to be developed further.
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| References | |
| Additional Infomation |
CARM1-IN-7G is a valuable research tool for studying the role of arginine methylation in gene expression and disease. It is used to probe the function of CARM1 in various cellular processes, including transcription, mRNA splicing, and DNA damage repair. It is not an approved drug.
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| Molecular Formula |
C26H21BR2NO3
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|---|---|
| Molecular Weight |
555.26
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| Exact Mass |
552.989
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| CAS # |
1020399-49-8
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| Related CAS # |
CARM1-IN-1 hydrochloride;2070018-31-2
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| PubChem CID |
24827559
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| Appearance |
Yellow to orange solid powder
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| LogP |
6.112
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
32
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| Complexity |
670
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C\1N(C/C(=C\C2=CC(=C(C=C2)O)Br)/C(=O)/C1=C/C3=CC(=C(C=C3)O)Br)CC4=CC=CC=C4
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| InChi Key |
KNMFTTWVELIVCC-CLVAPQHMSA-N
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| InChi Code |
InChI=1S/C26H21Br2NO3/c27-22-12-18(6-8-24(22)30)10-20-15-29(14-17-4-2-1-3-5-17)16-21(26(20)32)11-19-7-9-25(31)23(28)13-19/h1-13,30-31H,14-16H2/b20-10+,21-11+
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| Chemical Name |
(3E,5E)-1-benzyl-3,5-bis[(3-bromo-4-hydroxyphenyl)methylidene]piperidin-4-one
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| Synonyms |
CARM1 IN 7G CARM1IN7G CARM1-IN-7G
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 35 mg/mL (~63.03 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.50 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (4.50 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8010 mL | 9.0048 mL | 18.0096 mL | |
| 5 mM | 0.3602 mL | 1.8010 mL | 3.6019 mL | |
| 10 mM | 0.1801 mL | 0.9005 mL | 1.8010 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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