2. Epigenetics Vitamin D Related/Nuclear Receptor Immunology/Inflammation
  3. Histone Methyltransferase Estrogen Receptor/ERR IFNAR
  4. CARM1-IN-6

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.

CARM1-IN-6

CARM1-IN-6 Chemical Structure

CAS No. : 1269199-96-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of CARM1-IN-6:

CARM1-IN-6 Related Antibodies

Top Publications Citing Use of Products

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

View All Estrogen Receptor/ERR Isoform Specific Products:

View All Isoforms
Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

IC50 & Target

CARM1

12.3 μM (IC50)

CARM1

0.6785 μM (Kd)

ERα

 

In Vitro

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.

CARM1-IN-6 Related Antibodies

RT-PCR[1]

Cell Line: Wild-type and CARM1-knockout MCF7 cells, MDA-MB-231 cells
Concentration: 0.25, 5, 10 μM
Incubation Time: 4 days
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.

Cell Cytotoxicity Assay[1]

Cell Line: MCF7, T47D, BT474, MDA-MB-231, MDA-MB-468, HCC1806, and HCC1937 cells
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
Incubation Time: 7 days
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).

Cell Proliferation Assay[1]

Cell Line: MCF7, 4T1 cells
Concentration: 2.5 μM
Incubation Time: 1, 2, 3, 4 days
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).

Cell Proliferation Assay[1]

Cell Line: MCF7, MDA-MB-231 cells
Concentration: 2.5, 5, 10 μM
Incubation Time: 10 days
Result: Suppressed colony formation in MCF7 and MDA-MB-231 cells in a dose-dependent manner.
In Vivo

CARM1-IN-6 (compound iCARM1) (25 and 50 mg/kg; i.p.; every other day for 4 weeks) suppresses ERα-positive breast tumor growth in MCF7 mouse xenografts[1].
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.

Animal Model: Female BALB/C nude\r\nmice (4-6 weeks old) subcutaneously implanted with MCF7 cells[1]
Dosage: 25, 50 mg/kg
Administration: i.p.; every other day for 4 weeks
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).
Animal Model: Female BALB/C nude mice (4-6 weeks old) subcutaneously implanted with MDA-MB-231 cells[1]
Dosage: 25, 50 mg/kg
Administration: i.p.; daily for 11 days
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.
Animal Model: Female BALB/c wild-type mice (4-6 weeks old) subcutaneously implanted with 4T-1 cells[1]
Dosage: 25, 50 mg/kg
Administration: i.p.; daily for 14 days
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.
Molecular Weight

391.51

Formula

C23H29N5O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CN(C)CCN(CC1)CCN1C2=NC=C(C(C3=CC=C(C)C=C3)=N2)C4=COC=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5542 mL 12.7711 mL 25.5421 mL
5 mM 0.5108 mL 2.5542 mL 5.1084 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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C2

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Volume (final)

V2

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
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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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
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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CARM1-IN-6 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CARM1-IN-61269199-96-3Histone MethyltransferaseEstrogen Receptor/ERRIFNARInterferon-α/β receptorInterferon-alpha/beta receptortype I IFNendocrine therapy drugsISGsCARM1breast cancer cellsMCF7 cellsBALB/c nude miceetoposidebreast cancerERαInhibitorinhibitorinhibit

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