Art. -Nr.: HY-163561

CARM1-IN-6

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CARM1-IN-6 is a potent CARM1 inhibitor that inhibits CARM1 enzymatic activity with an IC₅₀ of 12.3 μM and a K_d 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.

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Reinheit: 99.59%
CAS. Nr.: 1269199-96-3
Formel: C₂₃H₂₉N₅O
Molecular Weight:391.51

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

CARM1-IN-6 Chemical Structure

CAS. Nr.: 1269199-96-3

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

CARM1

12.3 μM (IC₅₀)

CARM1

0.6785 μM (Kd)

ERα

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen :

Alle Estrogen Receptor/ERR Isoform-spezifische Produkte anzeigen :

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 EC₅₀values 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.

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.

Chemical Information

CAS. Nr. 1269199-96-3
Appearance Solid
Molecular Weight 391.51
Formel C₂₃H₂₉N₅O
Color White to off-white
SMILES

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

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5542 mL

12.7711 mL

25.5421 mL

5 mM

0.5108 mL

2.5542 mL

5.1084 mL

10 mM

0.2554 mL

1.2771 mL

2.5542 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.39 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Peng BL, et al. A CARM1 Inhibitor Potently Suppresses Breast Cancer Both In Vitro and In Vivo. J Med Chem. 2024;67(10):7921-7934. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

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CARM1-IN-6

Epigenetics Compound Library

Immunology/Inflammation Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Pyroptosis Compound Library

Anti-Breast Cancer Compound Library

Anti-Blood Cancer Compound Library

Nuclear Receptor Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Autoimmune Disease Compound Library

Anti-Hematopathy Compound Library

Immunopotentiator Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Alle Estrogen Receptor/ERR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CARM1-IN-6

Epigenetics Compound Library

Immunology/Inflammation Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Pyroptosis Compound Library

Anti-Breast Cancer Compound Library

Anti-Blood Cancer Compound Library

Nuclear Receptor Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Autoimmune Disease Compound Library

Anti-Hematopathy Compound Library

Immunopotentiator Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Alle Estrogen Receptor/ERR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CARM1-IN-6 Related Classifications

HY-163561 Related Classifications