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Art. -Nr.: HY-161334

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CARM1-IN-4

CARM1-IN-4 (compound 11f) is a potent CARM1 inhibitor with IC₅₀s of 9 nM and 56 nM for CARM1 and PRMT1, respectively. CARM1-IN-4 displays significant anti-proliferative effects on colorectal cancer cell lines. CARM1-IN-4 effectively inhibits the methyltransferase activity of CARM1 and prevents methylation of downstream proteins. CARM1-IN-4 induces apoptosis and shows antitumor activity.

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CAS. Nr.: 2878481-07-1
Formel: C₂₄H₄₂N₂O₄
Molecular Weight:422.60

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (269 KB)

CARM1-IN-4 Chemical Structure

CAS. Nr.: 2878481-07-1

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

CARM1

9 nM (IC₅₀)

PRMT1

56 nM (IC₅₀)

PRMT6

30 nM (IC₅₀)

PRMT8

31 nM (IC₅₀)

PRMT3

2637 nM (IC₅₀)

PRMT5

>100,000 nM (IC₅₀)

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	3.13 μM Compound: 11f	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth by CCK-8 assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth by CCK-8 assay	[PMID: 38460270]

In Vitro

CARM1-IN-4 (compound 11f) exhibits significant anti-proliferative activity in the HCT116 cell lines (IC₅₀=3.13 μM)^[1].
CARM1-IN-4 (0.625-5 μM; 72 h) causes a dose-dependent induction of apoptosis in HCT116 cell^[1].
CARM1-IN-4 (0.625-10 μM; 48 h) effectively inhibits the methyltransferase activity of CARM1, influencing the levels of asymmetric demethylation on CARM1 substrates within a cellular environment^[1].
CARM1-IN-4 exhibits a relatively high mitochondrial stability, with an extended half-life in mouse mitochondria (T_1/2=217 min)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis^[1]

Cell Line:

HCT116 cells
Concentration:

0.625, 1.25, 2.5, 5 μM
Incubation Time:

72 h
Result:

Illustrated a noticeable increase in the overall percentages of both early and late apoptotic cells.

Western Blot Analysis^[1]

Cell Line:

HCT116 cells
Concentration:

0.625, 1.25, 2.5, 5, 10 μM
Incubation Time:

48 h
Result:

Caused dose-dependent reductions in global asymmetric dimethylarginine (aDMA) and asymmetric dimethyl-PABP1 levels in HCT116 cells.

In Vivo

CARM1-IN-4 (compound 11f; 10, 25 mg/kg/day; ip; for 12 days) shows evident inhibitory effect in BALB/c nude mice bearing subcutaneous HCT116 xenograft^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

6 to 8-week-old female BALB/c nude mice bearing subcutaneous HCT116 xenograft^[1]
Dosage:

10, 25 mg/kg
Administration:

Intraperitoneal injection; daily; for 12 days
Result:

Showed evident inhibitory effect.

Chemical Information

CAS. Nr. 2878481-07-1
Molecular Weight 422.60
Formel C₂₄H₄₂N₂O₄
SMILES

CN(C[C@@H](O)CNC)CC1=CC=CC=C1OC2CCC(COCC)(COCC)CC2
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (269 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]. Chenyu Liu, et al. Structure-based discovery of potent CARM1 inhibitors for colorectal cancer therapy. Eur J Med Chem. 2024 Mar 4:269:116288. [Content Brief]

Calculators

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)}

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.

Keywords

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

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CARM1-IN-4

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

CARM1-IN-4 Related Classifications

HY-161334 Related Classifications