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Art. -Nr.: HY-158158

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CARM1-IN-5

CARM1-IN-5 (Compound 17e) is a potent and selective inhibitor of CARM1 (IC₅₀= 2 nM). CARM1-IN-5 effectively prevents CARM1 from methylating substrate proteins by directly interacting with CARM1. CARM1-IN-5 exhibits significant antiproliferative effects on melanoma cell lines.

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CAS. Nr.: 3036054-38-0
Formel: C₂₂H₂₆ClN₃O₂S
Molecular Weight:431.98

Speicherung:

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

Data Sheet (277 KB)

CARM1-IN-5 Chemical Structure

CAS. Nr.: 3036054-38-0

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Fluorescent Dye

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

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

Biologische Aktivität

Beschreibung

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A2058	IC₅₀	1.74 μM Compound: 17e	Antiproliferative activity against human A2058 cells assessed as reduction in cell viability measured after 4 days by CCK8 method Antiproliferative activity against human A2058 cells assessed as reduction in cell viability measured after 4 days by CCK8 method	[PMID: 38574345]
A-375	IC₅₀	0.55 μM Compound: 17e	Antiproliferative activity against human A-375 cells assessed as reduction in cell viability measured after 4 days by CCK8 method Antiproliferative activity against human A-375 cells assessed as reduction in cell viability measured after 4 days by CCK8 method	[PMID: 38574345]

In Vitro

CARM1-IN-5 is selective for CARM1. IC₅₀ is 2 ± 1 nM (CARM1), 213 ± 45 nM (PRMT1), 942 ± 78 nM (PRMT3), 64 ± 9 nM (PRMT6), 73 ± 8 nM (PRMT8), >100,000 nM ( PRMT5), >100,000 nM (PRMT7)^[1].
CARM1-IN-5 antiproliferative activity against two melanoma cell lines was IC₅₀ = 0.55 ± 0.03 μM (A375); 1.74 ± 0.07 μM (A2058)^[1].
CARM1-IN-5 (0-5 μM; 72 h) can enter A375 Cells and bind directly to CARM1. CARM1-IN-5 also can affect the level of asymmetric dimethylation of CARM1 substrates in the cellular environment by inhibiting the methyltransferase activity of CARM1^[1].

In vitro metabolic stability in Mouse Liver Microsomes^[1]

t_1/2 (min)	Cl (mL/min/kg)
41.5	132

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

Western Blot Analysis^[1]

Cell Line:

A375 Cells
Concentration:

0; 0.3; 0.6; 1.2; 2.5; 5μM
Incubation Time:

72h
Result:

Enhanced protein thermal stability of CARM1 in a concentration-dependent manner.
Reduced asymmetric dimethyl-PABP1 and overall aDMA levels in a dose-dependent manner.

In Vivo

CARM1-IN-5 (i.p.; 10 mg/kg/day and 25 mg/kg/day; 14 days) inhibits tumor growth in BALB/c nude mice bearing subcutaneous A375 xenograft^[1].

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

Animal Model:

BALB/c nude mice bearing subcutaneous A375 xenograft ^[1]
Dosage:

10 mg/kg/daily; 25 mg/kg/daily for 14 days
Administration:

i.p.
Result:

TGI was 63% (25 mg/kg) and 55% (10 mg/kg).
Significantly reduced asymmetric dimethylation by western blotting.

Chemical Information

CAS. Nr. 3036054-38-0
Molecular Weight 431.98
Formel C₂₂H₂₆ClN₃O₂S
SMILES

CN(CC1=CC=CC=C1OCC2=CC(Cl)=C(C=C2)C3=NC=CS3)C[C@H](CNC)O
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 (277 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]. Liu Z, et al. Development of (2-(Benzyloxy)phenyl)methanamine Derivatives as Potent and Selective Inhibitors of CARM1 for the Treatment of Melanoma. J Med Chem. 2024 Apr 25;67(8):6313-6326. [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.

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Biologische Aktivität
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- In Vitro
- In Vivo
Chemical Information
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CARM1-IN-5

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

CARM1-IN-5 Related Classifications

HY-158158 Related Classifications