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Art. -Nr.: HY-114510

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PRMT/HKMT-IN-1

PRMT/HKMT-IN-1 is an epigenetic multi-target protein arginine methyltransferases (PRMTs) and histone lysine methyltransferases (HKMTs) inhibitor. PRMT/HKMT-IN-1 inhibits Aspergillus nidulans RmtA with an IC₅₀ of 29 μM. PRMT/HKMT-IN-1 inhibits human PRMT1, p300/CBP HAT, CARM1, SET7, SIRT1 and SIRT2. PRMT/HKMT-IN-1 inhibits methylation of histone H3K4, H4R3, and H3R17 residues. CBP/p300-IN-23 induces apoptosis, arrests cell cycle in S phase, and triggers granulocytic differentiation in leukemia cells. PRMT/HKMT-IN-1 can be used for the research of leukemia.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 1020399-52-3
Formel: C₁₉H₁₂Br₄O₄
Molecular Weight:623.92

Speicherung:

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

PRMT/HKMT-IN-1 Chemical Structure

CAS. Nr.: 1020399-52-3

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Preis

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Use of MCE Products

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

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

CBP/p300

SIRT1

SIRT2

Alle Discoidin Domain Receptor Isoform-spezifische Produkte anzeigen :

DDR1
DDR2

Alle Histone Acetyltransferase Isoform-spezifische Produkte anzeigen :

Alle Sirtuin Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
U-937	Inhibition	61 % Compound: 4j	Inhibition of human p300/CBP in U937 cells at 50 uM assessed as histone H3 acetylation Inhibition of human p300/CBP in U937 cells at 50 uM assessed as histone H3 acetylation	[PMID: 18348515]

In Vitro

PRMT/HKMT-IN-1 (Compound 4j) inhibits fungal RmtA with an IC₅₀ of 29 μM^[1].
PRMT/HKMT-IN-1 (50 μM) inhibits human PRMT1 activity by 91.1% using histone H4 as substrate^[1].
PRMT/HKMT-IN-1 (100 μM; 90 min) strongly inhibits human CARM1 and SET7^[1].
PRMT/HKMT-IN-1 (50 μM; 24 h) reduces H3K4, H4R3, and H3R17 methylation in U937 cells^[1].
CBP/p300-IN-23 (50 μM; 90 min) inhibits p300/CBP HAT activity by 61%^[1].
PRMT/HKMT-IN-1 (25 μM; 2 h) inhibits SIRT1 and SIRT2^[1].
PRMT/HKMT-IN-1 (25 μM; 30 h) induces 28% apoptosis in human leukemia U937 cells^[1].
PRMT/HKMT-IN-1 (0.5-5 μM; 30 h) induces dose-dependent granulocytic differentiation in human leukemia U937 cells, with 96.1% CD11c-positive cells at 5 μM after 30 h of treatment^[1].
CBP/p300-IN-23 (25 μM; 30 h) induces S phase cell cycle arrest in human leukemia U937 cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

Human leukemia U937 cells
Concentration:

50 μM
Incubation Time:

24 h
Result:

Strongly inhibited H3K4 monomethylation.
Inhibited H4R3 monomethylation.
Inhibited H3R17 dimethylation.

Apoptosis Analysis^[1]

Cell Line:

Human leukemia U937 cells
Concentration:

25 μM
Incubation Time:

30 h
Result:

Induced 28% apoptosis in U937 cells.

Cell Differentiation Assay^[1]

Cell Line:

Human leukemia U937 cells
Concentration:

0.5-5 μM
Incubation Time:

30 h
Result:

Induced 96.1% CD11c-positive/PI-negative cells at 5 μM.
Induced 67% CD11c-positive/PI-negative cells at 1 μM.
Induced 59% CD11c-positive/PI-negative cells at 0.5 μM, showing a dose-dependent differentiating effect.

Cell Cycle Analysis^[1]

Cell Line:

Human leukemia U937 cells
Concentration:

25 μM
Incubation Time:

30 h
Result:

Induced cell cycle arrest in S phase.

Related Protocols :

Chemical Information

CAS. Nr. 1020399-52-3
Molecular Weight 623.92
Formel C₁₉H₁₂Br₄O₄
SMILES

O=C1C(=CC2=CC(Br)=C(O)C(Br)=C2)COCC1=CC3=CC(Br)=C(O)C(Br)=C3
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

Handling Instructions (2659 KB)

Verweise

[1]. Mai A, et al. epigenetic multiple ligands: mixed histone/protein methyltransferase, acetyltransferase, and class III deacetylase (sirtuin) inhibitors. J Med Chem. 2008;51(7):2279-2290. [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.

Bioz

MOQ

Minimum order quantity

100 mg

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

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PRMT/HKMT-IN-1

Alle Discoidin Domain Receptor Isoform-spezifische Produkte anzeigen

Alle Histone Acetyltransferase Isoform-spezifische Produkte anzeigen

Alle Sirtuin Isoform-spezifische Produkte anzeigen