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Art. -Nr.: HY-176230

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DNMT-IN-5

DNMT-IN-5 is a stable and efficient DNA methyltransferase (DNMT) inhibitor with high stability and high activity with an IC₅₀ of 0.78 nM. DNMT-IN-5 exhibits sub-micromolar DNMT3A inhibitory activity, upregulates the expression of DNMT-targeted genes, impairs cell proliferation, and triggers a critical cell cycle arrest. DNMT-IN-5 can be used for the study of p53-depleted colorectal cancer.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 3126555-64-1
Formel: C₁₆H₁₂BrClO₃
Molecular Weight:367.62

Speicherung:

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

Data Sheet (278 KB)

DNMT-IN-5 Chemical Structure

CAS. Nr.: 3126555-64-1

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Preis

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Menge

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Use of MCE Products

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

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

DNMT3A

9.15 μM (IC₅₀)

Alle DNA Methyltransferase Isoform-spezifische Produkte anzeigen :

In Vitro

DNMT-IN-5 (compound 34b) (0.1-30 μM; 3 days) still exhibits the activity of a DNMT 3A inhibitor at the nanomolar level, with an IC₅₀ value of 9.15 μM in HCT-116 cells^[1].
DNMT-IN-5 (5 μM; 0-5 days) significantly induces the upregulation of p15 and p16 expression by 1.76 (88%)-fold and 1.34 (67%)-fold, respectively in HCT-116 cells^[1].
DNMT-IN-5 (5 μM; 5 days) on DNMT-regulated genes varies by cell type and is most pronounced in HCT-116 cells^[1].
DNMT-IN-5 (5 μM; 5 days) triggers a critical cell cycle arrest in the G1/S transition, notably in p53-depleted HCT-116 colorectal cancer cells^[1].

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

Cell Viability Assay^[1]

Cell Line:

HCT-116
Concentration:

0.1 μM; 1 μM; 10 μM; 100 μM
Incubation Time:

3 days
Result:

Showed very similar cytotoxicity (IC₅₀ = 9.15 μM) among themselves and reference compound MLo1506 (IC₅₀ = 8.18 μM).

RT-PCR^[1]

Cell Line:

HCT-116
Concentration:

5 μM
Incubation Time:

0 d; 2 d; 5d
Result:

Significantly induced the upregulation of p15 expression by 1.76 (88%)-fold, compared to nontreated cells.
Increased p16 expression by 1.34 (67%)-fold.

Cell Cycle Analysis^[1]

Cell Line:

HCT-116, DU-145, U2OS
Concentration:

5 μM
Incubation Time:

5 days
Result:

Did not alter p15 expression in p53-KO cells but successfully induced p16 re-expression.
Strongly impaired the G1/S transition in the absence of p53 and led to a substantial population of defective replicating cells.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 3126555-64-1
Molecular Weight 367.62
Formel C₁₆H₁₂BrClO₃
SMILES

CO[C@]1(C2=CC=CC=C2)OC3=CC=CC=C3C([C@@]1(Cl)Br)=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 (278 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]. 1. Calzaferri F et al. Rational Design and Synthesis of Highly Stable Haloflavanone DNA Methyltransferase Inhibitors Inducing Tumor Suppressor Gene Re-expression in Cancer Cells. J Med Chem. 2025 Jun 12;68(11):10704-10721. doi: 10.1021. [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

Keywords

MOQ

Minimum order quantity

100 mg

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

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DNMT-IN-5

Alle DNA Methyltransferase Isoform-spezifische Produkte anzeigen