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Art. -Nr.: HY-182009

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DNMT-IN-6

DNMT-IN-6 is a DNA methyltransferase inhibitor with activity against DNMT1, DNMT3A, and DNMT3B. DNMT-IN-6 drives demethylation, and restores TMS1 tumor suppressor gene expression. DNMT-IN-6 induces apoptosis, causes G2/M phase arrest, disrupts mitochondrial integrity, and activates the intrinsic caspase cascade (3/7/9). DNMT-IN-6 inhibits tumor growth, and improves survival in xenograft models. DNMT-IN-6 can be used for the research of cancer, such as diffuse large B-cell lymphoma.

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CAS. Nr.: 3038316-36-5
Formel: C₁₉H₁₈AsNO₃S₂
Molecular Weight:447.40

Speicherung:

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

DNMT-IN-6 Chemical Structure

CAS. Nr.: 3038316-36-5

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Use of MCE Products

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

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

Caspase 3

Caspase 9

DNMT1

DNMT3A

DNMT3B

Alle DNA Methyltransferase Isoform-spezifische Produkte anzeigen :

Alle Caspase Isoform-spezifische Produkte anzeigen :

In Vitro

DNMT-IN-6 (Compound CZ2) (0.2-1.4 μM; 24-48 h) potently inhibits proliferation of SUDHL-4, SUDHL-6, and DB DLBCL cell lines in a dose- and time-dependent manner, with 24 h IC₅₀ values of 0.67 μM, 0.72 μM, and ~0.90 μM respectively, and exhibits minimal cytotoxicity to normal HK-2 and MIN-6 cells^[1].
DNMT-IN-6 (1 μM; 24 h) induces mitochondrial membrane depolarization in SUDHL-4 and SUDHL-6 DLBCL cells^[1].
DNMT-IN-6 (1 μM; 24 h) significantly induces apoptosis in SUDHL-4 and SUDHL-6 DLBCL cells, and activates caspase-3 and caspase-9^[1].
DNMT-IN-6 (1 μM; 24 h) reduces intracellular ATP levels in SUDHL-4 and SUDHL-6 DLBCL cells^[1].
DNMT-IN-6 (1 μM; 24 h) induces G2/M cell cycle arrest in SUDHL-6 DLBCL cells^[1].
DNMT-IN-6 (1 μM; 24 h) reduces TMS1 promoter methylation, increases TMS1 expression, and decreases DNMT1, DNMT3A, and DNMT3B expression in SUDHL-4 and SUDHL-6 DLBCL cells^[1].
DNMT-IN-6 (1 μM; 24 h) inhibits the binding of DNMT3A to the TMS1 promoter in SUDHL-4 DLBCL cells, contributing to TMS1 promoter demethylation^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

diffuse large B-cell lymphoma (DLBCL) cell lines SUDHL-4, SUDHL-6, DB; normal human cell lines HK-2, MIN-6
Concentration:

0.2, 0.4, 0.6, 0.8, 1.0, 1.2, 1.4 μM
Incubation Time:

24, 36. 48 h
Result:

Inhibited proliferation of DLBCL cells in a dose- and time-dependent manner.
Reduced IC₅₀ in SUDHL-4 cells to 0.67±0.08 μM at 24 h, and 0.38±0.05 μM at 48 h.
Reduced IC₅₀ in SUDHL-6 cells to 0.72±0.09 μM at 24 h, and 0.41±0.06 μM at 48 h.
Maintained an IC₅₀ of ~0.90 μM in DB cells across 24-48 h.
Showed minimal cytotoxicity to HK-2 and MIN-6 normal cells at 1 μM for 24 h.

Apoptosis Analysis^[1]

Cell Line:

DLBCL cell lines SUDHL-4, SUDHL-6
Concentration:

1 μM
Incubation Time:

24 h (CZ2 treatment); 1 h (Z-VAD-FMK pre-incubation)
Result:

Significantly increased the percentage of apoptotic (Annexin V+/PI- early apoptotic and Annexin V+/PI+ late apoptotic/necrotic) cells in SUDHL-4 and SUDHL-6 cells.
Was effectively blocked by pre-incubation with Z-VAD-FMK (HY-16658B) in SUDHL-4 cells.
Increased caspase-3 and caspase-9 levels.

Cell Cycle Analysis^[1]

Cell Line:

DLBCL cell line SUDHL-6
Concentration:

1 μM
Incubation Time:

24 h
Result:

Induced G2/M cell cycle arrest in SUDHL-6 cells, with a significant increase in the percentage of cells in G2/M phase.

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	AUC_0-t	AUC_0-∞	MRT_0-t	MRT_0-∞	C₀	V_ss	V_z	CL
Mice^[1]	3.5 mg/kg	i.v.	2.68 h	0.083 h	1155.00 ng/mL	572.26	617.02	1.37 h	2.18 h	3121.62 ng/mL	13.60 L/kg	23.68 L/kg	99.50 mL/min/kg

In Vivo

DNMT-IN-6 (Compound CZ2) (3.5 mg/kg; i.p.; every other day; 12 days) achieves 71.39% tumor growth inhibition, reduces tumor weight, prolongs survival, and modulates the TMS1/DNMT3A axis with a favorable safety profile in BALB/c nude mice bearing SUDHL-4 DLBCL xenografts^[1].

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

Animal Model:

BALB/c nude (4-6 week-old male; subcutaneous xenograft via injection of 1×10⁷ SUDHL-4 cells)^[1]
Dosage:

3.5 mg/kg
Administration:

i.p.; every other day; 12 days
Result:

Achieved 71.39% tumor growth inhibition.
Significantly reduced final tumor weight compared to controls.
Significantly prolonged overall survival of tumor-bearing mice.
Significantly upregulated TMS1 protein expression and downregulated DNMT3A protein expression in tumor tissue.
Showed no significant alteration in peripheral white blood cell counts, no significant histopathological changes in heart, liver, or kidney tissues, and no significant difference in kidney injury markers KIM-1 and NGAL relative to controls.

Chemical Information

CAS. Nr. 3038316-36-5
Molecular Weight 447.40
Formel C₁₉H₁₈AsNO₃S₂
SMILES

O=C(NC1=CC=C(C=C1)[As]2SCCCS2)/C=C/C3=CC4=C(OCO4)C=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]. Mei W, et al. Epigenetic reprogramming by organic arsenic CZ2 elicits potent antitumor responses in DLBCL through TMS1 restoration. Bioorg Chem. Published online March 9, 2026. [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

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100 mg

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

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DNMT-IN-6

Alle DNA Methyltransferase Isoform-spezifische Produkte anzeigen

Alle Caspase Isoform-spezifische Produkte anzeigen