2. Epigenetics Apoptosis Metabolic Enzyme/Protease
  3. DNA Methyltransferase Apoptosis Caspase Mitochondrial Metabolism
  4. 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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DNMT-IN-6

DNMT-IN-6 Chemical Structure

CAS No. : 3038316-36-5

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DNMT-IN-6 Related Antibodies

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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Description

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[1].

IC50 & Target[1]

Caspase 3

 

Caspase 9

 

DNMT1

 

DNMT3A

 

DNMT3B

 

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.

DNMT-IN-6 Related Antibodies

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 T1/2 Tmax Cmax AUC0-t AUC0-∞ MRT0-t MRT0-∞ C0 Vss Vz 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.
Molecular Weight

447.40

Formula

C19H18AsNO3S2
CAS No.
SMILES

O=C(NC1=CC=C(C=C1)[As]2SCCCS2)/C=C/C3=CC4=C(OCO4)C=C3
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Purity & Documentation
References
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DNMT-IN-6 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

DNMT-IN-63038316-36-5DNA MethyltransferaseApoptosisCaspaseMitochondrial MetabolismDNMTsDNA MTasesMIN-6DB DLBCL cell linesDNMT3ADNMT1SUDHL-4HK-2TMS1DNMT3BSUDHL-6diffuse large B-cell lymphomaInhibitorinhibitorinhibit

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