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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 3038316-36-5
- 分子式: C19H18AsNO3S2
- 分子量:447.40
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
生物活性
製品説明
IC50 & Target
[1]|
Caspase 3 |
Caspase 9 |
DNMT1 |
DNMT3A |
DNMT3B |
体外実験
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 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.
-
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 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 |
体内実験
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.
化学情報
-
CAS 番号 3038316-36-5
-
分子量 447.40
-
分子式 C19H18AsNO3S2
-
SMILES
O=C(NC1=CC=C(C=C1)[As]2SCCCS2)/C=C/C3=CC4=C(OCO4)C=C3
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
DNMT-IN-6 関連分類
HY-182009 関連分類
Powered by Bioz