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

DNMT-IN-6 是一种 DNA 甲基转移酶抑制剂，对 DNMT1、DNMT3A 和 DNMT3B 均具有活性。DNMT-IN-6 可驱动去甲基化，并恢复 TMS1 抑癌基因的表达。DNMT-IN-6 可诱导细胞凋亡 (apoptosis)，引发 G2/M 期阻滞，破坏线粒体完整性，并激活内源性 caspase 级联反应 (3/7/9)。DNMT-IN-6 可抑制肿瘤生长，并改善异种移植模型中的存活率。DNMT-IN-6 可用于癌症研究，例如弥漫性大 B 细胞淋巴瘤。

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DNMT-IN-6

DNMT-IN-6 Chemical Structure

CAS No. : 3038316-36-5

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DNMT-IN-6 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

 

体外研究
(In Vitro)

DNMT-IN-6 (Compound CZ2) (0.2-1.4 μM; 24-48 h) 可强效且呈剂量和时间依赖性地抑制 SUDHL-4、SUDHL-6 和 DB 弥漫性大 B 细胞淋巴瘤 (DLBCL) 细胞系的增殖，其 24 h 的 IC50 值分别为 0.67 μM、0.72 μM 和 ~0.90 μM；且对正常 HK-2 和 MIN-6 细胞的细胞毒性极低[1]。
DNMT-IN-6 (1 μM; 24 h) 可诱导 SUDHL-4 和 SUDHL-6 弥漫大 B 细胞淋巴瘤 (DLBCL) 细胞发生线粒体膜去极化[1]。
DNMT-IN-6 (1 μM; 24 h) 可显著诱导 SUDHL-4 和 SUDHL-6 弥漫性大 B 细胞淋巴瘤 (DLBCL) 细胞发生凋亡，且能激活 caspase-3 和 caspase-9[1]。
DNMT-IN-6 (1 μM; 24 h) 可降低 SUDHL-4 和 SUDHL-6 弥漫性大 B 细胞淋巴瘤 (DLBCL) 细胞内的 ATP 水平[1]。
DNMT-IN-6 (1 μM; 24 h) 可诱导 SUDHL-6 弥漫性大 B 细胞淋巴瘤 (DLBCL) 细胞发生 G2/M 期细胞周期阻滞[1]。
DNMT-IN-6 (1 μM; 24 h) 可降低 TMS1 启动子甲基化水平，上调 TMS1 的表达，并下调 SUDHL-4 和 SUDHL-6 弥漫性大 B 细胞淋巴瘤 (DLBCL) 细胞中 DNMT1、DNMT3A 及 DNMT3B 的表达[1]。
DNMT-IN-6 (1 μM; 24 h) 可抑制 DNMT3A 与 SUDHL-4 弥漫性大 B 细胞淋巴瘤 (DLBCL) 细胞中 TMS1 启动子的结合，进而促进 TMS1 启动子去甲基化[1]。

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

DNMT-IN-6 相关抗体:

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.
药代动力学
(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
体内研究
(In Vivo)

DNMT-IN-6 (Compound CZ2)(3.5 mg/kg；腹腔注射；每 2 天 1 次；共 12 天) 在携带 SUDHL-4 DLBCL 异种移植物的 BALB/c 裸鼠中可实现 71.39% 的肿瘤生长抑制率，降低肿瘤重量，延长生存期，并调控 TMS1/DNMT3A 轴，且具有良好的安全性特征[1]。

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.
分子量

447.40

Formula

C19H18AsNO3S2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

DNMT-IN-6 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

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

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