2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease Immunology/Inflammation NF-κB Apoptosis
  3. Topoisomerase Reactive Oxygen Species Apoptosis Survivin Bcl-2 Family IAP DNA/RNA Synthesis
  4. Topoisomerase I inhibitor 17

Topoisomerase I inhibitor 17 (Compound 7h) 是一种 Topoisomerase I (Top1) 抑制剂。Topoisomerase I inhibitor 17 减少 DDX5，并逆转 DDX5 对 Top1 活性的锁定。Topoisomerase I inhibitor 17 诱导 Top1 介导的 DNA 损伤，促进 活性氧 (ROS) 产生。Topoisomerase I inhibitor 17 诱导凋亡 (减少抗凋亡蛋白 XIAP, Bcl-2, Survivin 且增加促凋亡蛋白Bax, γH2AX)。Topoisomerase I inhibitor 17 还阻止 G2/M 检查点的进展，诱导细胞周期阻滞。Topoisomerase I inhibitor 17 显著抑制结直肠癌细胞集落形成和细胞迁移的能力。Topoisomerase I inhibitor 17 有效减少人 PDX 肿瘤小鼠肿瘤。

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Topoisomerase I inhibitor 17 Chemical Structure

Topoisomerase I inhibitor 17 Chemical Structure

CAS No. : 2413582-45-1

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Topoisomerase I inhibitor 17 相关抗体

Top Publications Citing Use of Products

查看 Topoisomerase 亚型特异性产品:

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Topoisomerase Topo I Topo II

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim

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cIAP cIAP-1 cIAP-2 XIAP

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Topoisomerase I inhibitor 17 (Compound 7h) is a Topoisomerase I (Top1) inhibitor. Topoisomerase I inhibitor 17 reduces DDX5 and reverses the locking of Top1 activity by DDX5. Topoisomerase I inhibitor 17 induces Top1-mediated DNA damage and promotes reactive oxygen species (ROS) production. Topoisomerase I inhibitor 17 induces Apoptosis (reduces antiapoptotic proteins XIAP, Bcl-2, Survivin and up-regulates pro-apoptotic proteins Bax, γH2AX). Topoisomerase I inhibitor 17 also blocks the progression of the G2/M checkpoint and induces cell cycle arrest. Topoisomerase I inhibitor 17 significantly inhibits colony formation and cell migration in colorectal cancer cells. Topoisomerase I inhibitor 17 effectively reduces tumors in human PDX tumor mice[1].

IC50 & Target[1]

Bax

 

Bcl-2

 

Top1

 

XIAP

 

体外研究
(In Vitro)

Topoisomerase I inhibitor 17 (5-500 nM, 72 h) 对四种癌细胞 (HepG2、A549、HeLa 和 HCT116) 抗增殖，其 IC50 分别为 136.6, 33.7, 72.9 和 36.1 nM[1]。
Topoisomerase I inhibitor 17 可穿过 Caco-2 细胞单层，从顶端到基底侧的表观渗透系数为 2.24 μcm/s (0.5-1.0 μM, 4 h)，Caco-2 细胞的存活率超过 90% (0.2-1.0 μM, 4 h)[1]。
Topoisomerase I inhibitor 17 (5-100 nM, 12-72 h) 显著抑制增殖诱导的集落形成，浓度依赖性抑制 HCT116 细胞迁移，增加 ROS 生成[1]。
Topoisomerase I inhibitor 17 (0-50 μM, 48 h) 以剂量依赖性方式诱导 HCT116 细胞凋亡和细胞周期停滞，阻止 G2/M 检查点的进展[1]。
Topoisomerase I inhibitor 17 抑制 HCT116 细胞中的 DDX5 表达 (100 μM, 48-72 h)，解除 DDX5 阻断的 Top1 活性 (5 和 50 μM)[1]。

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

Topoisomerase I inhibitor 17 相关抗体:

Cell Cycle Analysis[1]

Cell Line: HCT116
Concentration: 0, 2.5, 10, 50 nM
Incubation Time: 48 h
Result: Halted the progression of the G2/M checkpoint, resulted in a significant accumulation of cells at this critical pre-division stage, with increases in cell number observed at G2/M phases of 2.05% (0 nM), 33.48% (2.5 nM), 55.28% (5 nM) and 64.01% (10 nM), respectively.

Apoptosis Analysis[1]

Cell Line: HCT116
Concentration: 50, 100 nM
Incubation Time: 72 h
Result: Reduced expression of anti-apoptotic proteins (e.g. Survivin).
Upregulated the pro-apoptotic proteins Bax and γH2AX in a dose-dependent manner.
体内研究
(In Vivo)

Topoisomerase I inhibitor 17 (2-15 mg/kg, i.p., 一周一次，持续 4 周) 通过浓度依赖性的肿瘤抑制作用和可接受的毒性，有效减少人结肠癌 PDX 肿瘤小鼠的肿瘤[1]。

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

Animal Model: FL118 colorectal cancer (CRC) patient-derived xenograft (PDX) tumors models using a limited number of severe combined immunodeficiency (SCID) mice[1]
Dosage: 2, 8 and 15 mg/kg
Administration: Intraperitoneal injection (i.p.)
Result: Regressed CRC PDX27454 tumors after 21 days with no recurrence within 35 days through a concentration-dependent tumor-suppressive effect and acceptable toxicity at 15 mg/kg.
Displayed stable mouse body weights.
分子量

516.47

Formula

C28H21FN2O7
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

Topoisomerase I inhibitor 17 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

Topoisomerase I inhibitor 172413582-45-1Topoisomerase I inhibitor17Topoisomerase I inhibitor-17TopoisomeraseReactive Oxygen SpeciesApoptosisSurvivinBcl-2 FamilyIAPDNA/RNA SynthesisAntitumorCytotoxicityHepG2Caco-2ProliferationMigrationPDXInhibitorinhibitorinhibit

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