2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  3. DNA/RNA Synthesis Pyruvate Kinase
  4. Multi-target kinase-IN-9

Multi-target kinase-IN-9 是一种具有抗增殖和抗血管生成活性的多靶点酶抑制剂，对肝癌细胞表现出显著的选择性。Multi-target kinase-IN-9 通过广泛结合 DNA 聚合酶 β、丙酮酸激酶 (Pyruvate Kinase) M2 (PKM2) 等多种关键酶的活性位点或 ATP 结合区域，全面破坏 DNA 修复与复制、糖酵解、染色质动态及转录程序，并阻断癌症干细胞的自我更新。Multi-target kinase-IN-9 可导致基因组不稳定性、溶酶体功能障碍及自噬流中断，进而诱导肿瘤细胞死亡，有效抑制肿瘤增殖、侵袭、转移与血管生成，并显著降低异种移植模型中的肿瘤体积。Multi-target kinase-IN-9 可用于肝癌相关研究。

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Multi-target kinase-IN-9

Multi-target kinase-IN-9 Chemical Structure

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Multi-target kinase-IN-9 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

Multi-target kinase-IN-9 is a multi-target enzyme inhibitor with antiproliferative and antiangiogenic activities, and exhibits remarkable selectivity against hepatocellular carcinoma cells. By broadly binding to the active sites or ATP-binding regions of multiple key enzymes including DNA polymerase β, Pyruvate Kinase M2 (PKM2), Multi-target kinase-IN-9 comprehensively disrupts DNA repair and replication, glycolysis, chromatin dynamics and transcriptional programs, and blocks the self-renewal of cancer stem cells. Multi-target kinase-IN-9 induces genomic instability, lysosomal dysfunction and autophagic flux impairment, thereby triggering tumor cell death, effectively inhibiting tumor proliferation, invasion, metastasis and angiogenesis, and significantly reducing tumor volume in xenograft models. Multi-target kinase-IN-9 is applicable to hepatocellular carcinoma-related research[1].

IC50 & Target

DNA Polymerase

 

PKM2

 

体外研究
(In Vitro)

Multi-target kinase-IN-9 (compound 2c) (3.12-100 μM; 48 h) 对 HepG2 肝癌细胞具有剂量依赖性的抗增殖作用，处理 48 h 后其 IC50 为 23 μM，GI50 为 6.25 μM[1]。
Multi-target kinase-IN-9 与 PKM2 结合，Kd 值为 5.7 μM[1]。
Multi-target kinase-IN-9 可高亲和力结合 MeCP2+DNA 复合物中的 DNA (Kd=0.69 μM)，并以中等亲和力结合游离的 MeCP2 (Kd=12.27 μM)[1]。

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

Multi-target kinase-IN-9 相关抗体:

Cell Viability Assay[1]

Cell Line: HepG2 hepatocellular carcinoma cells
Concentration: 3.12-100 μM
Incubation Time: 48 h
Result: Caused a moderate decrease in HepG2 cell growth at 3.12 μM.
Resulted in a nearly 40-50% reduction in cell viability at 6.25 μM and above.
Exhibited an IC50 of 23 μM and a GI50 of 6.25 μM.
体内研究
(In Vivo)

Multi-target kinase-IN-9 (compound 2c) (23 μM；局部给药；单次) 可显著抑制鸡胚雏鸡
绒毛尿囊膜 (CAM) 模型中的肝细胞癌肿瘤生长，在 IC50 剂量处理 48 小时内将平均肿瘤体积降至基线水平的 65%[1]。
Multi-target kinase-IN-9 (10-1000 μM；局部施用) 在鸡 CAM 模型中表现出剂量依赖性的抗血管生成活性，在 1000 μM 剂量下效果最强，在较低剂量下及随时间推移活性逐渐降低[1]。

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

Animal Model: ROSS308 fertilized eggs[1]
Dosage: 10-1000 μM
Administration: topical; single dose
Result: Achieved a mean antiangiogenic score of around 1.5 at 24 h and around 1.0 at 48 h at 1000 μM.
Achieved a mean antiangiogenic score of around 1.0 at 24 h and 0.5 at 48 h at 100 μM.
Achieved a mean antiangiogenic score below 0.5 at 24 h, with no detectable activity (score 0) at 48 h at 10 μM.
分子量

350.41

Formula

C20H15FN2OS
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

Multi-target kinase-IN-9 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

Multi-target kinase-IN-9DNA/RNA SynthesisPyruvate KinaseDNA ligase 1DNA polymerase betamethyl-CpG binding protein 2tyrosyl-DNA phosphodiesterase 1aldehyde dehydrogenase 1A1pyruvate kinase M2hepatocellular carcinoma cellslysosomal alpha-glucosidaseanti-silencing function 1A histone chaperoneATP-dependent DNA helicase Q1Inhibitorinhibitorinhibit

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