1. JAK/STAT Signaling Stem Cell/Wnt Apoptosis NF-κB Metabolic Enzyme/Protease Immunology/Inflammation Epigenetics Cell Cycle/DNA Damage
  2. STAT Apoptosis Reactive Oxygen Species (ROS) PARP
  3. KB-15

KB-15 是一种 STAT3 抑制剂。KB-15 对 AGS 胃癌细胞 (IC50 = 0.29 μM) 和 BGC-823 胃癌细胞 (IC50 = 0.65 μM) 表现出强大的抗增殖活性。KB-15 通过抑制 STAT3 磷酸化、下调 HO-1 表达以及促进细胞内活性氧 (ROS) 积累来发挥抗肿瘤作用。KB-15 诱导 G0/G1 期细胞周期阻滞和细胞凋亡 (apoptosis),并抑制胃癌细胞的集落形成和迁移。KB-15 在 BGC-823 皮下移植瘤模型中显示出极佳的抗肿瘤效果.

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KB-15

KB-15 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

KB-15 is a STAT3 inhibitor. KB-15 exhibits potent anti-proliferative activity against AGS gastric cancer cells (IC50 = 0.29 μM) and BGC-823 gastric cancer cells (IC50 = 0.65 μM). KB-15 exerts anti-tumor effects by inhibiting STAT3 phosphorylation, downregulating HO-1 expression, and promoting intracellular ROS accumulation. KB-15 induces G0/G1 phase cell cycle arrest and apoptosis, as well as suppresses colony formation and migration of gastric cancer cells. KB-15 demonstrates excellent anti-tumor efficacy in BGC-823 subcutaneous xenograft model. KB-15 can be used for the study of gastric cancer[1].

体外研究
(In Vitro)

KB-15 (72 小时) 对 AGS 胃癌细胞 (IC50 = 0.29 μM) 和 BGC-823 胃癌细胞 (IC50 = 0.65 μM) 表现出强效的抗增殖活性[1]
KB-15 (0.25-2 μM,14 天) 对 AGS 和 BGC-823 胃癌细胞显示出强效的集落形成抑制活性[1]
KB-15 (0.5-2 μM,24 小时) 在 BGC-823 细胞中显示出强效的 ROS 诱导活性[1]
KB-15 (0.25-2 μM,24-36 小时) 在 AGS 和 BGC-823 细胞中表现出强效的 G0/G1 期阻滞活性并诱导凋亡[1]
KB-15 (0.5-2 μM,24 小时) 以浓度依赖方式抑制 STAT3 激活并在 BGC-823 细胞中下调 HO-1 表达[1]

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

Cell Cycle Analysis[1]

Cell Line: AGS and BGC-823 cells
Concentration: 0.25, 0.5, 1, 2 μM
Incubation Time: 36 h
Result: Induced concentration-dependent increase in the proportion of G0/G1 phase cells.

Apoptosis Analysis[1]

Cell Line: BGC-823 cells
Concentration: 0.5, 1, 2 μM
Incubation Time: 24 h
Result: Increased the total apoptosis rate in a concentration-dependent manner.
Upregulated pro-apoptotic proteins Cleaved-PARP and Bax.

Western Blot Analysis[1]

Cell Line: BGC-823 cells
Concentration: 0.5, 1, 2 μM
Incubation Time: 24 h
Result: Inhibited STAT3 activation in a concentration-dependent manner and downregulated HO-1.
体内研究
(In Vivo)

KB-15 (2.5 mg/kg,腹腔注射,每日一次,连续 14 天) 在 BGC-823 皮下异种移植模型中显示出极佳的抗肿瘤效能[1]

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

Animal Model: BGC-823 cells (5 × 107 in serum-free medium) were subcutaneously implanted into the left axillary area of 6-week-old male BALB/c (nu/nu) nude mice[1]
Dosage: 2.5 mg/kg
Administration: i.p. once daily for 14 consecutive days
Result: Achieved a tumor growth inhibition (TGI) rate of 53.3% at a dose of 2.5 mg/kg.
Reduced the expression of phosphorylated STAT3 (p-STAT3) and HO-1 protein in BGC-823 xenograft tumor tissues.
Increased the expression of pro-apoptotic proteins Cleaved-PARP and Bax, and decreased the expression of apoptotic protease Procaspase-3 in tumor tissues.
分子量

430.11

Formula

C18H12Cl4N2O2

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
  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • 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.

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KB-15
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HY-175542
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