1. Metabolic Enzyme/Protease Apoptosis Immunology/Inflammation NF-κB
  2. Pyruvate Kinase Apoptosis Endogenous Metabolite Reactive Oxygen Species (ROS)
  3. PKM2-IN-12

PKM2-IN-12 是一种口服有效的 PKM2 抑制剂,其 IC50 为 10 nM。PKM2-IN-12 抑制 COLO-205 细胞增殖和迁移,阻滞细胞周期并诱导细胞凋亡 (apoptosis)。PKM2-IN-12 显著降低了细胞中的乳酸、丙酮酸和 ROS 水平。PKM2-IN-12 在小鼠模型中既直接杀伤癌细胞,又恢复被破坏的肠道微生态平衡。PKM2-IN-12 可用于研究结肠直肠癌。

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PKM2-IN-12

PKM2-IN-12 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

PKM2-IN-12 is an orally active PKM2 inhibitor with an IC50 of 10 nM. PKM2-IN-12 inhibits COLO-205 cell proliferation and migration, arrests the cell cycle, and induces apoptosis. PKM2-IN-12 significantly reduces cellular levels of lactate, pyruvate, and ROS. PKM2-IN-12 directly kills cancer cells and restores disrupted gut microbiota balance in mice model. PKM2-IN-12 can be used to study colorectal cancer[1].

IC50 & Target[1]

PKM2

10 nM (IC50)

体外研究
(In Vitro)

PKM2-IN-12 (Compound 10j) (24 h) 在 COLO-205、CAL-27 和 MCF-7 细胞中表现出显著不同的敏感性,IC50 值分别为 4.21、13.3 和 22.34 μM[1]
PKM2-IN-12 (4.21 μM, 48 h) 主要通过诱导晚期凋亡杀死 COLO-205 细胞,并将细胞阻滞在 G2 期[1]
PKM2-IN-12 (4.21 μM) 显著抑制 COLO-205 细胞的迁移能力[1]
PKM2-IN-12 (4.21 μM, 0-48 h) 显著降低 COLO-205 细胞内乳酸、丙酮酸和活性氧 (ROS) 的水平[1]
PKM2-IN-12 (4.21 μM, 48 h) 在 COLO-205 细胞中可增加 PKM2 单体和四聚体的表达,但对 PKM1 没有影响[2]

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

体内研究
(In Vivo)

PKM2-IN-12 (Compound 10j) (50-100 mg/kg,口服,每三天一次,持续 72 天) 能有效抑制结肠炎相关结直肠癌 (CAC) 模型中的肿瘤生长,并逆转小鼠肠道菌群失衡[1]

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

Animal Model: AOM (HY-111375)/DSS (HY-116282C)-induced colitis-associated colorectal cancer (CAC) model established in BALB/c mice[1]
Dosage: 50, 75 and 100 mg/kg
Administration: Oral administration (p.o,), once every three days for 72 days
Result: Significantly inhibited tumor formation and reduce tumor burden.
Increased the length of the colon, and maintain the stable weight of the mice.
Significantly restored the alpha diversity of the intestinal microbiota in mice.
Reduced the pathological scores of the colon tissue, including inflammatory cell infiltration, epithelial damage and abnormal glandular structure.
分子量

465.35

Formula

C23H14Cl2N4OS

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

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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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产品名称:
PKM2-IN-12
目录号:
HY-178748
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