2. Metabolic Enzyme/Protease Apoptosis
  3. Pyruvate Kinase Apoptosis
  4. PKM2-IN-6

PKM2-IN-6 (compound 7d) 是一种有效的和具有口服活性的 PKM2 抑制剂，IC50 值为 23 nM。PKM2-IN-6 诱导细胞凋亡 (apoptosis) 和细胞周期停滞在 G2 期。PKM2-IN-6 在 mRNA 水平降低 PKM1 和 PKM2 的表达。PKM2-IN-6 显示出抗癌活性，具有研究三阴性乳腺癌的潜力。

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PKM2-IN-6 Chemical Structure

PKM2-IN-6 Chemical Structure

CAS No. : 771467-00-6

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PKM2-IN-6 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PKM2-IN-6 (compound 7d) is a potent and orally active PKM2 inhibitor with an IC50 value of 23 nM. PKM2-IN-6 induces apoptosis and cell cycle arrest at G2 phase. PKM2-IN-6 reduces the level of PKM1 and PKM2 at the mRNA level. PKM2-IN-6 shows anticancer activity and has the potential for the research of triple-negative breast cancer[1].

IC50 & Target

IC50: 23 nM (PKM2)[1]
体外研究
(In Vitro)

PKM2-IN-6 (compound 7d) (0, 20, 40, 60, 80, 100 μM; 48 h) 对 COLO-205，A-549、MCF-7 细胞显示细胞毒性，IC50 值分别为 18.33、47.00、19.80 μM[1]。
PKM2-IN-6 (14.38 μM; 48 h) 诱导细胞凋亡和细胞周期停滞在 G2 期[1]。
PKM2-IN-6 (14.38 μM; 24 h) 可在 mRNA 水平上降低 PKM1 和 PKM2 的表达[1]。

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

PKM2-IN-6 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: COLO-205, A-549, MCF-7 cells
Concentration: 0, 20, 40, 60, 80, 100 μM
Incubation Time: 48 h
Result: Showed cell cytotoxicity with IC50s of 18.33, 47.00, 19.80 µM for COLO-205, A-549, MCF-7 cells, respectively.

RT-PCR[1]

Cell Line: 4T1 cells
Concentration: 14.38 μM
Incubation Time: 24 h
Result: Significantly reduced the level of PKM1 and PKM2 at the mRNA level.

Apoptosis Analysis[1]

Cell Line: 4T1 cells
Concentration: 14.38 μM
Incubation Time: 48 h
Result: Induced apoptosis the percentage of live cells depreciated from 82.64% in control to 5.44% and the percentage of late apoptotic cells was 50.32% and necrotic cells were 44.08% in 2D culture; the difference is diminished as 89.05% of live cells in control dropped down to 52.45% and the percentage of late apoptotic cells was lesser (only 9.84%) and necrotic cells were 36.62% in 3D cell culture.
体内研究
(In Vivo)

PKM2-IN-6 (25, 50 mg/kg; p.o.; daily for 3 weeks) 可减少小鼠的肿瘤体积和重量[1]。

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

Animal Model: 6-8 weeks, Female CD-1 nude mice (4T1-Red-FLuc cells)[1]
Dosage: 25, 50 mg/kg
Administration: P.o.; daily for 3 weeks
Result: Showed a significant regression in tumor volume and rendered significant reduction in tumor weight.
分子量

322.38

Formula

C17H14N4OS
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

PKM2-IN-6 相关分类

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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:

PKM2-IN-6771467-00-6Pyruvate KinaseApoptosisG2 phase4T1 cellsanticancerbreast cancerPKM1PKM2Inhibitorinhibitorinhibit

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