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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5 mg ￥2650
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10 mg ￥4000
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Customer Review

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
性状

固体

颜色

Off-white to pink

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 125 mg/mL (387.74 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.1019 mL 15.5096 mL 31.0193 mL
5 mM 0.6204 mL 3.1019 mL 6.2039 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

PKM2-IN-6 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.1019 mL 15.5096 mL 31.0193 mL 77.5482 mL
5 mM 0.6204 mL 3.1019 mL 6.2039 mL 15.5096 mL
10 mM 0.3102 mL 1.5510 mL 3.1019 mL 7.7548 mL
15 mM 0.2068 mL 1.0340 mL 2.0680 mL 5.1699 mL
20 mM 0.1551 mL 0.7755 mL 1.5510 mL 3.8774 mL
25 mM 0.1241 mL 0.6204 mL 1.2408 mL 3.1019 mL
30 mM 0.1034 mL 0.5170 mL 1.0340 mL 2.5849 mL
40 mM 0.0775 mL 0.3877 mL 0.7755 mL 1.9387 mL
50 mM 0.0620 mL 0.3102 mL 0.6204 mL 1.5510 mL
60 mM 0.0517 mL 0.2585 mL 0.5170 mL 1.2925 mL
80 mM 0.0388 mL 0.1939 mL 0.3877 mL 0.9694 mL
100 mM 0.0310 mL 0.1551 mL 0.3102 mL 0.7755 mL
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.

Keywords:

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

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