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

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.

For research use only. We do not sell to patients.

PKM2-IN-6 Chemical Structure

PKM2-IN-6 Chemical Structure

CAS No. : 771467-00-6

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Based on 1 publication(s) in Google Scholar

PKM2-IN-6 Related Antibodies

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Description

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]
In Vitro

PKM2-IN-6 (compound 7d) (0, 20, 40, 60, 80, 100 μM; 48 h) shows cytotoxicity with IC50s of 18.33, 47.00, 19.80 µM for COLO-205, A-549, MCF-7 cells, respectively[1].
PKM2-IN-6 (14.38 μM; 48 h) induces apoptosis and cell cycle arrest at G2 phase[1].
PKM2-IN-6 (14.38 μM; 24 h) reduces the PKM1 and PKM2 at the mRNA level[1].

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

PKM2-IN-6 Related Antibodies

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.
In Vivo

PKM2-IN-6 (25, 50 mg/kg; p.o.; daily for 3 weeks) decreases the tumor volume and tumor weight in mice[1].

MedChemExpress (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.
Molecular Weight

322.38

Formula

C17H14N4OS
CAS No.
Appearance

Solid

Color

Off-white to pink

SMILES

COC1=CC=CC=C1NC2=NC(C3=CN=C4C=CC=CN43)=CS2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (387.74 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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
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PKM2-IN-6 Related Classifications

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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