PKM2 inhibitor Chemical Properties

Boiling point:

496.5±55.0 °C(Predicted)

Density 

1.302±0.06 g/cm3(Predicted)

storage temp. 

Sealed in dry,Store in freezer, under -20°C

solubility 

DMF: 1 mg/ml; DMSO: insol; Ethanol: insol; PBS (pH 7.2): insol

form 

A solid

pka

0.81±0.20(Predicted)

color 

Light yellow to yellow

PKM2 inhibitor Usage And Synthesis

Uses

PKM2-IN-1, is a pyruvate kinase M2 (PKM2) inhibitor with an IC50 of 2.95 μM.

Biological Activity

Pyruvate kinase M2 (PKM2) inhibitor superior to shikonin.
Compound 3k (C3k) is a pyruvate kinase M2 (PKM2) inhibitor with 3-fold higher potency than shikonin (IC50 = 2.95 and 8.82 μM, respectively, by in vitro PKM2 LDH coupled assay). C3k exhibits potent cancer cell-selective antiproliferative activity in high PKM2-expressing cancer cultures (HCT116/HeLA/H1299 IC50 = 0.18/0.29/1.56 μM with C3k, 1.84/2.45/1.88 μM with shikonin) with much less cytotoxicity toward normal BEAS-2B human bronchial epithelial cells (IC50 = 18.46 μM; IC50 = 5.36 μM with shikonin).