PKM2-IN-1

SKU: orb1303093

Description

PKM2-IN-1

Research Area

Metabolism Research

Key Properties

• CAS Number: 94164-88-2
• MW: 345.48
• Purity: 99.49%
• Formula: C₁₈H₁₉NO₂S₂
• SMILES: CC1=C(CSC(=S)N2CCCCC2)C(=O)c2ccccc2C1=O
• Target: PKM
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:1 mg/mL (2.89 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  PKM2:2.95 μM
• In Vitro:
  Results show that most o the tested compounds exhibit some degree of PKM2 Inhibition and some compounds, such as PKM2-IN-1 (compound 3k) and 6d, display more potent activity tha the positive control shikonin the representative compounds PKM2-IN-1, 6d display dose-dependent Inhibition of PKM2 with less Inhibition of PKM1 and PKL like shikonin. Among All tested compounds the most potent compounds are 3a, PKM2-IN-1 and 3r, which exhibit IC50 Values against HCT116 and Hela cells ranging from 0.39 to 0.41 μM, 0.18 to 0.29 μM and 0.18 to 0.38 μM, respectively
• Cell Research:
  Cell lines (HCT116, Hela, H1299, BEAS-2B) are cultured in RPMI 1640 containing 9% fetal bovine serum (FBS) at 37℃n 5% CO2. Cell viability is detected wit the MTS assay according to the manufacturer's instructions. Briefly, 5000 cells in per well are plated in 96-well plates. After incubated for 12 h the cells are treated with different concentration of tested compound (including PKM2-IN-1) or DMSO (as negative control) for 48 h. Then 20 μL MTS is added in per well and incubated at 37℃or 3 h the absorbance of Each well is determined by a microplate reader at a 490 nM wavelength the IC50 Values are calculated using Prism Graphpad software o the triplicate experiment.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

Inhibitor, inhibit, Pyruvate Kinase, compound 3k, PKM2 IN 1, PKM2 inhibitor, PKM2IN1, PKM-2-IN-1, PKM2-IN-1, PKM1, PKM2

Compound Identifiers

PubChem CID

131698387