PKM2 inhibitor ( PKM2 inhibitor; MDK4882 )

Catalog No. M19274 CAS No. 94164-88-2

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Product Name

PKM2 inhibitor
Note

Research use only, not for human use.
Brief Description

PKM2 inhibitor(Compound 3K) displays PKM2 inhibitory activity with the IC50 value of 2.95 μM. The IC50 value for PKM1 is 4-5-fold higher than that for PKM2.
Description

MDK4882, also known as PKM2 inhibitor or compound 3k, is a PKM2 inhibitor. MDK4882 was first described in Eur J Med Chem. 2017;138:343-352. Currently there is no formal name. We temporarily name it MDK4882 for the convenience of communication, in which the last 4 digit of CAS# is used. MDK4882 displayed more potent PKM2 inhibitory activity than the reported optimal PKM2 inhibitor shikonin. MDK4882 also showed nanomolar antiproliferative activity toward a series of cancer cell lines with high expression of PKM2 including HCT116, Hela and H1299 with IC50 values ranging from 0.18 to 1.56 μM. MDK4882 exhibited more cytotoxicity on cancer cells than normal cells.
Synonyms

PKM2 inhibitor; MDK4882
Pathway

Others
Target

Other Targets
Recptor

PKM1; PKM2
Research Area

——
Indication

——

CAS Number

94164-88-2
Formula Weight

345.48
Molecular Formula

C18H19NO2S2
Purity

98%
Solubility

DMSO : 5.56 mg/mL 16.09 mM; H2O : < 0.1 mg/mL
SMILES

CC1=C(C(=O)c2ccccc2C1=O)CSC(=S)N1CCCCC1
Chemical Name

(3-methyl-1,4-dioxo-1,4-dihydronaphthalen-2-yl)methyl piperidine-1-carbodithioate

1. Ning X, et al. Eur J Med Chem. 2017 Sep 29;138:343-352.

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