PKM2 inhibitor

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PKM2抑制剂(Compound 3K)表现出PKM2抑制活性，IC50值为2.95 μM。 PKM1 的 IC50 值比 PKM2 高 4-5 倍。

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.

PKM2-IN-1 (compound 3k) is a pyruvate kinase M2 (PKM2) inhibitor with an IC50 of 2.95±0.53 μM. Results show that most of 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 than 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.

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PKM2 inhibitor | MDK4882

Others

Other Targets

PKM1| PKM2

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94164-88-2

345.48

C18H19NO2S2

>98% (HPLC)

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

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

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

(-20℃)

With Ice Pack

≥ 2 years