Pyridoclax

Research use only, not for human use.

Pyridoclax (MR29072) is a highly potent Mcl-1 inhibitor with Kd of 25 nM, disrupts Mcl-1/Bim interaction.

Pyridoclax (MR29072) is a highly potent Mcl-1 inhibitor with Kd of 25 nM, disrupts Mcl-1/Bim interaction; strongly sensitizes ovarian cancer chemoresistant IGROV1-R10 cells to Bcl-xL targeting siRNA and ABT-737, leading to massive apoptosis, can not induce cell death as single agents; induces ER stress and modifies Bcl-2 family expression, but its cytotoxic effect does not require these events.

Pyridoclax directly binds to Mcl-1. Without cytotoxic activity when administered as a single agent, Pyridoclax induces apoptosis in combination with Bcl-xL-targeting siRNA or with ABT-737 in ovarian, lung, and mesothelioma cancer cells. Pyridoclax directly binds to Mcl-1, and hence sensitizes ovarian carcinoma cells to Bcl-xL-targeting strategies. Pyridoclax induces apoptosis in ovarian, and also in lung, and mesothelioma cancer cells when it is administrated in combination with Bcl-xL-targeting siRNA or Bcl-xL targeting molecules such as ABT-737 or its orally available derivative ABT-263.

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MR-29072

Angiogenesis

Bcl-2

Bcl-2

Cancer

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1651890-44-6

426.5118

C29H22N4

>98% (HPLC)

10 mM in DMSO

CC1=CC(C2=NC=C(C3=CC=CN=C3)C=C2/C=C/C4=CC=CC=C4)=CN=C1C5=CC=CN=C5

(E)-3'-methyl-3''-styryl-3,2':5',2'':5'',3'''-quaterpyridine

(-20℃)

With Ice Pack

≥ 2 years