Bax activator compound 106

Research use only, not for human use.

A specific, small molecule Bax agonist that promotes Bax-dependent but not Bak-dependent apoptosis.

A specific, small molecule Bax agonist that promotes Bax-dependent but not Bak-dependent apoptosis; alters Bax protein stability in vitro and promotes the insertion of Bax into mitochondria, leading to Bax-dependent permeabilization of the mitochondrial outer membrane; induces significant cell death and caspase 3/7 activation in Bax-expressing cells, inhibits the growth of transplanted tumors as a single agent.

Bax activator-1 (20-80 μM; 48 hours) induces Bax-dependent tumor cell apoptosis in a dose-dependent fashion.Apoptosis Analysis Cell Line:Lewis Lung Carcinoma tumor cells, human non-small cell lung carcinoma A549 cells, human pancreatic carcinoma Panc-1 cells Concentration:20 μM, 40 μM , 60 μM , 80 μM Incubation Time:48 hours Result:Induced apoptotic cell death in the murine Lewis Lung Carcinoma (LLC), human non-small cell lung carcinoma A549 cells and PANC-1 human pancreatic carcinoma cells in a dose-dependent fashion.

Bax activator-1 (40 mg/kg; given i.p., each day for 13 days) inhibits lung tumor growth in C57BL/6 female mice. Animal Model:Eight-week old C57BL/6 female mice (with Lewis Lung Carcinoma tumor cells)Dosage:40 mg/kg Administration:Given i.p., each day for 13 days Result:Exhibited anti-tumor activity as a single-agent.

ZINC14750348

Angiogenesis

Bcl-2

Bcl-2

——

——

1638526-94-9

488.632

C29H36N4O3

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (511.65 mM)

O=C(C1=NN(CC2=CC=CC(OC)=C2)C3=C1CN(CC4=CC=C(C)C(C)=C4)CC3)N5C[C@H](O)CCC5

5-[(3,4-dimethylphenyl)methyl]-1-[(3-methoxyphenyl)methyl]-6,7-dihydro-4H-pyrazolo[4,3-c]pyridin-3-ium-3-yl}-[(3R)-3-hydroxypiperidin-1-yl]methanone

(-20℃)

With Ice Pack

≥ 2 years