Bcl-2-IN-10

Names

[ CAS No. ]:
2773354-28-0

[ Name ]:
Bcl-2-IN-10

Biological Activity

[Description]:

Bcl-2-IN-10 is an active Bcl-2 inhibitor that can release up to four nitric oxide (NO) molecules. Bcl-2-IN-10 has cytotoxic activities against cancer cells, such as human leukemia, breast cancer and lung cancer. Bcl-2-IN-10 induces cell apopotosis and arrest cell cycle of G2/M phase, and can be used in cancer-related research[1].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Bcl-2 Family
Signaling Pathways >> Apoptosis >> Apoptosis
Research Areas >> Cancer

[Target]

Bax


[In Vitro]

Steroid sulfatase-IN-2 (compound 1, 0-20 μM approximately, 72 h) inhibits different cancer cells with IC50s ranging from 1.26 μM to 17.86 μM[1]. Steroid sulfatase-IN-2 (1 μM, 5 h) releases up to four molecules of nitric oxide[1]. Steroid sulfatase-IN-2 (8 μM, 8-72 h) induces leukemia cell CCRF-CEM apoptosis via MAPKs pathways, arrests cell in the G2/M phase, and increases ratio of Bax/Bcl-2[1]. Apoptosis Analysis[1] Cell Line: CEM cells Concentration: 8 μM Incubation Time: 8, 24, 48 or 72 h Result: Induced apoptosis in a time-dependent and dose-dependent manner. Cell Cycle Analysis[1] Cell Line: CEM cells Concentration: 8 μM Incubation Time: 8, 24, 48 or 72 h Result: Arrested cell in the G2/M phase. Western Blot Analysis[1] Cell Line: CEM cells Concentration: 0-8 μM Incubation Time: 72 h Result: Increased the levels of JNK and p38, and the levels of phosphorylated JNK and p38. Decreased Bcl-2 level in a time- and dose-dependent manner, and increased pro-apoptotic Bax level.

[References]

[1]. Xun Ji, et al. Double-component diazeniumdiolate derivatives as anti-cancer agents. Bioorg Med Chem. 2020 Apr 15;28(8):115405.

Chemical & Physical Properties

[ Molecular Formula ]:
C22H25N11O12

[ Molecular Weight ]:
635.50


Related Compounds