Background:

IC50: 293.95 μM

BH3I-1 is an inhibitor of Bcl-2 or Bcl-XL.

It has been reported that a disregulation of the Bcl-2/ Bcl-XL family proteins may result in the development of cancer, since the failure of the inactivation of pro-apoptotic pathways, or the activation of anti-apoptotic pathways, may occur in the regulation processes.

In vitro: The Bcl-2 inhibitors BH3I-1 and it analog BH3I-2 had been applied as lead compounds to find possible Bcl-2 or Bcl-X(L) inhibitors by using computer-assisted screening of in-house database. The identified compounds were further studied regarding their possible application as a drug. It was found that the induction of apoptosis, which was shown as number of hypodiploid cells, was increased by adding BH3I-1 and it analog BH3I-2 to Bjab Bcl-XL and Bjab neo/mock cells. In addition, the effects of the pro-apoptotic proteins Bax and Bak on the induction of apoptosis via BH3I-1 and it analog BH3I-2 were investigated with a variety of knockout cell lines, and resulted showed that the presence or absence of Bak or Bax has no significant influence on the amount of apoptotic events induced by BH3I-1 and it analog BH3I-2 [1].

In vivo: Currently, there is no animial in vivo data reported.

Clinical trial: Up to now, BH3I-1 is still in the preclinical development stage.

Reference:
[1] Füllbeck M,Gebhardt N,Hossbach J,Daniel PT,Preissner R.  Computer-assisted identification of small-molecule Bcl-2 modulators. Comput Biol Chem.2009 Dec;33(6):451-6.