BH3I-1 (Synonyms: BHI1; BH 3I1) |
カタログ番号GC18136 |
BH3I-1 は Bcl-2 ファミリーのアンタゴニストであり、FP アッセイで 2.4±0.2 μM の Ki で Bak BH3 ペプチドの Bcl-xL への結合を阻害します。 BH3I-1 は、p53/MDM2 ペアに対して 5.3 μM の Kd を持っています。
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Cas No.: 300817-68-9
Sample solution is provided at 25 µL, 10mM.
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.
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