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Catalog No.
Bcl-2 or Bcl-XL inhibitor
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Email: [email protected]

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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.

[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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
Cas No.300817-68-9
Solubility≥40 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
Chemical Name(E)-2-(5-(4-bromobenzylidene)-4-oxo-2-thioxothiazolidin-3-yl)-3-methylbutanoic acid
SDFDownload SDF
Canonical SMILESCC(C(N(C1=S)C(/C(S1)=C([H])\C2=CC=C(Br)C=C2)=O)C(O)=O)C
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

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