BH3I-1
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 400.31 |
| Cas No. | 300817-68-9 |
| Formula | C15H14BrNO3S2 |
| 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 |
| SDF | Download SDF |
| Canonical SMILES | CC(C(N(C1=S)C(/C(S1)=C([H])\C2=CC=C(Br)C=C2)=O)C(O)=O)C |
| Shipping Condition | Evaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request. |
| General tips | For 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. |
Quality Control & MSDS
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Chemical structure
