Molecular Weight(MW): 409.23
HA14-1 is a non-peptidic ligand of a Bcl-2 surface pocket with IC50 of ~9 μM.
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ABT-737, Obatoclax, and HA14-1 eradicated the H1975 early tumor prosurvival resistance against dual-TKIs inhibition by erlotinib/SU11274 (ERL/SU). The experiment was carried out with H1975 cells , cells were pretreated with dual EGFR-MET inhibitors here, i.e., erlotinib (1 μmol/L)/SU11274 (1 μmol/L). BH3-mimetic used in treatment days 7-9 were all 2 μmol/L in concentration. Top, crystal violet cell survival staining assay. Bottom, BH3-mimetic treatment of the dual ERL/SU-resistant tumor cells induced a proapoptotic response.
Cancer Res 2011 71(13), 4494-505. HA14-1 purchased from Selleck.
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Choose Selective Bcl-2 Inhibitors
|Description||HA14-1 is a non-peptidic ligand of a Bcl-2 surface pocket with IC50 of ~9 μM.|
HA14-1 is a small molecule and nonpeptidic ligand of a Bcl-2 surface pocket with IC50 of approximately 9 μM. HA14-1 induces the apoptosis of HL-60 cells in a dose-dependent manner via caspase activation.  HA14-1 shows cytotoxic effects on HF1A3, HF4.9 and HF28RA follicular lymphoma B cell lines with LC50 of 4.5 μM, 12.6 μM and 8.1 μM respectively. HA14-1 induces apoptosis of HF1A3, HF4.9 and HF28RA cells via caspase and ROS. 
|In vivo||HA14-1(400 nM) treatment did not have any significant effect on the growth of glioblastoma tumors in immunodeficient mice. But HA14-1 (400 nM) increases the effect of the DNA-damaging agent etoposide (2.5 mg/Kg) on glioblastoma growth in vivo. |
Affinity determination:The binding affinity of organic compounds to Bcl-2 protein in vitro is determined by a competitive binding assay based on fluorescence polarization. For this assay, 5-carboxyfluorecein is coupled to the N terminus of a peptide, GQVGRQLAIIGDDINR, derived from the BH3 domain of Bak (Flu-BakBH3), which has been shown to bind to the surface pocket of the Bcl-xL protein with high-affinity. According to our molecular modeling studies and binding measurement using fluorescence polarization, the Flu-BakBH3 peptide binds the surface pocket of Bcl-2 with a similar affinity. Bcl-2 used in this assay is a recombinant GST-fused soluble protein. Flu-BakBH3 and Bcl-2 protein are mixed in the presence or absence of organic compounds under standard buffer conditions and are incubated for 30 min. The binding of Flu-BakBH3 to Bcl-2 protein is measured on a LS-50 luminescence spectrometer equipped with polarizers using a dual path length quartz cell (500 μl). The fluorophore is excited with vertical polarized light at 480 nm (excitation slit width 15 nm), and the polarization value of the emitted light is observed through vertical and horizontal polarizers at 530 nm (emission slit width 15 nm). The binding affinity of each compound for Bcl-2 protein is assessed by determining the ability of different concentrations of the compound to inhibit Flu-BakBH3 binding to Bcl-2.
|In vitro||DMSO||82 mg/mL (200.37 mM)|
|Ethanol||82 mg/mL (200.37 mM)|
|In vivo||Add solvents to the product individually and in order:
1% DMSO+30% polyethylene glycol+1% Tween 80
For best results, use promptly after mixing.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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