Home Apoptosis Bcl-2 inhibitor HA14-1

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HA14-1 Bcl-2 inhibitor

Cat.No.S1071

HA14-1 is a non-peptidic ligand of a Bcl-2 surface pocket with IC50 of ~9 μM.
HA14-1 Bcl-2 inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 409.23

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Quality Control

Batch: Purity: >97%
97

Solubility

In vitro
Batch:

DMSO : 82 mg/mL (200.37 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 82 mg/mL

Water : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 409.23 Formula

C17H17BrN2O5

 Storage (From the date of receipt)
CAS No. 65673-63-4 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CCOC(=O)C1=C(OC2=C(C1C(C#N)C(=O)OCC)C=C(C=C2)Br)N

Mechanism of Action

Targets/IC50/Ki
Bcl-2
9 μM
In vitro

HA14-1 is a small molecule and nonpeptidic ligand of a Bcl-2 surface pocket with IC50 of approximately 9 μM. This compound induces the apoptosis of HL-60 cells in a dose-dependent manner via caspase activation. It 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. This chemical induces apoptosis of HF1A3, HF4.9 and HF28RA cells via caspase and ROS.

Kinase Assay
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 vivo

HA14-1(400 nM) treatment did not have any significant effect on the growth of glioblastoma tumors in immunodeficient mice. But this compound increases the effect of the DNA-damaging agent on glioblastoma growth in vivo.

References

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