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HA14-1

SKU: orb1306869

Description

HA14-1 is a cell-permeable, non-peptidic small molecule antagonist of the anti-apoptotic proteins Bcl-2 and Bcl-XL, binding to a surface pocket with an IC50 of approximately 9 µM. It is utilized in apoptosis research to investigate protein interactions and has been applied in both in vitro cell-based assays and in vivo xenograft studies to probe cancer biology.

Research Area

Cell Biology

Images & Validation

Key Properties

CAS Number65673-63-4
MW409.23
Purity98.00% (May vary between batches)
FormulaC17H17BrN2O5
SMILESCCOC(=O)C(C#N)C1C(C(=O)OCC)=C(N)Oc2ccc(Br)cc12
TargetBcl-2 Family
Solubility10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.89 mM);Ethanol:40.9 mg/mL (99.94 mM);DMSO:40.9 mg/mL (99.94 mM)

Bioactivity

Target IC50
Bcl-2:9 μM
In Vivo
When applied to follicular lymphoma cell lines HF1A3, HF4.9, and HF28RA, HA14-1 exhibits cytotoxicity with LC50 values of 4.5/12.6/8.1 μM, respectively. HA14-1 induces apoptosis in HL-60 cells in a dose-dependent manner through the activation of caspases. Moreover, HA14-1 triggers apoptosis in HF4.9, HF1A3, and HF28RA cells through caspase and ROS (Reactive Oxygen Species) pathways.
In Vitro
In immunodeficient mice, HA14-1 (400 nM) does not significantly affect the growth of glioblastomas on its own. However, in vivo, HA14-1 (400 nM) enhances the efficacy of the DNA-damaging agent etoposide (2.5 mg/kg) in inhibiting the growth of glioblastomas.
Cell Research
The cytotoxic effects of HA14-1 against different FL cell lines are determined by the MTT assay. Briefly, the cells (5000/well) are incubated in triplicate in 96-well plate in the presence or absence of HA14-1 for 20 h at 37 °C. Thereafter, the MTT solution is added to each well. After 4 h incubation at 37 °C, the optical density (OD) is measured by means of 96-well plate reader, with the extraction buffer as a blank. The following formula is used: percentage cell viability = (OD of the experiment samples/OD of the control) × 100. Sigmoidal dose-response curves are fitted to the mean cell viability plotted against log HA14-1 dose and lethal concentration 50% (LC50) values are calculated from the resulting curves using Prism 4.0 softw(Only for Reference)

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

HA14 1, HA141, HA-14-1, HA14-1, Inhibitor, inhibit, Bcl-2 Family, Bcl-2

Similar Products

  • HA14-1 [orb1224323]

    >98% (HPLC)

    65673-63-4

    409.2313

    C17H17BrN2O5

    500 mg, 200 mg, 10 mg, 25 mg, 50 mg, 100 mg, 1 g
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Key Properties

No computed properties available.

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HA14-1 (orb1306869)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

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1 ml x 10 mM (in DMSO)
¥ 910.00
10 mg
¥ 1,040.00
25 mg
¥ 1,430.00
50 mg
¥ 1,690.00
100 mg
¥ 2,210.00
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