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HA14-1

Cat. No. M3753
HA14-1 Structure
Size Price Availability Quantity
10mg USD 50  USD50 In stock
50mg USD 150  USD150 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

HA14-1 is a small molecule which has the potential of inducing apoptosis in cancerous cells. HA14-1 manifests an antagonistic effect on antiapoptotic protein Bcl-2 and consequently induces cell death in various cancerous cell lines. HA-14-1 also has the ability to inhibit ceramide glucosyltransferase. The IC50 value of HA14-1 against ceramide glucosyltransferase is 4.5μM, which is lower than that reported for Bcl-2 in vitro. Kinetic analyses revealed that HA14-1 is a competitive and mixed-type inhibitor with respect to C6-NBD-ceramide and UDP-glucose, respectively.P53 pathway to be the probable mechanism of action for the induction of apoptosis in HeLa cell by downregulating the effect of anti-apoptotic proteins suggesting that HA14-1 may provide therapeutic potential for the treatment of human cervical cancer.

Protocol
Cell Experiment
Cell lines HF1A3, HF4.9 and HF28RA cells
Preparation method Determining the cytotoxic effects of HA14-1 against different FL cell lines by the MTT assay. Briefly, incubating the cells (5000/well) in triplicate in 96-well plate in the presence or absence of HA14-1 for 20 h at 37 °C. Thereafter, adding the MTT solution to each well. After 4 h incubation at 37 °C, measuring the optical density (OD) 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
Concentrations ~25 μM
Incubation time 20 h
Animal Experiment
Animal models Female Swiss nude mice bearing BeGBM xenografts
Formulation Free RPMI 1640-50% DMSO.
Dosages 400 nM
Administration Inject at the site of cell injection.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 409.23
Formula C17H17BrN2O5
CAS Number 65673-63-4
Purity >98%
Solubility DMSO
Storage at -20°C
References

[1] Rehman K, et al. Chem Biol Drug Des. Effect of HA14-1 on apoptosis-regulating proteins in HeLa cells.

[2] Ranjan K, et al. Biofactors. Regulation of HA14-1 mediated oxidative stress, toxic response, and autophagy by curcumin to enhance apoptotic activity in human embryonic kidney cells.

[3] Niino S, et al. Biochem Biophys Res Commun. A small molecule inhibitor of Bcl-2, HA14-1, also inhibits ceramide glucosyltransferase.

[4] Nyhan MJ, et al. Br J Cancer. The BH3 mimetic HA14-1 enhances 5-fluorouracil-induced autophagy and type II cell death in oesophageal cancer cells.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: HA14-1 supplier, Bcl-2, inhibitors

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