HA14-1

Alias: HA 141, HA-141, HA141
Cat No.:V0007 Purity: ≥98%
HA14-1 is a novel, potent and non-peptidic inhibitor of a B-cell lymphoma 2 (Bcl-2)surface pocket with IC50 of ~9 μM.
HA14-1 Chemical Structure CAS No.: 65673-63-4
Product category: Bcl-2
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

HA14-1 is a novel, potent and non-peptidic inhibitor of a B-cell lymphoma 2 (Bcl-2) surface pocket with IC50 of ~9 μM. By imitating the BH3 domain necessary for the formation of homo- and hetero-dimers, HA14-1 binds to Bcl-2 and inhibits Bcl-2 by blocking the binding of these proteins. HA14-1 has received a lot of attention in apoptosis research, which makes it more promising as a cancer treatment.

Biological Activity I Assay Protocols (From Reference)
Targets
Bcl-2 (IC50=9 μM ); Bcl-xL
ln Vitro
HA14-1 is a nonpeptidic ligand of a Bcl-2 surface pocket. Apaf-1 and caspases are activated by HA14-1, possibly by binding to the Bcl-2 protein and preventing it from performing its intended function. As a series of synthetic analogs derived from HA14-1 containing various modifications are found to have greatly different Bcl-2 binding activities, it appears that the interaction of HA14-1 with the Bcl-2 surface pocket is specific for the chemical structure of HA14-1. HL-60 cells are exposed to various concentrations of HA14-1 for 4 hours in order to investigate the impact of HA14-1 on cell viability. HL-60 cells are killed by HA14-1 in a dose-dependent manner. More than 90% of the cells lose viability at a concentration of 50 M of HA14-1[1]. HA14-1 is a Bcl-2/Bcl-xL antagonist[2].
ln Vivo
Swiss nude mice injected with human glioblastoma multiforme cells are also given i.p. low doses of Etoposide (2.5 mg/kg in 200 L of 0.9% NaCl 5 days a week starting on day 2 after cell injection) along with HA14-1 or mock treatment to examine whether HA14-1 treatment might increase the efficacy of another antitumoral treatment. Etoposide treatment is insufficient to stop the growth of glioblastoma cells on its own, but when combined with HA14-1, it significantly slows tumor growth, as shown by the ability of the combined therapy to lengthen the tumor volume's time to double[3].
Animal Protocol
Formulated in Free RPMI 1640-50% DMSO.; 400 nM; Inject at the site of cell injection
Female Swiss nude mice bearing BeGBM xenografts.
References

[1]. Structure-based discovery of an organic compound that binds Bcl-2 protein and induces apoptosis of tumor cells. Proc Natl Acad Sci U S A. 2000 Jun 20;97(13):7124-9.

[2]. Initiation of apoptosis and autophagy by the Bcl-2 antagonist HA14-1. Cancer Lett. 2007 May 8;249(2):294-9.

[3]. The small organic compound HA14-1 prevents Bcl-2 interaction with Bax to sensitize malignant glioma cells to induction of cell death. Cancer Res. 2006 Mar 1;66(5):2757-64.

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These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C17H17BRN2O5
Molecular Weight
409.23
Exact Mass
408.03
Elemental Analysis
C, 49.89; H, 4.19; Br, 19.53; N, 6.85; O, 19.55
CAS #
65673-63-4
Appearance
Solid powder
SMILES
CCOC(=O)C1=C(OC2=C(C1C(C#N)C(=O)OCC)C=C(C=C2)Br)N
InChi Key
SXJDCULZDFWMJC-UHFFFAOYSA-N
InChi Code
InChI=1S/C17H17BrN2O5/c1-3-23-16(21)11(8-19)13-10-7-9(18)5-6-12(10)25-15(20)14(13)17(22)24-4-2/h5-7,11,13H,3-4,20H2,1-2H3
Chemical Name
ethyl 2-amino-6-bromo-4-(1-cyano-2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate
Synonyms
HA 141, HA-141, HA141
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~82 mg/mL (~200.4 mM)
Water: <1 mg/mL
Ethanol: ~82 mg/mL (~200.4 mM)
Solubility (In Vivo)
1% DMSO+30% polyethylene glycol+1% Tween 80: 30mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.4436 mL 12.2181 mL 24.4361 mL
5 mM 0.4887 mL 2.4436 mL 4.8872 mL
10 mM 0.2444 mL 1.2218 mL 2.4436 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Biological Data
  • HA14-1
    Apoptosis induced by HA14-1 in HL-60 cells as indicated by DNA ladders. Proc Natl Acad Sci U S A. 2000 Jun 20; 97(13): 7124–7129.
  • HA14-1

    Effect of HA14-1 on Apaf-1−/− and Apaf-1+/+ cells. Apaf-1-deficient mouse embryonic fibroblast (Apaf-1−/−) and NIH 3T3 (Apaf-1+/+) cells were treated with 50 μM HA14-1 for 24 h. Percent cell death was determined by using Trypan blue staining. To examine the role of caspases in the death of Apaf-1+/+ cells induced by HA14-1, cells were preincubated with zVAD-fmk for 2 h before the treatment of the compound.
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