HA14-1 Inhibitor CAS No. 65673-63-4

Cat. No.	Name	Size	Price	Add Cart
KI3520	HA14-1	10 mg	$96

Chemical Characteristic

Product Name	HA14-1
CAS No.	65673-63-4
Molecular Weight	409.23
Formula	C₁₇H₁₇BrN₂O₅
Chemical Name	2-Amino-6-bromo-alpha-cyano-3-(ethoxycarbonyl)-(alphaR,4R)-rel-4H-1-benzopyran-4-acetic acid ethyl ester
Smiles	C1(=C(C(c2c(O1)ccc(c2)Br)[C@@H](C(=O)OCC)C#N)C(=O)OCC)N
Chemical Structure

Biological activities

HA14-1 is a B-cell lymphoma 2 (Bcl-2) antagonist. HA14-1 competitively blocks the binding of a Bak BH3 peptide with an IC50 of 9 µM. HA14-1 binds the surface pocket of Bcl-2 that mediates antiapoptotic interactions, triggering apoptosis in a Bcl-2-transfected cell line. HA14-1 (5-12.5 µM) predominantly triggers apoptosis in necrotic cells.^[1] HA14-1inhibits follicular lymphoma B cell lines HF4.9 with a LC50 of 4.5 µM. HA14-1also induces apoptosis in follicular lymphoma B cells. HA14-1 (3.5 µM) significantly increases the cytotoxicity of dexamethasone.^[2] HA14-1 strongly inhibits Bcl-2/Bax interactions and prevents the interaction between Bcl-2 and the BH3-only protein Bim. HA14-1 efficiently induces cell death in a broad spectrum of AML blasts.^[3] HA14-1 increases sensitivity of human glioblastoma cells to radiotherapy-induced apoptosis and chemotherapy-induced apoptosis. In vivo in swiss nude mice, HA14-1 significantly restrains glioblastoma tumor growth by increasing the effect of the DNA-damaging agent etoposide.^[4]

Protocols

In vitro, HA14-1 is dissolved in DMSO and stored at -70?C in 1mM aliquots.^[2]

References

[1] Lickliter JD, et al. HA14-1 selectively induces apoptosis in Bcl-2-overexpressing leukemia/lymphoma cells, and enhances cytarabine-induced cell death. Leukemia. 2003, 17(11): 2074-2080. [2] Skommer J, et al. HA14-1, a small molecule Bcl-2 antagonist, induces apoptosis and modulates action of selected anticancer drugs in follicular lymphoma B cells. Leuk Res. 2006, 30(3):322-331. [3] Oliver L, et al. HA14-1, a small molecule inhibitor of Bcl-2, bypasses chemoresistance in leukaemia cells. Leuk Res. 2007, 31(6): 859-863. [4] Manero F, et al. 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, 66(5): 2757-2764.

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