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| HA14-1Bcl-2 inhibitor,potent and cell-permeable |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
- View current batch:
- Purity = 98.79%
- COA (Certificate Of Analysis)
- HPLC
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
| HA14-1 is a non-peptidic ligand of a Bcl-2 surface pocket with IC50 of 9 μM | ||||||
| Targets | Bcl-2 | |||||
| IC50 | 9 μM | |||||
| Cell experiment [1-3]: | |
Cell lines | HL-60 cells, follicular lymphoma B cell lines, HF1A3, HF4.9 and HF28RA cells |
Preparation method | The solubility of this compound in DMSO is >20.5 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reacting condition | 50 μM, 4 h |
Applications | In HL-60 cells, HA14-1 induced cell death in a dose-dependent manner. HA14-1 (50 μM) caused the loss of viability in more than 90% of the cells. In HL-60 cells, treatment with 50 μM HA14-1 by 3 h displayed the characteristic pattern of DNA fragmentation. HA14-1 decreased cell viability and induced apoptosis in follicular lymphoma B cell lines, HF1A3, HF4.9 and HF28RA cells. HA14-1 (10-20 μmol/L) increased sensitivity of human glioblastoma cells to radiotherapy-induced apoptosis and chemotherapy-induced apoptosis. |
| Animal experiment [3]: | |
Animal models | Swiss nude mice challenged with BeGBM cells |
Dosage form | Intraperitoneal injection, 400 nM, once weekly from day 2 |
Application | In Swiss nude mice challenged with BeGBM cells, HA14-1 (400 nmol, once weekly from day 2) did not have any significant effect on the growth of glioblastoma tumors in immunodeficient mice. HA14-1 (400 nM) increased the effect of the DNA-damaging agent etoposide (2.5 mg/kg) on glioblastoma growth in vivo. |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1]. Wang J L, Liu D, Zhang Z J, et al. Structure-based discovery of an organic compound that binds Bcl-2 protein and induces apoptosis of tumor cells[J]. Proceedings of the National Academy of Sciences, 2000, 97(13): 7124-7129. [2]. Skommer J, Wlodkowic D, Mtt M, et al. HA14-1, a small molecule Bcl-2 antagonist, induces apoptosis and modulates action of selected anticancer drugs in follicular lymphoma B cells[J]. Leukemia research, 2006, 30(3): 322-331. [3]. Manero F, Gautier F, Gallenne T, et al. The small organic compound HA14-1 prevents Bcl-2 interaction with Bax to sensitize malignant glioma cells to induction of cell death[J]. Cancer research, 2006, 66(5): 2757-2764. | |
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| Cas No. | 65673-63-4 | SDF | Download SDF |
| Chemical Name | ethyl 2-amino-6-bromo-4-(1-cyano-2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate | ||
| Canonical SMILES | CCOC(=O)C1=C(OC2=C(C1C(C#N)C(=O)OCC)C=C(C=C2)Br)N | ||
| Formula | C17H17BrN2O5 | M.Wt | 409.23 |
| Solubility | ≥20.45mg/mL in DMSO | Storage | Desiccate at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
HA14-1 is a potent small-molecule inhibitor of B-cell lymphoma 2 (Bcl-2), a protein factor binding to and inactivating pro-apoptotic proteins (such as Bax and BH3-only family proteins) to suppress apoptosis, that potently inhibits the anti-apoptotic of Bcl-2 and induces apoptosis with values of 50% inhibition concentration IC50 ranging from 10 to 20 μM in NIH3T3, HL60 and lung cancer H1299 cell lines. HA14-1 binds to Bcl-2 by mimicking the BH3 domain required for homo- and hetero-dimer formation and hence prevents the binding of these proteins subsequently resulting in the inhibition of Bcl-2. HA14-1 has been widely investigated in studies of apoptosis, which potentiates it to be used for the treatment of cancer.
Reference
Chen J, Freeman A, Liu J, Dai Q, Lee RM. The apoptotic effect of HA14-1, a Bcl-2-interacting small molecular compound, requires Bax translocation and is enhanced by PK11195. Mol Cancer Ther. 2002 Oct;1(12):961-7.
Niino S, Nakamura Y, Hirabayashi Y, Nagano-Ito M, Ichikawa S. A small molecule inhibitor of Bcl-2, HA14-1, also inhibits ceramide glucosyltransferase. Biochem Biophys Res Commun. 2013 Apr 5;433(2):170-4. doi: 10.1016/j.bbrc.2013.02.052. Epub 2013 Feb 26.
