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HA14-1

HA14-1 is a novel cell-permeable low molecular weight Bcl-2 ligand which antagonizes its function and induces apoptosis. In HL-60 cells 50 µM HA14-1 effectively induced apoptosis associated with loss of mitochondrial membrane potential and activation of caspases -9 and -3.

Current developer:  Enzo Life Sciences, Inc.

1. Moon, Dong-Oh; Kim, Mun-Ock; Kang, Sang-Hyuck; Choi, Yung Hyun; Park, Sung Yong; Kim, Gi-Young. HA14-1 sensitizes TNF- -induced apoptosis via inhibition of the NF- B signaling pathway: Involvement of reactive oxygen species and JNK. Cancer Letters (Shannon, Ireland) (2010), 292(1), 111-118. CODEN: CALEDQ ISSN:0304-3835. AN 2010:455737

2. Heikaus, Sebastian; Pejin, Igor; Gabbert, Helmut Erich; Ramp, Uwe; Mahotka, Csaba. PIDDosome expression and the role of caspase-2 activation for chemotherapy-induced apoptosis in RCCs. Cellular Oncology (2010), 32(1,2), 29-42. CODEN: COENCD ISSN:1570-5870. AN 2010:278784

3. Park, Cheol; Jin, Cheng-Yun; Kwon, Hyun Ju; Hwang, Hye Jin; Kim, Gi-Young; Choi, Il Whan; Kwon, Taeg Kyu; Kim, Byung-Woo; Kim, Wun-Jae; Choi, Yung Hyun. Induction of apoptosis by esculetin in human leukemia U937 cells: Roles of Bcl-2 and extracellular-regulated kinase signaling. Toxicology in Vitro (2010), 24(2), 486-494. CODEN: TIVIEQ ISSN:0887-2333. CAN 152:517049 AN 2010:231922

4. Wolkowicz, Paul E. Anti-arrhythmia agents, methods of their use, methods for their identification, and kits thereof. PCT Int. Appl. (2010), 140pp. CODEN: PIXXD2 WO 2010019914 A2 20100218 CAN 152:279546 AN 2010:213921

5. Borgovan, Theodor; Bellistri, John-Paul S.; Slack, Kristen N.; Kopelovich, Levy; Desai, Manisha; Joe, Andrew K. Inhibition of BCL2 expression and activity increases H460 sensitivity to the growth inhibitory effects of polyphenon E. Journal of Experimental Therapeutics and Oncology (2009), 8(2), 129-144. CODEN: JETOFX ISSN:1359-4117. AN 2010:192272

6. Tan, Mingqi; Bian, Mingyan. Effect of HA14-1 for sensitizing chemotherapy of murine lewis lung carcinoma treated by cyclophosphamide. Zhongguo Yike Daxue Xuebao (2009), 38(10), 737-740. CODEN: ZYDXEN ISSN:0258-4646. AN 2010:191651

7. Chen, Mu-Kuan; Yang, Shun-Fa; Lai, Jui-Chung; Yeh, Kun-Tu; Yang, Jia-Sin; Chen, Li-Sheng; Chen, Hui-Chuan. Expression of bcl-2 correlates with poor prognosis and modulates migration of nasopharyngeal carcinoma cells. Clinica Chimica Acta (2010), 411(5-6), 400-405. CODEN: CCATAR ISSN:0009-8981. CAN 152:545332 AN 2010:134528

8. Tan, Mingqi; Bian, Mingyan. Experimental study of HA14-1-induced apoptosis of lewis lung cancer cell. Zhongguo Yike Daxue Xuebao (2009), 38(9), 668-670. CODEN: ZYDXEN ISSN:0258-4646. AN 2010:52707

9. Arisan, Elif Damla; Kutuk, Ozgur; Tezil, Tugsan; Bodur, Cagri; Telci, Dilek; Basaga, Huveyda. Small inhibitor of Bcl-2, HA14-1, selectively enhanced the apoptotic effect of cisplatin by modulating Bcl-2 family members in MDA-MB-231 breast cancer cells. Breast Cancer Research and Treatment (2010), 119(2), 271-281. CODEN: BCTRD6 ISSN:0167-6806. AN 2009:1580212

10. Simonin, Karin; Brotin, Emilie; Dufort, Sandrine; Dutoit, Soizic; Goux, Didier; N'Diaye, Monique; Denoyelle, Christophe; Gauduchon, Pascal; Poulain, Laurent. Mcl-1 is an important determinant of the apoptotic response to the BH3-mimetic molecule HA14-1 in cisplatin-resistant ovarian carcinoma cells. Molecular Cancer Therapeutics (2009), 8(11), 3162-3170. CODEN: MCTOCF ISSN:1535-7163. CAN 152:90006 AN 2009:1388522

11. Zhang, Xing-Ding; Wang, Ye; Wu, Jun-Chao; Lin, Fang; Han, Rong; Han, Feng; Fukunaga, Kohji; Qin, Zheng-Hong. Down-regulation of Bcl-2 enhances autophagy activation and cell death induced by mitochondrial dysfunction in rat striatum. Journal of Neuroscience Research (2009), 87(16), 3600-3610. CODEN: JNREDK ISSN:0360-4012. CAN 151:489126 AN 2009:1288236

12. Karmakar, Surajit; Davis, Kristin A.; Choudhury, Subhasree Roy; Deeconda, Anurag; Banik, Naren L.; Ray, Swapan K. Bcl-2 inhibitor and apigenin worked synergistically in human malignant neuroblastoma cell lines and increased apoptosis with activation of extrinsic and intrinsic pathways. Biochemical and Biophysical Research Communications (2009), 388(4), 705-710. CODEN: BBRCA9 ISSN:0006-291X. CAN 151:520439 AN 2009:1120317

13. Martin, Aditi Pandya; Park, Margaret A.; Mitchell, Clint; Walker, Teneille; Rahmani, Mohamed; Thorburn, Andrew; Haussinger, Dieter; Reinehr, Roland; Grant, Steven; Dent, Paul. BCL-2 family inhibitors enhance histone deacetylase inhibitor and sorafenib lethality via autophagy and overcome blockade of the extrinsic pathway to facilitate killing. Molecular Pharmacology (2009), 76(2), 327-341. CODEN: MOPMA3 ISSN:0026-895X. CAN 151:350322 AN 2009:933299

14. Mohan, Nishant; Karmakar, Surajit; Choudhury, Subhasree Roy; Banik, Naren L.; Ray, Swapan K. Bcl-2 inhibitor HA14-1 and genistein together adeptly down regulated survival factors and activated cysteine proteases for apoptosis in human malignant neuroblastoma SK-N-BE2 and SH-SY5Y cells. Brain Research (2009), 1283 155-166. CODEN: BRREAP ISSN:0006-8993. CAN 151:328238 AN 2009:904007

15. Hertan, Lauren M.; Koumenis, Constantinos. Piling up the JNK. Drug synergy through ER stress. Cancer Biology & Therapy (2009), 8(9), 820-822. CODEN: CBTAAO ISSN:1538-4047. CAN 151:542702 AN 2009:897434

16. Dasmahapatra, Girija; Lembersky, Dmitry; Rahmani, Mohamed; Kramer, Lora; Friedberg, Jonathan; Fisher, Richard I.; Dent, Paul; Grant, Steven. Bcl-2 antagonists interact synergistically with bortezomib in DLBCL cells in association with JNK activation and induction of ER stress. Cancer Biology & Therapy (2009), 8(9), 808-819. CODEN: CBTAAO ISSN:1538-4047. AN 2009:897432

17. Charpentier, Xavier; Gabay, Joelle E.; Reyes, Moraima; Zhu, Jing W.; Weiss, Arthur; Shuman, Howard A. Chemical genetics reveals bacterial and host cell functions critical for type IV effector translocation by Legionella pneumophila. PLoS Pathogens (2009), 5(7), No pp. given. CODEN: PPLACN ISSN:1553-7374. CAN 152:546278 AN 2009:851541

18. Sun, Q.; Ming, L.; Thomas, S. M.; Wang, Y.; Chen, Z. G.; Ferris, R. L.; Grandis, J. R.; Zhang, L.; Yu, J. PUMA mediates EGFR tyrosine kinase inhibitor-induced apoptosis in head and neck cancer cells. Oncogene (2009), 28(24), 2348-2357. CODEN: ONCNES ISSN:0950-9232. CAN 151:93501 AN 2009:545507

19. Lee, Jung Tae; Lee, Tae-Jin; Park, Jong-Wook; Kwon, Taeg Kyu. Se-methylselenocysteine sensitized TRAIL-mediated apoptosis via down-regulation of Bcl-2 expression. International Journal of Oncology (2009), 34(5), 1455-1460. CODEN: IJONES ISSN:1019-6439. CAN 151:440051 AN 2009:543107

20. Jin, Cheng-Yun; Park, Cheol; Lee, Jun-Hyuk; Chung, Kyung Tae; Kwon, Taeg Kyu; Kim, Gi-Young; Choi, Byung Tae; Choi, Yung Hyun. Naringenin-induced apoptosis is attenuated by Bcl-2 but restored by the small molecule Bcl-2 inhibitor, HA 14-1, in human leukemia U937 cells. Toxicology in Vitro (2009), 23(2), 259-265. CODEN: TIVIEQ ISSN:0887-2333. CAN 150:321352 AN 2009:163039

21. Martin, Stuart S.; Cheung, Agnes; Whipple-Bettes, Rebecca. Apoptotic pathway targeting for the diagnosis and treatment of cancer. PCT Int. Appl. (2008), 81pp. CODEN: PIXXD2 WO 2008144506 A1 20081127 CAN 150:720 AN 2008:1448457

22. Hamada, Nobuyuki; Kataoka, Keiko; Sora, Sakura; Hara, Takamitsu; Omura-Minamisawa, Motoko; Funayama, Tomoo; Sakashita, Tetsuya; Nakano, Takashi; Kobayashi, Yasuhiko. The small-molecule Bcl-2 inhibitor HA14-1 sensitizes cervical cancer cells, but not normal fibroblasts, to heavy-ion radiation. Radiotherapy and Oncology (2008), 89(2), 227-230. CODEN: RAONDT ISSN:0167-8140. CAN 150:277516 AN 2008:1352384

23. Hetschko, Holger; Voss, Valerie; Senft, Christian; Seifert, Volker; Prehn, Jochen H. M.; Koegel, Donat. BH3 mimetics reactivate autophagic cell death in anoxia-resistant malignant glioma cells. Neoplasia (Ann Arbor, MI, United States) (2008), 10(8), 873-885. CODEN: NEOPFL ISSN:1522-8002. CAN 150:419243 AN 2008:1263151

24. Kessel, David; Price, Michael; Reiners, John J., Jr. The Bcl-2 antagonist HA14-1 forms a fluorescent albumin complex that can be mistaken for several oxidized ROS probes. Photochemistry and Photobiology (2008), 84(5), 1272-1276. CODEN: PHCBAP ISSN:0031-8655. CAN 149:323080 AN 2008:1131905

25. Diaz-Prieto, Natacha; Herrera-Peco, Ivan; de Diego, Antonio Miguel G.; Ruiz-Nuno, Ana; Gallego-Sandin, Sonia; Lopez, Manuela G.; Garcia, Antonio G.; Cano-Abad, Maria F. Bcl2 mitigates Ca2+ entry and mitochondrial Ca2+ overload through downregulation of L-type Ca2+ channels in PC12 cells. Cell Calcium (2008), 44(4), 339-352. CODEN: CECADV ISSN:0143-4160. CAN 149:466954 AN 2008:1071508

26. Heikaus, Sebastian; van den Berg, Linda; Kempf, Tobias; Mahotka, Csaba; Gabbert, Helmut Erich; Ramp, Uwe. HA14-1 is able to reconstitute the impaired mitochondrial pathway of apoptosis in renal cell carcinoma cell lines. Cellular Oncology (2008), 30(5), 419-433. CODEN: COENCD ISSN:1570-5870. CAN 150:326697 AN 2008:1066252

27. Nikitina, L. S.; Glazova, M. V.; Dorofeeva, N. A.; Chernigovskaya, E. V. Effect of apoptotic proteins on function of rat vasopressin-and dopaminergic hypothalamic neurons. Journal of Evolutionary Biochemistry and Physiology (2008), 44(3), 365-372. CODEN: JEBPA9 ISSN:0022-0930. CAN 150:160354 AN 2008:1020818

28. Wlodkowic, Donald; Skommer, Joanna; Hillier, Chris; Darzynkiewicz, Zbigniew. Multiparameter detection of apoptosis using red-excitable SYTO probes. Cytometry, Part A (2008), 73A(6), 563-569. CODEN: CPAYAV ISSN:1552-4922. CAN 150:116662 AN 2008:802127

29. Srimatkandada, Pavani; Loomis, Regina; Carbone, Rocco; Srimatkandada, Srinivasan; Lacy, Jill. Combined proteasome and Bcl-2 inhibition stimulates apoptosis and inhibits growth in EBV-transformed lymphocytes: a potential therapeutic approach to EBV-associated lymphoproliferative diseases. European Journal of Haematology (2008), 80(5), 407-418. CODEN: EJHAEC ISSN:0902-4441. CAN 149:769 AN 2008:624481

30. Guan, M.; Tripathi, V.; Zhou, X.; Popescu, N. C. Adenovirus-mediated restoration of expression of the tumor suppressor gene DLC1 inhibits the proliferation and tumorigenicity of aggressive, androgen-independent human prostate cancer cell lines: prospects for gene therapy. Cancer Gene Therapy (2008), 15(6), 371-381. CODEN: CGTHEG ISSN:0929-1903. CAN 149:143354 AN 2008:580579

31. Moon, Dong-Oh; Kim, Mun-Ock; Choi, Yung Hyun; Kim, Nam Deuk; Chang, Jeong-Hyun; Kim, Gi-Young. Bcl-2 overexpression attenuates SP600125-induced apoptosis in human leukemia U937 cells. Cancer Letters (Shannon, Ireland) (2008), 264(2), 316-325. CODEN: CALEDQ ISSN:0304-3835. CAN 149:462274 AN 2008:570147

32. Moon, Dong-Oh; Kim, Mun-Ock; Choi, Yung Hyun; Kim, Gi-Young.  -Sitosterol induces G2/M arrest, endoreduplication, and apoptosis through the Bcl-2 and PI3K/Akt signaling pathways. Cancer Letters (Shannon, Ireland) (2008), 264(2), 181-191. CODEN: CALEDQ ISSN:0304-3835. CAN 149:462269 AN 2008:570132

33. Kessel, David. Promotion of PDT efficacy by a Bcl-2 antagonist. Photochemistry and Photobiology (2008), 84(3), 809-814. CODEN: PHCBAP ISSN:0031-8655. CAN 148:465946 AN 2008:561895

34. Chernigovskaya, Elena V.; Nikitina, Liubov S.; Dorofeeva, Nadezhda A.; Glazova, Margarita V. Effects of selective Bcl-2 inhibitor HA14-1 treatments on functional activity of magnocellular vasopressinergic neurons of rat hypothalamus. Neuroscience Letters (2008), 437(1), 59-64. CODEN: NELED5 ISSN:0304-3940. CAN 149:119821 AN 2008:559851

35. Elinson, Michail N.; Dorofeev, Alexander S.; Miloserdov, Fedor M.; Ilovaisky, Alexey I.; Feducovich, Sergey K.; Belyakov, Pavel A.; Nikishin, Gennady I. Catalysis of salicylaldehydes and two different C-H acids with electricity: first example of an efficient multicomponent approach to the design of functionalized medicinally privileged 2-amino-4H-chromene scaffold. Advanced Synthesis & Catalysis (2008), 350(4), 591-601. CODEN: ASCAF7 ISSN:1615-4150. CAN 150:191273 AN 2008:521171

36. Mohammad, Ramzi; Giri, Anshu; Goustin, Anton-Scott. Small-molecule inhibitors of Bcl-2 family proteins as therapeutic agents in cancer. Recent Patents on Anti-Cancer Drug Discovery (2008), 3(1), 20-30. CODEN: RPADDY ISSN:1574-8928. CAN 148:369151 AN 2008:362361

37. Kessel, David; Price, Michael; Haagenson, Kelly. Promotion of PDT efficacy by HA14-1. Proceedings of SPIE (2008), 6845(Optical Methods for Tumor Treatment and Detection: Mechanisms and Techniques in Photodynamic Therapy XVII), 684502/1-684502/7. CODEN: PSISDG ISSN:0277-786X. CAN 149:419930 AN 2008:323907

38. Xue, Hongman; Chen, Chun; Zhang, Jianyu; Zhang, Jinhua; Li, Wenyi. Effects of VPA in combination with HA14-1 on a Bcl-2 overexpressed leukemia cell line BALL-1. Zhongguo Bingli Shengli Zazhi (2006), 22(11), 2227-2230. CODEN: ZBSZEB ISSN:1000-4718. CAN 152:26172 AN 2008:294760

39. Hetschko, Holger; Voss, Valerie; Horn, Sigrid; Seifert, Volker; Prehn, Jochen H. M.; Koegel, Donat. Pharmacological inhibition of Bcl-2 family members reactivates TRAIL-induced apoptosis in malignant glioma. Journal of Neuro-Oncology (2008), 86(3), 265-272. CODEN: JNODD2 ISSN:0167-594X. CAN 148:462637 AN 2008:286838

40. Mortenson, Melinda M.; Galante, Joseph G.; Gilad, Oren; Schlieman, Michael G.; Virudachalam, Subbulakshmi; Kung, Hsing-Jien; Bold, Richard J. BCL-2 functions as an activator of the AKT signaling pathway in pancreatic cancer. Journal of Cellular Biochemistry (2007), 102(5), 1171-1179. CODEN: JCEBD5 ISSN:0730-2312. CAN 148:188716 AN 2007:1426303

41. Ren, Yuan; Chen, Zhengming; Chen, Liwei; Woods, Nicholas T.; Reuther, Gary W.; Cheng, Jin Q.; Wang, Hong-gang; Wu, Jie. Shp2E76K Mutant Confers Cytokine-independent Survival of TF-1 Myeloid Cells by Up-regulating Bcl-XL. Journal of Biological Chemistry (2007), 282(50), 36463-36473. CODEN: JBCHA3 ISSN:0021-9258. CAN 148:52948 AN 2007:1403443

42. Wlodkowic, Donald; Skommer, Joanna; Pelkonen, Jukka. Brefeldin A triggers apoptosis associated with mitochondrial breach and enhances HA14-1- and anti-Fas-mediated cell killing in follicular lymphoma cells. Leukemia Research (2007), 31(12), 1687-1700. CODEN: LEREDD ISSN:0145-2126. CAN 148:440380 AN 2007:1291972

43. Obame, Fatou Nsoure; Zini, Roland; Souktani, Rachid; Berdeaux, Alain; Morin, Didier. Peripheral benzodiazepine receptor-induced myocardial protection is mediated by inhibition of mitochondrial membrane permeabilization. Journal of Pharmacology and Experimental Therapeutics (2007), 323(1), 336-345. CODEN: JPETAB ISSN:0022-3565. CAN 147:419720 AN 2007:1122310

44. Schwartz, Pamela S.; Manion, Michael K.; Emerson, Christine B.; Fry, John S.; Schulz, Craig M.; Sweet, Ian R.; Hockenbery, David M. 2-Methoxy antimycin reveals a unique mechanism for Bcl-xL inhibition. Molecular Cancer Therapeutics (2007), 6(7), 2073-2080. CODEN: MCTOCF ISSN:1535-7163. CAN 147:314299 AN 2007:749014

45. Oliver, Lisa; Mahe, Beatrice; Gree, Rene; Vallette, Francois M.; Juin, Philippe. HA14-1, a small molecule inhibitor of Bcl-2, bypasses chemoresistance in leukaemia cells. Leukemia Research (2007), 31(6), 859-863. CODEN: LEREDD ISSN:0145-2126. CAN 147:398098 AN 2007:632485

46. Su, Yaming; Zhang, Xiaoping; Sinko, Patrick J. Exploitation of drug-induced Bcl-2 overexpression for restoring normal apoptosis function: A promising new approach to the treatment of multidrug resistant cancer. Cancer Letters (Amsterdam, Netherlands) (2007), 253(1), 115-123. CODEN: CALEDQ ISSN:0304-3835. CAN 147:268604 AN 2007:631221

47. Kessel, David; Reiners, John J. Initiation of apoptosis and autophagy by the Bcl-2 antagonist HA14-1. Cancer Letters (Amsterdam, Netherlands) (2007), 249(2), 294-299. CODEN: CALEDQ ISSN:0304-3835. CAN 146:513984 AN 2007:343783

48. Xing, Chengguo; Doshi, Jignesh M. Studies on the stability of HA 14-1, a small molecule antagonist for anti-apoptotic Bcl-2 protein. Abstracts of Papers, 233rd ACS National Meeting, Chicago, IL, United States, March 25-29, 2007 (2007), MEDI-449. CODEN: 69JAUY AN 2007:295878

49. Wlodkowic, Donald; Skommer, Joanna; Pelkonen, Jukka. Towards an understanding of apoptosis detection by SYTO dyes. Cytometry, Part A (2007), 71A(2), 61-72. CODEN: CPAYAV ISSN:1552-4922. CAN 147:253215 AN 2007:238113

50. Witters, Lois M.; Witkoski, Amy; Planas-Silva, Maricarmen D.; Berger, Mark; Viallet, Jean; Lipton, Allan. Synergistic inhibition of breast cancer cell lines with a dual inhibitor of EGFR-HER-2/neu and a Bcl-2 inhibitor. Oncology Reports (2007), 17(2), 465-469. CODEN: OCRPEW ISSN:1021-335X. CAN 146:330182 AN 2007:198697