ARQ-171
ARQ-171 is a second-generation E2F1 pathway activator with potential antineoplastic activity. ARQ 171 induces the expression of E2F transcription factor 1, thereby activating the E2F1-mediated checkpoint process. As a result, this agent exerts anti-tumor activity through checkpoint activation independent of p53 mediated tumor suppression. E2F1, down-regulated in cancer cells, regulates expression of genes involved in the cell cycle progression from G1 into S phase. The G1/S checkpoint process selectively induces cell cycle arrest in cancer cells with irreparable DNA damages and triggers subsequent apoptosis, while allowing cell division to proceed in cells without or with minor reparable DNA damage.
1: de Andrade CP, de Oliveira EC, Leal JS, de Almeida LL, de Castro LA, da Silva SC, Driemeier D. Report of outbreaks of classical scrapie in Dorper sheep and associated prion protein gene polymorphisms in affected flocks. Trop Anim Health Prod. 2015 May 21. [Epub ahead of print] PubMed PMID: 25995150.
2: Reis F, Kido RY, Mesquita JA, Oshima MM, Montenegro MA. Megalencephalic leukoencephalopathy with subcortical cysts (MLC) - a case with clinical and magnetic resonance imaging (MRI) dissociation. Arq Neuropsiquiatr. 2015 Feb;73(2):171-2. doi: 10.1590/0004-282X20140206. PubMed PMID: 25742591.
3: McGovern G, Martin S, Jeffrey M, Bellworthy SJ, Spiropoulos J, Green R, Lockey R, Vickery CM, Thurston L, Dexter G, Hawkins SA, González L. Influence of breed and genotype on the onset and distribution of infectivity and disease-associated prion protein in sheep following oral infection with the bovine spongiform encephalopathy agent. J Comp Pathol. 2015 Jan;152(1):28-40. doi: 10.1016/j.jcpa.2014.09.004. Epub 2014 Nov 27. PubMed PMID: 25435510.
4: Savarese LG, Ferreira-Neto GD, Herrero CF, Defino HL, Nogueira-Barbosa MH. Cauda equina redundant nerve roots are associated to the degree of spinal stenosis and to spondylolisthesis. Arq Neuropsiquiatr. 2014 Oct;72(10):782-7. PubMed PMID: 25337731.
5: Andrade-Silva SG, Caranti DA, Sallet JA, Leal LP, Leal AJ, Dâmaso AR. Age and gender may influence the results of Roux-en-Y gastric bypass? Metabolic syndrome parameters. Arq Gastroenterol. 2014 Jul-Sep;51(3):171-9. PubMed PMID: 25296075.
6: Greenlee JJ, Kunkle RA, Richt JA, Nicholson EM, Hamir AN. Lack of prion accumulation in lymphoid tissues of PRNP ARQ/ARR sheep intracranially inoculated with the agent of scrapie. PLoS One. 2014 Sep 18;9(9):e108029. doi: 10.1371/journal.pone.0108029. eCollection 2014. PubMed PMID: 25233232; PubMed Central PMCID: PMC4169493.
7: Secundo Junior JA, Santos MA, Faro GB, Soares CB, Silva AM, Secundo PF, Teixeira CK, Oliveira JL, Barreto Filho JA, Sousa AC. Left atrial volume index and prediction of events in acute coronary syndrome: Solar Registry. Arq Bras Cardiol. 2014 Oct;103(4):282-91. Epub 2014 Aug 13. English, Portuguese. Erratum in: Arq Bras Cardiol. 2014 Dec;103(6):546. PubMed PMID: 25119895; PubMed Central PMCID: PMC4206358.
8: Abreu JS, Lima JW, Diógenes TC, Siqueira JM, Pimentel NL, Gomes Neto PS, Abreu ME, Paes Júnior JN. Coronary flow velocity reserve during dobutamine stress echocardiography. Arq Bras Cardiol. 2014 Feb;102(2):134-42. Epub 2013 Dec 21. PubMed PMID: 24676368; PubMed Central PMCID: PMC3987342.
9: González L, Pitarch JL, Martin S, Thurston L, Simmons H, Acín C, Jeffrey M. Influence of polymorphisms in the prion protein gene on the pathogenesis and neuropathological phenotype of sheep scrapie after oral infection. J Comp Pathol. 2014 Jan;150(1):57-70. doi: 10.1016/j.jcpa.2013.10.001. Epub 2013 Oct 10. PubMed PMID: 24342584.
10: Dozza AL, Krymchantowski AV. Adherence to migraine treatment does not depend on the number of prescribed medications. Arq Neuropsiquiatr. 2013 Mar;71(3):171-3. PubMed PMID: 23563717.
2: Reis F, Kido RY, Mesquita JA, Oshima MM, Montenegro MA. Megalencephalic leukoencephalopathy with subcortical cysts (MLC) - a case with clinical and magnetic resonance imaging (MRI) dissociation. Arq Neuropsiquiatr. 2015 Feb;73(2):171-2. doi: 10.1590/0004-282X20140206. PubMed PMID: 25742591.
3: McGovern G, Martin S, Jeffrey M, Bellworthy SJ, Spiropoulos J, Green R, Lockey R, Vickery CM, Thurston L, Dexter G, Hawkins SA, González L. Influence of breed and genotype on the onset and distribution of infectivity and disease-associated prion protein in sheep following oral infection with the bovine spongiform encephalopathy agent. J Comp Pathol. 2015 Jan;152(1):28-40. doi: 10.1016/j.jcpa.2014.09.004. Epub 2014 Nov 27. PubMed PMID: 25435510.
4: Savarese LG, Ferreira-Neto GD, Herrero CF, Defino HL, Nogueira-Barbosa MH. Cauda equina redundant nerve roots are associated to the degree of spinal stenosis and to spondylolisthesis. Arq Neuropsiquiatr. 2014 Oct;72(10):782-7. PubMed PMID: 25337731.
5: Andrade-Silva SG, Caranti DA, Sallet JA, Leal LP, Leal AJ, Dâmaso AR. Age and gender may influence the results of Roux-en-Y gastric bypass? Metabolic syndrome parameters. Arq Gastroenterol. 2014 Jul-Sep;51(3):171-9. PubMed PMID: 25296075.
6: Greenlee JJ, Kunkle RA, Richt JA, Nicholson EM, Hamir AN. Lack of prion accumulation in lymphoid tissues of PRNP ARQ/ARR sheep intracranially inoculated with the agent of scrapie. PLoS One. 2014 Sep 18;9(9):e108029. doi: 10.1371/journal.pone.0108029. eCollection 2014. PubMed PMID: 25233232; PubMed Central PMCID: PMC4169493.
7: Secundo Junior JA, Santos MA, Faro GB, Soares CB, Silva AM, Secundo PF, Teixeira CK, Oliveira JL, Barreto Filho JA, Sousa AC. Left atrial volume index and prediction of events in acute coronary syndrome: Solar Registry. Arq Bras Cardiol. 2014 Oct;103(4):282-91. Epub 2014 Aug 13. English, Portuguese. Erratum in: Arq Bras Cardiol. 2014 Dec;103(6):546. PubMed PMID: 25119895; PubMed Central PMCID: PMC4206358.
8: Abreu JS, Lima JW, Diógenes TC, Siqueira JM, Pimentel NL, Gomes Neto PS, Abreu ME, Paes Júnior JN. Coronary flow velocity reserve during dobutamine stress echocardiography. Arq Bras Cardiol. 2014 Feb;102(2):134-42. Epub 2013 Dec 21. PubMed PMID: 24676368; PubMed Central PMCID: PMC3987342.
9: González L, Pitarch JL, Martin S, Thurston L, Simmons H, Acín C, Jeffrey M. Influence of polymorphisms in the prion protein gene on the pathogenesis and neuropathological phenotype of sheep scrapie after oral infection. J Comp Pathol. 2014 Jan;150(1):57-70. doi: 10.1016/j.jcpa.2013.10.001. Epub 2013 Oct 10. PubMed PMID: 24342584.
10: Dozza AL, Krymchantowski AV. Adherence to migraine treatment does not depend on the number of prescribed medications. Arq Neuropsiquiatr. 2013 Mar;71(3):171-3. PubMed PMID: 23563717.
| Chemical | |
|---|---|
| CAS Num | NONE |
| IUPAC Chemical Name | NONE |
| Synonym | ARQ171; ARQ 171; ARQ-171 |
| Solubility | Soluble in DMSO, not in water |
| Biological | |
| Targets and Effects | E2F1 Activator |
| Pathways | Apoptosis |
| Physical | |
| Appearance | Solid powder |
| Purity | >98% (or refer to the Certificate of Analysis) |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| Storage Condition | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Shelf Life | >5 years if stored properly |
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