For research use only. Not for therapeutic Use.
BAY 87-2243（Cat No.:I000875）is a potent inhibitor of hypoxia-inducible factor-1 (HIF-1), a transcription factor that regulates cellular response to low oxygen levels and plays a critical role in tumor progression and survival under hypoxic conditions. By selectively targeting HIF-1α activity, BAY 87-2243 disrupts cancer cell adaptation to hypoxia, impairing cell survival pathways, angiogenesis, and metabolic adaptation essential for tumor growth. This compound has shown promise in preclinical cancer models, particularly for solid tumors. BAY 87-2243 aids research into anti-cancer therapies focused on overcoming hypoxia-driven resistance mechanisms.
| Catalog Number | I000875 |
| CAS Number | 1227158-85-1 |
| Synonyms | 5-(1-((2-(4-cyclopropylpiperazin-1-yl)pyridin-4-yl)methyl)-5-methyl-1H-pyrazol-3-yl)-3-(4-(trifluoromethoxy)phenyl)-1,2,4-oxadiazole |
| Molecular Formula | C26H26F3N7O2 |
| Purity | ≥95% |
| Target | HIF |
| Solubility | 10 mM in DMSO |
| Storage | Store at -20C |
| IC50 | 2.0 nM(CA9 in HCT116luc cells) |
| IUPAC Name | 5-[1-[[2-(4-cyclopropylpiperazin-1-yl)pyridin-4-yl]methyl]-5-methylpyrazol-3-yl]-3-[4-(trifluoromethoxy)phenyl]-1,2,4-oxadiazole |
| InChI | InChI=1S/C26H26F3N7O2/c1-17-14-22(25-31-24(33-38-25)19-2-6-21(7-3-19)37-26(27,28)29)32-36(17)16-18-8-9-30-23(15-18)35-12-10-34(11-13-35)20-4-5-20/h2-3,6-9,14-15,20H,4-5,10-13,16H2,1H3 |
| InChIKey | CDJNNOJINJAXPV-UHFFFAOYSA-N |
| SMILES | CC1=CC(=NN1CC2=CC(=NC=C2)N3CCN(CC3)C4CC4)C5=NC(=NO5)C6=CC=C(C=C6)OC(F)(F)F |
| Reference | </br>1:Targeting mitochondrial complex I using BAY 87-2243 reduces melanoma tumor growth. Schöckel L, Glasauer A, Basit F, Bitschar K, Truong H, Erdmann G, Algire C, Hägebarth A, Willems PH, Kopitz C, Koopman WJ, Héroult M.Cancer Metab. 2015 Oct 20;3:11. doi: 10.1186/s40170-015-0138-0. eCollection 2015. PMID: 26500770 Free PMC Article</br>2:18F-FAZA PET imaging response tracks the reoxygenation of tumors in mice upon treatment with the mitochondrial complex I inhibitor BAY 87-2243. Chang E, Liu H, Unterschemmann K, Ellinghaus P, Liu S, Gekeler V, Cheng Z, Berndorff D, Gambhir SS.Clin Cancer Res. 2015 Jan 15;21(2):335-46. doi: 10.1158/1078-0432.CCR-14-0217. Epub 2014 Nov 7. PMID: 25381339 Free PMC Article</br>3:BAY 87-2243, a novel inhibitor of hypoxia-induced gene activation, improves local tumor control after fractionated irradiation in a schedule-dependent manner in head and neck human xenografts. Helbig L, Koi L, Brüchner K, Gurtner K, Hess-Stumpp H, Unterschemmann K, Baumann M, Zips D, Yaromina A.Radiat Oncol. 2014 Sep 19;9:207. doi: 10.1186/1748-717X-9-207. PMID: 25234922 Free PMC Article</br>4:BAY 87-2243, a highly potent and selective inhibitor of hypoxia-induced gene activation has antitumor activities by inhibition of mitochondrial complex I. Ellinghaus P, Heisler I, Unterschemmann K, Haerter M, Beck H, Greschat S, Ehrmann A, Summer H, Flamme I, Oehme F, Thierauch K, Michels M, Hess-Stumpp H, Ziegelbauer K.Cancer Med. 2013 Oct;2(5):611-24. doi: 10.1002/cam4.112. Epub 2013 Aug 20. PMID: 24403227 Free PMC Article |
