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Chemical Structure : BAY 87-2243
CAS No.: 1227158-85-1
Catalog No.: PC-20172Not For Human Use, Lab Use Only.
BAY 87-2243 (BAY87-2243) is a highly potent, selective inhibitor of hypoxia-induced gene activation (IC50=0.7 nM), directly inhibits mitochondrial complex I.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 25 mg | $198 | In stock | |
| 50 mg | $298 | In stock | |
| 100 mg | $468 | In stock | |
| 250 mg | Get quote | ||
| 1 g | Get quote |
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BAY 87-2243 (BAY87-2243) is a highly potent, selective inhibitor of hypoxia-induced gene activation (IC50=0.7 nM), directly inhibits mitochondrial complex I.
BAY 87-2243 inhibits hypoxic induction of the HIF target gene CA9 on protein level in HCT116luc cells with IC50 of 2 nM.
BAY 87-2243 inhibits hypoxia-inducible factor (HIF-1α) and HIF-2α protein accumulation in hypoxic H460 cells H460 under hypoxia, but has no effect on HIF-1α protein levels induced by hypoxia mimetics and has no effect on prolyl hydroxylase 2 (PHD2) activity.
BAY 87-2243 suppresses HIF target gene expression in hypoxic lung cancer cells.
BAY 87-2243 inhibits mitochondrial oxygen consumption with IC50 of 10 nM.
BAY 87-2243 potently inhibits cell proliferation of H460 cells with EC50 of 3 nM.
BAY 87-2243 reduces tumor weight, HIF-1α protein, and HIF-1 target gene expression levels in H460 xenograft mouse model.
| M.Wt | 525.54 | |
| Formula | C26H26F3N7O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
1-Cyclopropyl-4-{4-[(5-methyl-3-{3-[4-(trifluoromethoxy)phenyl]-1,2,4-oxadiazol-5-yl}-1H-pyrazol-1-yl)methyl]pyri-din-2-yl}piperazine |
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1. Ellinghaus P, et al. Cancer Med. 2013 Oct;2(5):611-24.
2. Chang E,et al. Clin Cancer Res. 2015 Jan 15;21(2):335-46.
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