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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-HIF/HIF Prolyl-hydroxylase-BAY 87-2243
BAY 87-2243

Chemical Structure : BAY 87-2243

CAS No.: 1227158-85-1

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BAY 87-2243 (BAY87-2243)

货号: 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.

规格 价格 库存 数量
5 mg ￥780 In stock
10 mg ￥1180 In stock
25 mg ￥2180 In stock
50 mg ￥3580 In stock
100 mg ￥5480 In stock
250 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

BAY 87-2243 (BAY87-2243) is a highly potent, selective inhibitor of HIF-1, inhibits 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.

物理化学性质&存储条件

分子量 525.54
分子式 C26H26F3N7O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
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

参考文献

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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