ER-400583-00 | HIF-1α inhibitor | Probechem Biochemicals

Chemical Structure : ER-400583-00

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ER-400583-00 (HIF-1α inhibitor)

货号: PC-20456Not For Human Use, Lab Use Only.

ER-400583-00 is a small-molecule HIF-1α inhibitor, inhibits the induction of HIF-1 reporter activity in response to hypoxia with IC50 of 7.9 nM.

规格	价格	库存	数量
50 mg		Get quote
100 mg		Get quote
250 mg		Get quote

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生物&药学活性

ER-400583-00 is a small-molecule HIF-1α inhibitor, inhibits the induction of HIF-1 reporter activity in response to hypoxia with IC50 of 7.9 nM.
ER-400583-00 suppressed the hypoxia-induced accumulation of the messenger RNAs (CA9, VEGFA, and SLC2A1) in U251 cells, without effect on the amount of HIF-1α protein present in U251 cells under normoxic conditions.
ER-400583-00 suppressed the induction of HIF-1α protein in response to hypoxia with IC50 of 3.7 nM.
ER-400583-00 (100 mg/kg, oral) significantly decreased mRNA levels of the HIF-1 target genes CA9, VEGFA, and SLC2A1 24 h after treatment, significantly delayed tumor growth in human U251 tumor xenografts.
ER-400583-00 suppressed cell proliferation distal to the region of blood perfusion in U251 xenograft tumors, exhibited synergistic interaction when combined with radiation therapy.
ER-400583-00 suppressed the accumulation of HIF-1α protein under hypoxic conditions but did not affect HIF-1α mRNA levels.

物理化学性质&存储条件

分子量	486.62
分子式	C32H30N4O
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	N-(4-(phenylethynyl)phenyl)-4-((4-(pyridin-3-ylmethyl)piperazin-1-yl)methyl)benzamide

参考文献

1. Kiyoshi Okamoto, et al. Int J Mol Med. 2012 Apr;29(4):541-9.