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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-HIF/HIF Prolyl-hydroxylase-PHD inhibitor IOX5
PHD inhibitor IOX5

Chemical Structure : PHD inhibitor IOX5

CAS No.:

PHD inhibitor IOX5 (IOX5)

货号: PC-22353Not For Human Use, Lab Use Only.

IOX5 is a potent, selective HIF-prolyl hydroxylase (PHD) inhibitor with IC50 of 0.15 uM ((PHD2), does not inhibit other 2OG-dependent oxygenases (JMJD6, FIH, KDM6B etc.).

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

IOX5 is a potent, selective HIF-prolyl hydroxylase (PHD) inhibitor with IC50 of 0.15 uM ((PHD2), does not inhibit other 2OG-dependent oxygenases (JMJD6, FIH, KDM6B etc.).
IOX5 shown to compete with 2OG for binding to PHD2, stabilizes HIF-1α at 0.5 μM in HEK293T cells.
IOX5 does not inhibit any of the other tested human 2OG-dependent oxygenases, including FIH and the histone-modifying 2OG oxygenases lysine-specific demethylase 4A (KDM4A), lysine-specific demethylase 5B (KDM5B), lysine-specific demethylase 6B (KDM6B), JMJD6 at 100 μM and the prolyl hydroxylase OGFOD1 at 50 uM.
stabilizes HIF-1α and substantially impacts AML growth and survival in vitro.
IOX5 compromises both MLL-rearranged and non-MLL AML in vivo, decreases AML engraftment and increases survival in vivo but does not affect normal hematopoiesis.
IOX5 compromises AML in a HIF-α dependent manner, requires the intact HIF system to exhibit its anti-leukemic activity.

物理化学性质&存储条件

分子量 368.36
分子式 C17H19F3N4O2
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

4-oxo-6-(1H-pyrazol-1-yl)-N-(((1r,4r)-4-(trifluoromethyl)cyclohexyl)methyl)-1,4-dihydropyridine-3-carboxamide

参考文献

1. Lawson H, et al. Nat Cancer. 2024 Apr 18. doi: 10.1038/s43018-024-00761-w.

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