IOX2(IOX-2)|cas 931398-72-0|DC Chemicals

Cas No.:	931398-72-0
Chemical Name:	2-(1-Benzyl-4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carboxamido)acetic acid
Synonyms:	IOX 2;2-(1-Benzyl-4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carboxamido)acetic acid;2-[(1-benzyl-4-hydroxy-2-oxoquinoline-3-carbonyl)amino]aceticacid;IOX-2;N-?[[4-?Hydroxy-?2-?oxo-?1-?(phenylmethyl)?-?1,?2-?dihydro-?3-?quinolinyl]?carbonyl]?glycine;CS-0988;QCR-246;JICL38;N-[[1,2-Dihydro-4-hydroxy-2-oxo-1-(phenylmethyl)-3-quinolinyl]carbonyl]-glycine;N-[[4-Hydroxy-2-oxo-1-(phenylmethyl)-1,2-dihydro-3-quinolinyl]carbonyl]glycine;IOX2;IOX2(Glycine);AK176060;2-[(1-benzyl-4-hydroxy-2-oxoquinoline-3-carbonyl)amino]acetic acid;IOX2 sodium salt;MLS006011057;GTPL8229;AOB3949;HMS3651B12;BCP25372;BCP06141;s2919;IOX2, >=98% (HPLC);SB19301;SMR004702849
SMILES:	O([H])C1=C(C(N([H])C([H])([H])C(=O)O[H])=O)C(N(C([H])([H])C2C([H])=C([H])C([H])=C([H])C=2[H])C2=C([H])C([H])=C([H])C([H])=C21)=O
Formula:	C₁₉H₁₆N₂O₅
M.Wt:	352.3407
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	IOX2 is a specific prolyl hydroxylase-2 (PHD2) inhibitor with IC50 of 22 nM.
In Vivo:	To investigate the utility of IOX2 as in vivo functional probes, IOX2 is tested to upregulate HIF signaling in a whole organism, that is, transgenic zebrafish (Danio rerio). Because the expression of the PHD3 encoding gene is regulated by HIF in humans and zebrafish, PHD3 levels are a readout of HIF activity. A zebrafish hypoxia reporter line is generated expressing GFP with the phd3 promoter elements. Transgenic wild-type embryos at 3 days postfertilization treated with compounds (10 μM) for 2 days displayed clear increase in phd3:EGFP expression in the liver, relative to controls. Significant increases in GFP levels are observed with IOX2[1].
In Vitro:	IOX2 is at least 2-5000 fold selective, as judged by IC50 values, for PHD2 over the KDMs and Factor Inhibiting HIF(FIH)[1]. IOX2 significantly upregulates the transcription of VEGF-A and BNIP3 in normal human epidermal keratinocytes (NHEK) and normal human dermal fibroblasts (NHDF) when grown under normoxia and hypoxia. IOX2 efficiently promotes HIF-1α stability, nuclear translocation, and target gene expression in keratinocytes and fibroblasts. In addition, IOX2 significantly upregulates biosynthesis and transcription of VEGF-A and BNIP3 in sulfur mustard (SM)-exposed NHEK and NHDF grown under hypoxia. These results suggest that application of IOX2 is useful for restoring of SM-affected HIF-1α stability and signaling activity in keratinocytes and fibroblasts[2].

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