IOX2

SKU: orb1307371

Description

IOX2

Research Area

Epigenetics & Chromatin, Metabolism Research

Key Properties

• CAS Number: 931398-72-0
• MW: 352.34
• Purity: 99.81% (May vary between batches)
• Formula: C₁₉H₁₆N₂O₅
• SMILES: OC(=O)CNC(=O)c1c(O)c2ccccc2n(Cc2ccccc2)c1=O
• Target: HIF/HIF Prolyl-Hydroxylase
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.84 mM);DMSO:7 mg/mL (19.87 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  ELGN1:21 nM|PHD2:21 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). Owing to the expression of the PHD3 encoding gene being 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.
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• Cell Research:
  IOX2 is prepared in DMSO and stored, and then diluted with appropriate medium before use. Both VHL-defective (renal carcinoma cells with an empty vector, RCC4) and VHL-competent cells human embryonic kidney HEK293T, osteosarcoma U2OS and RCC4/VHLHA (RCC4 stably transfected with C-terminal HA-tagged wt VHL) are used. Cells are treated with DMSO (control) and tested compounds (e.g., IOX2) (dissolved in DMSO except for DMOG which is dissolved in PBS and added directly to culture medium) for 4-5 h. Cell extracts are probed with antibodies to hydroxy-Pro564 (CODD-OH) and hydroxy-Asn803 (CAD-OH). HIF-1α band intensities are used to normalize hydroxylation signals.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PHD2, inhibit, JICL-38, JICL 38, JICL38, IOX 2, IOX2, IOX-2, Inhibitor, Hypoxia-inducible factors, HIF/HIF Prolyl-Hydroxylase, HIF/HIF ProlylHydroxylase, HIF Prolyl-Hydroxylase, HIF/HIFProlylHydroxylase, HIF-PH, HIF ProlylHydroxylase, HIF, HIFs, HIFProlylHydroxylase

Compound Identifiers

PubChem CID

54685215