|
Toll Free: (877) 796-6397 -- USA and Canada only -- |
Fax: +1-832-582-8590 Orders: +1-832-582-8158 |
Tech Support: +1-832-582-8158 Ext:3 Please provide your Order Number in the email. |
Technical Data
| Formula | C19H16N2O5 |
|||
| Molecular Weight | 352.34 | CAS No. | 931398-72-0 | |
| Solubility (25°C)* | In vitro | DMSO | 7 mg/mL (19.86 mM) | |
| Water | Insoluble | |||
| Ethanol | Insoluble | |||
|
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
||||
Preparing Stock Solutions
Biological Activity
| Description | IOX2 (JICL38) is a potent inhibitor of HIF-1α prolyl hydroxylase-2 (PHD2) with IC50 of 21 nM in a cell-free assay, >100-fold selectivity over JMJD2A, JMJD2C, JMJD2E, JMJD3, or the 2OG oxygenase FIH. | ||
|---|---|---|---|
| Targets |
|
||
| In vitro | IOX2 potently inhibits PHD2 (IC50 of 21 nM) with over 100-fold selectivity compared to inhibition of JMJD2A, JMJD2C, JMJD2E, JMJD3, or the 2OG oxygenase FIH (IC50s <100 μM). IOX2 is active in cells, inhibiting HIF-1α hydroxylation in RCC4 cells at 50 μM. [1] Hypoxia Inducible Factor (HIF) is regulated by the hydroxylation of prolyl residues in oxygen-dependent degradation domains in the HIF-1α subunit, which mark it for degradation by the proteosome. 1,2 HIF prolyl hydroxylation is catalyzed by prolyl hydroxylase domain enzymes (PHD1, 2, and 3), members of the Fe(II) and 2-oxoglutarate (2OG) oxygenase family. They require dioxygen as a cosubstrate, thus acting as the hypoxia-sensing component of the HIF system. The activity of PHD is suppressed by hypoxia, increasing both the abundance and activity of the HIF transcriptional complex. [2] |
Protocol (from reference)
References
|
Customer Product Validation
-
Data from [Data independently produced by , , Arch Toxicol, 2016, 90(5):1141-50]
-
Data from [Data independently produced by , , Arch Toxicol, 2015, 10.1007/s00204-015-1549-y ]
-
Data from [Data independently produced by , , Thromb Haemost, 2017, 117(10):1875-1886]
Selleck's IOX2 has been cited by 20 publications
| Inhibition of CD38 enzymatic activity enhances CAR-T cell immune-therapeutic efficacy by repressing glycolytic metabolism [ Cell Rep Med, 2024, 5(2):101400] | PubMed: 38307031 |
| iASPP is essential for HIF-1α stabilization to promote angiogenesis and glycolysis via attenuating VHL-mediated protein degradation [ Oncogene, 2022, 41(13):1944-1958] | PubMed: 35169254 |
| Pseudohypoxic HIF pathway activation dysregulates collagen structure-function in human lung fibrosis [ Elife, 2022, 11e69348] | PubMed: 35188460 |
| Upregulation of HIF-1α contributes to complement activation in transplantation-associated thrombotic microangiopathy [ Br J Haematol, 2022, 10.1111/bjh.18377] | PubMed: 35864790 |
| Von Hippel-Lindau (VHL) small molecule inhibitor binding increases stability and intracellular levels of VHL protein [ J Biol Chem, 2021, S0021-9258(21)00710-9] | PubMed: 34174286 |
| ITRAQ-based quantitative proteomic analysis of MG63 in response to HIF-1α inducers. [ J Proteomics, 2020, 211:103558] | PubMed: 31655150 |
| Metabolic Rewiring in Response to Biguanides Is Mediated by mROS/HIF-1a in Malignant Lymphocytes. [ Cell Rep, 2019, 29(10):3009-3018] | PubMed: 31801069 |
| Propofol Alleviates Apoptosis Induced by Chronic High Glucose Exposure via Regulation of HIF-1α in H9c2 Cells [ Oxid Med Cell Longev, 2019, 2019:4824035] | PubMed: 31093315 |
| EZH2 regulates PD-L1 expression via HIF-1α in non-small cell lung cancer cells. [ Biochem Biophys Res Commun, 2019, 10.1016/j.bbrc.2019.07.039] | PubMed: 31331645 |
| RNA-seq analysis of PHD and VHL inhibitors reveals differences and similarities to the hypoxia response [ Wellcome Open Res, 2019, 04:17] | PubMed: 30801039 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.