| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| I407921-1ml |
1ml |
现货  |
|
| 英文别名 | JICL38 | Glycine, N-[[1,2-dihydro-4-hydroxy-2-oxo-1-(phenylmethyl)-3-quinolinyl]carbonyl]- |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | IOX2 |
| 生化机理 | IOX2 (JICL38) 是 HIF-1α 丙氨酰羟化酶-2 (PHD2) 的强效抑制剂，在无细胞试验中的 IC50 值为 21 nM，选择性大于 JMJD2A、JMJD2C、JMJD2E、JMJD3 或 2OG 加氧酶 FIH 的 100 倍。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | egl-9 家族缺氧诱导因子 1 抑制剂；赖氨酸去甲基化酶 2A 抑制剂；赖氨酸去甲基化酶 5C 抑制剂 |
| 产品介绍 |
IOX2是低氧诱导因子（HIF）脯氨酰羟化酶（PHD）抑制剂，在细胞中对PHD2/ELGN-1的IC50为21 nM，对FIH无活性。 Information IOX2 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. 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. 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. In vivo
cell lines： Concentrations： Incubation Time： Powder Purity:≥99% |
| ALogP | 1.153 |
|---|---|
| hba_count | 3 |
| HBD Count | 2 |
| Rotatable Bond | 5 |
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | OC(=O)CNC(=O)C1=C(O)C2=C(C=CC=C2)N(CC3=CC=CC=C3)C1=O |
| 分子量 | 352.34 |
| Reaxy-Rn | 12851765 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=12851765&ln= |
| DMSO(mg / mL) Max Solubility | 7 |
|---|---|
| DMSO(mM) Max Solubility | 19.87 |
| Water(mg / mL) Max Solubility | <1 |
| Reaxy-Rn | 12851765 |
|---|---|
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=12851765&ln= |
| Concentration(Compounding value) | 9.0-11.0(mmol/L) |
|---|---|
| Appearance(Colorless Transparent Liquid) | Pass |
| Record the entire process by video | Conform |
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