HIF
シグナル伝達経路
研究分野
阻害剤の選択性比較
| カタログ番号 | 製品カタログ | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | アルコール | ||
| S1233 | 2-Methoxyestradiol (2-MeOE2) | <1 mg/mL | 60 mg/mL | <1 mg/mL |
| S8771 | IDF-11774 | <1 mg/mL | 15 mg/mL | 5 mg/mL |
| S7309 | BAY 87-2243 | <1 mg/mL | 33 mg/mL | 8 mg/mL |
| S7946 | KC7F2 | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S7958 | Lificiguat(YC-1) | <1 mg/mL | 60 mg/mL | 60 mg/mL |
| S8441 | LW 6 | <1 mg/mL | 13 mg/mL | 1 mg/mL |
| S7612 | PX-478 2HCl | 78 mg/mL | 78 mg/mL | 78 mg/mL |
| S1007 | Roxadustat (FG-4592) | <1 mg/mL | 70 mg/mL | <1 mg/mL |
| S2919 | IOX2 | <1 mg/mL | 7 mg/mL | <1 mg/mL |
| S6490 | Vadadustat | <1 mg/mL | 61 mg/mL | 9 mg/mL |
| S8138 | Molidustat (BAY 85-3934) | <1 mg/mL | 3 mg/mL | <1 mg/mL |
| S7979 | FG-2216 | <1 mg/mL | 56 mg/mL | <1 mg/mL |
| S8171 | Daprodustat (GSK1278863) | <1 mg/mL | 10 mg/mL | <1 mg/mL |
| S8443 | MK-8617 | <1 mg/mL | 20 mg/mL | 1 mg/mL |
| S7483 | DMOG | 35 mg/mL | 35 mg/mL | 35 mg/mL |
亜型選択性的な製品
HIF製品
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S1233 |
2-Methoxyestradiol (2-MeOE2)2-Methoxyestradiol (2-MeOE2) depolymerizes microtubules and blocks HIF-1α nuclear accumulation and HIF-transcriptional activity. Phase 2. |
-S123306W0220150907.gif)
-S123306W0220150907.gif)
Pancreatic cancer cell lines (CFPAC-1 and BxPC-3) were treated with siHIF-1 and 2-ME and then evaluate the expression HIF-1α, CRT and P-eIF2α by Western blotting experiment.
|
|
| S8771 |
IDF-11774IDF-11774 is a hypoxia-inducible factor-1 (HIF-1) inhibitor. It reduces the HRE-luciferase activity of HIF-1α (IC50 = 3.65 μM) and blocks HIF-1α accumulation under hypoxia in HCT116 human colon cancer cells. |
||
| S7309 |
BAY 87-2243BAY 87-2243 is a potent and selective hypoxia-inducible factor-1 (HIF-1) inhibitor. Phase 1. |
Cells were plated at low density, treated with the indicated compounds and scored for resistance. Abbreviations: osimertinib (Osi), phenformin (Phen), metformin (Met), buformin (Buf), BAY 87-2243 (BAY), oligomycin (Oligo).
|
|
| S7946 |
KC7F2KC7F2 is a selective HIF-1α transcription inhibitor with IC50 of 20 μM in a cell-based assay. |
Western blot analysis showed that KC7F2 (10 nM) significantly decreased the expression of HIF-1α, p27 and flt-1, while KC7F2 (10 nM) elevated cyclin D1 and flk-1 levels after 24 h incubation compared with the 1% O2 condition.
|
|
| S7958 |
Lificiguat(YC-1)YC-1 is an nitric oxide (NO)-independent activator of soluble guanylyl cyclase(sGC) and an inhibitor of Hypoxia-inducible factor-1alpha (HIF-1alpha). |
||
| S8441 |
LW 6LW6 is a hypoxia-inducible factor 1(HIF) inhibitor which potently inhibits HIF-1α accumulation by degrading HIF-1α without affecting the HIF-1a mRNA levels during hypoxia. It inhibits hypoxia-induced HIF-1α transcription activity with IC50 of 2.64 μM in cell-based HRE-reporter gene assays. |
||
| S7612 |
PX-478 2HClPX-478 2HCl is an orally active, and selective hypoxia-inducible factor-1α (HIF-1α) inhibitor. Phase 1. |
Glucose uptake and lactate production were determined in H460 and A549 lung cancer cells in the presence of the HIF1α inhibitor, PX-478 (10 μM) (** p < 0.01)
|
|
| S1007 |
Roxadustat (FG-4592)Roxadustat (FG-4592) is an HIF-α prolyl hydroxylase inhibitor in a cell-free assay, stabilizes HIF-2 and induces EPO production. Phase 3. |
Immunoblots showing dose-dependent HIF-1α stabilization in U2OS, HeLa and Hep3b (and HIF-2α) cells after 6 hours treatment with FG-4592.
|
|
| S2919 |
IOX2IOX2 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. |
NHEK and NHDF are cultivated under normoxic (N) and hypoxic (H) conditions in the presence of IOX2 (50 μM), or vehicle control (DMSO). b HIF-1α levels are analyzed in cell extracts of NHEK (4 h) and NHDF (24 h) by immunoblotting with cellular β-actin as loading control. c Subcellular localization of HIF-1α is examined by immunoblotting analysis of HIF-1α in nuclear (Nu) and cytoplasmic (Cy) fractions with β-tubulin as cytosolic loading control.
|
|
| S6490新 |
VadadustatVadadustat is a novel, titratable, oral HIF-PH inhibitor. |
||
| S8138 |
Molidustat (BAY 85-3934)Molidustat (BAY 85-3934) is a potent hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor with IC50 of 480 nM, 280 nM, and 450 nM for PHD1, PHD2, and PHD, respectively. Phase 2. |
Western blot analysis of the indicated proteins after the treatment with BAY 85-394 (L).
|
|
| S7979 |
FG-2216FG-2216 is a potent, and orally active HIF prolyl 4-hydroxylase inhibitor with IC50 of 3.9 μM for PHD2. Phase 2. |
||
| S8171 |
Daprodustat (GSK1278863)Daprodustat (GSK1278863) is an orally administered hypoxia-inducible factor-prolyl hydroxylase (HIF-PH) inhibitor. Phase 2. |
||
| S8443 |
MK-8617MK-8617 is an orally active pan-inhibitor of Hypoxia-inducible factor prolyl hydroxylase 1−3 (HIF PHD1−3), inhibiting PHD1, 2, 3 with IC50s of 1.0, 1.0 and 14 nM, respectively. |
||
| S7483 |
DMOGDMOG is an antagonist of α-ketoglutarate cofactor and inhibitor for HIF prolylhydroxylase. |
Western blot was performed to analyze p65 signaling and the expression of Bcl2 and cleaved Caspase 3. GAPDH served as the loading control
|
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S1233 |
2-Methoxyestradiol (2-MeOE2)2-Methoxyestradiol (2-MeOE2) depolymerizes microtubules and blocks HIF-1α nuclear accumulation and HIF-transcriptional activity. Phase 2. |
-S123306W0220150907.gif)
-S123306W0220150907.gif)
Pancreatic cancer cell lines (CFPAC-1 and BxPC-3) were treated with siHIF-1 and 2-ME and then evaluate the expression HIF-1α, CRT and P-eIF2α by Western blotting experiment.
|
|
| S8771 |
IDF-11774IDF-11774 is a hypoxia-inducible factor-1 (HIF-1) inhibitor. It reduces the HRE-luciferase activity of HIF-1α (IC50 = 3.65 μM) and blocks HIF-1α accumulation under hypoxia in HCT116 human colon cancer cells. |
||
| S7309 |
BAY 87-2243BAY 87-2243 is a potent and selective hypoxia-inducible factor-1 (HIF-1) inhibitor. Phase 1. |
Cells were plated at low density, treated with the indicated compounds and scored for resistance. Abbreviations: osimertinib (Osi), phenformin (Phen), metformin (Met), buformin (Buf), BAY 87-2243 (BAY), oligomycin (Oligo).
|
|
| S7946 |
KC7F2KC7F2 is a selective HIF-1α transcription inhibitor with IC50 of 20 μM in a cell-based assay. |
Western blot analysis showed that KC7F2 (10 nM) significantly decreased the expression of HIF-1α, p27 and flt-1, while KC7F2 (10 nM) elevated cyclin D1 and flk-1 levels after 24 h incubation compared with the 1% O2 condition.
|
|
| S7958 |
Lificiguat(YC-1)YC-1 is an nitric oxide (NO)-independent activator of soluble guanylyl cyclase(sGC) and an inhibitor of Hypoxia-inducible factor-1alpha (HIF-1alpha). |
||
| S8441 |
LW 6LW6 is a hypoxia-inducible factor 1(HIF) inhibitor which potently inhibits HIF-1α accumulation by degrading HIF-1α without affecting the HIF-1a mRNA levels during hypoxia. It inhibits hypoxia-induced HIF-1α transcription activity with IC50 of 2.64 μM in cell-based HRE-reporter gene assays. |
||
| S7612 |
PX-478 2HClPX-478 2HCl is an orally active, and selective hypoxia-inducible factor-1α (HIF-1α) inhibitor. Phase 1. |
Glucose uptake and lactate production were determined in H460 and A549 lung cancer cells in the presence of the HIF1α inhibitor, PX-478 (10 μM) (** p < 0.01)
|
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S1007 |
Roxadustat (FG-4592)Roxadustat (FG-4592) is an HIF-α prolyl hydroxylase inhibitor in a cell-free assay, stabilizes HIF-2 and induces EPO production. Phase 3. |
2020, 34(2):2344-2358 2020, 211:103558 2019, 36(2):179-193 |
Immunoblots showing dose-dependent HIF-1α stabilization in U2OS, HeLa and Hep3b (and HIF-2α) cells after 6 hours treatment with FG-4592.
|
| S2919 |
IOX2IOX2 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. |
2020, 211:103558 2019, 2019:4824035 2019, 10.1016/j.bbrc.2019.07.039 |
NHEK and NHDF are cultivated under normoxic (N) and hypoxic (H) conditions in the presence of IOX2 (50 μM), or vehicle control (DMSO). b HIF-1α levels are analyzed in cell extracts of NHEK (4 h) and NHDF (24 h) by immunoblotting with cellular β-actin as loading control. c Subcellular localization of HIF-1α is examined by immunoblotting analysis of HIF-1α in nuclear (Nu) and cytoplasmic (Cy) fractions with β-tubulin as cytosolic loading control.
|
| S6490新 |
VadadustatVadadustat is a novel, titratable, oral HIF-PH inhibitor. |
||
| S8138 |
Molidustat (BAY 85-3934)Molidustat (BAY 85-3934) is a potent hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor with IC50 of 480 nM, 280 nM, and 450 nM for PHD1, PHD2, and PHD, respectively. Phase 2. |
2020, 34(2):2344-2358 2019, 12:9017-9027 2017, 7(13):3293-3305 |
Western blot analysis of the indicated proteins after the treatment with BAY 85-394 (L).
|
| S7979 |
FG-2216FG-2216 is a potent, and orally active HIF prolyl 4-hydroxylase inhibitor with IC50 of 3.9 μM for PHD2. Phase 2. |
2020, 34(2):2344-2358 |
|
| S8171 |
Daprodustat (GSK1278863)Daprodustat (GSK1278863) is an orally administered hypoxia-inducible factor-prolyl hydroxylase (HIF-PH) inhibitor. Phase 2. |
2020, 34(2):2344-2358 2019, 79(10):2564-2579 |
|
| S8443 |
MK-8617MK-8617 is an orally active pan-inhibitor of Hypoxia-inducible factor prolyl hydroxylase 1−3 (HIF PHD1−3), inhibiting PHD1, 2, 3 with IC50s of 1.0, 1.0 and 14 nM, respectively. |
2020, 34(2):2344-2358 |
|
| S7483 |
DMOGDMOG is an antagonist of α-ketoglutarate cofactor and inhibitor for HIF prolylhydroxylase. |
2019, 530:51-58 2018, 68(6):2359-2375 2018, 22(9):4507-4521 |
Western blot was performed to analyze p65 signaling and the expression of Bcl2 and cleaved Caspase 3. GAPDH served as the loading control
|
