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 |
| S2410 | Paeoniflorin | 96 mg/mL | 96 mg/mL | 96 mg/mL |
| S3239 | Emetine Dihydrochloride | -1 mg/mL | 100 mg/mL | -1 mg/mL |
| S9699 | Desidustat | -1 mg/mL | 12 mg/mL | -1 mg/mL |
| S9656 | Enarodustat (JTZ-951) | <1 mg/mL | 68 mg/mL | 2.5 mg/mL |
| S8449 | VH298 | <1 mg/mL | 100 mg/mL | 100 mg/mL |
| S0729 | TP0463518 | <1 mg/mL | 40 mg/mL | <1 mg/mL |
| S6684 | IOX4 | <1 mg/mL | 66 mg/mL | 3 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 |
| S6400 | Glucosamine | 36 mg/mL | 23 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 |
| S2937 | SYP-5 | <1 mg/mL | 62 mg/mL | <1 mg/mL |
| S7612 | PX-478 2HCl | 78 mg/mL | 78 mg/mL | 78 mg/mL |
| S5742 | Deferoxamine mesylate | -1 mg/mL | 100 mg/mL | -1 mg/mL |
| S8351 | PT2399 | <1 mg/mL | 84 mg/mL | '''84 mg/mL |
| S8352 | PT2385 | <1 mg/mL | 77 mg/mL | 5 mg/mL |
| S1232 | M1001 | <1 mg/mL | 65 mg/mL | <1 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 |
| S5804 | N-Acetylcysteine amide | 32 mg/mL | 32 mg/mL | 13 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, NSC 659853) depolymerizes microtubules and blocks HIF-1α nuclear accumulation and HIF-transcriptional activity. 2-Methoxyestradiol induces both autophagy and apoptosis in various carcinogenic cell lines. 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.
|
|
| S2410 |
PaeoniflorinPaeoniflorin is a herbal constituent extracted from the root of Paeonia albiflora Pall. Paeoniflorin reduces COX-2 expression. Paeoniflorin alleviates liver fibrosis by inhibiting HIF-1α through mTOR-dependent pathway. |
||
| S3239新 |
Emetine DihydrochlorideEmetine Dihydrochloride, a principal alkaloid extracted from the root of ipecac clinically used as an emetic and antiprotozoal drug, reduces HIFs (hypoxia-inducible factors; HIF-1α and HIF-2α), PDK1, RhoA, Rho-kinases (ROCK1 and ROCK2) and BRD4. Emetine Dihydrochloride inhibits cellular autophagy and has anti-malarial, anti-viral, anti-bacterial and anti-amoebic effect. |
||
| S9699新 |
DesidustatDesidustat (ZYAN1, ZYAN1-1001), an antianaemic drug candidate, is an orally active hypoxia-inducible factor (HIF) prolyl hydroxylase (PHD) inhibitor (HIF-PHI) that stimulates erythropoiesis. |
||
| S9656新 |
Enarodustat (JTZ-951)Enarodustat (JTZ-951) is a potent and orally active HIF prolyl hydroxylase inhibitor with IC50 of 0.22 μM for PHD2 and EC50 of 5.7 μM for EPO release from Hep3B cells. Enarodustat has the potential for the treatment of renal anemia. |
||
| S8449新 |
VH298VH298 is a potent VHL (Von Hippel-Lindau, the E3 ligase) inhibitor that stabilizes HIF-α. VH298 blocks the VHL:HIF-α interaction with Kd of 90 nM in isothermal titration calorimetry (ITC) and 80 nM in a competitive fluorescence polarization assay. VH-298 can be used in PROTAC technology. |
||
| S0729新 |
TP0463518TP0463518 is a potent hypoxia-inducible factor prolyl hydroxylases (PHDs) inhibitor with Ki of 5.3 nM for human PHD2. TP0463518 inhibits human PHD1, human PHD3 and monkey PHD2 with IC50 of 18 nM, 63 nM and 22 nM, respectively. |
||
| S6684新 |
IOX4IOX4 is a potent and selective HIF prolyl-hydroxylase 2 (PHD2) inhibitor with IC50 of 1.6 nM. IOX4 induces HIFα in various mouse tissues and human cell lines. |
||
| 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. BAY 87-2243 inhibits mitochondrial complex I activity, thus triggering a mitophagy-dependent ROS increase leading to necroptosis and ferroptosis. BAY 87-2243 exerts antitumor activity. 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.
|
|
| S6400 |
GlucosamineGlucosamine (2-amino-2-deoxy-D-glucose) is an amino sugar and a prominent precursor in the biochemical synthesis of glycosylated proteins and lipids. It is commonly used as a treatment for osteoarthritis. |
||
| S7958 |
Lificiguat (YC-1)Lificiguat (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. |
||
| S2937 |
SYP-5SYP-5 is an inhibitor of Hypoxia-inducible factor-1 (HIF-1) that suppresses tumor cell migration and invasion, as well as tumor angiogenesis. |
||
| S7612 |
PX-478 2HClPX-478 2HCl is an orally active, and selective hypoxia-inducible factor-1α (HIF-1α) inhibitor. PX-478 2HCl induces apoptosis and has anti-tumor activity. 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)
|
|
| S5742 |
Deferoxamine mesylateDeferoxamine mesylate (Desferrioxamine B) is the mesylate salt of Deferoxamine, which forms iron complexes and is used as a chelating agent. Deferoxamine is a ferroptosis inhibitor that stabilizes HIF-1α expression and improves HIF-1α transactivity in hypoxic and hyperglycemic states in vitro. Deferoxamine decreases beta-amyloid (Aβ) deposition and induces autophagy. |
||
| S8351新 |
PT2399PT2399 is a potent and orally available antagonist of HIF-2 that selectively disrupts the heterodimerization of HIF-2α with HIF-1β. |
||
| S8352 |
PT2385PT2385 is a HIF-2α antagonist with luciferase EC50 of 27 nM and no significant off-target activity. |
||
| S1232新 |
M1001M1001 is a weak agonist of hypoxia-inducible factor-2α (HIF-2α) that binds to the HIF-2α PAS-B domain with Kd of 667 nM. |
||
| 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. Roxadustat potentiates RSL3 induced ferroptosis. 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 (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. |
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 |
VadadustatVadadustat (AKB-6548, B-506, PG-1016548) is a novel, titratable, oral HIF-PH inhibitor. |
||
| S5804 |
N-Acetylcysteine amideN-acetylcysteine amide is a membrane penetrating antioxidant with anti-inflamatory activity through regulation of activation of NF-κB and HIF-1α as well as modulation of ROS. |
||
| 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 (Dimethyloxalylglycine) is an antagonist of α-ketoglutarate cofactor and inhibitor for HIF prolylhydroxylase, leading to stabilisation and accumulation of HIF-1α protein in the nucleus. DMOG enhances autophagy. |
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, NSC 659853) depolymerizes microtubules and blocks HIF-1α nuclear accumulation and HIF-transcriptional activity. 2-Methoxyestradiol induces both autophagy and apoptosis in various carcinogenic cell lines. 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.
|
|
| S2410 |
PaeoniflorinPaeoniflorin is a herbal constituent extracted from the root of Paeonia albiflora Pall. Paeoniflorin reduces COX-2 expression. Paeoniflorin alleviates liver fibrosis by inhibiting HIF-1α through mTOR-dependent pathway. |
||
| S3239新 |
Emetine DihydrochlorideEmetine Dihydrochloride, a principal alkaloid extracted from the root of ipecac clinically used as an emetic and antiprotozoal drug, reduces HIFs (hypoxia-inducible factors; HIF-1α and HIF-2α), PDK1, RhoA, Rho-kinases (ROCK1 and ROCK2) and BRD4. Emetine Dihydrochloride inhibits cellular autophagy and has anti-malarial, anti-viral, anti-bacterial and anti-amoebic effect. |
||
| S9699新 |
DesidustatDesidustat (ZYAN1, ZYAN1-1001), an antianaemic drug candidate, is an orally active hypoxia-inducible factor (HIF) prolyl hydroxylase (PHD) inhibitor (HIF-PHI) that stimulates erythropoiesis. |
||
| S9656新 |
Enarodustat (JTZ-951)Enarodustat (JTZ-951) is a potent and orally active HIF prolyl hydroxylase inhibitor with IC50 of 0.22 μM for PHD2 and EC50 of 5.7 μM for EPO release from Hep3B cells. Enarodustat has the potential for the treatment of renal anemia. |
||
| S8449新 |
VH298VH298 is a potent VHL (Von Hippel-Lindau, the E3 ligase) inhibitor that stabilizes HIF-α. VH298 blocks the VHL:HIF-α interaction with Kd of 90 nM in isothermal titration calorimetry (ITC) and 80 nM in a competitive fluorescence polarization assay. VH-298 can be used in PROTAC technology. |
||
| S0729新 |
TP0463518TP0463518 is a potent hypoxia-inducible factor prolyl hydroxylases (PHDs) inhibitor with Ki of 5.3 nM for human PHD2. TP0463518 inhibits human PHD1, human PHD3 and monkey PHD2 with IC50 of 18 nM, 63 nM and 22 nM, respectively. |
||
| S6684新 |
IOX4IOX4 is a potent and selective HIF prolyl-hydroxylase 2 (PHD2) inhibitor with IC50 of 1.6 nM. IOX4 induces HIFα in various mouse tissues and human cell lines. |
||
| 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. BAY 87-2243 inhibits mitochondrial complex I activity, thus triggering a mitophagy-dependent ROS increase leading to necroptosis and ferroptosis. BAY 87-2243 exerts antitumor activity. 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.
|
|
| S6400 |
GlucosamineGlucosamine (2-amino-2-deoxy-D-glucose) is an amino sugar and a prominent precursor in the biochemical synthesis of glycosylated proteins and lipids. It is commonly used as a treatment for osteoarthritis. |
||
| S7958 |
Lificiguat (YC-1)Lificiguat (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. |
||
| S2937 |
SYP-5SYP-5 is an inhibitor of Hypoxia-inducible factor-1 (HIF-1) that suppresses tumor cell migration and invasion, as well as tumor angiogenesis. |
||
| S7612 |
PX-478 2HClPX-478 2HCl is an orally active, and selective hypoxia-inducible factor-1α (HIF-1α) inhibitor. PX-478 2HCl induces apoptosis and has anti-tumor activity. 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 |
|---|---|---|---|
| S5742 |
Deferoxamine mesylateDeferoxamine mesylate (Desferrioxamine B) is the mesylate salt of Deferoxamine, which forms iron complexes and is used as a chelating agent. Deferoxamine is a ferroptosis inhibitor that stabilizes HIF-1α expression and improves HIF-1α transactivity in hypoxic and hyperglycemic states in vitro. Deferoxamine decreases beta-amyloid (Aβ) deposition and induces autophagy. |
2021, 12(1):647 2021, 1-14 2020, 10:949 |
| 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 |
|---|---|---|---|
| S8351新 |
PT2399PT2399 is a potent and orally available antagonist of HIF-2 that selectively disrupts the heterodimerization of HIF-2α with HIF-1β. |
||
| S8352 |
PT2385PT2385 is a HIF-2α antagonist with luciferase EC50 of 27 nM and no significant off-target activity. |
| 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 |
|---|---|---|---|
| S1232新 |
M1001M1001 is a weak agonist of hypoxia-inducible factor-2α (HIF-2α) that binds to the HIF-2α PAS-B domain with Kd of 667 nM. |
| 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. Roxadustat potentiates RSL3 induced ferroptosis. Phase 3. |
2021, 23(1)41 2020, 31 2020, 39(1):24 |
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 (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. |
2020, 211:103558 2019, 29(10):3009-3018 2019, 2019:4824035 |
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 |
VadadustatVadadustat (AKB-6548, B-506, PG-1016548) is a novel, titratable, oral HIF-PH inhibitor. |
2020, 10.1002/dta.2917 |
|
| S5804 |
N-Acetylcysteine amideN-acetylcysteine amide is a membrane penetrating antioxidant with anti-inflamatory activity through regulation of activation of NF-κB and HIF-1α as well as modulation of ROS. |
2021, 12(1):647 2020, 121:105703 2019, 19(2):258-265 |
|
| 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, 22;11(5):390 2020, 34(2):2344-2358 2020, 10.1016 |
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 2020, 210:111980 |
|
| 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 2019, 33(11):12630-12643 2019, 317(5):F1265-F1273 |
|
| S7483 |
DMOGDMOG (Dimethyloxalylglycine) is an antagonist of α-ketoglutarate cofactor and inhibitor for HIF prolylhydroxylase, leading to stabilisation and accumulation of HIF-1α protein in the nucleus. DMOG enhances autophagy. |
2020, e50827 2020, 20 2020, 10.1038/s41388-020-01474-x |
Western blot was performed to analyze p65 signaling and the expression of Bcl2 and cleaved Caspase 3. GAPDH served as the loading control
|
