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)
カタログ番号	製品カタログ	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
S8449	VH298	<1 mg/mL	100 mg/mL	'100 mg/mL
S6684	IOX4	<1 mg/mL	66 mg/mL	3 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
S7612	PX-478 2HCl	78 mg/mL	78 mg/mL	'78 mg/mL
S8352	PT2385	<1 mg/mL	77 mg/mL	5 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
S2431	TMTD (Tetramethylthiuram disulfide)	<1 mg/mL	48 mg/mL	''<1 mg/mL

亜型選択性的な製品

HIF製品

All (21) HIF阻害剤(10) HIF拮抗剤(1) HIFモジュレータ(9)

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.	Cancer Cell Int, 2020, 19;20:58 Redox Biol, 2020, 28:101355 Front Pharmacol, 2020, 11:6	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-11774 IDF-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.
S8449^新	VH298 VH298 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.
S6684^新	IOX4 IOX4 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.
S7309	BAY 87-2243 BAY 87-2243 is a potent and selective hypoxia-inducible factor-1 (HIF-1) inhibitor. Phase 1.	J Exp Clin Cancer Res, 2020, 39(1):24 Stem Cells Int, 2020, 10;2020:2016809 Mol Cell, 2019, 10.1016/j.molcel.2019.10.023	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	KC7F2 KC7F2 is a selective HIF-1α transcription inhibitor with IC50 of 20 μM in a cell-based assay.	Diabetologia, 2020, 63(1):149-161 Cell Death Dis, 2020, 27;11(4):290 Nat Commun, 2019, 10(1):2679	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	Glucosamine Glucosamine 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) YC-1 is an nitric oxide (NO)-independent activator of soluble guanylyl cyclase(sGC) and an inhibitor of Hypoxia-inducible factor-1alpha (HIF-1alpha).	Sci Rep, 2020, 7;10(1):7714 Biomed Pharmacother, 2020, 123:109742 ACS Nano, 2019, 13(2):2176-2189
S8441	LW 6 LW6 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.	Oncol Lett, 2019, 17(6):5005-5011
S7612	PX-478 2HCl PX-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.	Biol Reprod, 2020, 102(1):116-132 Int Immunopharmacol, 2020, 1;83:106438 Biochem Biophys Res Commun, 2020, 4;526(3):799-804	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)
S8352	PT2385 PT2385 is a HIF-2α antagonist with luciferase EC50 of 27 nM and no significant off-target activity.
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.	J Med Chem, 2020, 31 J Exp Clin Cancer Res, 2020, 39(1):24 FASEB J, 2020, 34(2):2344-2358	Immunoblots showing dose-dependent HIF-1α stabilization in U2OS, HeLa and Hep3b (and HIF-2α) cells after 6 hours treatment with FG-4592.
S2919	IOX2 IOX2 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.	J Proteomics, 2020, 211:103558 Cell Rep, 2019, 29(10):3009-3018 Oxid Med Cell Longev, 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^新	Vadadustat Vadadustat is a novel, titratable, oral HIF-PH inhibitor.
S5804	N-Acetylcysteine amide N-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.	Int J Biochem Cell Biol, 2020, 121:105703 Pancreatology, 2019, 19(2):258-265 Biochem Biophys Res Commun, 2019, 508(4):1271-1278
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.	Cell Death Dis, 2020, 22;11(5):390 FASEB J, 2020, 34(2):2344-2358 J Pharmacol Sci, 2020, 10.1016	Western blot analysis of the indicated proteins after the treatment with BAY 85-394 (L).
S7979	FG-2216 FG-2216 is a potent, and orally active HIF prolyl 4-hydroxylase inhibitor with IC50 of 3.9 μM for PHD2. Phase 2.	FASEB J, 2020, 34(2):2344-2358
S8171	Daprodustat (GSK1278863) Daprodustat (GSK1278863) is an orally administered hypoxia-inducible factor-prolyl hydroxylase (HIF-PH) inhibitor. Phase 2.	FASEB J, 2020, 34(2):2344-2358 Cancer Res, 2019, 79(10):2564-2579
S8443	MK-8617 MK-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.	FASEB J, 2020, 34(2):2344-2358 Am J Physiol Renal Physiol, 2019, 317(5):F1265-F1273
S7483	DMOG DMOG 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.	Cell Death Differ, 2020, 20 Cells, 2020, 9(3) Int Immunopharmacol, 2020, 1;83:106438	Western blot was performed to analyze p65 signaling and the expression of Bcl2 and cleaved Caspase 3. GAPDH served as the loading control
S2431^新	TMTD (Tetramethylthiuram disulfide) TMTD (Tetramethylthiuram disulfide) can reduce the growth performance of chickens through decreasing liver index, whereas increasing kidney, cardiac, and spleen index, and induces tibial dyschondrolplasia (TD) by changing the expressions of VEGF, HIF-1α and WNT4. TMTD (Tetramethylthiuram disulfide) is widely used in rubber processing as an ultra accelerator for low-temperature cures and in agriculture as an important pesticide.

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.	Cancer Cell Int, 2020, 19;20:58 Redox Biol, 2020, 28:101355 Front Pharmacol, 2020, 11:6	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-11774 IDF-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.
S8449^新	VH298 VH298 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.
S6684^新	IOX4 IOX4 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.
S7309	BAY 87-2243 BAY 87-2243 is a potent and selective hypoxia-inducible factor-1 (HIF-1) inhibitor. Phase 1.	J Exp Clin Cancer Res, 2020, 39(1):24 Stem Cells Int, 2020, 10;2020:2016809 Mol Cell, 2019, 10.1016/j.molcel.2019.10.023	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	KC7F2 KC7F2 is a selective HIF-1α transcription inhibitor with IC50 of 20 μM in a cell-based assay.	Diabetologia, 2020, 63(1):149-161 Cell Death Dis, 2020, 27;11(4):290 Nat Commun, 2019, 10(1):2679	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	Glucosamine Glucosamine 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) YC-1 is an nitric oxide (NO)-independent activator of soluble guanylyl cyclase(sGC) and an inhibitor of Hypoxia-inducible factor-1alpha (HIF-1alpha).	Sci Rep, 2020, 7;10(1):7714 Biomed Pharmacother, 2020, 123:109742 ACS Nano, 2019, 13(2):2176-2189
S8441	LW 6 LW6 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.	Oncol Lett, 2019, 17(6):5005-5011
S7612	PX-478 2HCl PX-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.	Biol Reprod, 2020, 102(1):116-132 Int Immunopharmacol, 2020, 1;83:106438 Biochem Biophys Res Commun, 2020, 4;526(3):799-804	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
S8352	PT2385 PT2385 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

S8352

PT2385

PT2385 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
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.	J Med Chem, 2020, 31 J Exp Clin Cancer Res, 2020, 39(1):24 FASEB J, 2020, 34(2):2344-2358	Immunoblots showing dose-dependent HIF-1α stabilization in U2OS, HeLa and Hep3b (and HIF-2α) cells after 6 hours treatment with FG-4592.
S2919	IOX2 IOX2 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.	J Proteomics, 2020, 211:103558 Cell Rep, 2019, 29(10):3009-3018 Oxid Med Cell Longev, 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^新	Vadadustat Vadadustat is a novel, titratable, oral HIF-PH inhibitor.
S5804	N-Acetylcysteine amide N-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.	Int J Biochem Cell Biol, 2020, 121:105703 Pancreatology, 2019, 19(2):258-265 Biochem Biophys Res Commun, 2019, 508(4):1271-1278
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.	Cell Death Dis, 2020, 22;11(5):390 FASEB J, 2020, 34(2):2344-2358 J Pharmacol Sci, 2020, 10.1016	Western blot analysis of the indicated proteins after the treatment with BAY 85-394 (L).
S7979	FG-2216 FG-2216 is a potent, and orally active HIF prolyl 4-hydroxylase inhibitor with IC50 of 3.9 μM for PHD2. Phase 2.	FASEB J, 2020, 34(2):2344-2358
S8171	Daprodustat (GSK1278863) Daprodustat (GSK1278863) is an orally administered hypoxia-inducible factor-prolyl hydroxylase (HIF-PH) inhibitor. Phase 2.	FASEB J, 2020, 34(2):2344-2358 Cancer Res, 2019, 79(10):2564-2579
S8443	MK-8617 MK-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.	FASEB J, 2020, 34(2):2344-2358 Am J Physiol Renal Physiol, 2019, 317(5):F1265-F1273
S7483	DMOG DMOG 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.	Cell Death Differ, 2020, 20 Cells, 2020, 9(3) Int Immunopharmacol, 2020, 1;83:106438	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
S2431^新	TMTD (Tetramethylthiuram disulfide) TMTD (Tetramethylthiuram disulfide) can reduce the growth performance of chickens through decreasing liver index, whereas increasing kidney, cardiac, and spleen index, and induces tibial dyschondrolplasia (TD) by changing the expressions of VEGF, HIF-1α and WNT4. TMTD (Tetramethylthiuram disulfide) is widely used in rubber processing as an ultra accelerator for low-temperature cures and in agriculture as an important pesticide.

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

S2431^新

TMTD (Tetramethylthiuram disulfide)

TMTD (Tetramethylthiuram disulfide) can reduce the growth performance of chickens through decreasing liver index, whereas increasing kidney, cardiac, and spleen index, and induces tibial dyschondrolplasia (TD) by changing the expressions of VEGF, HIF-1α and WNT4. TMTD (Tetramethylthiuram disulfide) is widely used in rubber processing as an ultra accelerator for low-temperature cures and in agriculture as an important pesticide.

研究分野別

製品類型

HIF

シグナル伝達経路

研究分野

阻害剤の選択性比較

亜型選択性的な製品

HIF製品