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
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

All (15) HIF阻害剤(7) HIFモジュレータ(8) 新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.	Mol Cell, 2019, 10.1016/j.molcel.2019.10.023 Eur Rev Med Pharmacol Sci, 2019, 23(3):1055-1062 Nat Commun, 2018, 9(1):5009	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.
S7309	BAY 87-2243 BAY 87-2243 is a potent and selective hypoxia-inducible factor-1 (HIF-1) inhibitor. Phase 1.	Mol Cell, 2019, 10.1016/j.molcel.2019.10.023 J Exp Clin Cancer Res, 2019, 38(1):204 Exp Ther Med, 2019, 17(6):4547-4553	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.	Nat Commun, 2019, 10(1):2679 Naunyn Schmiedebergs Arch Pharmacol, 2019, 10.1007/s00210-019-01746-8 Stem Cell Res Ther, 2018, 9(1):280	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).	ACS Nano, 2019, 13(2):2176-2189 Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-18-4145 Cancer Cell Int, 2019, 19:17
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. Phase 1.	J Exp Med, 2019, 216(10):2231-2241 J Exp Med, 2019, 216(10):2231-2241 Mol Ther, 2019, 27(10):1810-1824	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.	Cancer Cell, 2019, 36(2):179-193 Cell, 2019, 36(2):179-193 J Clin Invest, 2019, 129(1):336-348	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.	Oxid Med Cell Longev, 2019, 2019:4824035 Biochem Biophys Res Commun, 2019, 10.1016/j.bbrc.2019.07.039 Wellcome Open Res, 2019, 04:17	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.
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.	Theranostics, 2017, 7(13):3293-3305	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.
S8171	Daprodustat (GSK1278863) Daprodustat (GSK1278863) is an orally administered hypoxia-inducible factor-prolyl hydroxylase (HIF-PH) inhibitor. Phase 2.	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.
S7483	DMOG DMOG is an antagonist of α-ketoglutarate cofactor and inhibitor for HIF prolylhydroxylase.	Virology, 2019, 530:51-58 Hepatology, 2018, 68(6):2359-2375 J Cell Mol Med, 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

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.	Mol Cell, 2019, 10.1016/j.molcel.2019.10.023 Eur Rev Med Pharmacol Sci, 2019, 23(3):1055-1062 Nat Commun, 2018, 9(1):5009	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.
S7309	BAY 87-2243 BAY 87-2243 is a potent and selective hypoxia-inducible factor-1 (HIF-1) inhibitor. Phase 1.	Mol Cell, 2019, 10.1016/j.molcel.2019.10.023 J Exp Clin Cancer Res, 2019, 38(1):204 Exp Ther Med, 2019, 17(6):4547-4553	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.	Nat Commun, 2019, 10(1):2679 Naunyn Schmiedebergs Arch Pharmacol, 2019, 10.1007/s00210-019-01746-8 Stem Cell Res Ther, 2018, 9(1):280	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).	ACS Nano, 2019, 13(2):2176-2189 Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-18-4145 Cancer Cell Int, 2019, 19:17
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. Phase 1.	J Exp Med, 2019, 216(10):2231-2241 J Exp Med, 2019, 216(10):2231-2241 Mol Ther, 2019, 27(10):1810-1824	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.	Cancer Cell, 2019, 36(2):179-193 Cell, 2019, 36(2):179-193 J Clin Invest, 2019, 129(1):336-348	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.	Oxid Med Cell Longev, 2019, 2019:4824035 Biochem Biophys Res Commun, 2019, 10.1016/j.bbrc.2019.07.039 Wellcome Open Res, 2019, 04:17	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.
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.	Theranostics, 2017, 7(13):3293-3305	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.
S8171	Daprodustat (GSK1278863) Daprodustat (GSK1278863) is an orally administered hypoxia-inducible factor-prolyl hydroxylase (HIF-PH) inhibitor. Phase 2.	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.
S7483	DMOG DMOG is an antagonist of α-ketoglutarate cofactor and inhibitor for HIF prolylhydroxylase.	Virology, 2019, 530:51-58 Hepatology, 2018, 68(6):2359-2375 J Cell Mol Med, 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

Tags: HIF pathway | HIF cancer | hypoxia-inducible factor cancer | HIF-1 cancer | HIF activation | HIF-1 pathway | hypoxia-inducible factor pathway | HIF-1 activation | HIF-1α pathway | HIF inhibitor review

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