HIF

シグナル伝達経路

研究分野

阻害剤の選択性比較
溶解度

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
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 (14) HIF阻害剤(7) HIFモジュレータ(7) 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.	Nucleic Acids Res, 2015, 10.1093/nar/gkv379 Mol Cell Endocrinol, 2018, 10.1016/j.mce.2018.05.002 Australas J Dermatol, 2015, 10.1111/ajd.12340	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^新	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.	Vascul Pharmacol, 2016, 10.1016/j.vph.2016.05.002 Pathol Oncol Res, 2016, 10.1007/s12253-016-0076-3 Oncotarget, 2016, 7(52):86313-86325	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.	Stem Cell Res Ther, 2018, 9(1):280 Respir Physiol Neurobiol, 2018, 247:87-95	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 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.
S7612	PX-478 2HCl PX-478 2HCl is an orally active, and selective hypoxia-inducible factor-1α (HIF-1α) inhibitor. Phase 1.	Theranostics, 2018, 8(3):610-626 Br J Pharmacol, 2017, 174(5):409-423 Am J Cancer Res, 2017, 7(5):1198-1212	Canonical hedgehog transactivates HIF-1α, which mediates the angiogenic properties of HSCs. HSCs were treated with PX-478, cyclopamine or GANT-58 at indicated concentrations for 24 h (A-C） or 3 h (D). (A) Cell viability was determined using Cell Counting Kit-8. Data were expressed as percentage of control value (n = 6). P < 0.05 versus control, non-parametric analyses with Kruskal-Wallis H test. (B, E) Real-time PCR analyses of angiogenic cytokines (B) and HIF-1α (E). Data were expressed as fold of control value (n = 6). P < 0.05 versus control, non-parametric analyses with Kruskal-Wallis H test. (C, F) Western blot analyses of angiogenic cytokines (C) and HIF-1α (F) (n = 3). (D) Tubulogenesis assay with quantification of number of closed intercellular compartments (100× magnification) (n = 5). *P < 0.05 versus control, Student's t-test.
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.	J Hepatol, 2014, 61(4):746-54 Chem Sci, 2017, 10.1039/C7SC02103H Cell Physiol Biochem, 2018, 46(6):2460-2470	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.	Arch Toxicol, 2016, 90(5):1141-50 Arch Toxicol, 2015, 10.1007/s00204-015-1549-y Int J Low Extrem Wounds, 2015, 14(1):63-72	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.
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.
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.	Hepatology, 2018, 68(6):2359-2375 Theranostics, 2017, 7(13):3293-3305 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.	Nucleic Acids Res, 2015, 10.1093/nar/gkv379 Mol Cell Endocrinol, 2018, 10.1016/j.mce.2018.05.002 Australas J Dermatol, 2015, 10.1111/ajd.12340	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^新	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.	Vascul Pharmacol, 2016, 10.1016/j.vph.2016.05.002 Pathol Oncol Res, 2016, 10.1007/s12253-016-0076-3 Oncotarget, 2016, 7(52):86313-86325	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.	Stem Cell Res Ther, 2018, 9(1):280 Respir Physiol Neurobiol, 2018, 247:87-95	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 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.
S7612	PX-478 2HCl PX-478 2HCl is an orally active, and selective hypoxia-inducible factor-1α (HIF-1α) inhibitor. Phase 1.	Theranostics, 2018, 8(3):610-626 Br J Pharmacol, 2017, 174(5):409-423 Am J Cancer Res, 2017, 7(5):1198-1212	Canonical hedgehog transactivates HIF-1α, which mediates the angiogenic properties of HSCs. HSCs were treated with PX-478, cyclopamine or GANT-58 at indicated concentrations for 24 h (A-C） or 3 h (D). (A) Cell viability was determined using Cell Counting Kit-8. Data were expressed as percentage of control value (n = 6). P < 0.05 versus control, non-parametric analyses with Kruskal-Wallis H test. (B, E) Real-time PCR analyses of angiogenic cytokines (B) and HIF-1α (E). Data were expressed as fold of control value (n = 6). P < 0.05 versus control, non-parametric analyses with Kruskal-Wallis H test. (C, F) Western blot analyses of angiogenic cytokines (C) and HIF-1α (F) (n = 3). (D) Tubulogenesis assay with quantification of number of closed intercellular compartments (100× magnification) (n = 5). *P < 0.05 versus control, Student's t-test.

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.	J Hepatol, 2014, 61(4):746-54 Chem Sci, 2017, 10.1039/C7SC02103H Cell Physiol Biochem, 2018, 46(6):2460-2470	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.	Arch Toxicol, 2016, 90(5):1141-50 Arch Toxicol, 2015, 10.1007/s00204-015-1549-y Int J Low Extrem Wounds, 2015, 14(1):63-72	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.
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.
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.	Hepatology, 2018, 68(6):2359-2375 Theranostics, 2017, 7(13):3293-3305 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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