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)
DMSO アルコール
S1233 2-Methoxyestradiol (2-MeOE2) <1 mg/mL 60 mg/mL '<1 mg/mL
S2410 Paeoniflorin (NSC 178886) 96 mg/mL 96 mg/mL '96 mg/mL
S8771 IDF-11774 <1 mg/mL 15 mg/mL 5 mg/mL
S3233 Emetine hydrochloride -1 mg/mL 100 mg/mL -1 mg/mL
S0729 TP0463518 <1 mg/mL 40 mg/mL <1 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
S9699 Desidustat -1 mg/mL 12 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
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
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
S6684 IOX4 <1 mg/mL 66 mg/mL 3 mg/mL
S0908 β,β-Dimethylacrylshikonin ' mg/mL
S3589 Bendazol <1 mg/mL 42 mg/mL ''42 mg/mL
S5742 Deferoxamine mesylate (Ba 33112) -1 mg/mL 100 mg/mL -1 mg/mL
S8352 PT2385 <1 mg/mL 77 mg/mL 5 mg/mL
S8351 PT2399 <1 mg/mL 84 mg/mL ''''84 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
S2431 TMTD (Tetramethylthiuram disulfide) <1 mg/mL 48 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

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, 2-ME2) 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.

S2410

Paeoniflorin (NSC 178886)

Paeoniflorin (NSC 178886) 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.

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.

S3233

Emetine hydrochloride

Emetine hydrochloride (NSC 33669), 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 hydrochloride inhibits cellular autophagy and has anti-malarial, anti-viral, anti-bacterial and anti-amoebic effect.

S0729

TP0463518

TP0463518 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.

S7309

BAY 87-2243

BAY 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.

S7946

KC7F2

KC7F2 is a selective HIF-1α transcription inhibitor with IC50 of 20 μM in a cell-based assay.

S6400

Glucosamine

Glucosamine (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.

S9699

Desidustat

Desidustat (ZYAN1, ZYAN1-1001), an antianaemic drug candidate, is an orally active hypoxia-inducible factor (HIF) prolyl hydroxylase (PHD) inhibitor (HIF-PHI) that stimulates erythropoiesis.

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 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.

S9656

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

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.

S2937

SYP-5

SYP-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 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.

S6684

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.

S0908

β,β-Dimethylacrylshikonin

β,β-Dimethylacrylshikonin promotes angiogenesis by inducing eNOS, VEGF and HIF-1α expression through the PI3K-dependent pathway. β,β-Dimethylacrylshikonin is a naphthoquinone derivative isolated from Arnebia nobilis.

S3589

Bendazol

Bendazol (2-Benzylbenzimidazole, Dibazol, Dibazole, Bendazole, Tromasedan) is a hypotensive drug that enhances NO synthase activity in renal glomeruli and collecting tubules. Bendazol inhibits the progression of form-deprivation myopia (FDM) and suppresses the upregulation of HIF-1α.

S5742

Deferoxamine mesylate (Ba 33112)

Deferoxamine mesylate (Ba 33112, Desferrioxamine B, DFOM, NSC 644468) 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.

S8352

PT2385

PT2385 is a HIF-2α antagonist with luciferase EC50 of 27 nM and no significant off-target activity.

S8351

PT2399

PT2399 is a potent and orally available antagonist of HIF-2 that selectively disrupts the heterodimerization of HIF-2α with HIF-1β.

S1232

M1001

M1001 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.

S2919

IOX2

IOX2 (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.

S6490

Vadadustat

Vadadustat (AKB-6548, B-506, PG-1016548) 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.

S2431

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.

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.

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 (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.

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, 2-ME2) 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.

S2410

Paeoniflorin (NSC 178886)

Paeoniflorin (NSC 178886) 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.

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.

S3233

Emetine hydrochloride

Emetine hydrochloride (NSC 33669), 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 hydrochloride inhibits cellular autophagy and has anti-malarial, anti-viral, anti-bacterial and anti-amoebic effect.

S0729

TP0463518

TP0463518 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.

S7309

BAY 87-2243

BAY 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.

S7946

KC7F2

KC7F2 is a selective HIF-1α transcription inhibitor with IC50 of 20 μM in a cell-based assay.

S6400

Glucosamine

Glucosamine (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.

S9699

Desidustat

Desidustat (ZYAN1, ZYAN1-1001), an antianaemic drug candidate, is an orally active hypoxia-inducible factor (HIF) prolyl hydroxylase (PHD) inhibitor (HIF-PHI) that stimulates erythropoiesis.

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 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.

S9656

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

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.

S2937

SYP-5

SYP-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 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.

S6684

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.

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
S0908

β,β-Dimethylacrylshikonin

β,β-Dimethylacrylshikonin promotes angiogenesis by inducing eNOS, VEGF and HIF-1α expression through the PI3K-dependent pathway. β,β-Dimethylacrylshikonin is a naphthoquinone derivative isolated from Arnebia nobilis.

S3589

Bendazol

Bendazol (2-Benzylbenzimidazole, Dibazol, Dibazole, Bendazole, Tromasedan) is a hypotensive drug that enhances NO synthase activity in renal glomeruli and collecting tubules. Bendazol inhibits the progression of form-deprivation myopia (FDM) and suppresses the upregulation of HIF-1α.

S5742

Deferoxamine mesylate (Ba 33112)

Deferoxamine mesylate (Ba 33112, Desferrioxamine B, DFOM, NSC 644468) 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, 22(9):1107-1117

2021, 12(1):647

2021, 1-14

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.

S8351

PT2399

PT2399 is a potent and orally available antagonist of HIF-2 that selectively disrupts the heterodimerization of HIF-2α with HIF-1β.

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

M1001

M1001 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, 35(3):109020

2021, 6(18)e133690

2021, 10(6)1425

S2919

IOX2

IOX2 (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.

2021, S0021-9258(21)00710-9

2020, 211:103558

2019, 29(10):3009-3018

S6490

Vadadustat

Vadadustat (AKB-6548, B-506, PG-1016548) is a novel, titratable, oral HIF-PH inhibitor.

2020, 10.1002/dta.2917

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.

2021, 12(1):647

2020, 121:105703

2019, 19(2):258-265

S2431

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.

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.

2021, 35(3):109020

2021, 10.1002/jbmr.4272

2021, 12:678354

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.

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.

2021, 35(3):109020

2020, 34(2):2344-2358

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.

2020, 34(2):2344-2358

2019, 33(11):12630-12643

2019, 317(5):F1265-F1273

S7483

DMOG

DMOG (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.

2021, 10(6)1359

2021, 13(8):11705-11726

2021, 11(1):7023

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