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
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

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.

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

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

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.

S7946

KC7F2

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

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).

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. PX-478 2HCl induces apoptosis and has anti-tumor activity. Phase 1.

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.

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.

S6490

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.

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 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.

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.

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.

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

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

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.

S7946

KC7F2

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

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).

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. PX-478 2HCl induces apoptosis and has anti-tumor activity. Phase 1.

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.

2020, 31

2020, 39(1):24

2020, 34(2):2344-2358

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.

2020, 211:103558

2019, 29(10):3009-3018

2019, 2019:4824035

S6490

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.

2020, 121:105703

2019, 19(2):258-265

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.

2020, 22;11(5):390

2020, 34(2):2344-2358

2020, 10.1016

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

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-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, 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.

2020, 20

2020, 9(3)

2020, 1;83:106438

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

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.

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