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Results for "

Ph Inhibitors

" in MCE Product Catalog:

49

Inhibitors & Agonists

3

Biochemical Assay Reagents

2

Peptides

3

Isotope-Labeled Compounds

Targets Recommended: HIF/HIF Prolyl-Hydroxylase
Cat. No. Product Name Target Research Areas
  • HY-10499
    PH-064

    BIM-46187

    Others Neurological Disease
    PH-064 (BIM-46187) is an inhibitor of heterotrimeric G-protein complex.
  • HY-112798
    PH-002

    Others Neurological Disease
    PH-002 is an inhibitor of apolipoprotein (apo) E4 intramolecular domain interaction in neuronal cells that could rescue impairments of mitochondrial motility and neurite outgrowth.
  • HY-19548A
    BEC hydrochloride

    Arginase Metabolic Disease
    BEC hydrochloride is a slow-binding and competitive Arginase II inhibitor with Ki of 0.31 μM and 30 nM at pH 7.5 and pH 9.5, respectively.
  • HY-100230A
    ML133 hydrochloride

    Potassium Channel Others
    ML133 hydrochloride is a selective Kir2 family channels inhibitor, with an IC50 of 1.8 μM at pH 7.4 and 290 nM at pH 8.5.
  • HY-145616
    Sudocetaxel

    Microtubule/Tubulin Cancer
    Sudocetaxel is a microtubule depolymerization inhibitor for pH-sensitive docetaxel delivery.
  • HY-126193
    JS-K

    NO Synthase Apoptosis Cancer
    JS-K is a NO donor that reacts with glutathione to generate NO at physiological pH. JS-K inhibits proliferation, induces apoptosis, and disrupts the cell cycle of Jurkat T acute lymphoblastic leukemia cells.
  • HY-10403
    PH-797804

    p38 MAPK Autophagy Inflammation/Immunology Cancer
    PH-797804 is a ATP-competitive, selective p38α/p38β inhibitor (IC50=26 nM and Ki=5.8 nM for p38α; Ki=40 nM for p38β) and does not inhibit JNK2.
  • HY-132588
    Lumasiran

    ALN-G01

    Others Metabolic Disease
    Lumasiran (ALN-G01), a siRNA product, reduces hepatic oxalate production by targeting glycolate oxidase. By silencing the gene encoding glycolate oxidase, Lumasiran depletes glycolate oxidase and thereby inhibits the synthesis of oxalate, which is the toxic metabolite that is directly associated with the clinical manifestations of Primary hyperoxaluria type 1 (PH1).
  • HY-12063
    PHT-427

    Akt Apoptosis Cancer
    PHT-247 is an inhibitor of the pleckstrin homology (PH) domain of Akt, and it is also an inhibitor of PDPK1 with Kis of 2.7 µM and 5.2 µM and for Akt and PDPK1, respectively.
  • HY-17608
    Daprodustat

    GSK1278863

    HIF/HIF Prolyl-Hydroxylase Cardiovascular Disease
    Daprodustat (GSK1278863) is an orally active hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor being developed for the treatment of anemia associated with chronic kidney disease.
  • HY-Y1269
    Ammonium chloride

    Autophagy Cancer
    Ammonium chloride, as a heteropolar compound with pH value regulation, can cause intracellular alkalization and metabolic acidosis thus effecting enzymatic activity and influencing the process of biological system. Ammonium chloride is an autophagy inhibitor.
  • HY-145391
    Triperiden

    Influenza Virus Infection
    Triperiden is an inhibitor of influenza virus multiplication. Triperiden targets the haemagglutinin of fowl plague virus (FPV) for antiviral activity and acts by inhibiting the conformational change in the haemagglutinin at acid pH. Triperiden is also anticholinergic anti-parkinsonism drug.
  • HY-12654
    Molidustat

    BAY 85-3934

    HIF/HIF Prolyl-Hydroxylase Cardiovascular Disease
    Molidustat (BAY 85-3934) is a novel inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) with mean IC50 values of 480 nM for PHD1, 280 nM for PHD2, and 450 nM for PHD3.
  • HY-18749
    SC79

    Akt Cancer Inflammation/Immunology Neurological Disease
    SC79, a unique specific and BBB permeable Akt activator, activates Akt in the cytosol and inhibits Akt membrane translocation. SC79 specifically binds to the PH domain of Akt.
  • HY-101277
    Vadadustat

    PG-1016548; AKB-6548

    HIF/HIF Prolyl-Hydroxylase Cardiovascular Disease
    Vadadustat (PG-1016548) is a titratable, oral hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor. Vadadustat is an erythropoiesis-stimulating agent and has the potential for anemia treatment in chronic kidney disease in vivo.
  • HY-15529
    S0859

    Na+/HCO3- Cotransporter Cardiovascular Disease
    S0859 is a selective, high-affinity generic Na +/HCO3 - transporter (NBC) inhibitor. S0859 reversibly inhibits NBC-mediated intracellular pH (pHi) recovery (Ki=1.7 μM, full inhibition at approximately 30 μM).
  • HY-P0224
    N-Formyl-Met-Leu-Phe

    fMLP; N-Formyl-MLF

    TNF Receptor Inflammation/Immunology
    N-Formyl-Met-Leu-Phe (fMLP; N-Formyl-MLF) is a chemotactic peptide and a specific ligand of N-formyl peptide receptor (FPR). N-Formyl-Met-Leu-Ph is reported to inhibit TNF-alpha secretion.
  • HY-14179
    PPQ-102

    CFTR Inhibitor

    CFTR Others
    PPQ-102 (CFTR Inhibitor) is a reversible CFTR inhibitor that completely inhibits CFTR chloride currents (IC50 ~90 nM). PPQ-102 is not affected by membrane potential-dependent cell allocation or blocking efficiency (uncharged at physiological pH) and effectively prevents cyst enlargement in polycystic kidney disease.
  • HY-129457
    FINO2

    Ferroptosis Cancer
    FINO2 is a potent ferroptosis inducer. FINO2 inhibits GPX4 activity. FINO2 is a stable oxidant that oxidizes ferrous iron and stable at varying pH levels. FINO2 causes widespread lipid peroxidation.
  • HY-111549
    Bragsin1

    Others Cancer
    Bragsin1 is a potent, selective and noncompetitive inhibitor of the ArfGEF BRAG2, inhibits Arf GTPase activation, with an IC50 of 3 μM. Bragsin1 binds to PH domain of BRAG2, and is a noncompetitive interfacial inhibitor. Bragsin1 has no effect on the Sec7 domain of human ArfGEFs. Anti-cancer activity.
  • HY-15369
    FPA-124

    Akt Apoptosis Cancer
    FPA-124, a cell-permeable copper complex, is a selective Akt inhibitor with an IC50 of 0.1 μM. FPA-124 interacts with both the pleckstrin homology (PH) and the kinase domains of Akt. FPA-124 induces apoptosis.
  • HY-114174
    Fmoc-Ala-Glu-Asn-Lys-NH2

    Amyloid-β Neurological Disease
    Fmoc-Ala-Glu-Asn-Lys-NH2 is a selective asparagine endopeptidase (AEP) inhibitor peptide and suppresses amyloid precursor protein (APP) cleavage. AEP, a pH-controlled cysteine proteinase, is activated during ageing and mediates APP proteolytic processing.
  • HY-W009245
    Bz-RS-iSer(3-Ph)-OMe

    HIV Infection
    Bz-RS-iSer(3-Ph)-OMe (compound 2), a Taxol derivative, inhibits HSV replication cycle at low cytotoxicity, blocks mitotic divisions of Vero cells, influences M-MSV induced tumor size and affects immune response by inhibiting PHA-induced T lymphocyte proliferation.
  • HY-147414
    Vamotinib

    PF-114

    c-Met/HGFR Cancer
    Vamotinib (PF-114) is a potent, selective and orally active tyrosine kinase inhibitor. Vamotinib inhibits the autophosphorylation of BCR/ABL and BCR/ABL-T315I. Vamotinib induces apoptosis. Vamotinib shows anti-proliferative and anti-tumor activity. Vamotinib has the potential for the research of resistant philadelphia chromosome-positive (Ph+) leukemia.
  • HY-17507
    Pantoprazole

    BY1023; SKF96022

    Proton Pump Autophagy Apoptosis Cancer Inflammation/Immunology
    Pantoprazole (BY10232) is an orally active and potent proton pump inhibitor (PPI). Pantoprazole, a substituted benzimidazole, is a potent H +/K +-ATPase inhibitor with an IC50 of 6.8 μM. Pantoprazole improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole significantly increased tumor growth delay combined with Doxorubicin (HY-15142).
  • HY-17507B
    Pantoprazole sodium hydrate

    BY1023 sodium hydrate; SKF96022 sodium hydrate

    Proton Pump Autophagy Apoptosis Cancer Inflammation/Immunology
    Pantoprazole sodium hydrate (BY10232 sodium hydrate) is an orally active and potent proton pump inhibitor (PPI). Pantoprazole sodium hydrate, a substituted benzimidazole, is a potent H +/K +-ATPase inhibitor with an IC50 of 6.8 μM. Pantoprazole sodium hydrate improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole sodium hydrate significantly increased tumor growth delay combined with Doxorubicin (HY-15142).
  • HY-128590
    PHT-7.3

    Ras Cancer
    PHT-7.3 is a selective inhibitor of connector enhancer of kinase suppressor of Ras 1 (Cnk1) pleckstrin homology (PH) domain (Kd=4.7 μM). PHT-7.3 inhibits mut-KRas, but not wild-type KRas cancer cell and tumor growth and signaling. PHT-7.3 has antitumor activity.
  • HY-17507A
    Pantoprazole sodium

    BY1023 sodium; SKF96022 sodium

    Proton Pump Autophagy Apoptosis Cancer Inflammation/Immunology
    Pantoprazole sodium (BY10232 sodium) is an orally active and potent proton pump inhibitor (PPI). Pantoprazole sodium, a substituted benzimidazole, is a potent H +/K +-ATPase inhibitor with an IC50 of 6.8 μM. Pantoprazole sodium improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole sodium significantly increased tumor growth delay combined with Doxorubicin (HY-15142).
  • HY-15295
    Vonoprazan Fumarate

    TAK-438

    Proton Pump Metabolic Disease
    Vonoprazan Fumarate (TAK-438), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan Fumarate inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan Fumarate is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease.
  • HY-110077
    API-1

    Akt Apoptosis Cancer
    API-1, a potent Akt/PKB inhibitor, binds to the PH domain and inhibits Akt membrane translocation. API-1 efficiently reduces the phosphorylation levels of Akt with an IC50 of ∼0.8 μM. API-1 is selective for PKB and does not inhibit the activation of PKC, and PKA. API-1 also induces apoptosis by synergizing with TNF-related apoptosis-inducing ligand (TRAIL).
  • HY-D0861A
    EGTA tetrasodium

    Others Inflammation/Immunology
    EGTA tetrasodium is a specific calcium ion chelator. EGTA tetrasodium has an apparent calcium dissociation constant (Kd) of 60.5 nM at physiological pH (7.4) and has very high specificity for Ca 2+ over Mg 2+ (Mg 2+ Kd 1-10 mM). EGTA tetrasodium significantly inhibits the substrate adherence capacity of inflammatory macrophages.
  • HY-111550
    Bragsin2

    Others Cancer
    Bragsin2 is a potent, selective and noncompetitive nucleotide exchange factor BRAG2 inhibitor, with an IC50 of 3 μM. Bragsin2 binds at the interface between the PH domain of BRAG2 and the lipid bilayer, leads BRAG2 unable to activate lipidated Arf GTPase. Bragsin2 affects breast cancer stem cells.
  • HY-100007A
    Vonoprazan hydrochloride

    TAK-438 hydrochloride

    Proton Pump Bacterial Infection Endocrinology
    Vonoprazan hydrochloride, a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan hydrochloride inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan hydrochloride is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease. Vonoprazan hydrochloride can be used for eradication of Helicobacter pylori.
  • HY-124473
    Naphthofluorescein

    NaPhthafluorescein

    HIF/HIF Prolyl-Hydroxylase Cancer
    Naphthofluorescein inhibits the interaction between HIF-1 and Mint3. Naphthofluorescein suppresses Mint3-dependent HIF-1 activity and glycolysis in cancer cells and macrophages without cytotoxicity in vitro and adverse effect in vivo. Naphthofluorescein is also a fluorescent pH-sensitive probe that can be used for functional Cerenkov imaging.
  • HY-108460
    A-784168

    TRP Channel Neurological Disease
    A-784168 is a potent and orally active inhibitor of vanilloid receptor type 1 (TRPV1). Vanilloid receptor type 1 (TRPV1) is a ligand-gated nonselective cation channel that is considered to be an important integrator of various pain stimuli such as endogenous lipids, capsaicin, heat, and low pH. A-784168 has good CNS penetration.
  • HY-50868
    Bafetinib

    INNO-406; NS-187

    Bcr-Abl Src Apoptosis Cancer
    Bafetinib is a potent and orally active Lyn/Bcr-Abl tyrosine kinase inhibitor. Bafetinib augments the activities of several proapoptotic Bcl-2 homology (BH)3-only proteins (Bim, Bad, Bmf and Bik) and induces apoptosis in Ph + leukemia cells via Bcl-2 family-regulated intrinsic apoptosis pathway.
  • HY-128943
    MAC glucuronide phenol-linked SN-38

    Drug-Linker Conjugates for ADC Cancer
    MAC glucuronide phenol-linked SN-38 is a pH-susceptible lactone MAC glucuronide phenol-linked SN-38 (DNA topoisomerase I inhibitor) drug linker. MAC glucuronide phenol-linked SN-38 is cytotoxic across L540cy cells and Ramos cells with IC50 values of 113 and 67 ng/mL, respectively.
  • HY-17507S
    Pantoprazole-d6

    BY1023-d6; SKF96022-d6

    Proton Pump Autophagy Apoptosis Cancer Inflammation/Immunology
    Pantoprazole-d6 is deuterium labeled Pantoprazole. Pantoprazole (BY10232) is an orally active and potent proton pump inhibitor (PPI). Pantoprazole, a substituted benzimidazole, is a potent H+/K+-ATPase inhibitor with an IC50 of 6.8 μM. Pantoprazole improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole significantly increased tumor growth delay combined with Doxorubicin (HY-15142).
  • HY-17507S1
    Pantoprazole-d3

    BY1023-d3; SKF96022-d3

    Proton Pump Autophagy Apoptosis Cancer Inflammation/Immunology
    Pantoprazole-d3 is deuterium labeled Pantoprazole. Pantoprazole (BY10232) is an orally active and potent proton pump inhibitor (PPI). Pantoprazole, a substituted benzimidazole, is a potent H+/K+-ATPase inhibitor with an IC50 of 6.8 μM. Pantoprazole improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole significantly increased tumor growth delay combined with Doxorubicin (HY-15142).
  • HY-15893
    DMOG

    Dimethyloxallyl Glycine

    HIF/HIF Prolyl-Hydroxylase Autophagy Cancer
    DMOG (Dimethyloxallyl Glycine) is a cell permeable and competitive inhibitor of HIF-PH, which results in HIF-1α stabilisation and accmulation in vitro and in vivo. DMOG is an α-ketoglutarate analogue and inhibits α-KG-dependent hydroxylases. DMOG acts as a pro-angiogenic agent and plays a protective role in experimental model of colitis and diarrhoea via HIF-1 related signal. DMOG induces cell autophagy.
  • HY-100007
    Vonoprazan

    TAK-438 free base

    Proton Pump Bacterial Endocrinology
    Vonoprazan (TAK-438 free base), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease. Vonoprazan can be used for eradication of Helicobacter pylori.
  • HY-12914
    V116517

    TRP Channel Inflammation/Immunology Neurological Disease
    V116517 is a potent, orally active transient receptor potential vanilloid (TRPV1) antagonist. V116517 shows potent activity in inhibiting both capsaicin (CAP)- and acid (pH 5)-induced currents in rat DRG neurons expressing native TRPV (IC50=423.2 nM for CAP; IC50=180.3 nM for acid). V116517 can be used for the research of pain.
  • HY-14818
    Laninamivir

    R 125489

    Influenza Virus Infection
    Laninamivir (R 125489) is a potent influenza neuraminidase (NA) inhibitor with IC50s of 0.90 nM, 1.83 nM and 3.12 nM for avian H12N5 NA (N5), pH1N1 N1 NA (p09N1) and A/RI/5+/1957 H2N2 N2 (p57N2), respectively.
  • HY-128067
    5-(N,N-Hexamethylene)-amiloride

    Hexamethylene amiloride; HMA

    Sodium Channel HIV Apoptosis Cancer Infection
    5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) derives from an amiloride and is a potent Na +/H + exchanger inhibitor, which decreases the intracellular pH (pHi) and induces apoptosis in leukemic cells. 5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) is also an inhibitor of the HIV-1 Vpu virus ion channel and inhibits mouse hepatitis virus (MHV) replication and human coronavirus 229E (HCoV229E) replication in cultured L929 cells with EC50s of 3.91 μM and 1.34 μM, respectively.
  • HY-N0316
    Mollugin

    NF-κB Reactive Oxygen Species Apoptosis VEGFR c-Myc Cancer
    Mollugin is an orally active and potent NF-κB inhibitor. Mollugin induces S-phase arrest of HepG2 cells, and increased intracellular reactive oxygen species (ROS) levels. Mollugin induces DNA damage in HepG2 cells, as well as an increase in the expression of p-H2AX. Mollugin shows anti-cancer effect by inhibiting TNF-α-induced NF-κB activation. Mollugin enhances the osteogenic action of BMP-2 (bone morphogenetic protein 2) via the p38-Smad signaling pathway.
  • HY-18071A
    BI-9627 hydrochloride

    Na+/H+ Exchanger (NHE) Cardiovascular Disease
    BI-9627 hydrochloride is potent sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor, with IC50s of 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays, respectively. BI-9627 hydrochloride displays >30-fold selectivity against NHE2 and with no measurable inhibitory activity against the NHE3 isoform. BI-9627 hydrochloride shows low DDI (drug-drug interaction) potential, excellent pharmacokinetics in rat and dog, and remarkably potent activity in the isolated heart model of ischemia-reperfusion injury.
  • HY-14818S
    Laninamivir-d3

    Influenza Virus Infection
    Laninamivir-d3 (R 125489-d3) is the deuterium labeled Laninamivir. Laninamivir (R 125489) is a potent influenza neuraminidase (NA) inhibitor with IC50s of 0.90 nM, 1.83 nM and 3.12 nM for avian H12N5 NA (N5), pH1N1 N1 NA (p09N1) and A/RI/5+/1957 H2N2 N2 (p57N2), respectively.
  • HY-18071
    BI-9627

    Na+/H+ Exchanger (NHE) Cardiovascular Disease
    BI-9627 is potent sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor, with IC50s of 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays, respectively. BI-9627 displays >30-fold selectivity against NHE2 and with no measurable inhibitory activity against the NHE3 isoform. BI-9627 shows low DDI (drug-drug interaction) potential, excellent pharmacokinetics in rat and dog, and remarkably potent activity in the isolated heart model of ischemia-reperfusion injury.
  • HY-128946
    CL2A-SN-38

    Drug-Linker Conjugates for ADC Cancer Inflammation/Immunology
    CL2A-SN-38 is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody drug conjugate (ADC). CL2A-SN-38 provides significant and specific antitumor effects against a range of human solid tumor types. CL2A is a nonclaevable complicated PEG8- and triazole-containing PABC-peptide-mc linker. CL2A is cleavable through pH sensitivity, giving rise to bystander effect, and binds the antibody at a cysteine residue via a disulfide bond.