Enzyme Modulators

Phosphodiesterase inhibitor

Adefovir is an antiviral acyclic nucleoside phosphonate (ANP) analogue that works by blocking reverse transcriptase. This drug is used to treat infections associated with Hepatitis B. Adefovir dipivoxil is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready to use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Moexipril is an angiotensin converting enzyme inhibitor that is used for the treatment of hypertension. This drug is a prodrug for moexiprilat and works by relaxing the blood vessels causing them to widen and lowering blood pressure. Moexipril has been shown to be effective in treating metabolic disorders such as congestive heart failure. Moexipril HCl is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Acecelofenac is a non-steroidal anti-inflammatory drug that is used in the treatment of osteoarthritis, arthritis, and ankylosing spondylitis. This drug is also a cyclooxygenase inhibitor and works by inhibiting this enzyme so that pain and inflammation is reduced. Aceclofenac is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Amino acids 487-496 of Poly(ADP-ribose) polymerase 1 (PARP1). PARP1 is a nuclear DNA repair enzyme that binds to DNA when damage is detected. PARP1 coordinates double and single strand break repair by first cleaving NAD+ into nicotinamide and ADP-ribose, and then synthesising poly-(ADP-ribose) (PAR) chains from ADP-ribose on target proteins (PARylation). PARylation of histone proteins mediates relaxation of the chromatin and recruitment of DNA-break repair enzymes.PARP1 can also act as a transcriptional co-activator, modulating the expression of itself and many other genes by direct binding to or PARylation of enhancers and promoters. PARP1 is also involved in maintaining mtDNA.PARP1 belongs to the PARP family which has 7 known and 10 putative members. PARP1 accounts for >85% of the PARP activity in cellular systems.

Inhibitor of PDE4 enzyme

Selective and potent inhibitor of lysine acetyltransferases KAT6A and KAT6B with IC50 values in low nanomolar range. The compound is a reversible competitor of acetyl coenzyme A domain of KAT6A/B enzymes. It inhibits MYST-catalysed histone acetylation and was shown to arrest lymphoma progression in mice models. The compound opened the door to a new class of cancer therapeutics that could potentially direct the cancer cells in senescence or permanent dormancy.

Inhibits factor Xa; anti-thrombotic

Ramipril is an angiotensin-converting enzyme (ACE) inhibitor. It is used in the treatment of high blood pressure, congestive heart failure and other cardiovascular diseases. Ramipril inhibits the conversion of angiotensin I to angiotensin II by blocking ACE, which lowers blood pressure and reduces fluid retention.This product is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Inhibitor of isocitrate dehydrogenase 2

Cyclin-dependent kinase 8 (CDK8) and CDK19 inhibitor

Oseltamivir is a neuraminidase inhibitor that is used to treat influenza. It is an antiviral drug that is an inhibitor of influenza virus neuraminidase enzymes. This drug reduces viral infectivity and shedding. Oseltamivir phosphate is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Inhibitor of γ-secretase and Notch signalling

Nintedanib is an anti-inflammatory and anti-cancer drug. It is used for treatment of idiopathic pulmonary fibrosis. Nintedanib is a prodrug that is rapidly converted to the active form nintedanib, which inhibits angiogenesis by interfering with the activation of vascular endothelial growth factor receptor 1 (VEGFR1).  Nintedanib is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready to use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Binds to FK506 binding proteins (FKBPs) to form a complex that inhibits mammalian targets of rapamycin (mTOR). Blocks p70 S6 kinase activation by interleukin-2 and thereby inhibits proliferation of T cells. Induces differentiation of human pluripotent stem cells (hPSCs) to mesendoderm and blood progenitor cells.

High affinity inhibitor of glycogen synthase kinase GSK-3 with Ki of 0.6 nM. A 1070722 showed favourable characteristics for the penetration across blood brain barrier. A 1070722 was also shown to reduce the phosphorylation of microtubule-associated protein Tau.

Nafamostat is a broad-spectrum serine protease inhibitor produced by chemical synthesis. Nafamostat is effective through its antioxidant and anti-inflammatory activity. This drug is involved in inhibiting various enzyme systems such as coagulation and fibrinolytic systems. Nafamostat mesylate is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Ranolazine is a group P2 drug that reverses the pathogenic mechanism of myocardial infarction. It is used to treat chronic angina. It decreases myocardial wall tension and improves coronary blood flow. It inhibits the ryanodine receptor, which is responsible for regulating the release of intracellular calcium in cardiac and skeletal muscle cells. Furthermore, it is also effective at preventing atrial fibrillation and has been studied as monotherapy as well as in combination with other medications used to treat irregular heartbeat. Ranolazine is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Ruxolitinib is a janus tyrosine kinase inhibitor active specifically on sub-types JAK1 and JAK2 with IC50 values in the nanomolar range. JAK1 and JAK2 are kinases involved in the regulation of hematopoiesis. Clinically applied to the treatment of intermediate and high-risk myelofibrosis, ruxolitinib is usually well tolerated by patients.

Inhibitor of oxidative phosphorylation which acts on the F0F1 ATP synthase in the inner mitochondrial membrane and causes acute increase in mitochondrial membrane potential. Gboxin was shown to accumulate in mitochondria of cancer cells, to cause cellular toxicity and cell growth inhibition in mouse glioblastoma. However, Gboxin did not inhibit growth of mouse embryonic fibroblasts or neonatal astrocytes.

Inhibitor of glycogen synthase 3 (GSK-3) and cyclin-dependent kinases CDK1, CDK2 and CDK5. Kenpaullone can substitute transcription factor Klf4 in reprogramming of fibroblast to induced pluripotent stem cells when using the method of ectopic expression of transcriptional factors. In an in vitro model for Alzheimer’s disease, kenpaullone decreased production of amyloid beta peptides Aβ40 and Aβ42.

Rosuvastatin is a drug that belongs to the group of statins. It is used for the treatment of high cholesterol and as an adjunct therapy for patients with coronary heart disease. Rosuvastatin reduces serum cholesterol by inhibiting HMG-CoA reductase, which is the rate-limiting enzyme in the production of cholesterol. Furthermore, this drug has been shown to have anti-inflammatory properties, which may be due to its ability to inhibit prostaglandin synthesis. Rosuvastatin calcium is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Doxorubicin hydrochloride is an inhibitor of topoisomerase II with anti-neoplastic activity and belongs to the class of anthracyclines. It is cytotoxic, and interferes with the topoisomerase II-mediated repair of DNA causing accumulation of mutations. Doxorubicin also leads to the generation of reactive oxygen species (ROS), which further damages DNA as well as proteins and membranes. Doxorubicin is used as a chemotherapy treatment for various types of cancer, including breast cancer, lung cancer, ovarian cancer, and leukaemia. However, the compound presents with a risk of developing cardiomyopathy as well as drug resistance. Doxorubicin hydrochloride is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready to use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Inhibitor of PDE4 enzyme; anti-inflammatory

Thalidomide is a piperidinyl isoindole drug that is used to treat various cancers such as myeloma and erythema nodosum leprosum. This drug is immunosuppressive and has anti-angiogenic activity. Thalidomide’s mechanism of action is not fully understood however it is thought to block the activity of tumor necrosis factor-alpha (TNF-α). (+/-)-Thalidomide is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Ebselen is a non-toxic organoselenium compound with antioxidant, anti-inflammatory and cytoprotective properties. Ebselen is an inhibitor of lipoxygenases, nitric oxide (NO) synthases, protein kinase C, H+/K+-ATPase, thioredoxin reductase and NADPH oxidase. Recently, ebselen has been identified by several studies as a covalent inhibitor of the main protease Mpro from coronaviruses. For the SARS-CoV-2 main protease Mpro, the IC50 value is 0.67 μM and EC50 is 4.57 μM.

Lenvatinib is an anti-cancer drug that is a multi-kinase inhibitor for VEGFR1, VEGFR2 and VEGFR. It has been shown to be effective against several cancers such as thyroid cancer and is currently in clinical trials for the treatment of leukaemia and prostate cancer. Furthermore, Lenvatinib also inhibits the activity of other protein kinases, including those involved in inflammatory responses. Lenvatinib mesylate is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

5-Fluorouracil is a cytotoxic drug that inhibits the synthesis of DNA. It is used in combination therapy to treat cancer and is a pyrimidine analog. This drug inhibits the formation of thymidylate synthase from uracil. As a result, this leads to DNA and RNA synthesis inhibition and cell death. 5-Fluorouracil is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Protein kinase B (also known as RAC-alpha serine/threonine-protein kinase: Atk) is a serum and glucocorticoid-regulated protein kinase with three highly homologous isoforms (Akt1, 2 and 3). Akt1 and Akt3 are the predominant isoforms expressed in the brain, whereas Akt2 is mainly expressed in skeletal muscle and embryonic brown fat. These proteins play major regulatory roles in a range of physiological processes including: growth, proliferation, cell survival, angiogenesis, metabolism and Akt is also considered a proto-oncogene.This peptide (AKTide) is a selective substrate for these kinases and enables quick, easy and sensitive assays of Akt activity.

Inhibitor of HMG-CoA reductase

A potent and selective inhibitor of cell death-inducing kinase RIP2 (IC50 = 5 nM). Reduces release of pro-inflammatory cytokines. Inhibits production of TNF-α and IL-6 in intestinal explants from patients with Crohn's disease and ulcerative colitis.

Multi-kinase inhibitor; inhibits epoxide hydrolase; antineoplastic

Fosinopril belongs to the angiotensin-converting enzyme (ACE) inhibitor class of drugs, which prevents the conversion of angiotensin I to angiotensin II. This leads to decreases in blood pressure and slows down the progression of kidney disease, hypertension and heart failure. Fosinopril sodium salt is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Inhibitor of EGFR (ErbB1) and HER2 (ErbB2) receptor tyrosine kinases. Used for sensitization of HER2-overexpressing cancer cells to radiation as well as chemotherapy to tamoxifen- and trastuzumab-resistant cell lines. The compound blocks signalling via Akt and mitogen-activated protein kinase (MAPK) pathways leading to reduced cell survival. In trastuzumab resistant cancer cells, it inhibits HER2 phosphorylation, prevents receptor ubiquitination and causes accumulation of inactive HER2 dimers on the cell surface.

Inhibitor of tyrosinase in melanocytes: skin whitener

Potent inhibitor of histone deacetylase 6 (HDAC6), inducing elevated levels of acetylated α-tubulin. It inhibits pro-inflammatory cytokines TNF-α and IL-6 as well as nitric oxide secretion in human and murine macrophages. It is not neurotoxic and it rescues cognitive impairment in mice model for Alzheimer’s disease.

Cobicistat is an inhibitor of human cytochrome P450 3A enzymes (CYP) with no antiviral activity. Cobicistat is used in the treatment of HIV-1 infection, as an alternative to ritonavir, to increase the half-life of antiviral medications (von Hentig, 2016). Cobicistat acts as a booster by selectively inhibiting the hepatic degradation of the drugs, for example, in the pharmacological regime against HIV-1, which often includes protease inhibitors, such as, darunavir, atazanavir, and lopinavir, or the integrase inhibitor elvitegravir (Deeks, 2014).

Inhibitor of HIF-prolyl hydroxylase isozymes PHD1, PHD2 and PHD3 with Ki in nanomolar range. The compound mimics the binding of N-oxalylglycine, chelates catalytic iron and prevents substrate entry into catalytic site. Inhibition of PHD enzymes leads to stabilization of hypoxia-induced factors HIF1α and HIF2α, followed by the production of erythropoietin (EPO).

Gemcitabine is as a synthetic pyrimidine nucleoside prodrug. The hydrogen atoms on the 2' carbon of deoxycytidine are replaced by fluorine atoms. Gemcitabine works by being incorporated into the DNA of cancer cells during replication and inhibiting DNA synthesis. First gemcitabine is converted into its active form, gemcitabine triphosphate, by cellular enzymes including deoxycytidine kinase (DCK), after it is taken up by cancer cells. The gemcitabine triphosphate interferes with the normal functioning of the enzymes involved in replicating DNA, leading to the termination of DNA synthesis and ultimately, cell death. Gemcitabine is used as a chemotherapy drug used to treat various types of cancer, including pancreatic, lung, breast, and ovarian cancer. Gemcitabine is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready to use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Inhibitor of pan-Raf kinases

Inhibitor of Rho-kinases

Anti-rheumatic; immunosuppressant; neuroprotective; neuroregenerative

Inhibitor of FLT3 receptor tyrosine kinases; anti-neoplastic

Inhibitor of aurora kinases

Potent and selective MAP/ERK kinase 1/2 inhibitor. Reduces growth of tumor cells with B-Raf and Ras mutations. Tumor regression observed after chronic treatment in in vivo xenograft models. Enhances anti-tumor effect in combination with irinotecan or docetaxel.

Inhibitor of fibroblast growth factor receptors (FGFR1, FGFR2 and FGFR3). Demonstrated anti-tumor effects in pre-clinical models of FGFR-driven tumors. AZD 4547 resulted in tumor progression when applied on a patient-derived model of FGFR1-amplified squamous cell lung disease. Antineoplastic effects also observed in FGFR2-amplified gastric cancer.

(S)-Mephenytoin is a substrate of cytochrome P450 enzyme CYP2C19 (a hydroxylase). It is an effective anticonvulsant that improves control of seizures in patients. According to studies, the drug exhibits a genetic polymorphism in CYP2C19 that results in reduced metabolism in some individuals.  (S)-Mephenytoin is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

O6-Benzylguanine is a guanine analog that is an antineoplastic agent. It works by acting as a suicide inhibitor of the enzyme O6-alkylguanine-DNA alkyltransferase. This results to an interruption of DNA repair so that damage can occur to local tumor targets. O6-Benzylguanine is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Dorzolamide is a carbonic anhydrase inhibitor agent that is used to treat eye disorders such as glaucoma and ocular hypertension. Dorzolamide decreases intraocular pressure by blocking the activity of aqueous humor outflow. Dorzolamide HCl is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Inhibits proto-oncogene Pim kinases (Pim-1, Pim-2 and Pim-3); antineoplastic