Modulateurs d'enzymes

Potent agonist of a1β1γ1 5′-adenosine monophosphate-activated protein kinase (AMPK). It binds to the allosteric drug and metabolite (ADaM) site at the α- and β- subunit interface of AMPK. It has potential for the treatment of diabetic nephropathy. PF 06409577 reduces infections caused by flaviviruses, mediated by changes in the metabolism of lipids in host cells.

Antagonist of Wnt signalling pathway by inhibiting the activity of Porcn, a member of the membrane-bound O-acyltransferase (MBOAT) family. Porcn is required for the palmitoylation of Wnt, mediating its secretion and signalling. Inhibits self-renewal in embryonic stem cells, whilst promoting differentiation to epiblast stem cells.

Peptide derived from the endothelial nitric oxide synthase which synthesises nitric oxide in order to protect endothelial cells from vascular diseases, atherosclerosis and thrombosis.

Inhibitor of COX-1 and COX-2 cyclooxygenases

Farnesyl pyrophosphate synthase inhibitor; hepatic de novo lipogenesis inhibitor

HMG-CoA reductase inhibitor

Tenoxicam is a non-steroidal anti-inflammatory drug that is used to reduce pain and inflammation in conditions such as arthritis. This drug works by inhibiting the enzyme cyclooxygenase or COX. As a result of this inhibition, this drug reduces the production of prostaglandins and therefore leads to a decrease in pain and inflammation. Tenoxicam 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.

Selectively inhibits α- and ζ-thrombins and elicits procoagulant effects. Reduces platelet deposition in a rat carotid endarterectomy model. Has therapeutic potential as an anti-thrombotic agent in patients with heparin-associated thrombosis.

Inhibits acetylcholinesterase (AChE); antispasmodic agent

Short acting monoamine oxidase inhibitor

Inhibits histone deacetylase (HDAC)

Acetylcholinesterase inhibitor; therapy for Alzheimer's disease

Tadalafil analogue; PDE 5 inhibitor

Imatinib is a tyrosine kinase inhibitor drug that is used for the treatment of various leukaemias, gastrointestinal stromal tumours and myeloproliferative disease. This drug inhibits the BCR-ABL tyrosine kinase and thus prevents the downstream phosphorylation of target proteins. This drug also inhibits PDGF, SCF and c-kit. Imatinib 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.

Roflumilast is a selective phosphodiesterase-4 inhibitor that is used for the treatment of exacerbations in patients with chronic obstructive pulmonary disease (COPD). It is also used to treat plaque psoriasis. This drug has anti-inflammatory and immunomodulatory effects as it aids in increasing levels of cAMP. Roflumilast 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.

γ-secretase inhibitor; reduces amyloid-β in brainÂ

Inhibitor of HMG-CoA reductase

Flavoxate is a muscarinic antagonist and spasmolytic drug that is used for the relief of conditions associatied with a lack of muscle control in the bladder such as urine urgency. This drug acts as a direct antagonist on acetylcholine receptors. This action reduces the tonus of smooth muscles in the bladder. Flavoxate 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 O-GlcNAcase and N-acetylhexosaminidases

Inhibitor of ALK1, ALK2, ALK3 and ALK6 kinases and bone morphogenetic protein (BMP) pathway. LDN 1931189 is a dorsomorphin derivative that inhibits BMP-mediated activation of Smad, Akt and p38 signalling. LDN 193189 promotes differentiation of human pluripotent cells into PAX6+ anterior neural ectoderm. In combination with basic fibroblast growth factor (FGF2), LDN 193189 promotes differentiation of mouse pluripotent stem cells into inner ear sensory epithelium.

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.

Inhibits MET, VEGFR1-3, Tie and Ron tyrosine kinases; antineoplastic

Analeptic

HIF prolyl-hydroxylase inhibitor for treatment of anaemia

Ketoprofen is a non-steroidal anti-inflammatory drug (NSAID) that has been used to treat pain and inflammation. Ketoprofen inhibits the production of inflammatory prostaglandins, which are released by platelets in response to injury or infection. The main mechanism of action is inhibition of cyclooxygenase enzymes COX 1 and COX 2 at the level of transcriptional activation. This results in decreased levels of prostaglandins that mediate pain, fever and inflammation. Ketoprofen 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.

Erlotinib is a drug that is used to treat human malignancies. It is a type of kinase inhibitor that inhibits the EGFR tyrosine kinase, preventing the activation of downstream signalling pathways. Erlotinib has been shown to be effective in treating squamous cell carcinoma, melanoma, and other types of skin cancer. Additionally, Erlotinib has potential for use as an anti-inflammatory agent in the treatment of psoriasis and ulcerative colitis. Erlotinib 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 glycogen phosphorylase and alpha-glucosidases

Vitamin B3; antioxidant; favours cell repair

Sorafenib is a drug that belongs to the class of multikinase inhibitors. It inhibits a number of kinases, including the Mcl-1 protein, which is involved in apoptosis along with blocking picolinic acid (PA), an endogenous metabolite involved in apoptosis signal transduction. Sorafenib also binds to epidermal growth factor receptor (EGFR) on the surface of cancer cells, inhibiting the production of proteins that are required for angiogenesis, thus blocking the formation of new blood vessels. Sorafenib may also inhibit P-glycoprotein (Pgp) activity. Overall, these cytotoxic effects give Sorafenib anti-tumor properties, inhibiting angiogenesis and cellular transformation, which are the two main processes of tumor growth and metastasis. Sorafenib has been shown to be effective against a range of solid tumors such as breast, prostate and lung cancers and is also used for the treatment of metastatic colorectal cancer and renal cell carcinoma. A combination therapy group found that sorafenib was more effective when used with interferon alfa-2b for the treatment of advanced renal cell carcinoma. Sorafenib also has the potential for drug interactions with other drugs that are metabolized by cytochrome P450 enzymes. Sorafenib 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.

Rebamipide is a gastroprotective agent that is used to treat various gastrointestinal disorders such as gastric ulcers and GERD. This drug’s mechanism of action is not fully understood however, it is thought to exert its effects by promoting the secretion of protective mucus in the stomach and intestine, which helps to create a barrier against stomach acid and other irritants. Additionally, it has antioxidant and anti-inflammatory properties that can help reduce tissue damage. Rebamipide 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.

DPP-4 enzyme inhibitor; anti-diabetic

Inhibitor of S-adenosylhomocysteine hydrolase that disrupts histone methylation by EZH2. Anti-proliferative in some breast cancer and invasive prostate cancer cell lines. One of four key molecules required for inducing chemical reprogramming of somatic cells into induced pluripotent stem cells (iPSC).

eV1-2 is a selective εPKC inhibitor peptide which interferes with protein-protein interactions between the ϵPKC isozyme and its anchoring protein (ϵRACK). ϵPKC and ϵRACK regulate the contraction rate of heart muscle cells and provide protection from ischemia induced cell death. ϵV1-2 is derived from the C2 domain of ϵPKC, a region important for protein-protein interactions and thus acts as a competitive inhibitor of these interactions. The C2 region is well conserved between species, but different enough from other PKC isozymes to allow for targeted inhibition (ϵV1-2 is 88% identical between sea slugs and rat ϵPKC, yet only 36% identical between rat ϵPKC and rat θ'PKC). This peptide contains a C-terminal cysteine residue for conjugation to a carrier protein.

Dasatinib is a potent inhibitor of tyrosine kinases and is used in the treatment of chronic myelogenous leukemia, gastrointestinal stromal tumors, and other types of cancer. It also inhibits many SRC- family kinases. Dasatinib has been shown to inhibit the proliferation of cancer cells, leading to cell lysis. Additionally, it has anti-angiogenic effects in vivo, inhibiting the development of new blood vessels in solid tumours. Dasatinib monohydrate 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.

Neratinib is a protein kinase inhibitor that is used in the treatment of breast cancer. This drug binds to and inhibits EGFR, HER2 and HER4. As a result of this, it prevents autophosphorylation of tyrosine residues and reduces oncogenic signalling. Neratinib 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.

Activator of SIRT1 deacetylase

Pan-ALK receptor tyrosine kinase inhibitor

A potent inhibitor of ubiquitin activating enzyme E1. Lowers ubiquitin conjugates in cells, thereby disrupting cell signalling, cell cycle progression and repair of DNA damage. Anti-tumor effects have been demonstrated in vitro and in vivo. TAK 243 has been used to study the biology of ubiquitins and its potential as anti-cancer therapy.

Racecadotril is an anti-secretory enkephalinase inhibitor that is used in the treatment of diarrhea. This drug works by inhibiting the enzyme enkephalinase. As a result of this, this drug helps to reduce excess fluid and electrolyte loss from the intestines thereby decreasing the severity of diarrhea. Racecadotril 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.

Sunitinib is a receptor tyrosine kinase inhibitor and a chemotherapeutic agent used for the treatment of renal cell carcinoma. This drug can also be used to treat gastrointestinal tumors that are resistant to imatinib. Sunitinib inhibits VEGFR1, VEGFR2, VEGFR3, PDGFR and KIT tyrosine kinases. Sunitinib malate 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 Src and Abl tyrosine kinases; anti-proliferative; anti-migratory

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 c-Met kinase

Autophagy activator that acts through targeting the ATP6V1A subunit of vATPase

Selective inhibitor of the mutated RET variant RETV804M, which is the anticipated drug-resistant RET mutant that can occur in tumours treated with kinase inhibitors. The compound has a biochemical IC50 of 0.02 µM and selectivity for purified RETV804M over purified RET and KDR of 3.7 and 110, respectively. The efficacy of the compound was shown also in cell cultures with IC50 of 4.4 µM, and cell assay selectivity for RETV804M over RET and KDR of 0.89 and 2.3, respectively.

Inhibitor of CPT1 and CPT2 enzymes; inhibitor of mTORC1 kinase; anti-fungal

Tyrosine kinase inhibitor; antineoplastic activity; pro-apoptotic

Amlexanox is an antiallergic and anti-inflammatory drug that has been shown to be effective in treating rhinitis and allergic asthma in clinical studies. It prevents the slow-reacting substance of anaphylaxis (SRS-A) from being released chemically as a mediator and may have antagonistic effects on interleukin-3. Amlexanox 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.

ATP competitive JAK2 inhibitor

Pan-class I phosphatidylinositide 3-kinase (PI3K) inhibitor (IC50 = 3, 33, 3 and 75 nM at catalytic subunits p110α, p110β, p110δ and p110γ respectively). Inhibits proliferation in several cancer cell lines, such as glioblastoma, breast and prostate cancer cells. Has synergistic anti-cancer effect in combination with MEK/ERK kinase inhibitor GDC-0973 (cobimetinib).