Enzyme Modulators

Inhibitor of lipoprotein-associated phospholipase A2

Cyclooxygenase inhibitor; NSAID; an opthalmic analgesic

Dipeptidyl peptidase 4 (DPP4) inhibitor

Inhibitor of Polo-like kinase 1

Receptor tyrosine kinase inhibitor; anti-angiogenesis; anti-oncogenesis

Aminoglutethimide is an adrenocortical steroid synthesis inhibitor that is used for the treatment of Cushing’s syndrome. This drug is an aromatase inhibitor that blocks the production of adrenal steroids. Also, this drug blocks the conversion of androgens to estrogens. Aminoglutethimide has been studied for the treatment of cancers such as breast and prostate. Aminoglutethimide 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.

TPPB is a small molecule inhibitor, which is synthetically derived for targeted biochemical studies. It functions by selectively modulating G-protein-coupled receptor (GPCR) signaling pathways through the inhibition of specific protein-protein interactions. This mode of action makes TPPB an insightful tool for dissecting the complex mechanisms by which G-proteins relay extracellular signals to intracellular responses. In scientific research, TPPB is employed primarily for the investigation of signal transduction processes, particularly those involving the modulation of G-protein activities. Its ability to selectively inhibit certain pathways allows researchers to parse out individual signaling components and understand their roles in physiological and pathological processes. TPPB’s specificity has made it a valuable probe in pharmacological studies aiming to elucidate the intricacies of GPCR function and its implications in various diseases, providing insights that could potentially inform therapeutic strategies.

Lapatinib is an antineoplastic agent used to treat breast and lung cancer. This drug is also a tyrosine kinase inhibitor and inhibits human epidermal growth factor receptor type 2 (HER2/ERBB2) and epidermal growth factor receptor (HER1/EGFR/ERBB1). Lapatinib has shown to inhibit ERBB-driven tumor cell growth in vitro and in various animal models. Lapatinib base 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.

Selective inhibitor of the transforming growth factor beta receptor TGFβ1. RepSox can replace Sox, a transcriptional factor required for cell self-renewal, in reprogramming of adult cells to induced pluripotent stem cells (iPSCs). In the cloned interspecies embryos, RepSox induced expression of pluripotency regulatory genes Oct4 and Nanog, improved viability and developmental potential of embryos in the pre-implantation stage.

A potent inhibitor of phosphodiesterase type 9 (PDE9) tested in human and murine in vitro assays (IC50 values: 55 nM and 100 nM respectively). BAY 73-6691 induces long-term potentiation and improves memory in rodents. Has therapeutic potential for Alzheimer’s disease.

Inhibitor of VEGF receptors

Inhibitor of PDE4 enzyme; anti-inflammatory

Inhibits YAP/Tead transcriptional activity. Has anti-tumour effects on oesophageal adenocarcinoma with therapeutic potential in combination with 5-FU. Involved in ferroptosis, mediated by iron-dependent ROS.

Inhibitor of B-Raf mutant (V600E); anti-neoplastic

A reversible inhibitor of IGF-1R kinase and insulin receptor. Has anti-growth effects in mesenchymal, epithelial and hematopoietic tumor types. Synergistic with other cytotoxic, hormonal and targeted anti-cancer therapy.

Doxycycline is a tetracycline antibiotic that is used to treat a range of bacterial infections. It is a broad-spectrum antibiotic. This drug inhibits bacterial protein synthesis by binding to its 30S prokaryotic ribosomal subunit. It also inhibits the production of essential proteins required for the bacterial to survive. Doxycycline hyclate 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.

Phosphodiesterase 5 inhibitor; anti-impotence drug

Sildenafil is a potent inhibitor of cyclic guanosine monophosphate (cGMP) specific phosphodiesterase type 5 (PDE5), consequently preventing the degradation of cGMP in the smooth muscle cells of the pulmonary vasculature and penis. For this reason Sildenafil can be used to increase blood flow, decrease inflammation and mucus production in the lungs and also can be used in the treatment of erectile dysfunction in men. This is largely due to the increased availability of cGMP which can cause the relaxation of the smooth muscles to be prolonged. Sildenafil 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.

CBP/p300 histone acetyltransferase activator

Brinzolamide is a carbonic anhydrase inhibitor this is used for the treatment of ocular hypertension and glaucoma. Inhibition of carbonic anhydrase slows the formation of bicarbonate ions and as a result of this, it slows fluid flow in the eye, lowering the intraocular pressure. It has a high lipophilicity to enable diffusion across the blood-retinal barrier. Brinzolamide 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.

Rapamycin is a macrolide antibiotic that has been studied as a potential anticancer agent. It binds to FK506 binding proteins (FKBPs) to form a complex that inhibits mammalian targets of rapamycin (mTOR). Rapamycin also blocks p70 S6 kinase activation by interleukin-2 and thereby inhibits proliferation of T cells. It induces differentiation of human pluripotent stem cells (hPSCs) to mesendoderm and blood progenitor cells. Rapamycin - Bio-X ™ 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.

Nicotinamide is a form of vitamin B that is found in food and it used to treat many conditions such as pellagra and acne. It replenishes cellular energy and has anti-inflammatory effects. Nicotinamide is an inhibitor of the enzyme SIRT1 in vitro but can be a stimulator in cells. Nicotinamide 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.

Glutamine analogue and antagonist of glutamine-dependent amidotransferases, with antibiotic and antifungal properties. Inhibits purine biosynthesis, FGAM synthetase and glucosamine-6-phosphate isomerase that contributes to its antineoplastic property. Azaserine can also act as a carcinogen, by inducing DNA carboxymethylation. Protects endothelial cells from inflammation under hyperglycemic conditions, via antioxidant mechanisms, independent of hexosamine biosynthetic pathway.

Pomalidomide is an immunomodulatory agent that inhibits transcriptional regulation by interacting with the pomalidomide-binding protein, which prevents its interaction with RNA polymerase II and thereby prevents DNA transcription. The study with U266 cells demonstrated that pomalidomide targets CRBN, part of an E3 ligase complex, and inhibits its autoubiquinitation and supresses a critical gene (IRF4, interferon regulatory factor 4) for myeloma cell growth with concentrations up to 10 μM.In vitro assays have shown that pomalidomide has inhibitory effects on cell signaling pathways, such as the NF-κB pathway. Pomalidomide also decreases the production of proinflammatory cytokines, such as TNFα and IL-1β, by inhibiting their synthesis or their release from activated monocytes. Recently, the promoting effect of pomalidomide, as its analog lenalidomide, on erythropoiesis (production of red blood cells) has been investigated, demonstrating positive results for its use as a potential new therapy agent for β-hemoglobinopathies.

Decitabine is a synthetic cytosine analogue that incorporates into DNA and prevents DNA methylation via DNA (cytosine-5)-methyltransferase 1 (DNMT1) inhibition. It has demonstrated potent anti-leukaemic effects attributed to cell cycle arrest and induction of apoptosis. Also, it has anti-growth effects on solid tumor cell lines. Decitabine 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.

Zorubicin hydrochloride is an anthracycline antibiotic, which is a derivative of daunorubicin, sourced from Streptomyces bacteria. This compound exhibits its mode of action primarily through intercalation into DNA, inhibiting the progression of the enzyme topoisomerase II. This interference prevents DNA replication and RNA synthesis, leading to apoptosis in rapidly dividing cells, making it a potent chemotherapeutic agent. The primary use of Zorubicin hydrochloride is in oncological settings, particularly for the treatment of various cancers, including leukemias and solid tumors. Its efficacy is linked to its ability to intercalate into cellular DNA, which disrupts the proliferation of malignant cells. Researchers may focus on its pharmacokinetics and the development of resistance mechanisms in cancer cells. With its roots in microbial biochemistry, Zorubicin hydrochloride continues to be a subject of study for its cytotoxic properties and potential as a treatment option in multi-drug chemotherapy regimens.

Allosteric activator of AMP-activated protein kinase (AMPK) acting on the AMPK-β subunit with therapeutic potential in metabolic disorders such as diabetes, obesity, etc. A769662 also blocks the differentiation of mouse embryonic stem cells (mESCs) and maintains the mESCs in naïve state even in the absence of leukemia inhibitory factor (2i/L).

Inhibitor of NPM-ALK kinase

H-FERQHM-OH peptide, corresponding to RNase A 8-13 (Chain A of bovine pancreatic ribonuclease) is a non-amyloidogenic peptide, that can be used as a negative control in amyloid formation experiments together with CRB1001320.

Inhibits p38 MAP kinase; anti-inflammatory; neuroprotective

Please enquire for more information about 5-Fluoro-1-(tetrahydro-2-furyl)uracil including the price, delivery time and more detailed product information at the technical inquiry form on this page

ATP-competitive inhibitor of Met and VEGFR2

Thymidylate synthase inhibitor

Inhibitor of ADAM10 metalloprotease

Inhibits MEK1 and MEK2 kinases; targeted therapy for melanoma

During extraction of lecithin from egg yolk, peptide by-products can be isolated and purified by gel filtration. Within the by-products this has led to the discovery of biologically active value-added products. The egg yolk gel filtration (EFGF) fractions were analysed for their antioxidant and angiotensin converting enzyme (ACE) inhibitory activities. EYGF-33 predominantly contained 3 peptides - KLSDW, YPSPV, and MPVHTDAD). KLSDW in EYGF-33 was found to have strong antioxidant activity linked to the presence of the tryptophan residue. KLSDW had nearly comparable activity to the synthetic antioxidant BHA. KLSDW did not show any notable angiotensin converting enzyme (ACE) inhibitory activity.

Rigosertib sodium is an experimental chemotherapeutic agent that is a derivative of benzyl styryl sulfone. It is synthesized chemically and functions primarily by inhibiting key signaling pathways involved in cancer cell proliferation. Specifically, Rigosertib targets the RAS signaling pathway along with the phosphatidylinositol-3-kinase/AKT and polo-like kinase 1 (Plk1) pathways, impeding the progression of the cell cycle and inducing apoptosis in malignant cells. Rigosertib sodium is under investigation for its potential application in treating hematological malignancies and solid tumors, particularly myelodysplastic syndromes (MDS) and pancreatic cancer. By targeting multiple pathways that are typically upregulated in cancer cells, Rigosertib offers a mechanism by which cancer growth may be curtailed, providing a promising strategy for therapeutic intervention. Although primarily studied in the laboratory and clinical trial settings, ongoing research aims to elucidate its efficacy and safety profile, with hopes of integrating it into standard cancer treatment regimens upon successful validation.

Histone acetyltransferase inhibitor of p300/CBP; anti-proliferative

Inhibitor of ERK1 and ERK2 serine/threonine kinases

AMARA peptide is a fragment containing the phosphorylation site for AMP activated protein kinase (AMPK) and is a substrate for all AMPK subfamily kinases. As such it is used to measure AMPK related kinase activity.

Inhibitor of dihydroorotate dehydrogenase; anti-inflammatory; immunomodulatory

Inhibitor of glutaminase; glutamine analogue

NADPH oxidase inhibitor; anti-inflammatory

Inhibitor of mutant B-rafV600E protein that results in decreased proliferation of cancer cells with this mutation. Treatment of metastatic melanoma in patients harboring the V600E mutation, had improved disease outcome. This antitumor activity is enhanced when combined with MEK inhibitor trametinib.

Nociceptin/orphanin FQ peptide receptor antagonist

Inhibitor of p38 kinase

Cyclosporin G is an immunosuppressive agent, which is derived from fungal sources with a specific mode of action that involves inhibiting calcineurin. The source of Cyclosporin G is primarily from the fermentation of the fungus *Tolypocladium inflatum*. Its mode of action involves binding to the cytosolic protein cyclophilin in T-lymphocytes, which subsequently inhibits the phosphatase activity of calcineurin. This inhibition prevents the dephosphorylation and nuclear translocation of the nuclear factor of activated T-cells (NFAT), thereby reducing the transcription of interleukin-2 and other cytokines critical for T-cell activation. The primary use of Cyclosporin G is in preventing organ transplant rejection by suppressing the immune response. It is also being explored for potential applications in treating autoimmune diseases, where dampening the immune system can be beneficial. Ongoing research is investigating its pharmacokinetics and possible advantages over similar compounds, such as Cyclosporin A, focusing on its efficacy and side effect profile. Researchers in pharmacology and transplant immunology continue to study Cyclosporin G for its clinical applications and understand its broader impacts on immune modulation.

Fludarabine triphosphate trisodium is a nucleotide analog, which is a type of chemotherapy agent derived from purine nucleosides. This compound is the active metabolite of fludarabine, sourced from synthetic chemistry designed to mimic naturally occurring nucleotides involved in DNA replication. The mode of action involves its incorporation into the DNA strand during replication, where it effectively inhibits DNA polymerase and ribonucleotide reductase. This disruption impairs DNA synthesis, leading to apoptosis or programmed cell death, particularly in rapidly dividing cancer cells. The principal use of fludarabine triphosphate trisodium is in the treatment of hematological malignancies such as chronic lymphocytic leukemia (CLL) and, in certain cases, non-Hodgkin lymphoma. Its application is especially relevant in settings where conventional therapies might be less effective or where a nucleoside analog is particularly indicated. As a chemotherapeutic agent, it requires careful management due to its immunosuppressive profile, which is a critical consideration in the comprehensive care of patients undergoing treatment. Researchers continue to investigate its use in combination therapies aimed at enhancing efficacy while minimizing adverse effects.

Cell permeable peptide which is able to activate phosphoinositide 3- kinase, for which it binds with high affinity to the p85 subunit. 740 Y-P also has mitogenic activity as it is able to induce mitosis in muscle cells, and promotes cell survival in neurones. PI 3- kinase's are a family of enzymes involved in many cellular pathways including cell proliferation, growth, differentiation, survival, motility, and intracellular trafficking. PI 3 Kinases are therefore also involved in many cancers.

Nuclear Factor Erythroid 2-Related Factor 2 (Nrf2) and its negative regulator Kelch-Like ECH-Associated Protein 1 (Keap1) provide vital protection in maintaining cellular redox. In parallel, Nrf2 also aids the resolution of inflammation and also tissue repair. In homeostatic conditions, the transcription factor Nrf2 is controlled in a cytoplasmic complex with Keap1 with ubiquitination and protein degradation. Nrf2 has been linked to numerous cancers due to mutations affecting the binding region of Nrf2 to Keap1, resulting in Nrf2 dissociating from the complex. Nrf2 constitutively accumulates in the nucleus and activation of prosurvival genes that promote cancer cell proliferation.The Neh2 region of Nrf2 interacts with Keap1, as shown by nuclear magnetic resonance spectroscopy. The 16 amino acid peptide (AFFAQLQLDEETGEFL) (69-84) flanks the conserved ETGE motif and can replicate the binding to keap1.Therapeutics targeting the Nrf2 signalling pathway and activation of Nrf2 is a keen area of research, with many cancers being linked to Nrf2, particularly pancreatic cancer. Additionally, activation of Nrf2 has become a possible target as a treatment for COVID. Nrf2 (69-84) replicating full-length Nrf2 binding has been helpful in all cases.