Modulateurs d'enzymes

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). YPSPV in EYGF-33 was found to have minimal antioxidant activity. However, YPSPV showed notably high angiotensin converting enzyme (ACE) inhibitory activity, it exceeded the positive control captopril.

Benazepril is a nonsteroidal anti-inflammatory drug that can be used to treat hypertension, heart failure and renal failure. It is an angiotensin-converting enzyme (ACE) inhibitor that blocks the conversion of angiotensin I to angiotensin II. This inhibition prevents the vasoconstrictive effects of this peptide, which are mediated through activation of the renin-angiotensin system. Benazepril 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.

Dipeptidyl peptidase-4 inhibitor; anti-diabetic agent

Inhibits type III tyrosine kinases (PDGFRα, PDGFRβ, FLT3)

Spirapril hydrochloride is an antihypertensive agent, which is a synthetic pharmaceutical compound designed to treat high blood pressure. The compound is derived from laboratory synthesis aimed at modulating the renin-angiotensin-aldosterone system. Its mode of action involves the inhibition of angiotensin-converting enzyme (ACE), which is crucial for the conversion of angiotensin I to the vasoconstrictor peptide angiotensin II. Angiotensin II is responsible for the constriction of blood vessels and an increase in blood pressure. By inhibiting this enzyme, Spirapril hydrochloride effectively reduces vascular resistance and lowers blood pressure. The primary application of Spirapril hydrochloride is in the management and treatment of hypertension, providing a means to control elevated blood pressure and reduce the risk of associated cardiovascular events. Additionally, it may be used adjunctively in treating certain heart conditions, improving cardiac function by decreasing preload and afterload on the heart. Its efficacy in hypertension management positions it as a critical agent in therapeutic regimens aiming at minimizing the long-term risks associated with chronic high blood pressure.

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. Pomalidomide 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 cathepsin K inhibitor; reduces bone resorption

A selective VHL inhibitor that stabilizes the hydroxylated form of HIF-α, resulting in upregulation of downstream target genes and proteins. Provides a tool for studying hypoxic signaling pathway.

mTOR kinase inhibitor; rapamycin analog; immunosuppressant

A potent ATP-competitive inhibitor of tropomyosin-related kinases (TRK1, TRK2 and TRK3), members of the receptor tyrosine kinase family of neurotrophin receptors. Tumors with oncogenic TRK fusions are sensitive to larotrectinib, leading to reduced proliferation and tumor growth in patients with soft tissue sarcoma, triple-negative breast cancer and lung cancer.

Inhibitor of histone deacetylases

A glycogen synthase kinase 3β- (GSK3β-) / crosstide fragment representing the phosphorylation site on GSK3β-. GSK3β- is a serine/threonine kinase which regulates glycogen synthase activity and is a key mediator of vertebrate development, tumourigenesis and cell differentiation. GSK3β- is phosphorylated by activated AKT/protein kinase B on serine 9- promoting its inactivation.

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 leucine-rich repeat kinase LRRK2Â

Inhibitor of vacuolar-type proton pump

Inhibitor of TOP1 topoisomerase; anti-cancer

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.

Oxaprozin is a non-steroidal anti-inflammatory drug (NSAID) used for the treatment of osteoarthritis and rheumatoid arthritis. This drug relieves swelling and inflammation by inhibiting the enzyme cyclooxygenase which in turn inhibits prostaglandin synthesis. Oxaprozin 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.

Nonsteroidal anti-inflammatory (NSAID)

Pralidoxime is a cholinesterase reactivator that is used for the treatment of organophosphate poisoning. When organophosphate binds to the esteratic site of acetylcholinesterase, it results in a reversible inactivation of the enzyme. However, by rupturing the phosphate-ester link that has been formed between the organophosphate and acetylcholinesterase, pralidoxime is able to reactivate the cholinesterase enzyme. Pralidoxime chloride 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

Inhibitor of B-RAF kinase

Thromboxane A2 synthetase inhibitor

Malotilate is a pharmacological agent that is used to treat symptoms of hepatitis, bowel disease, and collagen diseases. This drug reduces collagen synthesis and cell migration activity of fibroblasts in vitro. It also has been shown to facilitate liver regeneration in rats. Malotilate 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 tyrosinase in melanocytes: skin whitener

Phosphorylated EGFR peptide substrate.

Ubenimex is a protease inhibitor drug that is being studied for the treatment of acute myelocytic leukemia. This drug is an aminopeptidase N, B and leukotriene A4 hydrolase inhibitor. It is also used in the treatment of hypercholesterolaemia. Ubenimex 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.

Apremilast is the commercial name of a phosphodiesterase-4 (PDE4) inhibitor developed to treat chronic inflammatory disorders. Similarly to thalidomide, the apremilast molecule carries a phthalimide ring, but it lacks however the glutarimide ring needed to bind to cereblon, specifically targeted by thalidomide. As a drug, apremilast is indicated for the treatment of psoriasis and psoriatic arthritis. Apremilast 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.

Imatinib is a tyrosine kinase inhibitor that is used in the treatment of various leukemias and gastrointestinal stromal tumors. This drug inhibits the BCR-ABL tyrosine kinase. It is suggested that Imatinib also inhibits other tyrosine kinases such as PDGF, SCF and c-Kit. Imatinib 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.

Topoisomerase II and DNA helicase inhibitor

PI3K enzyme inhibitor

PI3K enzyme inhibitor; antineoplastic

Ile-Pro-Pro (IPP) has the ability to inhibit angiotensin-converting enzyme and stimulate the production of nitric oxide. It could be used to improve hypertension thus reducing the risk of cardiovascular diseases.

VEGFR tyrosine kinase inhibitor

Inhibitor of pan-class I PI3K family of lipid kinases; antineoplastic

A tyrosine kinase inhibitor with potent activity against EGFR, STAT3, JAK3/STAT, JAK3/AP-1 and JAK3/MAPK. Suppresses IL-2 signaling pathway, inhibits T-cell growth and activation of JAK3, AP-1, STAT, MAPK. Has anti-proliferative and anti-invasive effect on cancer cells.

Phosphodiesterase PDE4 inhibitor

Bortezomib is a selective and reversible inhibitor of the multicatalytic 26S proteasome. The inhibition of protein breakdown affects several metabolic pathways and leads to cell death. The compound is effective in treating t-cell lymphomas and multiple myeloma because it prevents the binding of myeloma cells to bone marrow stroma and inhibits osteoclast differentiation. Bortezomib 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.

Lovastatin is an HMG-CoA reductase inhibitor that is used to lower LDL cholesterol levels and to aid in the management of cardiovascular diseases. Animal studies have demonstrated that this drug has vasculoprotective properties. Lovastatin 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.

Sulindac is a non-steroidal anti-inflammatory drug that has anti-inflammatory and analgesic properties. It is used to relieve the pain of osteoarthritis and rheumatoid arthritis by reducing inflammation and inhibiting the production of prostaglandins, which are chemicals that cause inflammation. Sulindac 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 PARP1 and PARP2 enzymes

Imiquimod is a toll-like receptor 7 agonist drug that is used for the treatment of genital warts, basal cell carcinoma and condyloma acuminata. This drug works by relieving and controlling wart production. Studies in mice have shown that this drug may induce cytokines such as interleukins. Imiquimod helps to increase apoptosis of diseased tissues and an infiltration of lymphocytes into tumor lesions. Imiquimod 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 5-lipoxygenase activating protein_x000D_

A potent and selective c-Met inhibitor. Anti-tumour activity demonstrated in xenograft models in vivo. Forms a thioether conjugate by reacting with thiol groups in proteins. Non-small-cell lung carcinoma (NSCLC) tumour cells that overexpress c-MET have increased sensitivity to AMG458.

Inhibits cyclin-dependent kinase 4 and 6 (CDK4 and CDK6); antineoplastic

Inhibitor of vacuolar ATP-ases

Inhibitor of p38 MAPK kinase

Diacerein is a slow-onset anthraquinone IL-1 inhibitor that is used in the treatment of joint diseases such as osteoarthritis. This drug is also being studied for the treatment of insulin resistance and diabetes mellitus. Diacerein works to decrease inflammation and cartilage destruction by reducing the level of interleukin-1. Diacerein 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.

Anti-inflammtory drug

Potent and selective inhibitor of the glycogen synthase kinase GSK-3. Promotes cell renewal in embryonic stem cells by modulating Notch, MAPK and TGF-β signalling pathways, which are involved in pluripotency. It also affects the Wnt/β-catenin pathway and alters expression of genes coding for proteins, epigenetic regulatory elements and non-coding RNAs. The combination of CHIR 99021 and basic fibroblast growth factor (bFGF) allows long-term self-renewal in adult mouse retinal progenitor cells.

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.