Modulateurs d'enzymes

Nilotinib is tyrosine kinase inhibitor drug that is used to treat chronic myeloid leukemia (CML). It inhibits the activity of the BCR-ABL protein kinase, which is involved in the development of CML. Additionally, it inhibits PDGF and c-kit for the potential treatment of various leukemias. Nilotinib 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.

Dutasteride is an androgenic compound and a 5α-reductase inhibitor that is used to treat benign prostatic hyperplasia (BPH) and male pattern baldness. Dutasteride reduces prostate volume and improves symptoms of BPH by inhibiting the enzyme 5α-reductase, which converts testosterone to dihydrotestosterone. Dutasteride 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.

A cytidine analogue and inhibitor of DNA methyl transferases (DNMTs) with anti-cancer activity. This stable, hydrophilic compound forms covalent complexes between DNMT and zebularine-substrate DNA. It causes DNA lesions that block replication and cause replication fork collapse, leading to the formation of DNA double-strand breaks. It was also shown that zebularine-induced DNA methylation decrease in the IL-1β promoter region and disrupts molecular mechanisms of neuroinflammation. Moreover, this molecule down-regulates the DNA-methylation profile in the pluripotency genes’ promoters, which leads to improved development of somatic cell nuclear transfer (SCNT) embryos.

Inhibits proteosomes of class peptide epoxyketone; antineoplastic

A potent, reversible and slow-binding inhibitor of delta-5 desaturases (D5Ds), by binding to the desaturase domain. Inhibiting D5D has therapeutic applications in inflammatory diseases. This is due to the increase in anti-inflammatory DGLA-derived eicosanoids and decrease in pro-inflammatory AA-derived eicosanoids.

Phosphodiesterase (PDE5, 6, 9 and 11) inhibitor

A reversible and selective inhibitor of thrombin that rapidly binds to the catalytic site directly. Inhibits both soluble and bound forms of thrombin. Used for prophylaxis and treatment of heparin-induced thrombocytopenia type II.

An allosteric inhibitor of human methionine adenosyltransferase 2A (Mat2A), the extrahepatic isoform, with an IC50 value of 420nM. Binding of PF9366 to Mat2A overlaps with the binding site of Mat2B, a regulator of Mat2A. Mat2A inhibition in cells by PF 9366 reduces synthesis of S-adenosylmethionine (SAM).

GSK-126 is a potent inhibitor of histone lysine methyl transferase 2, which is encoded by the enhancer of zeste homolog 2 gene (EZH2). The EZH2 protein regulates cell cycle as it represses the Polycomb-Repressive Complex 2 (PRC2), allowing cells to divide actively. GSK-126 inhibits the EZH2 by targeting the catalytic domain (SET) of the enzyme and therefore blocks the PCR2 repression mechanism, resulting in cell proliferation arrest. The compound has shown therapeutic potential for a variety of cancers.

Irsogladine is a gastroprotective drug that is used for the treatment of GERD and gastric ulcers. This drug also has antioxidant properties. Irsogladine is a phosphodiesterase-4 inhibitor and increases levels of cAMP. It helps to prevent and heal damage to the stomach lining. Irsogladine maleate 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.

Substrate for proline-rich tyrosine kinase 2 (Pyk2)- can be used for substrate phosphorylation assays. Pyk2 is a member of the focal adhesion kinase (FAK) subfamily of cytoplasmic tyrosine kinases. Pyk2 is also known as: calcium-dependent tyrosine kinase (CADTK)- cellular adhesion kinase β- related adhesion focal tyrosine kinase (RAFTK)- or FAK2.Pyk2 functions as a scaffold protein, and it interacts with cytoplasmic proteins at focal adhesion sites to integrate different environmental signals. Pyk2 is activated by several stimuli, including elevated intracellular calcium levels, protein kinase C activation, and exposure to stress factors. Recently, Pyk2 has become a potentially important new therapeutic target or prognostic marker because overexpression of Pyk2 has been found in many human tumours.

Inhibitor and pseudosubstrate of DNA repair protein O6-methylguanine-DNA methyltransferase (MGMT). It is used as a sensitizer for the treatment of advanced solid tumors, including prostate, colorectal and central nervous system malignancies. Lomeguatrib inhibits the repair mechanism of DNA damage induced by alkylating agents such as temozolomide, and therefore potentiates its anti-cancer effects.

A protein kinase G selective substrate for use in kinases assays, with a preference for PKG Ialpha over PKG II. PKG is a serine/threonine-specific protein kinase activated by cyclin guanosine monophosphate (cGMP). PKG is involved in several signalling pathways including: smooth muscle relaxation, platelet function, cell division, nucleic acid synthesis and sperm metabolism.

Febuxostat is a non-purine xanthine oxidase inhibitor that is used for the treatment and management of hyperuricemia and chronic gouty arthritis. Febuxostat inhibits the uptake of uric acid from the blood into cells and thereby reduces its concentration in plasma. Additionally, this drug has been shown to have anti-inflammatory and antioxidant effects. Febuxostat 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 ornithine decarboxylase

Inhibitor of DNA polymerase; anti-leukemic agent

Inhibitor of dipeptidyl peptidase IV; anti-diabetic agent

Inhibitor of CDK4/6 serine/threonine kinases; antineoplastic

Inhibitor of CKD1, CDK2, and CDK4 serine/threonine kinases

Inhibitor of angiotensin converting enzyme

Ozagrel is an antiplatelet agent that is also a thromboxane A2 synthetase inhibitor. It is used for the treatment of bronchial asthma and cerebral ischemia. It blocks platelet aggregation and reduces hypersensitivity of bronchial muscles. Ozagrel 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.

Inhibitor of BRAG2-mediated activation of Arf GTP-ase. In vitro experiments showed that Bragsin2 inhibits the Arf GTP-ase activation that is mediated by a nucleotide exchange factor BRAG2 in a membrane-dependent manner. Bragsin2 interacts with the PH domain of BRAG2 protein as well as membrane, which prevents the activation of lipidated Arf. Bragsin2 affects the trans-Golgi network and was shown to affect the tumour sphere in breast cancer cell lines.

LOXO-305 is a small molecule inhibitor, which is a synthesized chemical compound designed to selectively target specific enzymes or pathways. Its source is rooted in medicinal chemistry and pharmacological research aimed at elucidating pathways involved in oncogenesis. The mode of action of LOXO-305 involves selectively inhibiting the Bruton’s tyrosine kinase (BTK), a key enzyme in the B-cell receptor signaling pathway. By binding to BTK, LOXO-305 disrupts its activity, thereby inhibiting downstream signaling pathways that promote cell survival and proliferation, particularly in malignant B-cells. LOXO-305 is used as a therapeutic agent in oncology, specifically targeting cancers with aberrations in the BTK pathway, such as certain forms of leukemia and lymphoma. Its selective inhibition profile allows for potentially reduced off-target effects compared to non-selective inhibitors. Its applications are primarily in treatment regimens for patients with relapsed or refractory disease who have mutations that either render other treatments ineffective or pose a high risk of relapse. Ongoing research continues to explore its efficacy in a variety of B-cell malignancies, potentially broadening its applicability in the oncology field.

ALK receptor tyrosine kinase inhibitor

Selective inhibitor histone methyltransferases SUV420H1 and SUV420H2 (IC50 values = 25 nM and 144 nM, respectively). Reduces histone H4K20me2 and H4K20me3 expression whilst increasing H4K20me1 global expression. Inhibits formation of p53-binding protein 1 (53BP1) foci upon ionizing radiation and reduces NHEJ-mediated DNA-break repair.

Inhibitor of dipeptidyl-peptidase; anti-diabetic agent

Tyrosine kinase inhibitor; affects EGFR receptor; pancreatic cancer treatment

Abiraterone is an antiandrogen drug used in the treatment of metastatic prostate cancer. It is a derivative of steroidal progesterone. This drug inhibits the enzyme CYP17 irreversibly, thus inhibiting the synthesis of androgen. It specifically inhibits the conversion of 17-hydroxyprognenolone to dehydroepiandrosterone to decrease serum levels of testosterone and other androgens. Abiraterone acetate 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 BCR-ABL1 kinase

Finasteride is an antiandrogenic drug that belongs to the group of 5-alpha reductase inhibitors, which are used for the treatment of benign prostatic hyperplasia and male pattern baldness. The conversion of testosterone to 5α-dihydrotestosterone (DHT) is blocked by type II 5α-reductase inhibition, which then results in significant increase in prostatic testosterone concentrations and minimal to moderate increases in serum and tissue DHT concentrations. A reduction in DHT concentration will cause a reduction in prostatic volume as DHT appears to be the main androgen responsible for stimulating prostatic growth. Finasteride 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 multiple tyrosine kinases (Abl1, Src family kinases, Tie-2 and VEGFR-2)

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.

Apatinib, also known as rivoceranib, is an inhibitor of the vascular endothelial growth factor receptor 2 (VEGFR2) tyrosine kinase. Apatinib targets VEGFR2 with its action and has proven to have strong anti-tumor effects in human cancers. In studies in mice, apatinib acted as an Inhibitor of VEGFR2 and played an antiangiogenic effect. Apatinib has been suggested for the treatment of ischemia-induced proliferative retinopathy and neovascular age-related macular degeneration.

BRAF kinase inhibitor; antineoplastic

A 939572 is an inhibitor of stearoyl-CoA desaturase 1 (SCD1). It exhibits anticancer activity as it inhibits cell growth and promotes cell death in human non-small cell lung carcinoma cells. A 939572 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.

Benserazide is a drug that is used for the treatment of Parkinson’s disease and restless leg syndrome. This drug is a decarboxylase inhibitor and is usually used in combination with Levodopa. Benserazide 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.

A selective inhibitor of MEK5 protein kinase with an IC50 value of 4.3 nM. Blocks transcriptional activation of myocyte-specific enhancer factor 2C (MEF2C). Inhibits phosphorylation of ERK5 protein kinase and thereby reverses inhibition of TNF signaling induced by fluid shear stress in endothelial cells. Induces apoptosis in FLT3-ITD cells.

Ibuprofen analogue; COX1/2 inhibitor

Inhibitor of calpain and cathepsin B

Inhibitor of PI3K kinase isoforms α, δ, and γ

Class 1 PI3K enzyme inhibitor; anti-neoplastic

Zonisamide is a type of anticonvulsant which is used in the treatment and study of the symptoms associated with epilepsy and Parkinson’s disease. Zonisamide reduces the high-frequency repetitive firing of action potentials in the brain by changing the fast inactivation threshold of voltage-dependent sodium channels. Zonisamide 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.

Cofactor for nitric oxide synthetase and Phe, Tyr and Trp hydroxylases

JAK2 inhibitor with potential antineoplastic activity

Inhibitor of discoidin domain receptor DDR1

A selective and potent inhibitor of phosphodiesterase 2 (PDE2). Raises cAMP and cGMP levels in neurons, improves social recognition and object memory in murine animals. Reverses anxiolytic effects induced by oxidative stress in mice by blocking cGMP-PKG signaling.

Inhibitor of ALK4, ALK5, and ALK7 receptors

Ampiroxicam is a non-steroidal anti-inflammatory drug (NSAID) used to relieve pain and inflammation for various conditions. This drug inhibits the enzyme cyclooxygenase which in turn inhibits prostaglandin synthesis resulting in a reduction of inflammation and pain. Ampiroxicam 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.

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.

Enalapril is a long-acting angiotensin-converting enzyme inhibitor. It is used to treat hypertension and congestive heart failure, as well as chronic cough due to postnasal drip or bronchitis. Enalapril is an active inhibitor of the synthesis of angiotensin II and other vasoconstrictor substances that are involved in the regulation of blood pressure. It binds reversibly to the active site on angiotensin-converting enzyme (ACE) and blocks its activity by forming strong hydrogen bonds with residues on ACE, thereby preventing it from converting angiotensin I into angiotensin II. This leads to a significant reduction in blood pressure. (S,S,S)-Enalapril maleate 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.