Enzyme Modulators

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.