Modulateurs d'enzymes

6-Thioguanine is a purine analog used in the therapy for leukemia and for remission consolidation in patients with acute nonlymphocytic anemia. This drug also has antimetabolite action. It replaces guanine during DNA replication. This substitution disrupts the accurate pairing of DNA bases, leading to errors in DNA replication and hinders cell division. 6-Thioguanine 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 interaction between the UNC119 chaperone and its cargo. Squarunkin A inhibits activation of Src kinase by interrupting the interaction between the myristoylated peptide at the N-terminus of the Src kinase and UNC119A chaperone (IC50 = 10 nM). Squarunkin A impairs the UNC119-mediated enrichment of plasma membrane with non-receptor protein tyrosine kinase Src, resulting in the decrease in Src autophosphorylation and decreased oncogenic Src signalling.

Apixaban is an anticoagulant agent used for the prophylaxis of stroke and deep vein thrombosis leading to pulmonary embolism. This drug is an inhibitor of factor Xa and prothrominase. As a result, this prevents the formation of a thrombus. Apixaban 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.

p38 MAP kinase antagonist

Inhibits phorbol ester TPA/PMA; immunosuppressant

Inhibitor of carbonic anhydrase; muscle relaxant

Hydroxychloroquine is a drug that is used to treat multiple types of autoimmune diseases, including rheumatoid arthritis, systemic lupus erythematosus and discoid lupus. It is a prodrug, which is activated in the liver to hydroxychloroquine. It inhibits the production of inflammatory cytokines and nitric oxide by binding to the toll-like receptor 4 (TLR4) and inhibiting signaling pathways downstream of TLR4 activation. Additionally, Hydroxychloroquine is used to prevent and treat malaria caused by parasitic protozoan from the Plasmodium genus. Furthermore, recent studies revealed that hydroxychloroquine has beneficial effects on COVID-19 patients, as the current evidence shows that hydroxychloroquine inhibits SARS CoV-2 entry in host cells by interfering with endocytosis and affecting the glycoprofile on the spike glycoprotein. Hydroxychloroquine sulfate 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 the histone methyltransferase SETD8 that supresses methylation of the K20 residue in histone 4. UNC 0379 treatment of human glioma reduced recruitment of 53BP1 protein to double strand breaks and sensitised cells to radiotherapy without altering cell cycle kinetics.

Inhibits JAK1 and JAK2 kinases

Potent and irreversible inhibitor of phosphoinositide-3-kinase (PtdIns-3-kinase) with IC50 of 0.1 nM. PX 866 inhibited cell motility and growth of 3D spheroids of glioblastoma, breast, prostate and colon cancer cell lines at low nanomolar concentrations. PX 866 also exhibited anti-tumoral activity in vivo in xenograft models for ovarian and lung cancer.

Reversible inhibitor of trypsin

The peptide IRW, characterised from egg protein, exhibits inhibitory properties against the angiotensin converting enzyme (ACE2) and could be used to prevent cardiovascular disease with further research. Treatment of hypertensive mice with IRW induced endothelium-dependent vasorelaxation and reduced vascular inflammation. The IRW tripeptide acts as anti-hypertensive by upregulating ACE2 activity via the Mas receptor (MasR) and upregulating Akt/eNOS signalling in the aorta. IRW also induces superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GPx) activity. These may play a factor in IRW's role as an anti-inflammatory. IRW shows promise as a nutraceutical for inflammatory conditions and a tool for drug development in cardiovascular disease.

Pritelivir mesylate is an antiviral compound, which is derived from thiazolylamide class molecules, with a targeted mechanism of action against the herpes simplex virus (HSV). It functions by inhibiting the viral helicase-primase complex, which is essential for the replication of viral DNA. This distinct mode of action differentiates it from traditional treatments like acyclovir, which targets viral DNA polymerase. Pritelivir mesylate is primarily used in the treatment and suppression of HSV infections, including HSV-1 and HSV-2. By targeting the helicase-primase, it effectively reduces the replication of the virus, leading to decreased viral shedding and lesion formation. Its unique pathway offers an alternative for cases where resistance to standard antivirals occurs. Given its potential, Pritelivir mesylate is under extensive study to better understand its efficacy and safety profile. Its promising results in early clinical trials may provide a significant advancement in antiviral therapies, offering new hope for managing and controlling HSV infections.

Teniposide is a cytotoxic drug that is used in the treatment of refractory childhood acute lymphoblastic leukemia. It has antitumour activity. It is a type II topoisomerase inhibitor. This drug inhibits DNA synthesis by forming a complex with topoisomerase II and DNA. Teniposide 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 lysophosphatidylserine hydrolysis by the integral membrane serine hydrolase ABHD12 (IC50 = 1.3 µM). Raised levels of lysophosphatidylserine were observed in mouse brain in vivo and in primary human macrophages. DO 264 had proinflammatory effects, following infection with lymphocytic choriomeningitis virus (LCV) clone 13 in mice, resulting in severe inflammatory lung damage.

Inhibitor of VEGFR, PDGR, c-Kit and Ret; inhibitor of angiogenesis

SU 3327, originally introduced as a thiadiazole JNK inhibitor (De et al. 2009) has recently been identified as having antibiotic activity against a broad range of bacteria including drug-resistant gram positive and negative strains (Strokes et al. 2020). This molecule has been given the fictional name ‘Halicin’ inspired by the AI approach used to discover its novel biological activity.

Mirodenafil dihydrochloride is a potent phosphodiesterase-5 (PDE5) inhibitor, which is a synthetic compound with a primarily chemical origin. Its mode of action involves the inhibition of the enzyme PDE5, which predominantly resides in the smooth muscle cells lining blood vessels. By inhibiting PDE5, Mirodenafil dihydrochloride effectively increases the levels of cyclic guanosine monophosphate (cGMP), leading to the relaxation of smooth muscle tissues and vasodilation. This mechanism of action makes Mirodenafil dihydrochloride particularly effective in the treatment of erectile dysfunction (ED). By enhancing blood flow to specific areas of the body, primarily the corpus cavernosum of the penis, it facilitates the achievement and maintenance of an erection in response to sexual stimulation. The compound’s selectivity for PDE5 over other phosphodiesterases minimizes potential side effects and enhances its therapeutic efficacy. As such, Mirodenafil dihydrochloride serves as a valuable tool in clinical settings for managing erectile dysfunction, providing an alternative for patients who may not respond to or tolerate other PDE5 inhibitors.

Inhibitor of BACE1 protease

Anagrelide is a thrombocytopenic drug that is used to treat thrombocythemia and related conditions. This drug works by decreasing the platelet count by suppressing transcription factors that are necessary for the maturation of platelets. This drug is also a phosphodiesterase III inhibitor. Anagrelide 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.