Enzyme Modulators

Aliskiren is a drug that belongs to the group of angiotensin receptor blockers. It is a renin inhibitor that is used for the treatment of hypertension, congestive heart failure, and renal impairment. Aliskiren inhibits the action of angiotensin II by blocking the binding of this hormone to its receptors.

Class 1 PI3K enzyme inhibitor; anti-neoplastic

A potent inhibitor of histone deacetylases (HDACs) of class I and II with anti-tumoral activity. The compound blocks HDAC catalytic activity by chelating zinc ion in the enzyme’s active site. Extensively used in research as epigenetic modifier able to block cell growth and downregulate proliferation-associated factors. It has also been reported that trichostatin A induces apoptosis via a histone-modification independent mechanism in oral squamous cell carcinoma cell lines. Initially discovered as anti-fungal compound from Streptomyces hygroscopicus for the control of fungal infections caused by the genus Trichophyton.

Anti-inflammtory drug

Inhibitor of monoamine oxidase

Inhibitor of topoisomerase TOP2

Topoisomerase II and DNA helicase inhibitor

Competitive, reversible inhibitor of α-glucosidases used for the control of postprandial hyperglycaemia in patients with type 2 diabetes mellitus. It inhibits digestive enzymes with α-glucosidase activity, which breakdown complex sugars to absorbable monosaccharides. It also reduces the levels of glycated haemoglobin (HbA1c).

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.

Inhibitor of p38 MAPK kinase

Inhibitor of FLT3 receptor tyrosine kinases; anti-neoplastic

Phosphodiesterase 5 inhibitor; anti-impotence drug

Inhibitor of ecto-ATPase which blocks the hydrolysis of nucleoside diphosphates and triphosphates in extracellular space. The compound inhibits NTPDase1, NTPDase 3, NTPDase 8 and NPP1and prolongs the effect of ATP on purinergic P2 receptors in environment with physiological concentrations of nucleotides. The compound has variable effectiveness as ecto-ATP inhibitor in mouse, rat, human and guineia pig tissues.

Etoposide is a cytotoxic drug used in cancer chemotherapy. It inhibits DNA replication through inhibition of DNA topoisomerase II, thus catalysing cell cycle arrest and apoptosis. 
Etoposide 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.

Proteosome inhibitor; antineoplastic

AKTide-2T is a 14-mer peptide which has the ability to bind to the substrate binding domain of Akt1 with a Ki of 12mM. AKt1 is part of the Akt kinase family which are serine/threonine kinase and it is ubiquitously expressed. AKt1 performs roles such as promoting endothelial neoplasms and through phosphorylating angiogenic substrates AKt1 plays a role in angiogenesis. AKT kinases as a whole perform functional roles in cell proliferation, cell growth, survival and intermediary metabolism.During peptide library screening, AKTide-2T was found to contain the optimal motif for successful binding to AKT. When phosphoamino acid analysis of AKTide-2T was carried out it was observed that although AKTide-2T contained two potential AKT phosphorylation sites: serine or threonine, AKT only phosphorylated the serine site. Furthermore it was found that AKTide-2T exhibits properties of being a competitive inhibitor for example it competitively inhibits histone H2B from being phosphorylated by AKT.