Modulateurs d'enzymes

Inhibitor of EGFR transmembrane receptor

Inhibitor of GSK3β kinase

Inhibits mTORC1 and mTORC2 serine/threonine kinases

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. Aliskiren hemifumarate 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.

HMG-CoA reductase antagonist

Abltide represents the optimal substrate peptide of Abl (or c-Abl), a non-receptor tyrosine kinase (NRTK) and the oncogenic Bcr-Abl tyrosine kinase (TK) (formed via a fusion between the Abelson (Abl) TK gene and the break point cluster region protein Brc). Abl was discovered as the gene from which the Abelson leukaemia virus derived its Gag-v-Abl oncogene.TKs are critical enzymes involved in multiple signalling pathways. However, Tks can promote cancer progression when deregulated, for example deregulated TK, Bcr-Abl gives rise to chronic myeloid leukaemia (CML) and Philadelphia chromosome-positive acute lymphocytic leukaemia (Ph+ ALL).Abl is activated by various signals including: growth factors, cytokines, cell adhesion, DNA damage and oxidative stress and results in the stimulation of both pro- and anti-apoptotic roles, cell proliferation or differentiation, retraction, or migration. Abl phosphorylates a large number of functionally diverse substrates, in part due to its ability to shuttle between the cytosol and the nucleus and bind both DNA and actin&mdash-two biopolymers with fundamental roles in almost all biological processes.

Inhibitor of histone deacetylase 3 (HDAC3) with IC50 in nanomolar range. BRD 9908 was shown to preserve the insulin-secreting pancreatic cells in nonobese diabetic mice. BRD 3308 supressed infiltration of mononuclear cells and prevented β-cell death in vivo as well as increased basal insulin secretion in vitro. Studies on HIV infection models showed that HDAC3 inhibition by BRD 3308 disrupts the HIV latency by increasing the gene expression from HIV promoter.

Gefitinib is an inhibitor of the epidermal growth factor receptor (EGFR) protein. This inhibition is on the EGFR tyrosine kinase domain, where Gefitinib bindings to the ATP-binding site. As a a tyrosine kinase inhibitor, Gefitinib blocks tumor growth and has led to its use in slowing the progression of non-small cell lung cancer. Gefitinib also inhibits invasion and metastasis through inhibition of macrophage receptor interacting protein kinase 2 (RIPK2), rather than EGFR. Gefitinib 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.

Natural anti-cancer agent; inhibitor of histone deacetylases

Vardenafil is a phosphodiesterase type 5 inhibitor that binds to intracellular targets and competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis thus increasing cGMP levels. Vardenafil can be used for the research of erectile dysfunction, hepatitis and diabetes. Vardenafil 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

Acid α-glucosidase (83-99) (human) is derived from the exogenous enzyme which degrades glycogen, maltose and isomaltose through targeting alpha -1,4 and alpha -1,6 linkages. Once synthesised in its precursor form, within the Golgi it is glycosylated and acquires mannose 6-phosphate residues. This allows it to be transported to the Lysosome in a multistep process.Pompe disease, also known as glycogen storage disease type II, can be diagnosed through the absence of acid α-glucosidase activity within patients. Therefore glycogen degradation in the lysosome is inhibited by this autosomal recessive disorder. This results in the accumulation of glycogen and tissue destruction, hence contributing to the pathologies of muscle weakness and respiratory failure, associated with infantile onset and adult onset Pompe disease.

SIRT1 activator

Inhibitor of DDP-4 peptidase

A brain-penetrant inhibitor of leucin-rich repeat kinase 2 (LRRK2) with IC50 = 0.76 nM and anti-parkinsonian activity. Gain-of-function mutations in LRRK2 gene lead to increased familial and idiopathic risk of developing the disease. The inhibitors of the kinase activity have therapeutic potential against Parkinson’s disease.

Inhibits Mer receptor tyrosine kinase (IC50 = 4.3 nM). Selective over Axl (84-fold) and Tyro3 (58-fold). UNC 2881 inhibits phosphorylation of Mer kinase in 697 B-ALL cells (IC50 = 22nM). Inhibits EGF-induced activation of a chimeric enzyme, composed of EGFR fused with Mer. Blocks collagen-mediated platelet aggregation, implying the potential of this compound for treating thrombosis.

Inhibitor of panPI3K/mTOR

Inhibitor of kinase domain of TGF-β receptor type 1

Zoledronic acid is a drug that is used for the treatment of malignancy associated with hypercalcemia and bone metastasis from tumors. This drug induces apoptosis pf hematopoietic tumor cells by inhibiting farnesyl diphosphate. Zoledronic acid is a bisphosphate that inhibits osteoclast function and bone resorption. Zoledronic acid monohydrate 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 CDK2, JAK2 and FLT3; anticancer

Inhibitor of EGFR receptor