Modulatore dell'interazione proteina-proteina

A small molecule inhibitor of polycomb complex protein BMI-1, a gene often overexpressed in tumors and therefore a popular therapeutic target in cancer. Anti-tumor effects of PTC 209 have been demonstrated in colorectal carcinoma, acute myeloid leukemia, multiple myeloma and head neck squamous cell carcinoma. As a regulator of self-renewal, inhibition of BMI-1 by PTC 209 also reduces growth of colorectal cancer initiating cells.

Promotes binding of vWf to glycoproteins on platelets, inducing aggregation

<p>Microtubule-stabilizing agent; antineoplastic;</p>

<p>Docetaxel is a cytotoxic semi-synthetic taxane and is an anthracycline antibiotic. The compound is an anti-microtubule agent and has significant inhibitory activity in solid tumors either alone or in combination with other chemotherapeutic agents.<br>Docetaxel trihydrate 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&amp;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.</p>

<p>Inhibits RGS proteins, selective for RGS4</p>

<p>Activator of p53; inhibitor of NF-?B</p>

<p>Oxaliplatin is a platinum-based DNA-cross-linking agent. It is a chemotherapeutic drug, often used in combination with leucovorin, fluorouracil, and capecitabine. Oxaliplatin works by cross-linking DNA thus inhibiting the synthesis of RNA and proteins, which leads to cell death and inhibition of cancer cells growth. It is more effective than cisplatin or irinotecan in treating metastatic cancer. Oxaliplatin also has effects on Toll-like receptor 4 (TLR4) expression levels in vitro and in vivo models. In addition, oxaliplatin's effect on ATP binding cassette transporter proteins may be responsible for its antitumour activity against solid tumours.<br>Oxaliplatin 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&amp;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.</p>

Tubulin ligand which promotes microtubule assembly and stabilises microtubule cytoskeleton against depolymerisation. The compound has anti-tumoral activity since its interference with cytoskeleton dynamics affects the assembly of mitotic spindle, segregation of chromosomes, cell division and blocks the cell cycle in G1 or M phase. The compound is also used for the purification of tubulin or microtubule-associated proteins.

<p>A BCL-2 selective inhibitor with no effect on Bcl-xl and thereby prevents thrombocytopenia. Increased sensitivity observed in Bcl-2-dependent haematological tumour cell lines. Elicits additional benefits to tamoxifen treatment in ER-positive breast cancer xenografts.</p>

<p>Inhibitor of the Smoothened receptor and Hedgehog signalling pathway. Cyclopamine is a steroidal alkaloid that binds to the heptahelical bundle of Smoothened and negatively regulates transcription of downstream genes. In prostate cancer cells, cyclopamine inhibited cell growth, arrested cell cycle and in glioblastoma, it depleted stem cell-like cancer cells.</p>

Dual PI3K/mTOR inhibitor

<p>Inhibitor of Hsp90 chaperone protein; anti-neoplastic</p>

<p>A cytotoxic taxane and anti-microtubule agent with anti-proliferative activity. Docetaxel binds to the β-subunit of tubulin, which results in increased polymerisation and stabilisation of microtubules. The compound interferes with microtubule dynamics, which leads to the cell cycle arrest in the G2/M phase and apoptosis. The compound has significant inhibitory activity in solid tumors either alone or in combination with other chemotherapeutic agents.</p>

<p>A Bad-like BH3 mimetic with strong affinity for Bcl-xl, Bcl-2 and Bcl-w that promotes BIM-mediated apoptosis. Enhanced efficacy when combined with other chemotherapies in xenograft models of B-cell malignancies and SCLC. Has senolytic effects on senescent cells, demonstrating revival of aged HSCs in vivo.</p>

Levosimendan has been shown to act as a calcium sensitiser and increase cytosolic Ca2+ levels. It is an analog of the cardiac glycoside, ouabain. This drug has been shown to be effective for the treatment of congestive heart failure and is used to increase the heart’s contractility and decrease its rate in patients who have low cardiac output. Levosimendan also causes vasodilation by increasing nitric oxide production in vascular endothelial cells.

Rivaroxaban is a natural drug that is a direct factor Xa inhibitor. It has been shown to be an effective therapy for the treatment of atrial fibrillation, deep vein thrombosis (DVT) and pulmonary embolism (PE). It works by inhibiting the enzyme, thrombin, which is responsible for the formation of blood clots. Rivaroxaban also has an effect on the coagulation system by decreasing the levels of fibrinogen and increases in antithrombin III. This drug does not have any specific antidote, but it can be reversed with heparin. Pharmacodynamics and drug interactions have been studied extensively in preclinical models, demonstrated by the concentration–time curves.

<p>Recombinant protein against VEGF(A); binds placental growth factor (PIGF)</p>

<p>Efficient chemiluminescent NH2-coupling reagent for detection of proteins</p>

<p>Tubulin binding agent; targets tumour vasculature</p>

<p>HDM2 antagonist; inhibits interaction between MDM2 and p53</p>