Modulateur d'interaction protéine-protéine

BT13 is a GFL mimetic and a potent and selective activator of RET tyrosine kinase and its downstream signaling cascades. BT13 promoted neurite outgrowth from dorsal root ganglia sensory neurons, alleviated mechanical hypersensitivity and reversed injury-induced changes in dorsal root ganglia neurons in experimental animals with the spinal nerve ligation-induced neuropathy.

Antagonist of proto-oncogene MDM2 and its interaction with p53

Microtubule-stabilizing agent; antineoplastic;

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.
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&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.

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.
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&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 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.

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.

Anti-microtubular agent; antineoplastic

A potent inhibitor of Wnt/β-catenin signalling pathway that interferes with β-catenin/TFC4 interaction. Reduces growth and motility of colon cancer cells. Inhibits self-renewal, whilst inducing differentiation in cancer stem cells.

A chemical probe for the dual bromodomains of human transcription-initiation-factor TFIID subunit 1 (TAF1). GNE 371 binds TAF1 with an IC50 of 10 nM and is selective over other bromodomain family members. Exerts anti-proliferative effects in synergy with BET inhibitor JQ1.

Inhibitor of clathrin-mediated endocytosis (CME) and ligand to the clathrin heavy chain (CHC). ES9-17 is an inhibitor of the CHC function with EC50 of 13 μM in plant model Arabidopsis thaliana. ES9-17 is a non-protonophoric CME inhibitor and it does not alter the cytoplasmic pH levels substantially. In a mammalian cell line HeLa, ES9-17 reduced the uptake of transferrin, which is a CME-driven process.

Potent and selective inhibitor of polycomb repressive complex 2 (PRC2), by binding to the K27me3-pocket of the regulatory EED subunit. Inhibits H3K27 methylation in histone 3. Has anti-tumor activity in murine xenograft models. Synergistic with EZH2 inhibitor against cancer cell growth.

Reversible inhibitor of RGS proteins

Microtubule disrupter; anti-mitotic drug; anti-cancer alkaloid

Efficient chemiluminescent NH2-coupling reagent for detection of proteins

Inhibits anti-apoptotic proteins Bcl-2, Bcl-xl and Bcl-w. Synergistic with chemotherapy and radiotherapy in several tumour cell lines. Potent activity as a single agent in lymphoid cancer and small cell lung cancer (SCLC) cell lines. Causes tumour regression in SCLC xenograft tumour in vivo.

KRAS G12C inhibitor