Modulador de Interacção Proteína-Proteína

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.

Anti-microtubular agent; antineoplastic

Activator of RET signalling cascade and a derivative of a GFL mimetic compound BT 13. Molecular docking calculations and molecular dynamics simulations were performed in GDNF−GFRα1−RetA complex and showed that BT 18 binds to the allosteric site in GFRα1 as well as RetA surface interfacing GFRα1.

(2R)-Arimoclomol maleate is an investigational pharmaceutical compound, which is an orally bioavailable small molecule with pharmacological activity primarily targeting cellular protein homeostasis mechanisms. This therapeutic agent is derived from molecular chaperones and operates by selectively enhancing the expression of heat shock proteins (HSPs). The mechanism of action involves the modulation of the heat shock response, wherein (2R)-Arimoclomol maleate amplifies the natural cellular defense pathways against protein misfolding and aggregation.

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.

Autophagy inhibitor that selectively targets the StART domain of GRAMD1A

Inhibitor of BET bromodomain; antineoplastic

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.

17-AAG is the first clinically tested hsp90 inhibitor that exhibits antitumor activity. Its antitumor effects are documented in vivo for various animal models, including erbB2-dependent breast cancer, prostate cancer models, and melanoma.

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

KRAS G12C inhibitor

Induces Kruppel like factor 4 (KLF4) and reduces the expression of MYC.  Anti-tumor activity of APTO 253 has been demonstrated in AML and haematological malignancies. Inducing KLP4 expression in ovarian cancer cells using APT0 253 sensitises cells to cisplatin  and paclitaxel. BRCA1/2-deficient cancer cells are hypersensitive to APTO 253, which mediates its action by causing DNA damage.

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

Obatoclax mesylate is a synthetic small molecule, which is derived from chemical synthesis with a primary mode of action as a pan-BCL-2 inhibitor. This compound antagonizes multiple anti-apoptotic proteins within the BCL-2 family, ultimately promoting apoptosis in malignant cells. Its ability to inhibit these proteins disrupts the survival mechanisms that cancer cells exploit, potentially restoring apoptotic pathways that are often dysregulated in cancerous tissues.

Potent inhibitor of the interaction between defective cullin neddylation protein DCN1 and NEDD8-conjugating enzyme UBC12 with IC50 of 11 nM. WS 383 blocks the DCN1-UBC12 interaction in a reversible manner, selectively inhibits Cul3/1 neddylation and induces accumulation of p21, p27, and NRF2 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.

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.

Inhibits RGS proteins, selective for RGS4

Activator of p53; inhibitor of NF-?B

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.