Modulateur d'interaction protéine-protéine

Efficient chemiluminescent NH2-coupling reagent for detection of proteins

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

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.

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.

KRAS G12C inhibitor

A potent inhibitor of STING protein (stimulator of interferon genes), a protein that partakes in intracellular DNA sensing pathway.  H 151 blocks palmitoylation of STING, which is required for the formation of multimeric complexes for recruiting downstream signalling molecules. Inhibition of STING by H 151 reduces pro-inflammatory cytokine synthesis.

Racemic mixture of AMG 510

Promotes binding of vWf to glycoproteins on platelets, inducing aggregation

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. Obatoclax mesylate has been investigated primarily in the context of its cytotoxic effects against various forms of cancer, including hematological malignancies and solid tumors. Preclinical studies have highlighted its potential in inducing cell death selectively in cancer cells, providing a therapeutic avenue for targeting drug-resistant cellular populations. While it holds promise, its clinical application requires further investigation to fully understand its efficacy and safety profile.

Activates NRF2 signalling

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.

Gap-junction modulator; anti-migraine agent

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.

(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. The compound has been primarily investigated for its potential therapeutic applications in a range of neurodegenerative diseases, including Amyotrophic Lateral Sclerosis (ALS), Niemann-Pick disease type C, and Inclusion Body Myositis. Its ability to upregulate HSPs enables it to assist in the stabilization of protein structures, thereby mitigating cellular stress and turnover, which are critical factors in disease progression. Currently, (2R)-Arimoclomol maleate is under various phases of clinical trials, assessing its efficacy and safety. Its innovative approach in combating dysregulated proteostasis presents it as a candidate of significant interest within the field of neurodegenerative disease research.

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.

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.

HDM2 antagonist; inhibits interaction between MDM2 and p53

Inhibitor of NLRP3 inflammasome and suppressor of the inflammatory cytokine IL-1β secretion. The compound was tested in diabetic mice and was shown to decrease the incidence of cardiac arrythmias, which are common secondary complications in diabetes mellitus. MCC 950 has potential to reverse diabetes-induced pathologies in cardiac electrophysiology.

Reversible inhibitor of RGS proteins

A co-inducer of HSP that acts through heat shock factor 1 (HSF1) in cells undergoing cellular stress. Has therapeutic potential in motor neuron degenerative diseases. Potential treatment for liposomal storage disorders, such as Niemann-Pick disease type C.