Protein-Protein Interaction Modulator

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.

Inhibitor of BET bromodomain

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.

Inhibitor of transcriptional coactivator PGC-1a; anti-diabetic agent

Inhibitor of the Forkhead box M1 (FOXM1), an oncogene and a transcription factor regulating cell cycle progression, DNA damage repair and cell renewal. RCM 1 weakens the FOXM1 activity by inhibiting its nuclear localisation and increasing its degradation in proteasomes. The compound showed potential for asthma treatment since it inhibited goblet cell metaplasia and IL-13 signalling in mice.

Activater of the Nrf2 pathway and an inhibitor of the NF-κB pathway.  Possible applications have extended to anti-viral treatment of COVID-19.

Anti-microtubular agent; antineoplastic

Inhibitor of protein tyrosine phosphatase PTP1B

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.

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.

Tubulin binding agent; targets tumour vasculature

Inhibits the mitochondrial outer mebrane protein mitoNEET, anti-leukaemic

Heat shock protein 90 (HSP90) inhibitor

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. Rivaroxaban 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, our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

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.

Inhibitor of pan-sirtuins (IC50 = 15, 10, 33 µM for SIRT1, 2 and 3 respectively), by binding to the active catalytic site. Selectivity for sirtuins was demonstrated when tested for activity on a panel of kinases, nuclear receptors, ion channels, transporters and GPCRs.

Activator of p53; inhibitor of NF-?B

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.

Antagonist of proto-oncogene MDM2 and its interaction with p53

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.

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.

Autophagy inhibitor that selectively targets the StART domain of GRAMD1A

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.

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.

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

Inhibitor of BET bromodomain; antineoplastic

Inhibitor of Hsp90 chaperone protein; anti-neoplastic

Microtubule stabilizer; natural polyketide compound; antineoplastic

Inhibits N-Acetyl-mediated interaction between BE2M (E2 conjugating enzyme) and DCN1 (a component of E3 ligase complex). Also has inhibitory action on DCN2 and NEDD8 ubiquitin-like protein. Reduces anchorage-independent growth in DCN1-amplified cell line.

Microtubule-stabilizing agent; antineoplastic;

A calcium-binding protein S100A9 inhibitor with immunomodulatory activity that reduces pathology in experimental collagenase-induced osteoarthritis.