Modulatore dell'interazione proteina-proteina

<p>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.</p>

<p>Inhibits interaction between PD1 and PDL1 immune checkpoint proteins</p>

<p>Formyl peptide receptor-1 (FPR-1) antagonist</p>

Iguratimod is a drug that is used to treat autoimmune and inflammatory conditions such as rheumatoid arthritis. This drug works by suppressing the activity of inflammatory cells and cytokines such as interleukin-1 and tumor necrosis factor-alpha (TNF-alpha). By reducing the levels of these cytokines, Iguratimod helps to alleviate inflammation and joint damage associated with conditions like rheumatoid arthritis.

<p>Anti-microtubular agent; antineoplastic</p>

<p>Microtubule stabilizer; natural polyketide compound; antineoplastic</p>

<p>Gap-junction modulator; anti-migraine agent</p>

<p>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.</p>

<p>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.</p>

<p>Inhibits actin polymerization</p>

<p>Inhibits the mitochondrial outer mebrane protein mitoNEET, anti-leukaemic</p>

<p>(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.</p>

<p>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.</p>

<p>Racemic mixture of AMG 510</p>

<p>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.</p>

<p>Docetaxel is an antineoplastic agent that is used to treat various cancers such as breast and prostate cancer. This drug interferes with the normal function of microtubule growth. It is an anti-mitotic drug used in chemotherapy. Research has shown that this drug also induces programmed cell death in cancer cells.</p>

<p>Autophagy inhibitor that selectively targets the StART domain of GRAMD1A</p>

<p>Inhibitor of BET bromodomain; antineoplastic</p>

<p>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.</p>

<p>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.</p>

<p>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.</p>

<p>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.</p>

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

<p>Activates NRF2 signalling</p>

<p>Reversible inhibitor of RGS proteins</p>

<p>KRAS G12C inhibitor</p>

<p>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.</p>

<p>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.</p>

<p>Microtubule disrupter; anti-mitotic drug; anti-cancer alkaloid</p>

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

<p>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.</p>

<p>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.</p>

<p>Inhibitor of transcriptional coactivator PGC-1a; anti-diabetic agent</p>

<p>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.</p>

<p>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.</p>

<p>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.</p>

<p>Inhibitor of BET bromodomain</p>

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.

<p>Antagonist of proto-oncogene MDM2 and its interaction with p53</p>

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

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.

<p>Promotes binding of vWf to glycoproteins on platelets, inducing aggregation</p>

<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>