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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
2987 Results for "
target protein
" in MedChemExpress (MCE) Product Catalog:
Products (2987)
2987 Results for "target protein" in MCE Product Catalog:
669
669 Publications Verification
Target:
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ML385 is a potent and selective Nrf2 inhibitor with an IC50 of 1.9 μM. ML385 directly binds to the Neh1 domain of NRF2, interferes with the binding of the MAFG-NRF2 protein complex to the antioxidant response element (ARE) DNA sequence, thereby blocking the expression of downstream target genes of NRF2. ML385 can be used in studies related to adult T-cell leukemia, breast cancer, myocardial ischemia/reperfusion injury, non-small cell lung cancer, esophageal squamous cell carcinoma, head and neck squamous cell carcinoma, and lung squamous cell carcinoma .
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Category:
Quinones Plant Terpenoids Diterpenoids Salvia miltiorrhiza Bunge Extract Disease Research Fields Naphthalene Quinones Cancer Labiatae Extract
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40 Cited Publications
Synonyms: PKC412; CGP 41251
Midostaurin (PKC412; CGP 41251) is an orally active, reversible multi-targeted protein kinase inhibitor. Midostaurin inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM . Midostaurin also upregulates endothelial nitric oxide synthase (eNOS) gene expression. Midostaurin shows powerful anticancer effects .
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37 Cited Publications
Cat. No.: HY-16954
CAS No.: 1818885-28-7
Target:
PROTACs Epigenetic Reader Domain c-Myc Polo-like Kinase (PLK) CDK JAK STAT Pim Bcl-2 Family PAK Wnt β-catenin Caspase PARP Apoptosis Reactive Oxygen Species (ROS)
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ARV-825 is a BET protein PROTAC degrader that recruits cereblon, and it targets BRD2, BRD3, and BRD4 for degradation via the ubiquitin-proteasome pathway. ARV-825 downregulates c-MYC, PLK1, MYCN, CDK4/6, JAK2, pSTAT3/5, PIM1, and Bcl-xL, upregulates p21 and p27, and modulates H3K27Ac-mediated transcription, the G2/M checkpoint, the Wnt/β-catenin pathway, and amino acid transport pathways. ARV-825 induces G1 phase cell cycle arrest, caspase 3/PARP-mediated apoptosis, DNA damage, and reactive oxygen species (ROS) production, reduces mitochondrial respiration, and simultaneously inhibits cell proliferation, clonogenic growth, and cell migration. ARV-825 is used in research on gastric cancer, leukemia, neuroblastoma, and cholangiocarcinoma .
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36 Cited Publications
Cat. No.: HY-P0319
CAS No.: 402750-12-3
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36 Cited Publications
Cat. No.: HY-P0319A
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36 Cited Publications
Synonyms: RR82 hydrochloride
Research Areas:
Pyridostatin (RR82) hydrochloride is a G-quadruplex DNA stabilizing agent (Kd=490 nM) and can target DNA and RNA G4s in cells. Pyridostatin hydrochloride promotes growth arrest in human cancer cells by inducing replication- and transcription-dependent DNA damage. Pyridostatin hydrochloride targets the proto-oncogene Src. Pyridostatin hydrochloride reduced SRC protein levels and SRC-dependent cellular motility in human breast cancer cells .
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34 Cited Publications
FAPI-4 is a potent fibroblast activation protein (FAP) inhibitor for the targeting FAP. FAPI-4 can be used in cancer research. 68Ga-FAPI-4 PET/CT is a promising new diagnostic method for imaging various kinds of cancer, with good tumor-to-background contrast ratios .
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Takinib (EDHS-206) is an orally active and selective TAK1 inhibitor (IC50=9.5 nM), more than 1.5 log more potent than the second and third ranked targets, IRAK4 (120 nM) and IRAK1 (390 nM), respectively. Takinib is an inhibitor of autophosphorylated TAK1 that non-competitively binds within the ATP binding pocket. Takinib induces apoptosis following TNFα stimulation in cell models of rheumatoid arthritis and metastatic breast cancer. Takinib is also a P. falciparum protein kinase 9 (PfPK9) inhibitor (KD(app) of 0.46 μM) .
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30 Cited Publications
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ARV-771 is a BET PROTAC degrader, with Kd values of 34, 4.7, 8.3, 7.6, 9.6 and 7.6 nM against BRD2 (1), BRD2 (2), BRD3 (1), BRD3 (2), BRD4 (1) and BRD4 (2) , respectively. ARV-771 inhibits the transcription of AR/AR-v7 and its downstream target genes. By degrading BRD4 protein, ARV-771 enhances the sensitivity of prostate cancer cells to ferroptosis, suppresses cancer cell viability, and induces apoptosis. ARV-771 downregulates the levels of BRD4, c-MYC and AR-V7 in tumor tissues and inhibits tumor tissue growth. ARV-771 can be used in prostate cancer-related research .
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26 Cited Publications
Synonyms: 2-Bromopalmitic acid; 2-Bromopalmitate
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2-Bromohexadecanoic acid (2-Bromopalmitate; 2-BP) is a palmitoylation inhibitor targeting DHHC (Asp-His-His-Cys) protein palmitoyltransferase. 2-Bromohexadecanoic acid inhibits palmitoylation of GSDME-C during pyroptosis and inhibits BAK/BAX-Caspase 3-GSDME pathway-mediated pyroptosis .
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25 Cited Publications
Synonyms: GSK 525762C; I-BET 762 besylate
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Molibresib besylate (GSK 525762C; I-BET 762 besylate) is an orally active pan-BET inhibitor that targets and binds to BRD2, BRD3, BRD4 and BRDT. By competitively occupying acetylated lysine binding sites, Molibresib besylate disrupts the interaction between BET proteins and chromatin, thereby effectively inhibiting MYC expression and target gene transcription. Molibresib besylate exhibits broad antiproliferative activity, which not only inhibits cancer cell growth and induces growth arrest, but also downregulates mitosis-related genes and upregulates the level of p-ERK1/2. When combined with MEK inhibitors, Molibresib besylate shows a significant synergistic effect, reduces tumor burden in mouse models of leukemia, modulates the immune microenvironment and prolongs survival. Molibresib besylate is widely applicable to research related to acute myeloid leukemia, multiple myeloma, triple-negative breast cancer, small-cell lung cancer and various advanced refractory solid tumors .
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17 Cited Publications
Eeyarestatin I, a potent endoplasmic reticulum-associated protein degradation (ERAD) inhibitor, is a potent protein translocation inhibitor. Eeyarestatin I inhibits Sec61 translocon. Eeyarestatin I targets the p97-associated deubiquitinating process (PAD) and inhibits atx3-dependent deubiquitination. Eeyarestatin I interferes at a step prior to proteasomal degradation. Eeyarestatin I induces cell death via the proapoptotic protein NOXA and has anticancer effects .
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16 Cited Publications
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HLY78, a Lycorine (HY-N0288) derivative, is a potent activator of the Wnt/β-catenin signaling pathway. HLY78 targets the DIX domain of Axin and promotes the Axin-LRP6 (lipoprotein receptor-related protein 6) association, thus promoting LRP6 phosphorylation and Wnt signal transduction. HLY78 can be used for subarachnoid hemorrhage (SAH) research .
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16 Cited Publications
Cat. No.: HY-16657
CAS No.: 163847-77-6
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TAPI-1 is a broad-spectrum MMP inhibitor and NF-κB p65 inhibitor that targets ADAM17/TACE, ADAM10 and other proteins. TAPI-1 reduces the proteolytic cleavage of membrane-bound TNF-α, decreases TNF-α levels, inhibits NF-κB pathway activation, and downregulates profibrotic markers. TAPI-1 reduces the proportion of proinflammatory immune cells, alleviates cardiac and airway fibrosis, and improves cardiac function after myocardial infarction. Meanwhile, TAPI-1 inhibits the viability, migration and invasion of esophageal squamous cell carcinoma cells, enhances the chemosensitivity of Cisplatin (HY-17394), induces apoptosis, and shows low toxicity to normal esophageal epithelial cells. TAPI-1 can be widely used in studies related to myocardial infarction-induced heart failure, severe traumatic tracheal stenosis, esophageal squamous cell carcinoma and other conditions .
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Category:
Plant Withania somnifera Extract Other Families Extract Disease Research Fields Inflammation/Immunology Solanaceae Extract Steroids
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14 Cited Publications
Synonyms: Dioleoylphosphatidylethanolamine; 1,2-Dioleoyl-sn-glycero-3-phosphoethanolamine
Target:
Liposome Endogenous Metabolite ACSL Family Amino acid Transporter Ferroptosis Glutathione Peroxidase
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DOPE (Dioleoylphosphatidylethanolamine; 1,2-Dioleoyl-sn-glycero-3-phosphoethanolamine) is an orally active inhibitor of ferroptosis with anti-inflammatory and intestinal barrier maintenance activities. DOPE regulates the expression of ACSL4, SLC7A11 and GPX4 to restore the redox system balance, thereby reducing the levels of lipid peroxides, iron ions and intestinal inflammatory factors (IL-1β and IL-6). DOPE promotes the migration and proliferation of intestinal epithelial cells and increases the level of tight junction proteins; it also destabilizes endosomal membranes, mediates the conjugation of RVG peptides with mesenchymal stem cell-derived exosomes to enhance brain targeting. DOPE can be applied to research related to neonatal necrotizing enterocolitis and Alzheimer's disease .
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13 Cited Publications
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Autophinib is a potent, selective autophagy inhibitor with IC50s of 90 nM and 40 nM for starvation- and Rapamycin-induced autophagy, respectively. Autophinib is also an ATP competitive Vacuolar Protein Sorting 34 (VPS34) inhibitor with an IC50 of 19 nM. Autophinib inhibits autophagy induced by starvation or Rapamycin by targeting VPS34 .
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13 Cited Publications
Synonyms: GX15-070 Mesylate
Target:
Obatoclax Mesylate (GX15-070 Mesylate), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a Ki of 220 nM for BCL-2 . Obatoclax Mesylate induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax Mesylate has anti-cancer and broad-spectrum antiparasitic activity .
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Obatoclax (GX15-070), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a Ki of 220 nM for BCL-2 . Obatoclax induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax has anti-cancer and broad-spectrum antiparasitic activity .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
