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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
319 Results for "
binding models
" in MedChemExpress (MCE) Product Catalog:
Products (319)
319 Results for "binding models" in MCE Product Catalog:
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2 Cited Publications
Cat. No.: HY-P99171
CAS No.: 1129435-60-4
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CSRM617 hydrochloride is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a Kd of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 hydrochloride induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 hydrochloride is well tolerated in the prostate cancer mouse model
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Sm4 is a selective and orally active SOX18 inhibitor. Sm4 inhibits SOX18-DNA binding (IC50 = 97.5 μM); Sm4 disrupts the SOX18-RBPJ protein-protein interaction (IC50 = 42.3 μM). Sm4 blocks SOX18 DNA binding, disrupts multiple SOX18 protein-protein interactions with RBPJ, DDX1, DDX17, ILF3, SOX7 and STAT1, modulates SOX18 chromatin binding dynamics. Sm4 exerts anti‑angiogenic and anti‑lymphangiogenic effects, reduces tumor vascular density, triggers vascular defects in zebrafish, prolongs survival in mouse metastatic cancer models. Sm4 can be used for the research of breast cancer .
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NVS-STG2 is a molecular glue that targets STINGbinding to pockets between adjacent STING dimer transmembrane domains, effectively acting as a molecular glue. NVS-STGI enhances the activity of cGAMP by inducing the formation of more abundant and larger oligomers. NVS-STG2 produces antitumor activity in animal models .
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1 Cited Publications
Synonyms: 1-{4-[2-(5-Methylfuran-2-yl)quinoline-4-carbonyl]piperazin-1-yl}ethan-1-one
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E1231 is an orally active activator of Sirtuin 1 (SIRT1) (EC50=0.83 μM), to modulate cholesterol and lipid metabolism. E1231 interactes with SIRT1 (KD=9.61 μM) and deacetylated liver X receptor-alpha (LXRα), and increases ATP-binding cassette transporter A1 (ABCA1) expression. E1231 also reduces atherosclerotic plaque development in ApoE -/- mice model. E1231 can be used for research in cholesterol and lipid disorder-related diseases .
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1 Cited Publications
Cat. No.: HY-P2460
CAS No.: 172485-26-6
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Serpin B9-IN-1 (BTCA) is an inhibitor that specifically targets Serpin B9 (SB9); SB9 is a natural inhibitor of granzyme B (GrB) , but may promote the metastasis of lung cancer cells into the bone marrow. SB9-overexpressing cancer cells promote proliferation and metastasis in an immune cell-dependent manner by binding to GrB. Inhibition of SB9 by Serpin B9-IN-1 significantly inhibits immunotherapy of lung cancer bone metastases in the caudal artery (CA) mouse model (LCBM) .
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Cefpirome (HR-810) sulfate is a cephalosporin antibiotic that can cross cell membranes and the blood-brain barrier. Cefpirome sulfate binds to penicillin-binding proteins with high affinity, thereby inhibiting bacterial cell wall synthesis. Cefpirome sulfate exhibits bactericidal and growth-inhibitory activities against Gram-negative bacteria, Gram-positive bacteria, and susceptible anaerobic bacteria (including some β-lactamase-producing strains) .
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1 Cited Publications
Cat. No.: HY-W181530
CAS No.: 790245-61-3
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NCT02 is a molecular glue degrader based on the E3 ubiquitin ligase DDB1 that targets CDK12 and its binding partner CCNK. NCT02 triggers the ubiquitination and proteasomal degradation of CCNK, thereby downregulating CDK12 protein levels and inhibiting its downstream signaling pathways. NCT02 can induce tumor cell apoptosis, arrest the cell cycle, and selectively inhibit the proliferation of colorectal cancer cells carrying TP53 defects or belonging to the consensus molecular subtype CMS4. NCT02 has the potential to inhibit tumor growth in in vitro and in vivo models .
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Synonyms: PROTAC AR-V7 degrader-2
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MTX-23 is a PROTAC degrader targeting androgen receptor splice variant 7 (AR-V7) and full-length androgen receptor (AR-FL), with DC50 values of 0.37 μM and 2 μM, respectively. MTX-23 binds to the DNA-binding domains of AR-V7 and AR-FL, recruits the VHL E3 ubiquitin ligase (E3 ubiquitin ligase) and induces their degradation. MTX-23 reduces the proliferation of prostate cancer cells, promotes their apoptosis (apoptosis), and also inhibits tumor growth in mouse models. MTX-23 can be used for the research of prostate cancer .
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1 Cited Publications
Cat. No.: HY-W195984
CAS No.: 1016340-64-9
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Z57346765 is an inhibitor that targets the ADP-binding pocket of PGK1, with a Kd of 20.9 μM for human PGK1, and exhibits anticancer activity. Z57346765 reduces the activity of the metabolic enzyme PGK1 during glycolysis, regulates lipid peroxidation and cancer cell proliferation, and promotes lipid peroxidation in cervical cancer cells. Z57346765 inhibits the proliferation of cervical cancer and clear cell renal cell carcinoma cells in xenograft mouse models, and induces the expression of genes associated with cell metabolism, DNA replication and cell cycle. Z57346765 is used in research related to cervical cancer, clear cell renal cell carcinoma and breast cancer .
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VVD-130037 (BAY-3605349) is a covalent molecular glue and allosteric NRF2 degrader. VVD-130037 covalently binds to KEAP1 and allosterically enhances the affinity of KEAP1-CUL3, promotes the formation of the active KEAP1-CUL3 E3 ligase complex, and thereby enhances the ubiquitination and degradation of NRF2. VVD-130037 exhibits KEAP1 target-binding activity both in in vitro systems and mouse models, and it can be used in research related to NRF2-dependent cancers, solid tumors harboring KEAP1 nonsense mutations and frameshift mutations, as well as advanced solid tumors .
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1-Oleoyl-sn-glycero-3-phosphocholine (18:1 Lyso PC), a lysophospholipid, is a GPR82 inhibitor. 1-Oleoyl-sn-glycero-3-phosphocholine abrogates constitutive Gi-coupled GPR82 activity, shifts active/inactive equilibrium to inactive, suppresses Gi protein activation, increases cAMP production, and decreases GTPγS binding to Gαi proteins. 1-Oleoyl-sn-glycero-3-phosphocholine contributes to adipocyte lipolysis regulation.1-Oleoyl-sn-glycero-3-phosphocholine exhibits reduced serum levels in mouse models of steatohepatitis, linked to hepatic Lpcat 1-4 up-regulation .
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1 Cited Publications
Cat. No.: HY-W725179
CAS No.: 2044520-06-9
VK-2019 is an orally bioavailable selective inhibitor of EBNA1. By binding to the protein-DNA interface to interfere with the recruitment and anchoring of the viral DNA replication machinery, VK-2019 effectively blocks the replication and proliferation of EBV in latently infected cells. VK-2019 reduces the copy number and gene expression level of Epstein-Barr virus in tumor cells, decreases the number of EBER-positive cells, and exhibits significant antiviral, immunomodulatory and antiproliferative activities. VK-2019 successfully inhibits tumor growth in EBV-dependent xenograft models. VK-2019 has favorable systemic exposure and acceptable safety profiles, and is widely used in research on advanced nasopharyngeal carcinoma and various EBV-associated cancers .
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1 Cited Publications
Cat. No.: HY-172158
CAS No.: 140481-05-6
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ALKBH5-IN-5 is a highly selective ALKBH5 (IC50 = 0.62 μM, Kd = 804 nM). ALKBH5-IN-5 disrupts ALKBH5 binding to m 6A-RNA and 6mA-DNA substrates. ALKBH5-IN-5 promotes differentiation, induces apoptosis, cause G2-M phase arrest and exerts strong antiproliferative effects in cancer cells. ALKBH5-IN-5 reduces TACC3 and MYC protein levels and increases cleaved caspase-3 levels. ALKBH5-IN-5 exerts antitumor activity in tumor xenograft mice models. ALKBH5-IN-5 can be used for the research of acute myeloid leukemia .
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Synonyms: Cycloartenol ferulate; Cycloartenol ferulic acid ester
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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
