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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
2735 Results for "
complexes
" in MedChemExpress (MCE) Product Catalog:
Products (2735)
2735 Results for "complexes" in MCE Product Catalog:
Cat. No.: HY-169093
CAS No.: 2768610-97-3
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MS41 is a ENL PROTAC degrader with a DC50 of 3.50 nM. MS41 recruits the VHL E3 ubiquitin ligase, triggers ENL degradation via the ubiquitin-proteasome system, and simultaneously induces AF9 degradation. MS41 reduces the chromatin occupancy of ENL-associated transcription elongation complexes, suppresses oncogene expression, and activates differentiation gene expression. MS41 inhibits leukemia cell growth and induces cell cycle arrest and apoptosis. MS41 inhibits leukemia progression in xenograft mouse models. MS41 can be used for research on mixed lineage leukemia-rearranged leukemia and nephroblastoma .
Cat. No.: HY-169264
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SJYHJ-026 is a PROTAC degrader targeting PXR, with a DC50 of 86.6 nM in SNU-C4 HiBiT-PXR KI cells. SJYHJ-026 shows higher selectivity for PXR over CAR, VDR, FXR, LXRα and LXRβ, and can bind to VHL to form a PXR-SJYHJ-026-VHL complex, inducing proteasomal degradation of PXR. SJYHJ-026 blocks agonist-induced PXR-mediated gene expression (including CYP3A4) and reduces basal PXR activity at the CYP3A4 promoter. SJYHJ-026 can be used for the research of colorectal cancer .
Cat. No.: HY-170557
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Topoisomerase IIα-IN-10 (Compound 13r) is an inhibitor of Topoisomerase IIα. It binds to the active site of DNA when complexed with Topoisomerase IIα, and this binding is stabilized through interactions with DNA base pairs and amino acid residues. Topoisomerase IIα-IN-10 can induce Apoptosis by intercalating DNA and inhibiting Topoisomerase IIα, thereby disrupting the mitochondrial membrane potential and inhibiting the growth of HCT116 cell lines, with an IC50 of 4.37 μM against HCT116 cells. Topoisomerase IIα-IN-10 can be used for research in the field of cancer treatment .
Cat. No.: HY-172777
CAS No.: 3052432-15-9
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SDH-IN-25 is a succinate dehydrogenase (SDH) inhibitor (IC50 = 4.82 mg/L). SDH-IN-25 exhibited broad-spectrum and potent antifungal activity. SDH-IN-25 mimics the interaction pattern of commercial fungicide Fluxapyroxad (HY-135549) through binding to SDH amino acid residues (TRP173, TYR58, and ARG43). SDH-IN-25 can induce hyphal morphology, interfere with respiratory metabolism by binding to complex II, generate reactive oxygen species (ROS), and affect mitochondrial membrane potential (MMP) in mycelia. SDH-IN-25 can be studied in research for agricultural disease control .
Cat. No.: HY-173422
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MS2133 is a VHL-recruiting DOT1L PROTAC degrader. MS2133 possesses antiproliferative activity with a human DOT1L IC50 of 4.6 nM, forms a ternary complex with DOT1L and VHL E3 ligase to drive DOT1L ubiquitination and subsequent proteasomal degradation without affecting DOT1L mRNA transcription, inhibits the proliferation of mixed lineage leukemia-rearranged leukemia cells and downregulates H3K79Me2, restrains proliferation of both tumor and normal cells but lacks cytotoxicity against normal cells, and can be used for the research of mixed lineage leukemia-rearranged leukemia .
Cat. No.: HY-173499
CAS No.: 3077339-88-6
HLDA-212 is a non-covalent RIPTAC that targets FKBP (target protein, TP) and multiple CDK (effector protein, EP). HLDA-212 binds to FKBP and CDK to form a stable ternary complex (TP:RIPTAC:EP), and induces cell death by blocking FKBP function. HLDA-212 selectively inhibits the proliferation of CDK-expressing cells and accumulates in CDK-expressing cells in a CDK-dependent manner. HLDA-212 exhibits antiproliferative activity in 293_HFL cells (with a GI50 of 0.011 μM). HLDA-212 holds promise for the treatment of cancers with high FKBP expression .
Cat. No.: HY-174371
CAS No.: 3032576-92-1
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INNO-220 is an orally active, CRBN-dependent molecular glue degrader targeting CK1α. INNO-220 induces cell cycle arrest at G0/G1 phase and triggers apoptosis by degrading CK1α. INNO-220 disrupts the assembly and function of the CARD11/BCL10/MALT1 complex, thereby inhibiting NF-κB signaling in stimulated T cells and lymphoma cells that harbor an activating mutation in CARD11. INNO-220 provides a new direction for lymphoma research.
Cat. No.: HY-174439
CAS No.: 667882-55-5
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Nsp12-IN-2 (Compound 8), the triphosphate metabolite of 4'-thiouridine (HY-W113081), is a SARS-CoV-2 Nsp12 inhibitor. Nsp12-IN-2 inhibits the RNA-dependent RNA polymerase (RdRp) activity of the SARS-CoV-2 Nsp12-Nsp7-Nsp8 complex, terminates RNA synthesis and also blocks the RNAylation and NMPylation of Nsp9. Nsp12-IN-2 is promising for research of infections caused by SARS-CoV-2, other coronaviruses, and other RNA viruses .
Cat. No.: HY-175469
CAS No.: 2894060-67-2
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VNT-101 is an orally active influenza A (IAV) inhibitor. VNT-101 disrupts NP-NP PPI to block NP oligomerization and destabilize the viral ribonucleoprotein (RNP) complex, with potent antiviral activity across multiple influenza A subtypes. VNT-101 exhibits EC50 values of 4-5 nM in cellular cytopathic effect (CPE) assay, 4-8 nM in neuraminidase (NA) assay, and 21-45 nM in RNP assay. VNT-101 demonstrates robust in vivo antiviral efficacy in mice infected with lethal H1N1 virus. VNT-101 can be used for the study of influenza A infection .
Cat. No.: HY-178028
CAS No.: 3113303-04-8
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PRMT5-IN-53 is a gut-restricted and orally active PRMT5 inhibitor with pIC50s of ≥ 9.7 against hPRMT5 and mPRMT5. PRMT5-IN-53 binds to the PRMT5:MEP50 complex with a KD of 11.3 pM. PRMT5-IN-53 effectively inhibits PRMT5 locally in the intestines of mice, significantly reducing the number and area of polyps, while avoiding systemic hematological toxicity (such as anemia, neutropenia). PRMT5-IN-53 can be used for the study of colorectal cancer especially for familial adenomatous polyposis (FAP) .
Cat. No.: HY-181883
KRAS-IN-55 is a pan-KRAS inhibitor with IC50 values of 4.3, 9.6 and 1.6 nM against KRAS G12C, KRAS G12D and KRAS G12V, respectively. KRAS-IN-55 induces the formation of a new binding pocket on KRAS, thereby forming a high-affinity ternary complex with cyclophilin A (CYPA), inhibiting the interactions of KRAS with downstream effectors RAF and PI3K, and blocking oncogenic MAPK and PI3K signaling pathways. KRAS-IN-55 is applicable to cancer research such as colorectal cancer and non-small cell lung cancer .
Cat. No.: HY-182799
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IBA-12 is a IKZF2 molecular glue/PROTAC degrader with a DC50 of 276.2 nM (Jurkat cells) and 461.8 nM (Mino cells), and an IC50 of 179.9 nM. IBA-12 binds to the canonical tryptophan triad pocket of CRBN to form a ternary complex with IKZF2. IBA-12 induces IKZF2 degradation mediated by the CRBN-dependent ubiquitin-proteasome system, with no effect on other CRBN substrates. IBA-12 induces the production of interleukin-2 (IL-2) through degrading IKZF2. IBA-12 is applicable to cancer immunology research .
Cat. No.: HY-182800
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IBA-11 is a selective CRBN-dependented CK1α molecular glue degrader. IBA-11 binds to the canonical tri-tryptophan pocket of CRBN, forming a ternary complex with CK1α to mediate its degradation. IBA-11 induces CRBN-dependent ubiquitin-proteasome system-mediated degradation of CK1α. IBA-11 exhibits cytotoxicity against cancer cells. IBA-11 demonstrates in vitro metabolic stability in rat liver microsomes and minimal hERG inhibition. IBA-11 can be used for the research of cancer, such as acute myeloid leukemia .
Cat. No.: HY-183674
CAS No.: 3096958-11-8
MEK-IN-10 is an orally active pan-MEK/RAF non-degrading molecular glue with an IC50 of 782 nM against human MEK1. MEK-IN-10 blocks the phosphorylation of MEK and ERK, induces and stabilizes the MEK1-RAF complex, and disrupts the RAS-MAPK signaling pathway. MEK-IN-10 induces apoptosis in cancer cells and arrests cells at the G0/G1 phase. MEK-IN-10 induces tumor growth inhibition in mouse xenograft models. MEK-IN-10 can be used in the research of RAS-driven cancers, such as colorectal cancer and pancreatic cancer .
Cat. No.: HY-184248
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FM-74-103 is a selective GSPT1 PROTAC degrader and broad-spectrum antiviral agent. FM-74-103 recruits GSPT1 to the Cereblon E3 ligase to form a ternary complex, thereby driving GSPT1 ubiquitination and proteasomal degradation. FM-74-103 inhibits the replication of IAV, SARS-CoV-2 and CMV (including Nucleozin (HY-50001)-resistant influenza A virus). FM-74-103 can be used in research related to influenza A virus infection, SARS-CoV-2 infection and cytomegalovirus infection .
Cat. No.: HY-184923
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PROTAC BRD4 Degrader-48 is a BRD4 degrader with a Kd of 0.69 μM for human BRD4 and a DC50 of 0.21 μM. PROTAC BRD4 Degrader-48 binds to BRD4 and GID4 to form a ternary complex, and induces ubiquitination and degradation of BRD4 via the ubiquitin-proteasome pathway. PROTAC BRD4 Degrader-48 inhibits proliferation and migration of tumor cells, blocks tumor growth, and maintains degrading activity even in VHL- and CRBN-deficient models. PROTAC BRD4 Degrader-48 can be used in studies related to renal cell carcinoma .
Cat. No.: HY-184968
CAS No.: 3108071-48-0
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PROTAC NSD2 degrader-1 is a PROTAC degrader that selectively targets NSD2, with a DC50 of 0.37 μM. PROTAC NSD2 degrader-1 induces selective degradation of long and short isoforms of NSD2 containing the PWWP1 domain by forming a ternary complex with FBXO22. NSD2 degradation mediated by PROTAC NSD2 degrader-1 depends on the ubiquitin-proteasome system and the neddylation pathway. PROTAC NSD2 degrader-1 can be used in cancer-related research such as non-small cell lung cancer, multiple myeloma and prostate cancer .
Cat. No.: HY-187350
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LRPPRC-IN-1 is a LRPPRC inhibitor. LRPPRC-IN-1 exerts dual effects of inhibiting LRPPRC activity and inducing its degradation by binding to the RNA-binding domain of LRPPRC. LRPPRC-IN-1 downregulates the expression of mitochondrial OXPHOS complex subunits and ATP synthase, inhibits oxidative phosphorylation, reduces ATP production, suppresses the proliferation and colony formation of various cancer cells, and inhibits tumor growth in vivo. LRPPRC-IN-1 can be used in studies related to lung cancer, pancreatic cancer, breast cancer, esophageal cancer, colorectal cancer, lymphoma, melanoma, cervical cancer, ovarian cancer, and prostate cancer .
Cat. No.: HY-189057
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Anethole trithione derivative-1 is a derivative of Anethole trithione (HY-B1223), and also a regulator of sulfide:quinone oxidoreductase (SQR) and uncoupling protein 2 (UCP2), with mitochondrial uncoupling-inducing activity and neuroprotective activity. Anethole trithione derivative-1 mediates mitochondrial uncoupling via SQR-dependent reverse electron transport of complex I, ROS-dependent UCP2 activation, and reduction of mitochondrial membrane potential. Anethole trithione derivative-1 reduces brain damage and improves function in mouse models of ischemic and hemorrhagic stroke. Anethole trithione derivative-1 can be used in stroke research .
Cat. No.: HY-189143
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Xanthine oxidase-IN-24 is an orally active mixed-type inhibitor of xanthine oxidase, with an IC50 of 0.051 μM and a Ki of 0.162 μM. Xanthine oxidase-IN-24 interacts with both free xanthine oxidase and the xanthine-xanthine oxidase complex, and reduces uric acid production in vivo. In a rat model of hyperuricemia induced by Potassium oxonate (HY-17511), Xanthine oxidase-IN-24 dose-dependently lowers serum uric acid levels, improves renal function-related biochemical parameters such as creatinine and urea nitrogen, and alleviates histopathological damage to liver and kidney tissues. Xanthine oxidase-IN-24 can be used in the research of hyperuricemia .
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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
