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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
1618 Results for "
Covalent
" in MedChemExpress (MCE) Product Catalog:
Products (1618)
1618 Results for "Covalent" in MCE Product Catalog:
Cat. No.: HY-156052
CAS No.: 2077164-48-6
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CN-716 dihydrochloride is a reversible covalent flavivirus NS2B·NS3 protease inhibitor with antiviral activity. CN-716 dihydrochloride effectively inhibits the replication of dengue virus (DENV2), West Nile virus (WNV) and Zika virus (ZIKV). The IC50 values of CN-716 dihydrochloride against the proteases of the above three viruses are 0.066 μM, 0.11 μM and 0.25 μM, respectively, while the Ki values against the same proteases are 0.051 μM, 0.082 μM and 0.04 μM, respectively. CN-716 dihydrochloride can be used to study the infection mechanisms of dengue fever, West Nile fever and Zika virus infection .
Cat. No.: HY-159852
CAS No.: 2971769-60-3
BBO-10203 is a potent inhibitor of PI3Kα and KRAS G12C, selectively and covalently binding to Cys242 in the RAS-Binding Domain of PI3Kα, and inhibiting both the GTP-bound and GDP-bound states of KRAS G12C with an IC50 of 0.031 nM and an EC50 of 0.02 nM. BBO-10203 disrupts the interaction between RAS isoforms and PI3Kα, leading to the inhibition of RAS-mediated PI3Kα activation, and reduces pERK expression, cell growth, and induces G1 arrest and apoptosis. BBO-10203 can be used for the research of breast cancer, colorectal cancer, and non-small cell lung cancer .
Cat. No.: HY-165424
CAS No.: 3036456-18-2
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Cat. No.: HY-175292
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EGFR WT/T790M-IN-3 is an irreversible covalent EGFR WT and EGFR T790M inhibitor with IC50s value of 28.1 and 24.6 nM. EGFR WT/T790M-IN-3 hampers tubulin polymerization through IC50 value of 5.1 μM. EGFR WT/T790M-IN-3 shows significant anti-proliferative effects on HCT116 and T47D cells, with IC50 values of 3.12 and 4.12 μM, respectively. EGFR WT/T790M-IN-3 can be used for the study of cancers such as non-small cell lung cancer, colon cancer and breast cancer .
Cat. No.: HY-175756
CAS No.: 2901804-87-1
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SMARCA2/4 degrader-1 is a SMARCA2/4 molecular glue degrader with a DCAF16 EC50 of 110 nM. SMARCA2/4 degrader-1 covalently adducts at cysteine to form a ternary complex with SMARCA2/4 and recruits CUL4 DCAF16 and CRL1 FBXO22 E3 ligase complexes. SMARCA2/4 degrader-1 induces ubiquitination and proteasomal degradation of SMARCA2/4. SMARCA2/4 degrader-1 can be used for research of SMARCA4-deficient malignancies, non-small cell lung cancer (NSCLC), and colorectal cancer .
Cat. No.: HY-176239
PROTAC PI3Kδ degrader-1 is a Lysine-targeted covalent PI3Kδ PROTAC degrader with a DC50 of 3.98 nM. PROTAC PI3Kδ degrader-1 has a potent antiproliferative activity and selective PI3Kδ inhibition (IC50: 8 nM). PROTAC PI3Kδ degrader-1 also significantly degrades p-AKT, induces cell cycle arrest in G1 phase and prompts cell apoptosis and autophagy. PROTAC PI3Kδ degrader-1 effectively inhibits the tumor growth in SU-DHL-6 xenograft mice model .
Cat. No.: HY-179293
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SARS-CoV-2 PLpro-IN-3 (Compound 15) is a covalent inhibitor of the SARS-CoV-2 papain-like protease (PLpro), with an IC50 of 25 nM. SARS-CoV-2 PLpro-IN-3 has similar inhibitory activity against SARS-CoV PLpro (IC50 = 59 nM), but shows no inhibitory effect on human ubiquitin-specific protease 7 (USP7). The EC50 of SARS-CoV-2 PLpro-IN-3 in inhibiting SARS-CoV-2 replication in cells is 96 nM, significantly reducing the viral titer and viral RNA levels. SARS-CoV-2 PLpro-IN-3 can be used for studying SARS-CoV-2 drug resistance mutations .
Cat. No.: HY-180561
CAS No.: 3076807-15-0
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WWQ-03-012 is a selective DESI2 inhibitor with an IC50 of 47.3 nM. WWQ-03-012 binds covalently to DESI2, blocks its enzymatic activity, and inhibits DESI2-mediated deSUMOylation, deubiquitination and stabilization of mutant JAK2, thereby promoting the complete degradation of mutant JAK2 via the intracellular ubiquitin-proteasome system and inducing apoptosis, while exerting no significant effect on wild-type JAK2. WWQ-03-012 can be used for research on myeloproliferative neoplasms (MPN) and secondary acute myeloid leukemia (sAML), especially for hematological malignancies carrying the JAK2-V617F mutation and those resistant to Ruxolitinib (HY-50856) .
Cat. No.: HY-180814
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SKF-83566-PEG1-pomalidomide is an anti-tumor agent and is formed by the covalent connection of SKF-83566 (HY-103430A) (dopamine D1 receptor antagonist) and Pomalidomide (HY-10984) (immunomodulatory agent). SKF-83566-PEG1-pomalidomide can inhibit cancer cells invasion, migration and colony formation. SKF-83566-PEG1-pomalidomide can inhibit tumor growth and angiogenesis in MDA-MB-231 cell chicken embryo chorioallantoic membrane (CAM) xenograft model. SKF-83566-PEG1-pomalidomide can be used for research of breast cancer .
Cat. No.: HY-181482
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A1480LS is a peripherally restricted, orally active covalent and irreversible inhibitor of DAGLα and DAGLβ, with IC50 values of 6 nM and 4 nM against human targets, respectively, and IC50 values ≤15 nM across mouse, rat, dog, monkey and human systems. A1480LS reduces the levels of 2-arachidonoylglycerol, arachidonic acid, and cyclooxygenase- and lipoxygenase-derived eicosanoids. A1480LS inhibits injury-induced production of 2-arachidonoylglycerol and arachidonic acid in the peripheral sciatic nerve, and suppresses the responses of high-threshold and wide-dynamic-range-like dorsal horn neurons to mechanical stimulation. A1480LS alleviates pain behaviors in rat models of inflammatory pain, neuropathic pain and chemotherapy-induced peripheral neuropathy .
Cat. No.: HY-183723
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GAA-4OH is a potent and irreversible dihydroceramide desaturase-1 (DES1) inhibitor with an IC50 of 0.6 μM and a Ki of 139.5 nM. GAA-4OH undergoes oxidation to form a reactive iminoquinone that covalently blocks DES1’s catalytic cavity, causing permanent enzyme inactivation. GAA-4OH modulates sphingolipid balance by reducing ceramide-to-dihydroceramide ratios in liver tissue. GAA-4OH improves liver steatosis, inflammation, fibrosis, and reduces pro-inflammatory and pro-fibrogenic gene expression. GAA-4OH can be used for the research of metabolic dysfunction-associated steatotic liver disease (MASLD) .
Cat. No.: HY-187338
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CRBN ligand-908 is a cereblon (CRBN) ligand and also a HaloTag-binding degrader. CRBN ligand-908 competes with fluorescent lenalidomide ligands for binding to full-length CRBN protein. CRBN ligand-908 contains a chlorohexyl group that covalently reacts with HaloTag fused to target proteins. CRBN ligand-908 induces degradation of HaloTag-fused FAK, endogenous MARC1, and BRD4 proteins. CRBN ligand-908 is a proteasome- and Cullin-dependent degrader. CRBN ligand-908 does not induce degradation of the novel CRBN substrates GSPT1, SALL4, or CSNK1α. CRBN ligand-908 can be used to synthesize PROTACs, such as HaloPROTAC 4 (HY-187337) .
Cat. No.: HY-187459
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Topoisomerase I-IN-23 is a topoisomerase I inhibitor with anticancer activity. Topoisomerase I-IN-23 competitively binds to the hydrophobic pocket at the Topo I-DNA interface, stabilizes the covalent DNA-Topo I complex, downregulates Topo I protein expression in a concentration-dependent manner, induces S-phase cell cycle arrest in tumor cells, regulates the expression of apoptosis-related proteins Bax, Bcl-2 and cleaved caspase-3 to trigger apoptosis, and inhibits the migration and invasion of tumor cells. Topoisomerase I-IN-23 exhibits in vivo antitumor efficacy in xenograft models. Topoisomerase I-IN-23 can be used in research related to colorectal cancer, lung cancer and hepatocellular carcinoma .
Cat. No.: HY-187684
CAS No.: 3054389-11-3
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FR-027 is an orally active, blood-brain barrier permeable XPO1 inhibitor with an EC50 value of 54-69 nM in human cells. FR-027 covalently modifies Cys528 of XPO1 via nucleophilic aromatic substitution, maintaining the nuclear export signal binding groove of XPO1 in a closed conformation to block the nuclear export process, and inhibits XPO1 function without inducing its protein degradation. FR-027 promotes cancer cell apoptosis and inhibits the growth of hematological and solid tumor cells. FR-027 can be used in research related to acute lymphoblastic leukemia, ovarian cancer, glioblastoma, and primary central nervous system lymphoma .
Cat. No.: HY-188168
CAS No.: 99630-95-2
Synonyms: FMMT
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MDL 72394 (FMMT) is an orally active, blood-brain barrier-penetrant amino acid-based prodrug compound. MDL 72394 is decarboxylated by aromatic L-amino acid decarboxylase to generate the active metabolite MDL 72392 (HY-182727), which is a covalent irreversible MAO inhibitor. MDL 72394 is transported into the brain and synaptosomes via the L-neutral amino acid transport system and the norepinephrine transporter. MDL 72394 selectively inhibits MAO in noradrenergic and dopaminergic neurons without inhibiting serotonergic neurons. MDL 72394 increases hypothalamic extracellular 5-HT, tissue 5-HT, and pineal melatonin biosynthesis, and decreases 5-HIAA. MDL 72394 can be used in research related to MAO-mediated diseases, such as depression .
Cat. No.: HY-189062
ZJC-11 is a CDK7 inhibitor with an IC50 of 5.4 nM. ZJC-11 binds covalently to CDK7, inhibits CDK7-dependent phosphorylation of RNAPII at Ser2, Ser5 and Ser7 sites, and suppresses transcriptional processes. ZJC-11 acts as a cell cycle inhibitor, inhibits the G2/M checkpoint pathway, and induces G2/M phase arrest. ZJC-11 induces DNA damage-driven cellular senescence and cell death. ZJC-11 exhibits antiproliferative activity against triple-negative breast cancer both in vitro and in vivo. ZJC-11 can be used for research related to triple-negative breast cancer
Cat. No.: HY-189433
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Keap1-Nrf2 PPI-IN-2 is a Keap1-Nrf2 PPI inhibitor with an EC50 of 14.2 μM. Keap1-Nrf2 PPI-IN-2 covalently binds to Keap1 cysteine residues through its electrophilic itaconate moiety, disrupts the Keap1-Nrf2 protein-protein interaction, releases Nrf2, and promotes its nuclear translocation and antioxidant gene expression, thereby reducing ROS and inhibiting IL-13 production . Keap1-Nrf2 PPI-IN-2 can be used for research on atopic dermatitis .
Cat. No.: HY-D3573
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AF488 C5 Maleimide is a thiol-reactive Fluorescent dye used to label target proteins and bacterial structures. AF488 C5 Maleimide irreversibly forms covalent thioether conjugates with cysteine thiol groups. AF488 C5 Maleimide stabilizes pre-formed globular low-molecular-weight Tau protein oligomers by blocking cysteine-dependent tau protein aggregation, allowing observation of the internalization process of tau protein oligomers into neuronal cells via confocal microscopy. AF488 C5 Maleimide can label cysteine-modified pili; the outer membrane permeability varies among different bacterial species, allowing imaging via epifluorescence microscopy using a FITC filter set .
Cat. No.: HY-P10819
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Cat. No.: HY-P11306
CAS No.: 247068-92-4
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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
