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covalent+modification

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34

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24

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-B0671
    Vancomycin
    Maximum Cited Publications
    94 Publications Verification

    Bacterial Autophagy Antibiotic Infection Cancer
    Vancomycin is an antibiotic for the treatment of bacterial infections.
    Vancomycin
  • HY-16909
    Leptomycin B
    20+ Cited Publications

    CI 940; LMB

    CRM1 Fungal Antibiotic Infection Cancer
    Leptomycin B (CI 940; LMB) is a potent inhibitor of the nuclear export of proteins. Leptomycin B inactivates CRM1/exportin 1 by covalent modification at a cysteine residue. Leptomycin B is a potent antifungal antibiotic blocking the eukaryotic cell cycle .
    Leptomycin B
  • HY-N0191
    Andrographolide
    30+ Cited Publications

    Andrographis

    NF-κB SARS-CoV Influenza Virus Autophagy Parasite Infection Inflammation/Immunology Cancer
    Andrographolide is a NF-κB inhibitor, which inhibits NF-κB activation through covalent modification of a cysteine residue on p50 in endothelial cells without affecting IκBα degradation or p50/p65 nuclear translocation. Andrographolide has antiviral effects.
    Andrographolide
  • HY-P4153

    MK-0616 chloride

    PCSK9 Cardiovascular Disease
    Enlicitide chloride is an orally active inhibitor for PCSK9 that blocks the interaction between LPL receptor and PSCK9, with an IC50 of 2.5 nM. Enlicitide chloride can be used in the study of cardiovascular diseases such as atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, acute coronary syndrome or related cardiovascular and cardiometabolic disorders .
    Enlicitide chloride
  • HY-Y1353

    Biochemical Assay Reagents Others Metabolic Disease
    Di-tert-butyl dicarbonate (tBOC) is a covalent modification agent for hydroxyl groups (-OH) on the chitosan molecular chain. Di-tert-butyl dicarbonate selectively modifies chitosan and stabilizes the material structure through hydrophobic encapsulation. Di-tert-butyl dicarbonate reacts with the -OH groups of chitosan to form a hydrophobic layer, and in conjunction with triethylamine (TEA), removes trifluoroacetic acid (TFA) salts produced during the electrospinning process, preserving the nanofiber structure and high porosity of the membrane, and improving the material's cytocompatibility and mineralization-promoting ability. Di-tert-butyl dicarbonate can be used in research in the field of guided bone regeneration (GBR) .
    Di-tert-butyl dicarbonate
  • HY-128522

    Ras Cancer
    ARS-1323-alkyne is a covalent inhibitor probe that covalently binds to the Switch-II pocket (S-IIP) of the KRAS G12C mutant protein. ARS-1323-alkyne visualizes the covalent modification of KRAS G12C and quantitatively measures the binding efficiency of the inhibitor to the target. ARS-1323-alkyne can be used to validate the target occupancy of KRAS G12C inhibitors and the synergistic mechanism of combination therapy .
    ARS-1323-alkyne
  • HY-N0191R

    Andrographis (Standard)

    Reference Standards NF-κB SARS-CoV Influenza Virus Autophagy Parasite Infection Inflammation/Immunology Cancer
    Andrographolide (Standard) is the analytical standard of Andrographolide. This product is intended for research and analytical applications. Andrographolide is a NF-κB inhibitor, which inhibits NF-κB activation through covalent modification of a cysteine residue on p50 in endothelial cells without affecting IκBα degradation or p50/p65 nuclear translocation. Andrographolide has antiviral effects.
    Andrographolide (Standard)
  • HY-128661
    IDH1 Inhibitor 2
    4 Publications Verification

    Isocitrate Dehydrogenase (IDH) Metabolic Disease
    IDH1 Inhibitor 2 (compound 13) is a potent wild-type IDH1 inhibitor that exerts its activity through covalent modification of His315 with an IC50 value of 110 nM. IDH1 Inhibitor 2 can dose-dependently reduce the intracellular reduced glutamine metabolic flux, thereby affecting cellular metabolic homeostasis. IDH1 Inhibitor 2 can be used to study the role of IDH1 in cellular metabolic regulation and cancer development .
    IDH1 Inhibitor 2
  • HY-13943
    CNX-774
    2 Publications Verification

    Btk Cancer
    CNX-774 is an orally active, irreversible and selective BTK inhibitor, with an IC50 of < 1 nM. CNX-774 specifically targets Cysteine 481 of Btk for covalent modification .
    CNX-774
  • HY-P2265A

    SOS1 Ras Cancer
    SAH-SOS1A TFA is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A TFA binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM). SAH-SOS1A TFA directly and independently blocks nucleotide association. SAH-SOS1A TFA impairs KRAS-driven cancer cell viability and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .
    SAH-SOS1A TFA
  • HY-P2203
    SAHM1
    1 Publications Verification

    Notch Inflammation/Immunology
    SAHM1, a peptide mimetic of a dominant negative form of mastermind-like (MAML), inhibits canonical Notch transcription complex formation. SAHM1 can be used for the research of allergic airway inflammation in mice .
    SAHM1
  • HY-121539
    Supercinnamaldehyde
    1 Publications Verification

    TRP Channel Neurological Disease
    Supercinnamaldehyde is a potent transient receptor potential ankyrin 1 (TRPA1) activator with an EC50 value of 0.8 μM. Supercinnamaldehyde activates TRPA1 ion channels through covalent modification of cysteines .
    Supercinnamaldehyde
  • HY-119390

    DNA Methyltransferase Cancer
    AA-CW236 is a MGMT (O6-methylguanine DNA methyltransferase) inhibitor. AA-CW236 targets MGMT active site Cys145 for covalent modification .
    AA-CW236
  • HY-125273

    Fluorescent Dye Phosphoglycerate Dehydrogenase (PHGDH) Others
    DNS-pE is a 3-phosphoglycerate dehydrogenase (PHGDH) inhibitor with a Ki of 7.4 μM. DNS-pE selectively and irreversibly covalently modifies endogenous PHGDH in live mammalian cells, its vinyl sulfone moiety acts as a fluorescence quencher that becomes highly fluorescent upon covalent modification of PHGDH. DNS-pE can be used as a fluorescent dye for live-cell imaging .
    DNS-pE
  • HY-P1368
    Stressin I
    1 Publications Verification

    Cyclo(31-34)[DPhe12,Nle21,38,Glu31,Lys34]Ac-hCRF(4-41)

    CRFR Endocrinology
    Stressin I (Cyclo(31-34)[DPhe12,Nle21,38,Glu31,Lys34]Ac-hCRF(4-41)) is a potent CRF1 receptor-selective agonist with a Ki of 1.7 nM. Stressin I induces increases in adrenocorticotropic hormone (ACTH) levels in rats .
    Stressin I
  • HY-P1368A
    Stressin I TFA
    1 Publications Verification

    Cyclo(31-34)[DPhe12,Nle21,38,Glu31,Lys34]Ac-hCRF(4-41) TFA

    CRFR Endocrinology
    Stressin I (Cyclo(31-34)[DPhe12,Nle21,38,Glu31,Lys34]Ac-hCRF(4-41)) TFA is a potent CRF1 receptor selective agonist, Ki is 1.7 nM. Stressin I induces an increase in adrenocorticotropic hormone (ACTH) levels in rats .
    Stressin I TFA
  • HY-P2265

    SOS1 Ras Cancer
    SAH-SOS1A is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM), directly and independently blocks nucleotide association, impairs KRAS-driven cancer cell viability, and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .
    SAH-SOS1A
  • HY-P2261
    STAD 2
    1 Publications Verification

    PKA Infection
    STAD 2 is a potent and selective disruptor of PKA-RII, with a Kd of 6.2 nM. STAD 2 disrupts interactions between PKA and AKAP in an isoform-selective manner. STAD 2 displays antimalarial activity through a PKA-independent mechanism .
    STAD 2
  • HY-P1712A

    Biochemical Assay Reagents Metabolic Disease
    Arthrofactin (TFA) is an effective lipopeptide biosurfactant in Pseudomonas sp. MIS38. Arthrofactin (TFA) production is associated with multiple ATP dependent active transporter systems .
    Arthrofactin TFA
  • HY-P10964

    GHSR Endocrinology
    Tezusomant is a growth hormone receptor antagonist. Tezusomant is promising for research on diseases caused by excessive growth hormone secretion, such as acromegaly .
    Tezusomant
  • HY-W671129

    Antibiotic Fungal Infection
    Frenolicin B is a covalent enzyme inhibitor and an orally active antiparasitic agent, with an IC50 of 0.2 μM against human Prx1. Frenolicin B selectively inhibits Glutaredoxin 3 via covalent modification of the active-site cysteines Cys159/Cys261. Frenolicin B selectively inhibits Peroxiredoxin 1 via covalent modification of the active-site cysteines Cys83/Cys173. Frenolicin B can be used in research related to colon cancer, breast cancer, lung cancer and malaria .
    Frenolicin B
  • HY-P3223A

    Opioid Receptor Neurological Disease
    Biphalin acetate, a BBB-penetrable opioid peptide analog, contains two active enkephalin pharmacophores.Biphalin acetate has high affinity for opioid receptors. Biphalin acetate shows analgesic effect in acute, neuropathic, and chronic animal pain models. Biphalin acetate is also an antiviral, antiproliferative, anti-inflammatory, and neuroprotective agent .
    Biphalin acetate
  • HY-P2266

    Histone Methyltransferase Cancer
    SAH-EZH2, a stable EZH2 α-helical peptide, is an EZH2/EED interaction inhibitor. SAH-EZH2 targets native embryonic ectoderm development (EED), disturbs its interactions with EZH1 and EZH2, and selectively decreases trimethylation of H3K27 .
    SAH-EZH2
  • HY-P2203A

    Notch Cancer
    SAHM1 TFA is a Notch pathway inhibitor. SAHM1 TFA stabilizes hydrocarbon-stapled alpha helical peptide. SAHM1 TFA targets the protein-protein interface and prevents Notch complex assembly.
    SAHM1 TFA
  • HY-P10488

    Wnt Others Cancer
    cycFWRPW is a peptide inhibitor of TLE1. TLE1 is an oncogenic transcriptional co‐repressor that exerts its repressive effects through binding of transcription factors, and inhibits Wnt signaling .
    cycFWRPW
  • HY-P10212

    UCCB01-125

    iGluR Neurological Disease
    AVLX-125 (UCCB01-125) is a PSD-95 and PDZ domain inhibitor with Kd value of 10 nM. AVLX-125 can be used in the study of inflammatory pain .
    AVLX-125
  • HY-P3223

    Opioid Receptor Neurological Disease
    Biphalin TFA, a BBB-penetrable opioid peptide analog, contains two active enkephalin pharmacophores. Biphalin TFA has high affinity for opioid receptors. Biphalin TFA shows analgesic effect in acute, neuropathic, and chronic animal pain models. Biphalin TFA is also an antiviral, antiproliferative, anti-inflammatory, and neuroprotective agent .
    Biphalin TFA
  • HY-185225

    Drug Derivative Others
    cis-Vaccenic acid NHS ester is an N-hydroxysuccinimide (NHS)-activated ester derivative of cis-vaccenic acid (HY-113427A) (C18:1 n-7), which is commonly used as a fatty acid labeling reagent or covalent modification reagent .
    cis-Vaccenic acid NHS ester
  • HY-N0191S

    Andrographis-d

    Isotope-Labeled Compounds NF-κB SARS-CoV Influenza Virus Autophagy Parasite Infection Inflammation/Immunology Cancer
    Andrographolide-d (Andrographis-d) is the deuterium labeled Andrographolide (HY-N0191). Andrographolide is a NF-κB inhibitor, which inhibits NF-κB activation through covalent modification of a cysteine residue on p50 in endothelial cells without affecting IκBα degradation or p50/p65 nuclear translocation. Andrographolide has antiviral effects.
    Andrographolide-d
  • HY-N17580

    Renin Cardiovascular Disease
    Lyciumin D acts as an angiotensin-converting enzyme inhibitor and renin inhibitor. Lyciumin D can be used for the research of hypertension .
    Lyciumin D
  • HY-125040

    Endogenous Metabolite Inflammation/Immunology
    Isariin C is a flavonoid glycoside with antioxidant activity. Isariin C activates angiogenesis. Isariin C exhibits insecticidal activity in certain insects .
    Isariin C
  • HY-W1126955

    MK-0616 (decanoate)

    PCSK9 Metabolic Disease Inflammation/Immunology
    Enlicitide (MK-0616) decanoate is an orally active macrocyclic peptide PCSK9 inhibitor. Enlicitide decanoate binds to PCSK9, blocks its interaction with low-density lipoprotein receptor (LDLR), and enhances hepatic clearance of LDL-C. Enlicitide decanoate reduces atherogenic lipoproteins, including non-HDL cholesterol, apolipoprotein B, and lipoprotein (a). Enlicitide decanoate is applicable to research related to hypercholesterolemia, heterozygous familial hypercholesterolemia, and atherosclerotic cardiovascular disease .
    Enlicitide (decanoate)
  • HY-182744

    MDM-2/p53 Cancer
    LLQ-45 is a covalent p53 Y220C mutant protein agonist with an EC50 of 24.97 μM. LLQ-45 activates the anti-tumor function of p53 Y220C through covalent modification, restores its DNA-binding ability and enhances its thermal stability. LLQ-45 selectively inhibits the proliferation of p53 Y220C mutant tumor cells, suppresses cell growth and upregulates the expression of CDKN1A. LLQ-45 can be used in studies related to p53 Y220C mutant cancers .
    LLQ-45
  • HY-P11837

    Biochemical Assay Reagents Cancer
    NECT-224 is a bifunctional chelator and a nectin-4 targeting peptide conjugate. NECT-224 can be used as a PET imaging agent when labeled with 64Cu or 68Ga .
    NECT-224

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