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half-maximal

" in MedChemExpress (MCE) Product Catalog:

25

Inhibitors & Agonists

1

Biochemical Assay Reagents

1

Peptides

2

Natural
Products

1

Click Chemistry

1

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-138642
    Vepdegestrant
    5+ Cited Publications

    ARV-471

    		 PROTACs Estrogen Receptor/ERR Cancer
    Vepdegestrant (ARV-471) is an orally active PROTAC estrogen receptor degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC50) of about 2 nM .
    Vepdegestrant
  • HY-N6972
    Cepharanthine
    10+ Cited Publications

    		 Autophagy SARS-CoV Cytochrome P450 Apoptosis Parasite Infection Inflammation/Immunology Cancer
    Cepharanthine is a natural product that can be isolated from the plant Stephania cephalantha Hayata. Cepharanthine has anti-severe acute respiratory syndrome coronavirus 2 (anti-SARS-CoV-2) activities. Cepharanthine has good effective in suppressing viral proliferation (half maximal (50%) inhibitory concentration (IC50) and 90% inhibitory concentration (IC90) values of 1.90 and 4.46 μM . Cepharanthine can also effectively reverses P-gp-mediated multidrug resistance in K562 cells and increase enhances the sensitivity of anticancer agents in xenograft mice model . Cepharanthine shows inhibitory effects of human liver cytochrome P450 enzymes CYP3A4, CYP2E1 and CYP2C9. Cepharanthine has antitumor, anti-inflammatory and antinociceptive effects .
    Cepharanthine
  • HY-122826
    ZXH-3-26
    2 Publications Verification

    		 PROTACs Epigenetic Reader Domain Cancer
    ZXH-3-26 is a PROTAC connected by ligands for Cereblon and BRD4 with a DC50/5h of 5 nM. The DC50/5h refers to half-maximal degradation after 5 hours of treatment of ~ 5 nM .
    ZXH-3-26
  • HY-16910
    WIKI4
    4 Publications Verification

    		 PARP β-catenin Wnt Cancer
    WIKI4 is a potent tankyrase inhibitor with an IC50 of 26 nM for TNKS2. WIKI4 potently inhibits Wnt/β-catenin signaling and that its half-maximal response dose is 75 nM. WIKI4 mediates its effects on Wnt/β-catenin signaling by inhibiting the enzymatic activity of TNKS2 . WIKI4 is cytotoxic to SCLC cells with an IC50 value of 0.02 μM .
    WIKI4
  • HY-162501
    Yaddle1
    1 Publications Verification

    		 Piezo Channel Inflammation/Immunology
    Yaddle1 is an agonist of the mechano-activated ion channel (Piezo1) with a half-maximal effective concentration (MEC50) of 0.40 μM. Yaddle1 can significantly trigger Ca 2+ inflow in T cells and induce T cell activation response. Yaddle1 can be used in the study of vaccine adjuvants .
    Yaddle1
  • HY-105056
    Bretazenil

    Ro 16-6028

    		 GABA Receptor Neurological Disease
    Bretazenil (Ro 16-6028) is a partial agonist at the gamma-aminobutyric acid A (GABAA) receptor-linked benzodiazepine site. Bretazenil is potent benzodiazepine examined, exhibiting an IC50 (concentration at which half-maximal inhibition of specific [35S]TBPS binding occurs) of 6.1 nM. Bretazenil shows an EC50 of 10 nM for recombinant α1β1γ2. Anticonvulsant effects .
    Bretazenil
  • HY-P5485
    Dabcyl-QALPETGEE-Edans

    		Bacterial Others
    Dabcyl-QALPETGEE-Edans is a synthetic peptide substrate for fluorescence resonance energy transfer (FRET) detection of Sortase A (SrtA) enzymatic activity. Dabcyl-QALPETGEE-Edans is labeled at both ends with the fluorescent group Edans (donor) and the quencher Dabcyl (acceptor), respectively. Dabcyl-QALPETGEE-Edans's central sequence contains a conserved motif specifically recognized by SrtA. Dabcyl-QALPETGEE-Edans demonstrates high sensitivity in vitro assays, enabling precise determination of the half-maximal inhibitory concentration of SrtA .
    Dabcyl-QALPETGEE-Edans
  • HY-130654
    (S,R,S)-AHPC-C2-PEG4-N3

    VH032-C2-PEG4-N3

    		 E3 Ligase Ligand-Linker Conjugates Cancer
    (S,R,S)-AHPC-C2-PEG4-N3 (VH032-C2-PEG4-N3) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 4-unit PEG linker used in PROTAC technology. (S,R,S)-AHPC-C2-PEG4-N3 can be used in the synthesis of vRucaparib-TP4 (HY-130647). vRucaparib-TP4 a highly potent PARP1 degrader with a half-maximal degrading concentration (DC50) of 82 nM . (S,R,S)-AHPC-C2-PEG4-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
    (S,R,S)-AHPC-C2-PEG4-N3
  • HY-124892A
    Acetylethylcholine mustard hydrochloride

    Acetyl-AF64

    		 Histone Acetyltransferase Neurological Disease
    Acetylethylcholine mustard hydrochloride (Acetyl-AF64) is an inhibitor of choline acetyl-transferase that reduces the contraction frequency of the myotubes by inhibiting the synthesis of acetylethylcholine (Ach) with the half-maximal inhibitory concentration (IC50) of 1.22 mM. Acetylethylcholine mustard hydrochloride is an irreversible ligand for the high affinity choline transport system. Acetylethylcholine mustard hydrochloride is also a cholinotoxin. Acetylethylcholine mustard hydrochloride is a precursor for ethylcholine mustard aziridinium ion .
    Acetylethylcholine mustard hydrochloride
  • HY-177122
    Raxlaprazine etomoxil

    		Dopamine Receptor Neurological Disease
    Raxlaprazine etomoxil is a small molecule compound with dopamine D2 and D3 receptor modulating activity, which has potential application value in research related to mental illnesses. Raxlaprazine etomoxil exhibits high affinity for human recombinant D2L receptors, with an inhibition constant (Ki) of 1.95 nM. Raxlaprazine etomoxil effectively inhibits forskolin-stimulated cAMP accumulation, with an half maximal effective concentration (EC50) of 3.72 nM in functional activity experiments .
    Raxlaprazine etomoxil
  • HY-W040263
    TAPS sodium

    TAPS Na

    		 Biochemical Assay Reagents Others
    TAPS sodium is a biological buffer that protects the structural integrity of lysozyme bacteria and prevents them from thermal denaturation at high temperatures. A pKa of 8.1 for TAPS results in half-maximal connexin channel activity .
    TAPS sodium
  • HY-138642A
    (Rac)-Vepdegestrant

    (Rac)-ARV-471

    		 Estrogen Receptor/ERR PROTACs Cancer
    (Rac)-Vepdegestrant is the isomer of Vepdegestrant (HY-138642). Vepdegestrant ((R)-Lavandulol) is an orally active PROTAC estrogen receptor degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC50) of about 2 nM .
    (Rac)-Vepdegestrant
  • HY-125627
    CP-394531

    		Glucocorticoid Receptor Androgen Receptor Neurological Disease Metabolic Disease
    CP-394531 is an efficient and highly selective non-steroidal glucocorticoid receptor (GR) antagonist, with a Ki value of 0.1 nM. CP-394531 has a weak binding to androgen receptor (AR) (Ki = 130 nM), and has almost no effect on progesterone receptor (PR) and estrogen receptors (ERα, ERβ). CP-394531 completely blocks the half-maximal agonistic effect induced by Dexamethasone (HY-14648G), with a Kif of 4.1 nM. CP-394531 can be used to study various diseases such as diabetes, obesity, depression, neurodegenerative diseases, glaucoma and Cushing's disease .
    CP-394531
  • HY-106560
    Proglumetacin

    		COX SARS-CoV Inflammation/Immunology
    Proglumetacin is an orally active and potent cyclo-oxygenase inhibitor. Proglumetacin can inhibits SARS-CoV Mpro (main protease of the SARS-CoV-2), with an AC50 of 8.9 μM (activity concentration at half maximal activity). Proglumetacin has anti-inflammatory activity, can be used for inflammation (such as Rheumatoid arthritis, and Allergic air pouch inflammation) research[1][2][3].
    Proglumetacin
  • HY-116197
    CGP44532

    		GABA Receptor Neurological Disease
    CGP44532 is a GABAB receptor agonist with a pEC50 (geometric mean of the half-maximal effective concentration) value of 5.63 μM .
    CGP44532
  • HY-N6972R
    Cepharanthine (Standard)

    		Autophagy Reference Standards SARS-CoV Cytochrome P450 Apoptosis Parasite Infection Inflammation/Immunology Cancer
    Cepharanthine (Standard) is the analytical standard of Cepharanthine. This product is intended for research and analytical applications. Cepharanthine is a natural product that can be isolated from the plant Stephania?cephalantha?Hayata. Cepharanthine has anti-severe acute respiratory syndrome coronavirus 2 (anti-SARS-CoV-2) activities. Cepharanthine has good effective in suppressing viral proliferation (half maximal (50%) inhibitory concentration (IC50) and 90% inhibitory concentration (IC90) values of 1.90 and 4.46?μM . Cepharanthine can also effectively reverses P-gp-mediated multidrug resistance in K562 cells and increase enhances the sensitivity of anticancer agents in xenograft mice model . Cepharanthine shows inhibitory effects of human liver cytochrome P450 enzymes CYP3A4, CYP2E1 and CYP2C9. Cepharanthine has antitumor, anti-inflammatory and antinociceptive effects .
    Cepharanthine (Standard)
  • HY-145432
    PI3K-IN-28

    		PI3K Cancer
    PI3K-IN-28 (Compound 6c) is a potent inhibitor of PI3K. PI3K-IN-28 displays the most potent activity with lower toxic effects on MCF-10a. PI3K-IN-28 displays half-maximal inhibitory concentration (IC50, μM) values of 5.8, 2.3, and 7.9. PI3K-IN-28 is the most potent one with a selectivity index (SI) of 39 and is considered as a latent lead for further optimization of anticancer agents .
    PI3K-IN-28
  • HY-158053
    Antifungal agent 94

    		Fungal Infection
    Antifungal agent 94 (Compound 49) is a Flavonoid derivative, which exhibits antifungal activity with EC50 of 0.28 μM and a half-maximal effective concentration of 0.46 μg/mL against Rhizoctonia solani .
    Antifungal agent 94
  • HY-144107
    HCV-IN-34

    		HCV Infection
    HCV-IN-34 (compound 3i) is an orally active and potent HCV entry inhibitor. HCV-IN-35 shows excellent antiviral activity, with an EC50 of 0.010 μM and a CC50 (half-maximal cytotoxic concentration) of 8.23 μM .
    HCV-IN-34
  • HY-144109
    HCV-IN-36

    		HCV Infection
    HCV-IN-36 (compound (S)-3h) is an orally active and potent HCV entry inhibitor. HCV-IN-36 shows excellent antiviral activity, with an EC50 of 0.016 μM and a CC50 (half-maximal cytotoxic concentration) of 8.78 μM .
    HCV-IN-36
  • HY-144749
    AKR1C3-IN-5

    		Aldose Reductase Cancer
    AKR1C3-IN-5 (Compound 6e) is a potent inhibitor of AKR1C3. AKR1C3 enzyme is overexpressed in hormone-dependent prostate and breast tumors. AKR1C3-IN-5 derived from drupanin, which exhibits half-maximal inhibitory concentration (IC50) of 9.6 ± 3 μM and selectivity index (SI) of 5.5 against MCF-7 cells .
    AKR1C3-IN-5
  • HY-100981
    MR-16728 hydrochloride

    		Endogenous Metabolite Neurological Disease
    MR-16728 hydrochloride is a compound that promotes the release of acetylcholine and has activity that enhances the release of acetylcholine. MR-16728 hydrochloride inhibits acetylcholine release induced by KCl depolarization. MR-16728 hydrochloride also inhibits Ca(2+)-ATPase activity in pure presynaptic membranes. The half-maximal effect of MR-16728 hydrochloride occurs at a concentration of 13.5 μM. MR-16728 hydrochloride significantly enhances the release of acetylcholine in the presence of low concentrations of calcium (approximately 10 μM range). Enhanced acetylcholine release was also observed with MR-16728 hydrochloride in proteoliposomes loaded with mediator proteins .
    MR-16728 hydrochloride
  • HY-117106
    PNU-107484A

    		GABA Receptor Others
    PNU-107484A is a GABAA receptor ligand that exhibits target activity mechanisms dependent on α isoforms. In the α1β2γ2 subtype, PNU-107484A acts as a positive allosteric modulator, enhancing GABA-induced Cl - currents, while it inhibits the currents in the α3β2γ2 and α6β2γ2 subtypes. The half-maximal concentrations for the α1β2γ2, α3β2γ2, and α6β2γ2 subtypes are 3.1, 4.2, and 3.5 μM, respectively. PNU-107484A can be used as a probe to investigate the physiological roles of different α isoform subtypes .
    PNU-107484A
  • HY-105056R
    Bretazenil (Standard)

    Ro 16-6028 (Standard)

    		 Reference Standards GABA Receptor Neurological Disease
    Bretazenil (Standard) is the analytical standard of Bretazenil (HY-105056). This product is intended for research and analytical applications. Bretazenil (Ro 16-6028) is a partial agonist at the gamma-aminobutyric acid A (GABAA) receptor-linked benzodiazepine site. Bretazenil is potent benzodiazepine examined, exhibiting an IC50 (concentration at which half-maximal inhibition of specific [35S]TBPS binding occurs) of 6.1 nM. Bretazenil shows an EC50 of 10 nM for recombinant α1β1γ2. Anticonvulsant effects .
    Bretazenil (Standard)
  • HY-W283930
    YHV98-4

    		Tau Protein ATP Synthase Mitophagy Reactive Oxygen Species (ROS) Mitochondrial Metabolism Neurological Disease Inflammation/Immunology
    YHV98-4 is a selective, blood-brain barrier permeable Hv1 channel inhibitor. YHV98-4 specifically inhibits Hv1 with a half-maximal inhibitory concentration of 1 µM without inhibiting other ion channels. YHV98-4 reduces the propagation of p-tau. YHV98-4 increases ATP production, and enhances microglial mitophagy. YHV98-4 attenuates inflammatory pain via inhibition of Hv1 and ROS production. YHV98-4 enhances microglia-to-neuron mitochondrial transfer, promoting the delivery of functional mitochondria to rescue neuronal damage and improve cognitive function. YHV98-4 reduces inflammation. YHV98-4 can be used in the research of Alzheimer's disease .
    YHV98-4

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