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High-potency inhibitors

" in MedChemExpress (MCE) Product Catalog:

34

Inhibitors & Agonists

2

Fluorescent Dye

2

Isotope-Labeled Compounds

1

Click Chemistry

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-D0004
    Azure B

    Azure B chloride

    		 Monoamine Oxidase Neurological Disease
    Azure B is a cationic dye and the major metabolite of Methylene blue. Azure B is used in making Azure eosin stains for blood smear staining. Azure B is a high-potency, selective and reversible inhibitor of monoamine oxidases (MAO)-A, with IC50s of 11 and 968 nM for recombinant human MAO-A and MAO-B, respectively. Azure B possesses significant antidepressant-like effects .
    Azure B
  • HY-132889
    BPTF-IN-BZ1

    		Epigenetic Reader Domain Cancer
    BPTF-IN-BZ1, a BPTF inhibitor, possesses a high potency (Kd = 6.3 nM).
    BPTF-IN-BZ1
  • HY-12988
    C527
    1 Publications Verification

    		 Deubiquitinase Cancer
    C527 is a is a pan DUB enzyme inhibitor, with a high potency for the USP1/UAF1 complex (IC50=0.88 μM).
    C527
  • HY-151136
    DY-46-2

    		DNA Methyltransferase Cancer
    DY-46-2 is a high potency and selectivity novel non-nucleoside DNA methyltransferase 3A (DNMT3A) inhibitor with an IC50 value of 0.39 μM .
    DY-46-2
  • HY-120210
    XY018

    		ROR Inflammation/Immunology Cancer
    XY018 is a potent ROR-γ-selective antagonist. XY018 inhibits ROR-γ constitutive activity in 293T cells with high potency (EC50, 190 nM). XY018 binds to the ROR-γ hydrophobic ligand binding domain (LBD) .
    XY018
  • HY-D0004R
    Azure B (Standard)

    		Monoamine Oxidase Neurological Disease
    Azure B (Standard) is the analytical standard of Azure B. This product is intended for research and analytical applications. Azure B is a cationic dye and the major metabolite of Methylene blue. Azure B is used in making Azure eosin stains for blood smear staining. Azure B is a high-potency, selective and reversible inhibitor of monoamine oxidases (MAO)-A, with IC50s of 11 and 968 nM for recombinant human MAO-A and MAO-B, respectively. Azure B possesses significant antidepressant-like effects .
    Azure B (Standard)
  • HY-148899
    Mcl-1 inhibitor 10

    		Bcl-2 Family Cancer
    Mcl-1 inhibitor 10 (compound 43) is a relatively strong MCL-1 inhibitor (IC50=0.67 μM). Mcl-1 inhibitor 10 interacts with specific binding sites of MCL-1 protein to block the pro-survival signal of MCL-1 and push cancer cells into apoptosis. Mcl-1 inhibitor 10 can be used in the study of MCL-1 dependent cancers .
    Mcl-1 inhibitor 10
  • HY-132894
    Pixavir marboxilo

    		Influenza Virus Infection
    Pixavir marboxilo is an orally active cap-dependent endonuclease inhibitor with high potency. Pixavir marboxilo can be used for the research of influenza .
    Pixavir marboxilo
  • HY-126475
    KSK213

    		Bacterial Others
    KSK213 is a 1,2,3-triazole-based Chlamydia infectivity inhibitor with high potency (EC50 ≤ 20 nM) against Chlamydia infectivity.
    KSK213
  • HY-167717
    (Rac)-Eflucimibe

    (Rac)-F 12511

    		 Others Metabolic Disease
    (Rac)-Eflucimibe ((Rac)-F 12511) is an ACAT inhibitor with endogenous hypercholesterolemia modulating activity. (Rac)-Eflucimibe has shown high potency and efficacy as an anti-hypercholesterol compound in different hypercholesterolemia animal models .
    (Rac)-Eflucimibe
  • HY-19985
    PF-06459988

    		EGFR Cancer
    PF-06459988 is an orally activity, irreversible and mutant-selective inhibitor of EGFR mutant forms. PF-06459988 demonstrates high potency and specificity to the T790M-containing double mutant EGFRs. PF-06459988 can be used for the research of cancer .
    PF-06459988
  • HY-144110
    HCV-IN-37

    		HCV Infection
    HCV-IN-37 (Compound 3d) is a potent inhibitor of HCV. HCV-IN-37 is orally available and long-lasting in rat plasma after oral administration to rats by a single dose of 15 mg/kg. The high potency of active derivative HCV-IN-37 is primarily driven by the inhibitory effect on the virus entry stage .
    HCV-IN-37
  • HY-153612
    MMV009085

    		GLUT Parasite Infection Inflammation/Immunology
    MMV009085 is a potent PfHT1 (Plasmodium falciparum hexose transporter)-specific inhibitor and a potential anti-malarial agent . MMV009085 is also a human glucose transporter inhibitor, it has high potency in inhibiting both glucose uptake (IC50: 2.6 μM in glucose uptake assay) and growth of the parasites (EC50: 1.23±0.04 μM against 3D7) .
    MMV009085
  • HY-109189
    Rezivertinib
    1 Publications Verification

    BPI-7711

    		 EGFR Cancer
    Rezivertinib (BPI-7711) is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI). Rezivertinib exhibits high potency against the common activation EGFR and the resistance T790M mutations. Rezivertinib has excellent central nervous system (CNS) penetration and has antitumor activity .
    Rezivertinib
  • HY-163806
    NT376

    		HDAC Neurological Disease Cancer
    NT376 is a high potency and selectivity inhibitor of class-IIa Histone deacetylases (HDAC) with an IC50 value of 32 nM, similar to NT160 (HY-149285) (IC50= 46 nM) in HT-29 cells. NT376 is proming for research of various cancers and in the diseases of the central nervous system (CNS) such as Alzheimer’s and Huntington’s diseases .
    NT376
  • HY-115947
    Anticancer agent 33

    		Others Cancer
    Anticancer agent 33 (compound 3), a Squamocin and Bullatacin derivative, is a potent anticancer agent. Anticancer agent 33 shows high potency to inhibit 4T1 breast cancer cell line (A549, HeLa, HepG2 and MCF-7 cells) growth with IC50s of 1.9-5.4 µM .
    Anticancer agent 33
  • HY-151367
    SHR2415

    		ERK Cancer
    SHR2415 is a highly potent, selective and orally active ERK1/2 inhibitor. SHR2415 has inhibition activity for ERK1 and ERK2 with IC50 values of 2.8 nM and 5.9 nM, respectively. SHR2415 exhibits high potency with an IC50 value of 44.6 nM in Colo205 cells. SHR2415 can be used for the research of cancer .
    SHR2415
  • HY-125384
    ARN14686

    		Fluorescent Dye Inflammation/Immunology
    ARN14686 is an activity-based protein profiling (ABPP) probe. ARN14686 inhibits hNAAA with high potency (IC50=0.006 μM). ARN14686 interacts with NAAA via covalent binding to the N-terminal cysteine. ARN14686 binds only to the catalytically active form of NAAA, and may serve therefore as an efficient activity-based probe .
    ARN14686
  • HY-107390A
    AX-024 hydrochloride
    1 Publications Verification

    		 TNF Receptor Interleukin Related IFNAR Inflammation/Immunology Cancer
    AX-024 hydrochloride is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation with an IC50 ~1 nM. AX-024 hydrochloride modulates cell signaling by targeting SH3 domains. AX-024 hydrochloride has low-acute toxicity and high potency and selectivity, and strongly inhibit the production of IL-6, TNF-α, IFN-γ, IL-10 and IL-17A.
    AX-024 hydrochloride
  • HY-107390
    AX-024
    1 Publications Verification

    		 TNF Receptor Interleukin Related IFNAR Inflammation/Immunology Cancer
    AX-024 is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation with an IC50 ~1 nM. AX-024 modulates cell signaling by targeting SH3 domains. AX-024 has low-acute toxicity and high potency and selectivity, and strongly inhibit the production of IL-6, TNF-α, IFN-γ, IL-10 and IL-17A.
    AX-024
  • HY-106481
    Bufrolin

    		GPR35 Histamine Receptor Inflammation/Immunology
    Bufrolin is a Cromoglycate (histamine release inhibitor) analog and a high potency agonist of GPR35. Bufrolin promotes interactions between β-arrestin-2 and either human GPR35a or rat GPR35. Bufrolin also serves as antiallergic mast cell stabilizer and inhibit an anti-inflammatory response inducible by the internalization peptide. Bufrolin acts as an anti-inflammatory agent to be used in research of delivering pharmacol linked with internalization peptide .
    Bufrolin
  • HY-147947
    Tubulin polymerization-IN-30

    		Microtubule/Tubulin Cancer
    Tubulin polymerization-IN-30 (compound 6e) is a potent Tubulin polymerization inhibitor. Tubulin polymerization-IN-30 is a colchicine binding site inhibitor. Tubulin polymerization-IN-30 can disrupt intracellular microtubule organization, arrest cell cycle at the G2/M phase. Tubulin polymerization-IN-30 exhibits the high potency against the cancer cell lines including SGC-7901, A549 and HeLa, with IC50 values of 2.16, 2.21, and 0.403 μM .
    Tubulin polymerization-IN-30
  • HY-115981
    NS5A-IN-2

    		HCV Protease Infection
    NS5A-IN-2 (Compound 33) is a potent inhibitor of NS5A. NS5A-IN-2 has extremely high potency against HCV genotype 1b, improved activity against genotype 3a (GT 3a) and good metabolic stability . NS5A-IN-2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    NS5A-IN-2
  • HY-133129
    MS1943
    1 Publications Verification

    		 PROTACs Histone Methyltransferase Apoptosis Cancer
    MS1943 is an orally active, PROTAC-based, selective degrader of EZH2 that effectively reduces EZH2 levels in cells. MS1943 has anticancer activity and exhibits cytotoxic effects in a variety of TNBC cells while sparing normal cells. In addition, MS1943 maintains high potency (IC50=120 nM) in inhibiting EZH2 methyltransferase activity and is highly selective for EZH2. (Structure Note: RED, EZH2 ligand (HY-148458); Blue, Hyt (HY-W001578)) .
    MS1943
  • HY-155222
    TW9

    		Epigenetic Reader Domain HDAC Cancer
    TW9 is a potent dual inhibitor simultaneously targeting BET and HDAC proteins with KDs of 0.069 μM, 0.231 μM for BRD4(1), BRD4(2), and an IC50 of 0.29 μM for HDAC1, respectively. TW9 is a newly generated adduct of the BET inhibitor (+)-JQ1 (HY-13030) and class I HDAC inhibitor CI994 (HY-50934). TW9 shows high potency in suppressing tumor growth in pancreatic ductal adenocarcinoma (PDAC). TW9 improves the efficacy of the chemotherapeutic agent Gemcitabine (HY-17026) .
    TW9
  • HY-13238
    Dolutegravir
    Maximum Cited Publications
    24 Publications Verification

    S/GSK1349572

    		 HIV Integrase HIV Infection
    Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM) .
    Dolutegravir
  • HY-132231
    FD223

    		PI3K Apoptosis Cancer
    FD223 is a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor. FD223 displays high potency (IC50=1 nM) and good selectivity over other isoforms (IC50s of 51 nM, 29 nM and 37 nM, respectively for α, β and γ). FD223 exhibits efficient inhibition of the proliferation of acute myeloid leukemia (AML) cell lines by suppressing p-AKT Ser473 thus causing G1 phase arrest during the cell cycle. FD223 has potential for the research of leukemia such as AML .
    FD223
  • HY-13238A
    Dolutegravir sodium
    Maximum Cited Publications
    24 Publications Verification

    S/GSK1349572 sodium

    		 HIV Integrase HIV Infection
    Dolutegravir sodium (S/GSK1349572 sodium) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir sodium (S/GSK1349572 sodium) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir sodium (S/GSK1349572 sodium) retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM) .
    Dolutegravir sodium
  • HY-115982
    NS5A-IN-3

    		HCV Protease Infection
    NS5A-IN-3 (Compound 15) is a potent inhibitor of NS5A. NS5A-IN-3 has extremely high potency against HCV genotype 1b, improved activity against genotype 3a (GT 3a) and good metabolic stability. NS5A-IN-3 exhibits a higher resistance barrier than daclatasvir against genotype 1b . NS5A-IN-3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    NS5A-IN-3
  • HY-13238S1
    Dolutegravir-d3

    S/GSK1349572-d3

    		 Isotope-Labeled Compounds HIV Integrase HIV Infection
    Dolutegravir-d3 is the deuterium labeled Dolutegravir. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM)[1][2].
    Dolutegravir-d3
  • HY-13238S2
    Dolutegravir-d5

    S/GSK1349572-d5

    		 Isotope-Labeled Compounds HIV Integrase HIV Infection
    Dolutegravir-d5 is deuterium labeled Dolutegravir. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM)[1][2].
    Dolutegravir-d5
  • HY-13238R
    Dolutegravir (Standard)

    		HIV Integrase HIV Infection
    Dolutegravir (Standard) is the analytical standard of Dolutegravir. This product is intended for research and analytical applications. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM) .
    Dolutegravir (Standard)
  • HY-105099
    Rifalazil

    KRM-1648; ABI-1648

    		 DNA/RNA Synthesis Bacterial Infection Inflammation/Immunology
    Rifalazil (KRM-1648; ABI-1648), a rifamycin derivative, inhibits the bacterial DNA-dependent RNA polymerase and kills bacterial cells by blocking off the β-subunit in RNA polymerase . Rifalazil (KRM-1648; ABI-1648) is an antibiotic, exhibits high potency against mycobacteria, gram-positive bacteria, Helicobacter pylori, C. pneumoniae and C. trachomatis with MIC values from 0.00025 to 0.0025 μg/ml . Rifalazil (KRM-1648; ABI-1648) has the potential for the treatment of Chlamydia infection, Clostridium difficile associated diarrhea (CDAD), and tuberculosis (TB) .
    Rifalazil
  • HY-15334
    CEP-5214

    		VEGFR Cancer
    CEP-5214, derived from a new indenopyrrolocarbazole template, is a potent inhibitor of vascular endothelial growth factor R2 (VEGF-R2) tyrosine kinase. Structurally, it features optimal substitutions at positions 9 (ethoxymethyl) and 12 (hydroxypropyl) on the indeno[2,1-a]pyrrolo[3,4-c]carbazole-5-one scaffold, leading to high potency against VEGF-R2 (IC50 8 nM). Compound 21 (CEP-5214) exhibits low-nanomolar inhibition of human VEGF-R tyrosine kinases (IC50 4 nM for VEGF-R2/KDR), with good selectivity over other kinases. The compound demonstrated significant cellular and in vivo antitumor activity across various models and advanced into phase I clinical trials as a water-soluble prodrug (CEP-7055) to enhance oral bioavailability .
    CEP-5214

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