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Protein inhibition

" in MedChemExpress (MCE) Product Catalog:

193

Inhibitors & Agonists

5

Screening Libraries

2

Biochemical Assay Reagents

13

Peptides

1

MCE Kits

2

Inhibitory Antibodies

32

Natural
Products

1

Recombinant Proteins

5

Isotope-Labeled Compounds

4

Antibodies

4

Click Chemistry

2

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-B1898
    Metadoxine

    		PKA Metabolic Disease
    Metadoxine blocks adipocyte differentiation in association with inhibition of the protein kinase A-cAMP response element binding protein (PKA-CREB) pathway.
    Metadoxine
  • HY-145722
    Apatorsen sodium

    OGX-427 sodium

    		 HSP Cancer
    Apatorsen (sodium) is an antisense oligonucleotide designed to bind to Hsp27 mRNA, resulting in the inhibition of the production of Hsp27 protein.
    Apatorsen sodium
  • HY-P1479A
    Calmodulin-Dependent Protein Kinase II(290-309) acetate

    		Autophagy CaMK Neurological Disease
    Calmodulin-Dependent Protein Kinase II (290-309) acetate is a potent CaMK antagonist with an IC50 of 52 nM for inhibition of Ca2+/calmodulin-dependent protein kinase II .
    Calmodulin-Dependent Protein Kinase II(290-309) acetate
  • HY-15979
    H-89
    Maximum Cited Publications
    117 Publications Verification

    		 PKA Autophagy Neurological Disease
    H-89 is a potent and selective inhibitor of cyclic AMP-dependent protein kinase (protein kinase A) with IC50 of 48 nM and has weak inhibition on PKG, PKC, Casein Kinase, and others kinases.
    H-89
  • HY-N1743
    1-(4-Hydroxy-2-methoxyphenyl)-3-(4-hydroxy-3-prenylphenyl)

    		Phosphatase Metabolic Disease
    1-(4-Hydroxy-2-methoxyphenyl)-3-(4-hydroxy-3-prenylphenyl), isolated from Broussonetia kazinoki, shows in vitro inhibition of protein tyrosine phosphatase 1B (PTP1B) with an IC50 of 13.00 μM. PTP1B is a negative regulator of insulin action and an important mediator in the pathogenesis of insulinresistance and non-insulin dependent diabetes mellitus. PTP1B is regarded as a significant target for type 2 diabetes .
    1-(4-Hydroxy-2-methoxyphenyl)-3-(4-hydroxy-3-prenylphenyl)
  • HY-146752
    α-Amylase-IN-1

    		Others Others
    α-Amylase-IN-1 is a potent α-amylase inhibitor with an IC50 of 4.46 μM .
    α-Amylase-IN-1
  • HY-145722A
    Apatorsen

    OGX-427

    		 HSP Cancer
    Apatorsen is an antisense oligonucleotide designed to bind to Hsp27 mRNA, resulting in the inhibition of the production of Hsp27 protein.
    Apatorsen
  • HY-N3425
    Kazinol U

    		AMPK Others
    Kazinol U inhibits melanogenesis through the inhibition of tyrosinase-related proteins via AMPK activation .
    Kazinol U
  • HY-P1479
    Calmodulin-Dependent Protein Kinase II (290-309)

    		Autophagy CaMK Neurological Disease
    Calmodulin-Dependent Protein Kinase II (290-309) is a potent CaMK antagonist with an IC50 of 52 nM for inhibition of Ca2+/calmodulin-dependent protein kinase II .
    Calmodulin-Dependent Protein Kinase II (290-309)
  • HY-116529
    Lamellarin E

    		Others Others
    Lamellarin E is a biologically active marine alkaloid, while the Lamellarin series of alkaloids show potential cytotoxicity, topoisomerase I inhibition, protein kinase inhibition, multidrug resistance reversal, and anti-HIV-1 activity .
    Lamellarin E
  • HY-P3841
    Protein Kinase C (beta) Peptide

    		PKC Others
    Protein Kinase C β Peptide is a peptide fragment of Protein Kinase Cβ. Protein Kinase Cβ is related with hyperglycemia decreases endothelium-derived nitric oxide. Inhibition of Protein kinase Cβ prevents the reduction in endothelium-dependent vasodilation induced by acute hyperglycemia .
    Protein Kinase C β Peptide
  • HY-15979A
    H-89 dihydrochloride
    Maximum Cited Publications
    117 Publications Verification

    		 PKA Autophagy Others
    H-89 dihydrochloride is a potent and selective inhibitor of protein kinase A (PKA) with an IC50 of 48 nM and has weak inhibition on PKG, PKC, Casein Kinase.
    H-89 dihydrochloride
  • HY-12825
    BHPI

    		Estrogen Receptor/ERR Cancer
    BHPI is a potent inhibitor of nuclear estrogen–ERα-regulated gene expression; elicits sustained ERα-dependent activation of the endoplasmic reticulum (EnR) stress sensor, the unfolded protein response (UPR), and persistent inhibition of protein synthesis.
    BHPI
  • HY-139823
    PRMT5-IN-10

    		Histone Methyltransferase Others
    PRMT5-IN-10 has promising structure-dependent inhibition of the protein methyltransferase PRMT5:MEP50 complex.
    PRMT5-IN-10
  • HY-50883
    BMS 299897

    		γ-secretase Neurological Disease
    BMS 299897 is a sulfonamide γ-secretase inhibitor with an IC50 of 7 nM for Aβ production inhibition in HEK293 cells stably overexpressing amyloid precursor protein (APP).
    BMS 299897
  • HY-12089
    Torcetrapib

    CP-529414

    		 CETP Endocrinology
    Torcetrapib (CP-529414) is a selective, potent cholesteryl ester transfer protein (CETP) inhibitor. A typical inhibition curve for whole human plasma, having a CETP concentration of 37 nM .
    Torcetrapib
  • HY-139823A
    PRMT5-IN-11

    		Histone Methyltransferase Others
    PRMT5-IN-11 is a promising structure-dependent inhibition of the protein methyltransferase PRMT5:MEP50 complex in the (sub)micromolar range.
    PRMT5-IN-11
  • HY-164142
    ETB

    		HSP Cancer
    ETB is a potent Hsp60 chaperone activity inhibitor. ETB blockes the chaperone activities of the wild-type protein and of the C237A and C447A mutant proteins. ETB binds to Hsp60 Cys 442 and shows the resistance of the C442A mutant to ETB inhibition .
    ETB
  • HY-14855
    Tedizolid
    10+ Cited Publications

    TR 700; Torezolid; DA-7157

    		 Bacterial Antibiotic Infection
    Tedizolid (TR 700; Torezolid; DA-7157) is a novel oxazolidinone, acting through inhibition of bacterial protein synthesis by binding to 23S ribosomal RNA (rRNA) of the 50S subunit of the ribosome.
    Tedizolid
  • HY-157068
    icFSP1

    		Ferroptosis Cancer
    icFSP1 is a potent ferroptosis suppressor protein-1 (FSP1) inhibitor. icFSP1 does not competitively inhibit FSP1 enzyme activity, but instead triggers subcellular relocalization of FSP1 from the membrane and FSP1 condensation before ferroptosis induction, in synergism with GPX4 inhibition .
    icFSP1
  • HY-119220
    Granotapide

    JTT-130

    		 Microsomal Triglyceride Transfer Protein (MTP) Metabolic Disease
    Granotapide (JTT-130) is an orally active microsomal triglyceride transfer protein (MTP) inhibitor. Granotapide reduces absorption of cholesterol and triglycerides through inhibition of MTP. Granotapide can be used for the research of dyslipidemia .
    Granotapide
  • HY-124069
    M-525

    		Epigenetic Reader Domain Cancer
    M-525 is a first-in-class, highly potent, irreversible and covalent menin-MLL protein-protein interaction inhibitor. M-525 binds to menin with an IC50 of 3 nM and achieves low nanomolar potencies in cell growth inhibition and in suppression of MLL regulated gene expression in MLL leukemia cells. Anti-leukemia activity .
    M-525
  • HY-164041
    Staurosporine-Boc

    		PKC Others
    Staurosporine-Boc, a natural product isolated from the actinomyces Streptomyces staurosporeus, is a potent non-selective inhibitor of protein kinase. Staurosporine-Boc inhibits a variety of protein kinases, including protein kinase C (PKC), tyrosine kinase, and serine/threonine kinase. Because of its broad inhibition profile, Staurosporine-Boc is widely used as a tool compound in biological research, especially when studying cell signaling pathways .
    Staurosporine-Boc
  • HY-N0044
    Ginsenoside Re
    2 Publications Verification

    Ginsenoside B2; Panaxoside Re; Sanchinoside Re

    		 Amyloid-β NF-κB JNK Endogenous Metabolite Neurological Disease Inflammation/Immunology Cancer
    Ginsenoside Re (Ginsenoside B2) is an extract from Panax notoginseng. Ginsenoside Re decreases the β-amyloid protein (Aβ). Ginsenoside Re plays a role in antiinflammation through inhibition of JNK and NF-κB.
    Ginsenoside Re
  • HY-110258
    ML334
    5+ Cited Publications

    LH601A

    		 Keap1-Nrf2 Cancer
    ML334 is a potent, cell permeable activator of NRF2 by inhibition of Keap1-NRF2 protein-protein interaction. ML334 binds to Keap1 Kelch domain with a Kd of 1 μM. ML334 stimulates NRF2 expression and nuclear translocation and induces antioxidant response elements (ARE) activity .
    ML334
  • HY-120760
    L-691831

    		Others Others
    L-691831 is a ligand for 5-lipoxygenase activating protein binding assays that has utility as a tool for studying 5-lipoxygenase activating protein (FLAP) related activities. L-691831 can be used to measure the affinity of FLAP on the leukocyte membrane for leukotriene synthesis inhibitors, with binding being correlated with inhibition of leukotriene synthesis.
    L-691831
  • HY-15880
    CCT007093
    2 Publications Verification

    		 Phosphatase Apoptosis Autophagy Cancer
    CCT007093 is an effective protein phosphatase 1D (PPM1D Wip1) inhibitor. Wip1 inhibition can activate the mTORC1 pathway and enhance hepatocyte proliferation after hepatectomy .
    CCT007093
  • HY-100585
    Splitomicin

    Splitomycin

    		 HDAC Cancer
    Splitomicin (Splitomycin) is a selective Sir2p inhibitor. Splitomicin inhibits NAD +-dependent HDAC activity of Sir2 protein. Splitomicin induces dose-dependent inhibition of HDAC in the yeast extract with an IC50 of 60 μM .
    Splitomicin
  • HY-15874
    Fiboflapon

    GSK2190915; AM-803

    		 FLAP Leukotriene Receptor Inflammation/Immunology
    Fiboflapon (GSK2190915; AM-803) is a potent and orally bioavailable 5-lipoxygenase-activating protein (FLAP) inhibitor with a potency of 2.9 nM in FLAP binding, an IC50 of 76 nM for inhibition of LTB4 in human blood .
    Fiboflapon
  • HY-15874A
    Fiboflapon sodium

    GSK2190915 sodium salt; AM-803 sodium

    		 FLAP Leukotriene Receptor Inflammation/Immunology
    Fiboflapon sodium (GSK2190915; AM-803) is a potent and orally bioavailable 5-lipoxygenase-activating protein (FLAP) inhibitor with a potency of 2.9 nM in FLAP binding, an IC50 of 76 nM for inhibition of LTB4 in human blood .
    Fiboflapon sodium
  • HY-17593
    Solithromycin
    2 Publications Verification

    CEM-101; OP-1068

    		 Bacterial Antibiotic Infection
    Solithromycin (CEM-101) is an orally bioavailable, effective antimicrobial agent, with IC50s for inhibition of cell viability, protein synthesis, and growth rate are 7.5 ng/mL, 40 ng/mL, and 125 ng/mL for Streptococcus pneumonia, Staphylococcus aureus, and Haemophilus influenzae, respectively. Solithromycin binds to the large 50S subunit of the ribosome and inhibits protein biosynthesis .
    Solithromycin
  • HY-N10649
    PTP1B-IN-21

    		Phosphatase Metabolic Disease
    PTP1B-IN-21 is a selective inhibitor of protein tyrosine phosphatase 1B (PTP1B; IC50=1.56 μM) over the highly homologous T-cell protein tyrosine phosphatase (TCPTP; IC50>100 μM), which is a key target for type 2 diabetes inhibition .
    PTP1B-IN-21
  • HY-B0751
    Fumagillin

    Amebacilin; NSC9168

    		 Parasite HIV Antibiotic Infection
    Fumagillin(NSC9168) is an antimicrobial compound first isolated in 1949 from the fungus Aspergillus fumigatu. Fumagillin can inhibits HIV‐1 infection through the inhibition of HIV-1 viral protein R (Vpr) activity.
    Fumagillin
  • HY-101712
    TRC051384
    4 Publications Verification

    		 HSP Neurological Disease
    TRC051384 is a potent inducer of heat shock protein 70 (HSP70). TRC051384 exhibits protective effects against neuronal trauma via inhibition of necroptosis. TRC051384 can be used for the research of ischemic stroke .
    TRC051384
  • HY-N6036
    Ganoderic acid F
    1 Publications Verification

    		 Others Cancer
    Ganoderic acid F is a ganoderic acid. Ganoderic acid F exhibits antitumor and antimetastatic activities through inhibition of angiogenesis and alteration of proteins involving cell proliferation and/or cell death, carcinogenesis, oxidative stress, calcium signaling, and endoplasmic reticulum stress .
    Ganoderic acid F
  • HY-124109
    TRC051384 hydrochloride

    		HSP Cardiovascular Disease Neurological Disease
    TRC051384 hydrochloride is a potent inducer of heat shock protein 70 (HSP70). TRC051384 hydrochloride exhibits protective effects against neuronal trauma via inhibition of necroptosis. TRC051384 hydrochloride can be used for the research of ischemic stroke .
    TRC051384 hydrochloride
  • HY-P3026
    Bowman-birk inhibitor

    		Others Cancer
    The Bowman-Birk inhibitor, a highly cross-linked protein featuring seven disulfide bridges, possesses spatially distinct domains specifically designed for the inhibition of both trypsin and chymotrypsin, showcasing its significant role as a plant protease inhibitor with anticarcinogenic properties.
    Bowman-birk inhibitor
  • HY-P1597
    Malantide
    1 Publications Verification

    		 PKA PKC Cancer
    Malantide is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide is a highly specific substrate for PKA with a Km of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts . Malantide is also an efficient substrate for PKC with a Km of 16 μM .
    Malantide
  • HY-111557
    YM-254890
    5+ Cited Publications

    		 P2Y Receptor Cardiovascular Disease
    YM-254890 is a selective Gαq/11 protein inhibitor isolated from Chromobacterium sp. YM-254890 shows no inhibition of other G protein subtypes. YM-254890 inhibits platelet aggregation induced by ADP by blocking the P2Y1 signal transduction pathway, with an IC50 value below 0.6 μM .
    YM-254890
  • HY-112400
    Bisindolylmaleimide V

    BIM V

    		 Ribosomal S6 Kinase (RSK) Cancer
    Bisindolylmaleimide V is a cell-permeable negative control for protein kinase C inhibition studies with an IC50 value over 100 µM . Bisindolylmaleimide V blocks the activation of mitogen-stimulated protein kinase p70 s6k/p85 s6k (S6K) in vivo with an IC50 of 8 µM .
    Bisindolylmaleimide V
  • HY-N10648
    PTP1B-IN-20

    		Phosphatase Metabolic Disease
    PTP1B-IN-20 is a selective inhibitor of protein tyrosine phosphatase 1B (PTP1B; IC50=1.05 μM) over the highly homologous T-cell protein tyrosine phosphatase (TCPTP; IC50=78.0 μM), which is a key target for type 2 diabetes inhibition .
    PTP1B-IN-20
  • HY-118041
    PMPMEase-IN-1

    		Others Cancer
    PMPMEase-IN-1 is an allylated methylated protein methylesterase inhibitor with the property of inhibiting PMPMEase activity. PMPMEase-IN-1 may provide a useful strategy for cancer inhibition by enhancing its affinity for polyisoprenyl derivatives. PMPMEase-IN-1 showed the potential to have an effective concentration (EC50) value in causing degeneration of human neuroblastoma SH-SY5Y cells. Specific inhibition of PMPMEase-IN-1 may help regulate the metabolism of polyisoprenyl proteins and thus maintain normal cell survival. Further development and application of PMPMEase-IN-1 may open up new avenues for inhibiting degenerative diseases and cancer .
    PMPMEase-IN-1
  • HY-N10616
    Pseudobaptigenin

    		Others Metabolic Disease
    Pseudobaptigenin is a flavonoid. Pseudobaptigenin shows very good anticataract activity. Pseudobaptigenin has good binding affinity for the inhibition of glycation against γ-crystallin protein. Pseudobaptigenin also has good ADMET (Absorption, Distribution, Metabolism, Excretion and Toxicity) property .
    Pseudobaptigenin
  • HY-P1597A
    Malantide TFA

    		PKA PKC Cancer
    Malantide TFA is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide TFA is a highly specific substrate for PKA with a Km of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts . Malantide TFA is also an efficient substrate for PKC with a Km of 16 μM .
    Malantide TFA
  • HY-156568
    SMD-3040

    		PROTACs Epigenetic Reader Domain Cancer
    SMD-3040 is a potent and selective of SMARCA2 PROTAC degrader (DC50: 12 nM). SMD-3040 contains SMARCA2/4 ligand, linker and VHL ligand. SMD-3040 demonstrates excellent degradation selectivity for SMARCA2 protein over SMARCA4 protein.SMD-3040 achieves strong tumor growth inhibition in xenograft models .
    SMD-3040
  • HY-B0479
    Thiamphenicol

    Thiophenicol; Dextrosulphenidol

    		 Beta-lactamase Bacterial Antibiotic Infection
    Thiamphenicol (Thiophenicol), a methyl-sulfonyl derivative of Chloramphenicol, is a broad-spectrum antimicrobial antibiotic. Thiamphenicol acts by binding to the 50S ribosomal subunit, leading to inhibition of protein synthesis and bacteriostatic effect (against Gram-negative, Gram-positive aerobic and anaerobic bacteria) .
    Thiamphenicol
  • HY-162257
    BTK-IN-34

    		Btk Cancer
    BTK-IN-34 (compound 9h) is a selective BTK inhibitor. BTK-IN-34 shows antiproliferative activity in RAMOS cells through selective inhibition of pBTK (Tyr223) without affecting Lyn and Syk, upstream proteins in the BCR signaling pathway .
    BTK-IN-34
  • HY-108602
    Bryostatin 3

    		PKC Cancer
    Bryostatin 3, a macrocyclic lactone, is a protein kinase C activator, with a Ki of 2.75 nM. Bryostatin 3 can block 12-O-tetradecanoylphorbol-13-acetate (TPA) inhibition of cell proliferation, yet did not block TPA-enhanced cell-substratum adhesion .
    Bryostatin 3
  • HY-141543
    YW2065

    		β-catenin Cancer
    YW2065 is an Axin-1 stabilizer. Axin-1 is a scaffolding protein that regulates proteasome degradation of β-catenin. YW2065 exhibits anti-colorectal cancer effects via dual activities of wnt/β-catenin signaling inhibition and AMPK activation .
    YW2065
  • HY-14855R
    Tedizolid (Standard)

    		Bacterial Antibiotic Infection
    Tedizolid (Standard) is the analytical standard of Tedizolid. This product is intended for research and analytical applications. Tedizolid (TR 700; Torezolid; DA-7157) is a novel oxazolidinone, acting through inhibition of bacterial protein synthesis by binding to 23S ribosomal RNA (rRNA) of the 50S subunit of the ribosome.
    Tedizolid (Standard)

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