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Results for "

peptidomimetics

" in MedChemExpress (MCE) Product Catalog:

63

Inhibitors & Agonists

2

Screening Libraries

20

Peptides

5

Isotope-Labeled Compounds

3

Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-15871
    GGTI298 Trifluoroacetate
    5+ Cited Publications

    		 Apoptosis Cancer
    GGTI298 Trifluoroacetate is a CAAZ peptidomimetic geranylgeranyltransferase I (GGTase I) inhibitor, which can inhibit Rap1A with IC50 of 3 μM; little effect on Ha-Ras with IC50 of >20 μM.
    GGTI298 Trifluoroacetate
  • HY-10235
    Telaprevir
    Maximum Cited Publications
    44 Publications Verification

    VX-950

    		 HCV Protease HCV SARS-CoV Infection
    Telaprevir (VX-950) is a highly selective, reversible, and potent peptidomimetic inhibitor of the HCV NS3-4A protease, the steady-state inhibitory constant (Ki) of Telaprevir is 7 nM against a genotype 1 (H strain) NS3 protease domain plus a NS4A cofactor peptide . Telaprevir inhibits SARS-CoV-2 3CL pro activity .
    Telaprevir
  • HY-14588
    Lopinavir
    15+ Cited Publications

    ABT-378

    		 HIV HIV Protease SARS-CoV Infection Neurological Disease Cancer
    Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 14.2 μM .
    Lopinavir
  • HY-P3212
    Allo-aca
    Maximum Cited Publications
    10 Publications Verification

    		 Neuropeptide Y Receptor Others Cancer
    Allo-aca, a leptin peptidomimetic, is a potent, specific leptin receptor antagonist peptide. Allo-aca blocks leptin signaling and action in numerous in vitro and in vivo models .
    Allo-aca
  • HY-15872A
    FTI-277 hydrochloride
    5+ Cited Publications

    		 Farnesyl Transferase Apoptosis Ras Infection Cancer
    FTI-277 hydrochloride is an inhibitor of farnesyl transferase (FTase); a highly potent Ras CAAX peptidomimetic which antagonizes both H- and K-Ras oncogenic signaling. FTI-277 hydrochloride can inhibit hepatitis delta virus (HDV) infection.
    FTI-277 hydrochloride
  • HY-P4210
    Sulanemadlin
    1 Publications Verification

    ALRN-6924; MP-4897

    		 MDM-2/p53 Cancer
    Sulanemadlin (ALRN-6924) is a potent and cell-permeating p53-based peptidomimetic macrocycles. Sulanemadlin is a inhibitor of the p53-MDM2, p53-MDMX, or both p53 and MDM2 and MDMX protein-protein interactions. Sulanemadlin can be used for cancers research .
    Sulanemadlin
  • HY-101511
    TTT-28

    		P-glycoprotein Cancer
    TTT-28 is a synthesized thiazole-valine peptidomimetic, a novel selective inhibitor of ABCB1 (P-gp/MDR1) with high efficacy and low toxicity, which reverses the ATP-binding cassette sub-family B member 1 (ABCB1)-mediated multidrug resistance (MDR) by selectively blocking the efflux function of ABCB1 .
    TTT-28
  • HY-123972
    SEC inhibitor KL-2
    1 Publications Verification

    KL-2

    		 DNA/RNA Synthesis Cancer
    SEC inhibitor KL-2 (KL-2), a peptidomimetic lead compound, is a potent, selective super elongation complex (SEC) inhibitor and disrupts the interaction between the SEC scaffolding protein AFF4 and P-TEFb, resulting in impaired release of Pol II from promoter-proximal pause sites and a reduced average rate of processive transcription elongation. SEC inhibitor KL-2 exhibits an dose-dependent inhibitory effect on AFF4-CCNT1 interaction with a Ki of 1.50 μM .
    SEC inhibitor KL-2
  • HY-100876
    GGTI298

    		Apoptosis Cancer
    GGTI298 is a CAAZ peptidomimetic geranylgeranyltransferase I (GGTase I) inhibitor, strongly inhibiting the processing of geranylgeranylated Rap1A with little effect on processing of farnesylated Ha-Ras, with IC50 values of 3 and > 20 μM in vivo, respectively.
    GGTI298
  • HY-W008235
    Fmoc-N-Me-Ala-OH

    		Amino Acid Derivatives Drug Intermediate Cancer
    Fmoc-N-Me-Ala-OH is an Fmoc-protected N-methyl-L-alanine and also a building block for solid-phase peptide synthesis. As a building block, Fmoc-N-Me-Ala-OH is used to synthesize peptidomimetic antagonists of XIAP BIR3 derived from Smac/DIABLO .
    Fmoc-N-Me-Ala-OH
  • HY-P1102
    TC14012
    4 Publications Verification

    		 CXCR HIV Infection Cancer
    TC14012, a serum-stable derivative of T140, is a selective and peptidomimetic CXCR4 antagonist with an IC50 of 19.3 nM. TC14012 is a potent CXCR7 agonist with an EC50 of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 has anti-HIV activity and anti-cancer activity .
    TC14012
  • HY-126322
    DVD-445

    		TrxR Cancer
    DVD-445 (Compound 7) is a potent peptidomimetic covalent thioredoxin reductase 1 (TrxR1) inhibitor with an IC50 of 0.60 μM for rat TrxR1. DVD-445 has good anticancer application .
    DVD-445
  • HY-P10816
    PACE4 Inhibitory peptide C23

    Ac-(DLeu)LLLRVK-Amba

    		 Bacterial Infection Cancer
    PACE4 Inhibitory peptide C23 (Compound C23; Ac-(DLeu)LLLRVK-Amba)), a potent peptidomimetic inhibitor, is a PACE4 inhibitor. PACE4 Inhibitory peptide C23e shows antiproliferative effects against PCa cell lines (Ki = 5 nM; IC50 = 25 and 40 μM for DU145 and LNCaP, respectively). PACE4 Inhibitory peptide C23 also blocks tumor growth in vivo in LNCaP xenograft-bearing mice .
    PACE4 Inhibitory peptide C23
  • HY-136541
    YB-0158
    2 Publications Verification

    Wnt pathway inhibitor 2

    		 Wnt Apoptosis Cancer
    YB-0158 (Wnt pathway inhibitor 2) is a reverse-turn peptidomimetic and a potent colorectal cancer stem cell (CSC) targeting agent. YB-0158 disrupts Sam68-Src interactions and induces apoptosis in CRC cells. Anti-cancer activities .
    YB-0158
  • HY-161177
    PROTAC SARS-CoV-2 3CLPro degrader 2

    		PROTACs SARS-CoV Virus Protease Infection
    PROTAC KRAS G12D degrader 2 is a peptidomimetic PROTAC specifically targeting the dimeric SARS-CoV-2 3CL Pro protein. PROTAC KRAS G12D degrader 2 inhibits SARS-CoV-2 3CLPro with an IC50 of 21.2 μM. PROTAC KRAS G12D degrader 2 specifically binds to the active site of SARS-CoV-2 3CL Pro. PROTAC KRAS G12D degrader 2 reduces protein levels of SARS-CoV-2 3CL Pro without affecting cell viability. PROTAC KRAS G12D degrader 2 can be used for the study of viral infections in Coronavirus genera .
    PROTAC SARS-CoV-2 3CLPro degrader 2
  • HY-W061614
    (4R)-1-Boc-4-fluoro-D-proline

    		Amino Acid Derivatives Others
    (4R)-1-Boc-4-fluoro-D-proline is an amino acid derivative that can be used for preparation of peptidomimetics, dihydropyridopyrimidines and pyridopyrimidines .
    (4R)-1-Boc-4-fluoro-D-proline
  • HY-12369
    GGTI-2133
    1 Publications Verification

    		 GGTase Inflammation/Immunology
    GGTI-2133, a peptidomimetic, is a selective geranylgeranyltransferase I (GGTase-I) inhibitor with an IC50 of 38 nM. GGTI-2133 shows 140-fold selectivity over farnesyltransferase (FTase) (IC50 of 5.4 μM). GGTI-2133 inhibits the geranylation of Rap-1A with an IC50 of 10 μM. GGTI-2133 can be used for the study of eosinophilic airway inflammation such as asthma .
    GGTI-2133
  • HY-126327A
    UNC4976 TFA

    		Histone Methyltransferase Cancer
    UNC4976 TFA is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 TFA simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA .
    UNC4976 TFA
  • HY-139311
    YH-53

    		SARS-CoV Infection
    YH-53 is a potent 3CL pro inhibitor with Ki values of 6.3 nM, 34.7 nM for SARS-CoV-1 3CL pro and SARS-CoV-2 3CL pro, respectively. YH-53 strongly blocks the SARS-CoV-2 replication. YH-53 is a peptidomimetic compound with a unique benzothiazolyl ketone. YH-53 has the potential for COVID-19 research .
    YH-53
  • HY-175597
    ClpP modulator-1

    		ClpP Infection
    ClpP modulator-1 (Compound BC8a), a peptidomimetic, is an allosteric ClpP modulator. ClpP modulator-1 is a ClpP activator at low concentration with EC50s of 0.35 and 0.58  μM for for Neisseria meningitides ClpP (NmClpP) and Escherichia coli ClpP (EcClpP), resepectively. ClpP modulator-1 also inhibits peptidase activity at high concentration by competitively inhibiting substrate protein (LY-AMC) binding to ClpP C sites. ClpP modulator-1 has antibacterial activity. ClpP modulator-1 can be used for bacterial infections research .
    ClpP modulator-1
  • HY-W012166
    N-Succinimidyl bromoacetate

    NHS-Bromoacetate

    		 Biochemical Assay Reagents Infection
    N-Succinimidyl bromoacetate (NHS-Bromoacetate) is a heterobifunctional crosslinking reagent, mainly used to modify the ɛ-amino group of lysine side chains. By covalently linking its bromoacetyl moiety to the ɛ-amino group of lysine in peptidomimetics, N-Succinimidyl bromoacetate enables their conjugation with thiol-modified nanoparticles via thioether bonds. N-Succinimidyl bromoacetate also performs bromoacetylation modification on carrier proteins, which then forms stable thioether bonds with the thiol groups of cysteine in peptides, thus efficiently preparing soluble peptide-protein conjugates with high substitution ratios. N-Succinimidyl bromoacetate can be used to prepare activated Sepharose derivatives for affinity chromatography, protein affinity labeling reagents, and peptide-protein immunogen conjugates with non-immunogenic linkages. N-Succinimidyl bromoacetate is applicable to studies related to HIV-1 infection and glioblastoma multiforme .
    N-Succinimidyl bromoacetate
  • HY-P1750
    Shepherdin (79-87)

    		HSP Survivin Cancer
    Shepherdin (79-87) is amino acids 79 to 87 fragment of Shepherdin. Shepherdin is a peptidomimetic antagonist of the complex between Hsp90 and Survivin. Anticancer activity .
    Shepherdin (79-87)
  • HY-P1750A
    Shepherdin (79-87) TFA

    		HSP Survivin Cancer
    Shepherdin (79-87) TFA is amino acids 79 to 87 fragment of Shepherdin. Shepherdin is a peptidomimetic antagonist of the complex between Hsp90 and Survivin. Anticancer activity .
    Shepherdin (79-87) TFA
  • HY-116254
    L-739750

    		Farnesyl Transferase Others
    L-739750 is a selective protein farnesyltransferase (PFTase) inhibitor (IC50: 0.4 nM). PFTase utilizes farnesyl diphosphate to farnesylate the cysteine residue of protein substrates having a C-terminal CAAX motif. L-739750 is a selective CAAX peptidomimetic .
    L-739750
  • HY-P2713
    OM99-2

    		Beta-secretase Neurological Disease
    OM99-2, an eight residue peptidomimetic, tight-binding inhibitor of human brain memapsin 2 with a Ki value of 9.58 nM . OM99-2 is significantly advanced the development of BACE1 inhibitor . OM99-2 has the potential for the research of the Alzheimer's disease .
    OM99-2
  • HY-12369A
    GGTI-2133 TFA

    		GGTase Inflammation/Immunology
    GGTI-2133 TFA, a peptidomimetic, is a selective geranylgeranyltransferase I (GGTase-I) inhibitor with an IC50 of 38 nM. GGTI-2133 TFA shows 140-fold selectivity over farnesyltransferase (FTase) (IC50 of 5.4 μM). GGTI-2133 TFA inhibits the geranylation of Rap-1A with an IC50 of 10 μM. GGTI-2133 TFA can be used for the study of eosinophilic airway inflammation such as asthma .
    GGTI-2133 TFA
  • HY-126327
    UNC4976

    		Histone Methyltransferase Cancer
    UNC4976 is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA .
    UNC4976
  • HY-P10407
    BM30

    		DNA Methyltransferase Cancer
    BM30 is a selective peptidomimetic NTMT1 and NTMT2 inhibitor (IC50: 0.89 μM for NTMT1) .
    BM30
  • HY-151709A
    N3-L-Cit-OH (DCHA)

    		ADC Linker Others
    N3-L-Cit-OH DCHA is a click chemistry reagent containing an azide group. N3-L-Cit-OH DCHA can be used to construct peptidomimetic ADC linkers using Click-chemistry . It contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing alkyne groups. It can also undergo ring strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing DBCO or BCN groups.
    N3-L-Cit-OH (DCHA)
  • HY-P11260
    MD5

    		Ser/Thr Protease Thrombin Metabolic Disease
    MD5 is a selective TMPRSS6 mimetic peptide inhibitor with an IC50 for recombinant human TMPRSS6 protein of 22 nM and a Ki of 3.4 nM. MD5 exhibits the significantly reduced inhibitory effect on Matriptase, with an IC50 of 352 nM and a Ki of 99.2 nM. MD5 exhibits good target specificity and only has a weak inhibitory effect on thrombin (Thrombin), with Ki of 120 nM. MD5 demonstrates good initial drugability and can be used for the study of iron overload diseases (such as hereditary hemochromatosis, β-thalassemia) .
    MD5
  • HY-U00207
    MEN11467

    		Neurokinin Receptor Neurological Disease Endocrinology
    MEN11467 is a selective and orally- effective peptidomimetic tachykinin NK1 receptor antagonist.
    MEN11467
  • HY-P3212A
    Allo-aca TFA

    		Neuropeptide Y Receptor Cancer
    Allo-aca TFA, a leptin peptidomimetic, is a potent, specific leptin receptor antagonist peptide. Allo-aca TFA blocks leptin signaling and action in numerous in vitro and in vivo models .
    Allo-aca TFA
  • HY-128044
    Ftase inhibitor I

    B581

    		 Farnesyl Transferase Cancer
    Ftase inhibitor I (B581) is a potent, selective and peptidomimetic farnesyl transferase (FTase) inhibitor. Ftase inhibitor I shows selectivity for FTase over geranylgeranyl isoprenoid (Ras-GG) or the fatty acid myristate (Myr-Ras) .
    Ftase inhibitor I
  • HY-W142064
    Fmoc-L-photo-proline

    		Antibiotic Others
    Fmoc-L-photo-proline is a photo-crosslinking amino acid which can be incorporated into synthetic peptides using solid-phase Fmoc chemistry. Fmoc-L-photo-proline can synthesis of cyclic peptidomimetic antibiotic and be used for preparation of diverse peptide-based photoaffinity probes research .
    Fmoc-L-photo-proline
  • HY-P1102A
    TC14012 TFA

    		CXCR HIV Infection Cancer
    TC14012 TFA, a serum-stable derivative of T140, is a selective and peptidomimetic CXCR4 antagonist with an IC50 of 19.3 nM. TC14012 TFA is a potent CXCR7 agonist with an EC50 of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 TFA has anti-HIV activity and anti-cancer activity .
    TC14012 TFA
  • HY-10235S
    Telaprevir-d4

    VX-950-d4

    		 Isotope-Labeled Compounds HCV Protease HCV SARS-CoV Infection
    Telaprevir-d4 is the deuterium labeled Telaprevir. Telaprevir (VX-950) is a highly selective, reversible, and potent peptidomimetic inhibitor of the HCV NS3-4A protease, the steady-state inhibitory constant (Ki) of Telaprevir is 7 nM against a genotype 1 (H strain) NS3 protease domain plus a NS4A cofactor peptide . Telaprevir inhibits SARS-CoV-2 3CLpro activity .
    Telaprevir-d4
  • HY-14588S1
    Lopinavir-d8

    		Isotope-Labeled Compounds HIV HIV Protease SARS-CoV Infection
    Lopinavir-d8 (ABT-378-d8) is the deuterium labeled Lopinavir. Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 14.2 μM .
    Lopinavir-d8
  • HY-126039
    L-739758

    		Integrin Cardiovascular Disease
    L-739758 is an antagonist for αIIbβ3 integrin (platelet glycoprotein IIb/IIIa). L-739758 acts as a peptidomimetic, binds to αIIbβ3 integrin by mimicking the interaction of the RGD (arginine-glycine-aspartic acid) motif, and is involved in the blood coagulation process. L-739758 inhibits platelet aggregation, and is used for thrombosis research .
    L-739758
  • HY-151496
    H-Cys-Val-2-Nal-Met-OH

    		Others Others
    H-Cys-Val-2-Nal-Met-OH is a peptide. H-Cys-Val-2-Nal-Met-OH is a peptidomimetic derivative that can be used to label short peptide sequences .
    H-Cys-Val-2-Nal-Met-OH
  • HY-P2713A
    OM99-2 TFA

    		Beta-secretase Neurological Disease
    OM99-2 TFA, an eight residue peptidomimetic, tight-binding inhibitor of human brain memapsin 2 with a Ki value of 9.58 nM . OM99-2 TFA is significantly advanced the development of BACE1 inhibitor . OM99-2 has the potential for the research of the Alzheimer's disease .
    OM99-2 TFA
  • HY-P2269
    MAIT-203

    		Drug Derivative Cancer
    MAIT-203, a cyclopentyalanin-derived peptidomimetic, potently inhibits the interaction of adenomatous polyposis coli (APC) and Asef (RhoGEF4), but not APC-Sam68 or APC-striatin interactions. MAIT-203 binds APC-ARM with a Ki of 0.015 μM and a Kd of 0.036 μM. MAIT-203 significantly represses the migration and invasion of colorectal cancer cells.
    MAIT-203
  • HY-129563
    CGP 57813

    		HIV HIV Protease Infection
    CGP 57813 is a peptidomimetic inhibitor of HIV protease that can be encapsulated by nanoparticles composed of poly(D,L-lactic acid) (PLA) and pH-sensitive methacrylic acid copolymers and delivered into the body .
    CGP 57813
  • HY-168853
    Antibacterial agent 261

    		Bacterial Infection
    Antibacterial agent 261 (compound 43) is a potent inhibitor of peptidomimetic peptide deformylase (PDF), with IC50 of 2.5 and 10.6 nM for S. aureus and E. coli, respectively .
    Antibacterial agent 261
  • HY-143410
    Anti-inflammatory agent 16

    		TNF Receptor Inflammation/Immunology
    Anti-inflammatory agent 16 (compound 14), a peptidomimetic, shows potent anti-inflammatory activity. Anti-inflammatory agent 16 reduces TNFα, NO, CD40 and CD86 expression level .
    Anti-inflammatory agent 16
  • HY-W612269S
    Isonicotinoyl chloride-d4

    		Isotope-Labeled Compounds Others
    Isonicotinoyl chloride-d4 is the deuterated labeled Isonicotinoyl chloride (HY-W612269). N-Acetylglycine (Aceturic acid) is a minor constituent of numerous foods with no genotoxicity or acute toxicity. N-acetylglycine is used in biological research of peptidomimetics .
    Isonicotinoyl chloride-d4
  • HY-P10028
    DC432

    		Fluorescent Dye Cancer
    HCT116 is a peptidomimetic inhibitor of N-terminal methyltransferase 1/2 (NTMT1/2) with an IC50 of 54 nM. HCT116 can inhibit the N-terminal methylation level of NTMT1/2 substrates in HCT116 cells, and is used for the study of NTMT1/2 probes.
    DC432
  • HY-P10010
    DB21, Galectin-1 Antagonist

    		Galectin Cancer
    DB21, Galectin-1 Antagonist is a dibenzofuran conjugated peptidomimetic that acts as an allosteric inhibitor of galectin-1 (GAL1)binding to cell surface glycans. DB21, Galectin-1 Antagonis increases inhibition of angiogenesis and tumour growth in melanoma, lung adenocarcinoma and ovarian cancer models .
    DB21, Galectin-1 Antagonist
  • HY-176516
    dAPM-1 acetate

    Diarginine Peptidomimetic-1

    		 Antibiotic Infection
    dAPM-1 (acetate) is a peptidomimetic antibiotic agent. dAPM-1 (acetate) can selectively induces intracellular aggregation in B. subtilis. dAPM-1 (acetate) is active against S. aureus, methicillin-resistant S. aureus (MRSA), B. subtilis, E. faecium, and M. smegmatis with MICs of 8, 4, 4, 8, and 16 µg/ml, respectively .
    dAPM-1 acetate
  • HY-P2269A
    MAIT-203 acetate

    		Drug Derivative Cancer
    MAIT-203 acetate is a cyclopentyalanin-derived peptidomimetic, potently inhibits the interaction of adenomatous polyposis coli (APC) and Asef (RhoGEF4), but not APC-Sam68 or APC-striatin interactions. MAIT-203 acetate binds APC-ARM with a Ki value of 0.015 μM and aKd value of 0.036 μM. MAIT-203 acetate significantly represses the migration and invasion of colorectal cancer cells .
    MAIT-203 acetate
  • HY-126402
    Arg-Gly-Asp TFA

    		Integrin Cancer
    Arg-Gly-Asp (RGD) is a synthetic peptide corresponding to the cell adhesion sequence for the integrins αVβ1, αVβ3, αVβ5, αVβ6, αVβ8, α8β1, and α5β1. It is a component of radioligands and peptidomimetics that have been used in the study of integrin expression and activity in vivo.
    Arg-Gly-Asp TFA

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