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Results for "

non-competitive allosteric inhibitor

" in MedChemExpress (MCE) Product Catalog:

31

Inhibitors & Agonists

4

Peptides

4

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-15251
    Reparixin
    Maximum Cited Publications
    62 Publications Verification

    Repertaxin; DF 1681Y

    		 CXCR Inflammation/Immunology Endocrinology Cancer
    Reparixin is a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2 activation with IC50s of 1 and 100 nM, respectively.
    Reparixin
  • HY-12755
    ML141
    30+ Cited Publications

    CID-2950007

    		 Ras Apoptosis Cancer
    ML141 (CID-2950007) is a potent, allosteric, selective and reversible non-competitive inhibitor of Cdc42 GTPase. ML141 inhibits Cdc42 wild type and Cdc42 Q61L mutant with EC50s of 2.1 and 2.6 μM, respectively. ML141 shows low micromolar potency and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7). ML141 do not show cytotoxicity in multiple cell lines .
    ML141
  • HY-138630
    AG-270
    5+ Cited Publications

    		 Methionine Adenosyltransferase (MAT) Cancer
    AG-270 is an allosteric, noncompetitive, first-in-class, reversible and orally active MAT2A inhibitor, with an IC50 of 14 nM .
    AG-270
  • HY-137067
    IMT1B
    5+ Cited Publications

    LDC203974

    		 DNA/RNA Synthesis Cancer
    IMT1B (LDC203974) is an orally active, noncompetitive and specific allosteric inhibitor of mitochondrial RNA polymerase (POLRMT) and inhibits mitochondrial DNA (mtDNA) expression. IMT1B has anti-tumour effects .
    IMT1B
  • HY-W096171
    D-Dopa

    3-Hydroxy-D-tyrosine

    		 Carboxypeptidase Infection Neurological Disease
    D-Dopa (3-Hydroxy-D-tyrosine) is a potent, orally active, non-competitive and allosteric inhibitor of glutamate carboxypeptidase II (GCPII) with an IC50 of 200 nM. D-Dopa elevates brain dopamine and produce turning behavior in rats. D-Dopa inhibit severe fever with thrombocytopenia syndrome (SFTS) virus infection. D-Dopa can be used for neurological disease and virus infection research .
    D-Dopa
  • HY-100386
    Ticlopidine
    3 Publications Verification

    PCR 5332

    		 NTPDase Cytochrome P450 Cardiovascular Disease
    Ticlopidine (PCR 5332), an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC50 of 81.7 μM. Ticlopidine blocks several NTPDase isoenzymes with IC50s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively. Ticlopidine is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine inhibits CYP2C9 and CYP3A4 with IC50s of 26.0 and 32.3 μM, respectively.
    Ticlopidine
  • HY-12042
    Pimasertib
    5+ Cited Publications

    AS703026; MSC1936369B

    		 MEK Cancer
    Pimasertib (AS703026) is a highly selective, ATP non-competitive allosteric orally available MEK1/2 inhibitor .
    Pimasertib
  • HY-13965
    Parmodulin 2
    5 Publications Verification

    ML161

    		 Protease Activated Receptor (PAR) Cardiovascular Disease
    Parmodulin 2 (ML161) is an allosteric inhibitor of protease-activated receptor 1 (PAR1) with an IC50 of 0.26 μM . Parmodulin 2 is a potent and non-competitive inhibitor of SFLLRN-induced P-selectin expression leading to inhibition of platelet aggregation in vitro and platelet thrombus formation in vivo .
    Parmodulin 2
  • HY-B0153A
    Ticlopidine hydrochloride
    3 Publications Verification

    		 NTPDase Cytochrome P450 Cardiovascular Disease Neurological Disease Cancer
    Ticlopidine (PCR 5332) hydrochloride, an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC50 of 81.7 μM. Ticlopidine hydrochloride blocks several NTPDase isoenzymes with IC50s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively. Ticlopidine hydrochloride is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine hydrochloride inhibits CYP2C9 and CYP3A4 with IC50s of 26.0 and 32.3 μM, respectively .
    Ticlopidine hydrochloride
  • HY-123872
    MSC1094308
    1 Publications Verification

    		 p97 Cancer
    MSC1094308 is a non-competitive and reversible VPS4B/p97 (VCP) (I/II type AAA ATPase) allosteric inhibitor, with IC50 values of 0.71 μM and 7.2 μM for VPS4B and p97, respectively . MSC1094308 inhibits the D2 ATPase activity by binding to a agentable hotspot of p97. MSC1094308 can be used in study of cancer .
    MSC1094308
  • HY-50672
    MK-0731

    		Kinesin Apoptosis Lipoxygenase Cancer
    MK-0731 is a selective, non-competitive and allosteric kinesin spindle protein (KSP) inhibitor with an IC50 of 2.2 nM and a pKa of 7.6. MK-0731 is >20,000 fold selectivity against other kinesins. MK-0731 induces mitotic arrest and induces apoptosis in tumors. MK-0731 provides significant antitumor efficacy .
    MK-0731
  • HY-156659
    NC1

    		Phosphatase ERK Inflammation/Immunology
    NC1 is a selective non-competitive and allosteric lymphoid-specific tyrosine phosphatase (LYP) inhibitor, with a Ki value 4.3 μM. NC1 allosterically regulates LYP/PTPN22 activity by restricting WPD loop movement. NC1 inhibits LYP activity in lymphoid T cells and enhances T-cell receptor signaling. NC1 can be used for the research of autoimmune diseases .
    NC1
  • HY-15756
    PTP1B-IN-4
    1 Publications Verification

    		 Phosphatase Metabolic Disease
    PTP1B-IN-4 is a non-competitive allosteric inhibitor of the protein tyrosine phosphatase PTP1B, with an IC50 of 8 μM. PTP1B-IN-4 is potentail for the research of obesity and diabetes .
    PTP1B-IN-4
  • HY-100386R
    Ticlopidine (Standard)

    PCR 5332 (Standard)

    		 Reference Standards NTPDase Cytochrome P450 Cardiovascular Disease
    Ticlopidine (Standard) is the analytical standard of Ticlopidine. This product is intended for research and analytical applications. Ticlopidine (PCR 5332), an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC50 of 81.7 μM. Ticlopidine blocks several NTPDase isoenzymes with IC50s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively . Ticlopidine is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine inhibits CYP2C9 and CYP3A4 with IC50s of 26.0 and 32.3 μM, respectively .
    Ticlopidine (Standard)
  • HY-15251A
    (Rac)-Reparixin

    (Rac)-Repertaxin; (Rac)-DF 1681Y

    		 CXCR Inflammation/Immunology Endocrinology Cancer
    (Rac)-Reparixin is the isomer of Reparixin (HY-15251), and can be used as an experimental control. Reparixin is a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2 activation with IC50s of 1 and 100 nM, respectively.
    (Rac)-Reparixin
  • HY-P1259A
    PR-39 TFA

    		Proteasome Bacterial Inflammation/Immunology
    PR-39 TFA, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 TFAreversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 TFA stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice .
    PR-39 TFA
  • HY-129636
    CLH304a

    (E)-GABAB receptor antagonist 1

    		 GABA Receptor ERK Neurological Disease
    CLH304a (compound 14) is a specific and noncompetitive GABAB receptor negative allosteric modulator (NAM). CLH304a decreases GABA-induced IP3 production with an IC50 of 37.9 μM. CLH304a has no effect on other GPCR Class C members such as mGluR1, mGluR2, and mGluR5. CLH304a acts on the heptahelical domain of GB2 subunits and non-competitively inhibits the effect of agonists with inverse agonist properties. CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptor .
    CLH304a
  • HY-P4160
    PDC31

    THG113.31; ILGHXDYK

    		 Prostaglandin Receptor Endocrinology
    PDC31 (THG113.31; ILGHXDYK) is an allosteric and non-competitive inhibitor of FP Prostaglandin Receptor. PDC31 is the D-amino acid-based oligopeptide, is used for smooth muscle contractile agent. PDC31 decreases the strength and duration of uterine contractions in vivo, which can be used for research of preterm labor and primary dysmenorrhea (PD). PDC31 also enhances Ca 2+-dependent large-conductance K +-channel in human myometrial cells .
    PDC31
  • HY-P1259
    PR-39

    		Proteasome Bacterial Inflammation/Immunology
    PR-39, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 reversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice .
    PR-39
  • HY-12042A
    Pimasertib hydrochloride

    AS703026 hydrochloride; MSC1936369B hydrochloride

    		 MEK Cancer
    Pimasertib hydrochloride is a highly selective, ATP non-competitive allosteric orally available MEK1/2 inhibitor .
    Pimasertib hydrochloride
  • HY-15251R
    Reparixin (Standard)

    Repertaxin (Standard); DF 1681Y (Standard)

    		 CXCR Reference Standards Inflammation/Immunology Endocrinology Cancer
    Reparixin (Standard) is the analytical standard of Reparixin. This product is intended for research and analytical applications. Reparixin is a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2 activation with IC50s of 1 and 100 nM, respectively.
    Reparixin (Standard)
  • HY-179714
    DAM-001

    Z236004662

    		 Dopamine Transporter Neurological Disease
    DAM-001 (Z236004662) is a potent, non-competitive allosteric inhibitor for human dopamine transporter (hDAT) with an IC50 of 24.70 μM and 1.026 μM in the absence and presence of orthosteric inhibitor Nomifensine (HY-B1110) .
    DAM-001
  • HY-144396
    SHP2-IN-8

    		SHP2 Phosphatase Akt Apoptosis Cancer
    SHP2-IN-8 is a highly potent, selective, and cellularly active allosteric SHP2 inhibitor with IC50 value of 23 nM and Ki of 22 nM. SHP2-IN-8 is reversible and noncompetitive. SHP2-IN-8 causes a significant thermal shift with the ΔTm of 7.01 °C. SHP2-IN-8 induces the apoptosis and inhibits the phosphorylation of AKT in Hela cells .
    SHP2-IN-8
  • HY-100386S
    Ticlopidine-d4

    PCR 5332-d4

    		 Isotope-Labeled Compounds NTPDase Cytochrome P450 Cardiovascular Disease
    Ticlopidine-d4 is the deuterium labeled Ticlopidine. Ticlopidine (PCR 5332), an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC50 of 81.7 μM. Ticlopidine blocks several NTPDase isoenzymes with IC50s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively . Ticlopidine is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine inhibits CYP2C9 and CYP3A4 with IC50s of 26.0 and 32.3 μM, respectively .
    Ticlopidine-d4
  • HY-129636A
    (E/Z)-CLH304a

    GABAB receptor antagonist 1

    		 GABA Receptor ERK Neurological Disease
    (E/Z)-CLH304a (GABAB receptor antagonist 1) is a mixture of (E)-CLH304a and (Z)-CLH304a. (E)-CLH304a (CLH304a; HY-129636) is a specific and noncompetitive GABAB receptor negative allosteric modulator (NAM). CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptors .
    (E/Z)-CLH304a
  • HY-B0153AS
    Ticlopidine-d4 hydrochloride

    		Isotope-Labeled Compounds NTPDase Cytochrome P450 Cardiovascular Disease
    Ticlopidine-d4 hydrochloride is the deuterium labeled Ticlopidine hydrochloride (HY-B0153A). Ticlopidine (PCR 5332) hydrochloride, an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC50 of 81.7 μM. Ticlopidine hydrochloride blocks several NTPDase isoenzymes with IC50s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively . Ticlopidine hydrochloride is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine hydrochloride inhibits CYP2C9 and CYP3A4 with IC50s of 26.0 and 32.3 μM, respectively .
    Ticlopidine-d4 hydrochloride
  • HY-W707554
    Ticlopidine hydrochloride-d6

    		Isotope-Labeled Compounds Cytochrome P450 Cardiovascular Disease
    Ticlopidine hydrochloride-d6 is the deuterium labeled Ticlopidine hydrochloride (HY-B0153A). Ticlopidine (PCR 5332) hydrochloride, an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC50 of 81.7 μM. Ticlopidine hydrochloride blocks several NTPDase isoenzymes with IC50s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively . Ticlopidine hydrochloride is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine hydrochloride inhibits CYP2C9 and CYP3A4 with IC50s of 26.0 and 32.3 μM, respectively .
    Ticlopidine hydrochloride-d6
  • HY-B0153AR
    Ticlopidine hydrochloride (Standard)

    		Reference Standards NTPDase Cytochrome P450 Cardiovascular Disease
    Ticlopidine hydrochloride (Standard) is the analytical standard of Ticlopidine hydrochloride (HY-B0153A). This product is intended for research and analytical applications. Ticlopidine (PCR 5332) hydrochloride, an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC50 of 81.7 μM. Ticlopidine hydrochloride blocks several NTPDase isoenzymes with IC50s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively . Ticlopidine hydrochloride is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine hydrochloride inhibits CYP2C9 and CYP3A4 with IC50s of 26.0 and 32.3 μM, respectively .
    Ticlopidine hydrochloride (Standard)
  • HY-15251AR
    (Rac)-Reparixin (Standard)

    (Rac)-Repertaxin (Standard); (Rac)-DF 1681Y (Standard)

    		 CXCR Reference Standards Inflammation/Immunology Endocrinology Cancer
    (Rac)-Reparixin (Standard) is the analytical standard of (Rac)-Reparixin. This product is intended for research and analytical applications. (Rac)-Reparixin is the isomer of Reparixin (HY-15251), and can be used as an experimental control. Reparixin is a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2 activation with IC50s of 1 and 100 nM, respectively.
    (Rac)-Reparixin (Standard)
  • HY-183942
    USP7-IN-20

    		Deubiquitinase Apoptosis MDM-2/p53 PARP Caspase Cancer
    USP7-IN-20 is a highly selective USP7 inhibitor that binds allosterically to the allosteric pocket of USP7 in a non-competitive and reversible manner. USP7-IN-20 downregulates MDM2 protein levels and stabilizes p53, thereby inducing p21 expression and enhancing the ubiquitin-dependent degradation of MDM2. USP7-IN-20 effectively binds endogenous USP7 to inhibit cancer cell proliferation, and also induces apoptosis by promoting the cleavage of PARP and caspase 3. USP7-IN-20 can be widely used in cancer-related basic and translational research.
    USP7-IN-20
  • HY-166530S
    Ticlopidine-d6 hydrochloride

    		Isotope-Labeled Compounds Cytochrome P450 Cardiovascular Disease
    Ticlopidine-d6 hydrochloride is the deuterium labeled Ticlopidine hydrochloride. Ticlopidine (PCR 5332) hydrochloride, an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC50 of 81.7 μM. Ticlopidine hydrochloride blocks several NTPDase isoenzymes with IC50s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively . Ticlopidine hydrochloride is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine hydrochloride inhibits CYP2C9 and CYP3A4 with IC50s of 26.0 and 32.3 μM, respectively .
    Ticlopidine-d6 hydrochloride

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