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Results for "

allosteric inhibition

" in MedChemExpress (MCE) Product Catalog:

25

Inhibitors & Agonists

2

Peptides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-150056
    CB1R Allosteric modulator 3

    		Cannabinoid Receptor Arrestin Neurological Disease
    CB1R Allosteric modulator 3 is a CB1R positive allosteric modulator. CB1R Allosteric modulator 3 has potent inhibition of cAMP and β-Arrestin with EC50 values of 0.018 μM and 1.241 μM, respectively .
    CB1R Allosteric modulator 3
  • HY-125176
    G907
    1 Publications Verification

    		 Bacterial Infection
    G907 is a selective antagonist of ATP-binding cassette (ABC) transporter MsbA with anti-microbial activity. G907 inhibits E. coli MsbA with an IC50 value of 18 nM. G907 traps MsbA in an inward-facing, lipopolysaccharide-bound conformation by wedging into an architecturally conserved transmembrane pocket .
    G907
  • HY-101165
    Cyclothiazide

    		iGluR Neurological Disease
    Cyclothiazide, a positive allosteric modulator of AMPA receptors, is used frequently to block the desensitization of both native and heterologously expressed AMPA receptors. Cyclothiazide is known to produce a fast inhibition of AMPA receptor desensitization and a much slower potentiation of the AMPA current .
    Cyclothiazide
  • HY-103572
    MNI137

    		mGluR Neurological Disease
    MNI137 is a potent and selective negative allosteric modulator for group II mGluRs. MNI137 has IC50s values of 8.3 and 12.6 nM for human and rat mGlu2 inhibition of glutamate-induced calcium mobilization .
    MNI137
  • HY-W011102
    S-Trityl-L-cysteine

    NSC 83265; S-Tritylcysteine; 3-Tritylthio-L-alanine

    		 Kinesin Apoptosis Cancer
    S-Trityl-L-cysteine (NSC 83265) is a selective and allosteric kinesin Eg5 inhibitor with an IC50 of 1 μM for the inhibition of basal ATPase activity and 140 nM for the microtubule-activated ATPase activity. S-Trityl-L-cysteine has antitumor activities .
    S-Trityl-L-cysteine
  • HY-13965
    Parmodulin 2
    2 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-141524
    RMC-3943

    		SHP2 Phosphatase Cancer
    RMC-3943 is an allosteric SHP2 inhibitor (inhibition of full-length SHP2 in biochemical assay, IC50 = 2.19 nM) .
    RMC-3943
  • HY-163532
    FLS-359

    		Sirtuin Infection
    FLS-359 is a selective, orally active allosteric modulator for sirtuin 2, with the IC50 of 3 μM. FLS-359 exhibits antiviral activity against RNA and DNA virus, through inhibition of DNA/RNA replication .
    FLS-359
  • HY-121736
    AGI-12026

    AGI-026

    		 Isocitrate Dehydrogenase (IDH) Neurological Disease
    AGI-12026 is brain-penetrant dual inhibitor of mutant IDH1 and 2. AGI-12026 shows partial inhibition of the IDH1-R132H homodimer as allosteric modulators. AGI-12026 has the potential for research of glioma .
    AGI-12026
  • HY-121140
    AZ1729

    		Free Fatty Acid Receptor Metabolic Disease
    AZ1729 is a potent free fatty acid 2 receptor (FFA2) activator, acting as a direct allosteric agonist and as a positive allosteric modulator. AZ1729 increases the activity of the endogenously produced short chain fatty acid propionate in Gi-mediated pathways, but not at those transduced by Gq/G11. AZ1729 induces inhibition of isoproterenol-induced lipolysis in mouse adipocytes. AZ1729 also can Induce migration of human neutrophils. AZ1729 can be used for researching the signaling pathways of the physiological roles of FFA2 .
    AZ1729
  • HY-101165R
    Cyclothiazide (Standard)

    		iGluR Neurological Disease
    Cyclothiazide (Standard) is the analytical standard of Cyclothiazide. This product is intended for research and analytical applications. Cyclothiazide, a positive allosteric modulator of AMPA receptors, is used frequently to block the desensitization of both native and heterologously expressed AMPA receptors. Cyclothiazide is known to produce a fast inhibition of AMPA receptor desensitization and a much slower potentiation of the AMPA current .
    Cyclothiazide (Standard)
  • HY-19934A
    Pifusertib hydrochloride

    TAS-117 hydrochloride

    		 Akt Apoptosis Autophagy Cancer
    Pifusertib (TAS-117) hydrochloride is a potent, selective, orally active allosteric Akt inhibitor (with IC50s of 4.8, 1.6, and 44 nM for Akt1, 2, and 3, respectively). Pifusertib hydrochloride triggers anti-myeloma activities and enhances fatal endoplasmic reticulum (ER) stress induced by proteasome inhibition. Pifusertib hydrochloride induces apoptosis and autophagy .
    Pifusertib hydrochloride
  • HY-19934
    Pifusertib

    TAS-117

    		 Akt Apoptosis Autophagy Cancer
    Pifusertib (TAS-117) is a potent, selective, orally active allosteric Akt inhibitor (with IC50s of 4.8, 1.6, and 44 nM for Akt1, 2, and 3, respectively). Pifusertib triggers anti-myeloma activities and enhances fatal endoplasmic reticulum (ER) stress induced by proteasome inhibition. Pifusertib induces apoptosis and autophagy .
    Pifusertib
  • HY-120645
    BMS-986122

    		Opioid Receptor Neurological Disease
    BMS-986122 is a selective, potent positive allosteric modulator of the mu-opioid receptor (μ-OR). BMS-986122 shows potentiation of orthosteric agonist-mediated β-arrestin recruitment, adenylyl cyclase inhibition, and G protein activation. BMS-986122 potentiates DAMGO-mediated [ 35S]GTPγS binding in mouse brain membranes .
    BMS-986122
  • HY-122255
    LY487379

    		mGluR Neurological Disease
    LY487379 is a selective human mGluR2 positive allosteric modulator (PAM). LY487379 potentiates glutamate-stimulated [ 35S]GTPγS binding with EC50 values of 1.7 μM and >10 μM for mGlu2 and mGlu3 receptors respectively. LY487379 promotes cognitive flexibility and facilitates behavioral inhibition in a rat model. LY487379 can be used for schizophrenia research .
    LY487379
  • HY-148799
    Sevasemten

    		Myosin Others
    Sevasemten is an orally active allosteric inhibitor of skeletal muscle myosin that protects skeletal muscle from contraction-induced injury. Sevasemten exhibits selectively myosin inhibition with IC50s of ≤10 μM (skeletal), >100 μM (cardiac), respectively. Sevasemten decreases muscle damage biomarkers and fibrosis while increasing muscle strength and activity in in Duchenne muscular dystrophy disease models .
    Sevasemten
  • HY-103552
    LY487379 hydrochloride

    		mGluR Neurological Disease
    LY487379 hydrochloride is a selective human mGluR2 positive allosteric modulator (PAM). LY487379 hydrochloride potentiates glutamate-stimulated [ 35S]GTPγS binding with EC50 values of 1.7 μM and >10 μM for mGlu2 and mGlu3 receptors respectively. LY487379 hydrochloride promotes cognitive flexibility and facilitates behavioral inhibition in a rat model. LY487379 hydrochloride can be used for schizophrenia research .
    LY487379 hydrochloride
  • HY-122247
    PVZB1194

    		Kinesin Cancer
    PVZB1194 is a biphenyl-type inhibitor of Kinesin spindle protein Eg5 or KIF11. Eg5 is related to the cell cycle, and Eg5 inhibition can lead to cell cycle arrest and apoptosis. PVZB1194 exhibits anticancer potential via inhibiting Eg5 ATPase activity. PVZB1194 binds to the α4/α6 allosteric pocket, and shows ATP competetive activity .
    PVZB1194
  • HY-120355A
    AP14145 hydrochloride

    		Potassium Channel Cardiovascular Disease
    AP14145 hydrochloride is a potent KCa2 (SK) channel negative allosteric modulator with an IC50 of 1.1 μM for KCa2.2 (SK2) and KCa2.3 (SK3) channels. AP14145 hydrochloride inhibition strongly depends on two amino acids, S508 and A533 in the channel. AP14145 hydrochloride prolonged atrial effective refractory period (AERP) in rats and demonstrates antiarrhythmic effects in a Vernakalant-resistant porcine model of atrial fibrillation (AF) .
    AP14145 hydrochloride
  • HY-P0172A
    ATI-2341 TFA
    2 Publications Verification

    		 CXCR Inflammation/Immunology Endocrinology Cancer
    ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs) .
    ATI-2341 TFA
  • HY-P0172
    ATI-2341

    		CXCR Inflammation/Immunology Endocrinology Cancer
    ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs) .
    ATI-2341
  • HY-112289
    IDH889

    		Isocitrate Dehydrogenase (IDH) Cancer
    IDH889 is an orally available, brain penetrant, allosteric and mutant specific inhibitor of isocitrate dehydrogenase 1 (IDH1). IDH889 has potent selectivity for IDH1 R132* mutations, with IC50s of 0.02 μM, 0.072 μM and 1.38 μM for IDH1 R132H, IDH1 R132C and IDH1 wt, respectively. IDH889 shows potent cellular inhibition of R-2-hydroxyglutarate (2-HG) production with an IC50 of 0.014 μM .
    IDH889
  • HY-116152
    Cipepofol

    Ciprofol; HSK3486

    		 GABA Receptor Sirtuin Keap1-Nrf2 Apoptosis Cardiovascular Disease Neurological Disease Inflammation/Immunology
    Cipepofol (Ciprofol), a novel 2,6-disubstituted phenol derivative, is a positive allosteric modulator and direct agonist of the GABAA receptor. Cipepofol can cause the central nerve inhibition and promote sleep based on the structural modification of Propofol (HY-B0649). Cipepofol can activate the sirtuin1 (Sirt1)/Nrf2 pathway. Cipepofol protects the heart against Isoproterenol (ISO; HY-B0468)-induced myocardial infarction by reducing cardiac oxidative stress, inflammatory response and cardiomyocyte apoptosis .
    Cipepofol
  • HY-118285
    Ro4491533

    		mGluR Neurological Disease
    Ro4491533 is a selective, negative allosteric mGluR2/3 receptor modulator that is equally effective on both subtypes. Ro4491533 can completely block glutamate-induced calcium mobilization and glutamate-induced [35S]GTPγS binding accumulation. Ro4491533 has good pharmacokinetic properties in mice and rats, high oral bioavailability, and can pass through the blood-brain barrier. Ro4491533 can also reverse the motor inhibition effect of LY379268 in mice and show antidepressant activity in the forced swim test and tail suspension test.
    Ro4491533
  • HY-112289B
    (1R)-IDH889

    		Isocitrate Dehydrogenase (IDH) Cancer
    (1R)-IDH889 is the isomer of IDH889 (HY-112289), and can be used as an experimental control. IDH889 is an orally available, brain penetrant, allosteric and mutant specific inhibitor of isocitrate dehydrogenase 1 (IDH1). IDH889 has potent selectivity for IDH1 R132* mutations, with IC50s of 0.02 μM, 0.072 μM and 1.38 μM for IDH1 R132H, IDH1 R132C and IDH1 wt, respectively. IDH889 shows potent cellular inhibition of R-2-hydroxyglutarate (2-HG) production with an IC50 of 0.014 μM .
    (1R)-IDH889

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