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Results for "

IP accumulation

" in MedChemExpress (MCE) Product Catalog:

20

Inhibitors & Agonists

3

Peptides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-P3419
    PAMP-12 (unmodified)
    2 Publications Verification

    		 Mas-related G-protein-coupled Receptor (MRGPR) PERK Calcium Channel Cardiovascular Disease Inflammation/Immunology
    PAMP-12 (unmodified) is an endogenous peptide and is a MrgX2 agonist. PAMP-12 (unmodified) can reduce cAMP accumulation, increase Ca 2+ levels, enhance beta-arrestin recruitment, decrease IP-1, and increases phosphoERK. PAMP-12 (unmodified) can elicit hypotension through inhibiting catecholamine secretion from sympathetic nerve endings and adrenal chromaffin cells. PAMP-12 (unmodified) can be used for the research of hypotension and ulcerative colitis .
    PAMP-12 (unmodified)
  • HY-10559
    Nelotanserin
    2 Publications Verification

    APD125

    		 5-HT Receptor Neurological Disease Cancer
    Nelotanserin is a potent 5-HT2A inverse agonist, a moderately potent 5-HT2C partial inverse agonist and a weak 5-HT2B inverse agonist, with IC50s of 1.7, 79, 791 nM in IP accumulation assays, respectively.
    Nelotanserin
  • HY-139439
    SBI-581

    		Ser/Thr Protease Cancer
    SBI-581 is an orally active and potent selective serine-threonine kinase TAO3 inhibitor, with an IC50 of 42 nM. SBI-581 promotes TKS5α accumulation at RAB11-positive vesicles. SBI-581 inhibits invadopodia formation. SBI-581 shows reasonable pharmacokinetics in mice using IP injection. SBI-581 shows antitumor activity . SBI-581 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    SBI-581
  • HY-P4987
    TRAP-7

    		Protease Activated Receptor (PAR) Cardiovascular Disease
    TRAP-7 is a thrombin receptor (PAR) activating peptide. TRAP-7 stimulates total inositol phosphate (IP) accumulation and phosphorylation of a specific endogenous substrate for activated PKC. TRAP-7 can be used in cardiovascular disease research .
    TRAP-7
  • HY-13699
    NBI-42902

    		GnRH Receptor PERK Others
    NBI-42902 is an orally active, potent functional and competitive antagonist of GnRH receptor with an IC50 value of 0.79 nM, a Ki value of 0.56 nM, respectively. NBI-42902 inhibits GnRH-stimulated inositol phosphate (IP) accumulation, Ca 2+ flux, and ERK1/2 activation. NBI-42902 inhibits serum luteinizing hormone (LH) in castrated male macaques. NBI-42902 can be used for research on sex-hormone-related diseases .
    NBI-42902
  • HY-118806A
    AC-42 hydrochloride

    		mAChR Neurological Disease
    AC-42 hydrochloride is the hydrochloride salt form of AC-42 (HY-118806). AC-42 hydrochloride is an allosteric agonist for muscarinic M1 receptor with EC50s of 805 nM and 220 nM for human wild-type and Y381A mutated M1 receptors, respectively. AC-42 hydrochloride stimulates the inositol phosphate (IP)-accumulation and calcium mobilization in CHO cells .
    AC-42 hydrochloride
  • HY-108507
    MRT-10

    		Smo Cancer
    MRT-10 is a seven-transmembrane receptor smoothened (Smo) antagonist with an IC50 of 0.65 μM in the micromolar range in various Hedgehog (Hh) assays. MRT-10 binds to the Smo receptor at the level of the Bodipycyclopamine binding site. MRT-10 can be used for the research of cancer .
    MRT-10
  • HY-W565924
    STX107

    		mGluR ERK Neurological Disease
    STX107 is a metabotropic glutamate 5 (mGlu5) receptor negative allosteric modulator (NAM) with a pKi of 8.32. STX107 inhibits glutamate-induced Ca 2+ mobilization, IP1 accumulation, and ERK1/2 phosphorylation. STX107 also inhibits glutamate-induced mGlu5 internalization .
    STX107
  • HY-153095
    PF-6870961

    		GHSR Metabolic Disease
    PF-6870961 is an inverse agonist of GHSR1a with Ki values of 73.6 nM (human GHSR), 239 nM (rat GHSR), and 217 nM (dog GHSR), respectively. PF-6870961 inhibits the constitutive GHSR1a-induced IP accumulation with an IC50 value of 300 nM. PF-6870961 also inhibits constitutive GHSR1a β-arrestin mobilization with an IC50 value of 1.10 nM .
    PF-6870961
  • HY-175477
    UNC9750

    		DAPK DYRK PDGFR IPK Superfamily Cancer
    UNC9750 is an inositol phosphate multikinase (IPMK) inhibitor with IC50 values ​​of 31.6 and 374 nM for IPMK and IP6K2, respectively.. UNC9750 inhibits cellular accumulation of InsP5, the direct product of IPMK kinase activity, while having no effect on either InsP6 or InsP7 levels. UNC9750 has ≥ 75% inhibition of four kinases (DAPK1, DYRK1B, PDGFR, and KDR). UNC9750 can be used for the study of glioblastoma .
    UNC9750
  • HY-101607
    KT-362

    		Calcium Channel Cardiovascular Disease
    KT-362 is an intracellular calcium antagonist. KT-362 can inhibit NE-induced contractions and IP accumulation in vivo experiments .
    KT-362
  • HY-118806
    AC-42

    		mAChR Neurological Disease
    AC-42 is a poent M1 muscarinic selective allosteric agonist with EC50s of 805 nM and 220 nM for human wild-type and Y381A mutated M1 receptors, respectively. AC-42 stimulates the IP-accumulation and calcium mobilization in CHO cells .
    AC-42
  • HY-P3419A
    PAMP-12 (unmodified) TFA

    		Mas-related G-protein-coupled Receptor (MRGPR) PERK Calcium Channel Cardiovascular Disease Inflammation/Immunology
    PAMP-12 (unmodified) TFA is an endogenous peptide and is a MrgX2 agonist. PAMP-12 (unmodified) TFA can reduce cAMP accumulation, increase Ca 2+ levels, enhance beta-arrestin recruitment, decrease IP-1, and increases phosphoERK. PAMP-12 (unmodified) TFA can elicit hypotension through inhibiting catecholamine secretion from sympathetic nerve endings and adrenal chromaffin cells. PAMP-12 (unmodified) TFA can be used for the research of hypotension and ulcerative colitis .
    PAMP-12 (unmodified) TFA
  • HY-153095A
    PF-6870961 hydrochloride

    		GHSR Metabolic Disease
    PF-6870961 hydrochloride is an inverse agonist of GHSR1a with Ki values of 73.6 nM (human GHSR), 239 nM (rat GHSR), and 217 nM (dog GHSR), respectively. PF-6870961 hydrochloride inhibits the constitutive GHSR1a-induced IP accumulation with an IC50 value of 300 nM. PF-6870961 hydrochloride also inhibits constitutive GHSR1a β-arrestin mobilization with an IC50 value of 1.10 nM .
    PF-6870961 hydrochloride
  • HY-108507R
    MRT-10 (Standard)

    		Reference Standards Smo Cancer
    MRT-10 (Standard) is the analytical standard of MRT-10 (HY-108507). This product is intended for research and analytical applications. MRT-10 is a seven-transmembrane receptor smoothened (Smo) antagonist with an IC50 of 0.65 μM in the micromolar range in various Hedgehog (Hh) assays. MRT-10 binds to the Smo receptor at the level of the Bodipycyclopamine binding site. MRT-10 can be used for the research of cancer .
    MRT-10 (Standard)
  • HY-179606
    RWT9996

    		Transmembrane Glycoprotein Arrestin ERK Epigenetic Reader Domain Neurological Disease
    RWT9996 is a balanced GPR17 antagonist. RWT9996 has an inhibitory effect on G protein activation and β-arrestin-2 recruitment induced by MDL-29951. RWT9996 inhibits the phosphorylation of ERK/CREB and the accumulation of inositol phosphate (b IP1) induced by MDL-29951. RWT9996 can be used for the study of neurological diseases .
    RWT9996
  • HY-10559R
    Nelotanserin (Standard)

    APD125 (Standard)

    		 Reference Standards 5-HT Receptor Neurological Disease Cancer
    Nelotanserin (Standard) is the analytical standard of Nelotanserin (HY-10559). This product is intended for research and analytical applications. Nelotanserin is a potent 5-HT2A inverse agonist, a moderately potent 5-HT2C partial inverse agonist and a weak 5-HT2B inverse agonist, with IC50s of 1.7, 79, 791 nM in IP accumulation assays, respectively.
    Nelotanserin (Standard)
  • HY-180465
    5-HT2C agonist-12

    		5-HT Receptor Metabolic Disease
    5-HT2C agonist-12 (example.2) is a selective and orally active 5-HT2C receptor agonist. 5-HT2C agonist-12 can inhibit the accumulation of IP3 with an IC50 of 4.5 nM. 5-HT2C agonist-12 can induce a feeling of fullness, shorten the time of eating, and reduce calorie intake. 5-HT2C agonist-12 can be used for the research of obesity .
    5-HT2C agonist-12
  • HY-182360
    Cytisine-platinum(IV) prodrug-1

    		PERK Eukaryotic Initiation Factor (eIF) Bcl-2 Family Apoptosis Reactive Oxygen Species (ROS) STING DNA/RNA Synthesis PD-1/PD-L1 Cancer
    Cytisine-Platinum(IV) Prodrug-1 is a Pt(IV) prodrug incorporating the natural compound Cytisine (HY-N0175) with antiproliferative activity against tumor cells. Cytisine-Platinum(IV) Prodrug-1 promotes calcium transfer across the IP3R1-GRP75-VDAC1 axis to drive mitochondrial calcium overload. Cytisine-Platinum(IV) Prodrug-1 initiates unfolded protein response via PERK, eIF2α, ATF4, and CHOP to modulate Bcl-2 and Bax, triggering apoptosis. Cytisine-Platinum(IV) Prodrug-1 induces mitochondrial dysfunction, ROS production, reduced ATP synthesis, DNA damage, and S-phase cell cycle arrest. Cytisine-Platinum(IV) Prodrug-1 activates the cGAS-STING pathway, reduces PD-L1 expression, drives immunogenic cell death. Cytisine-Platinum(IV) Prodrug-1 exhibits high physiological stability, efficient cellular accumulation, and enhanced platinum-DNA binding, and inhibits tumor growth in mouse models with reduced systemic toxicity. Cytisine-Platinum(IV) Prodrug-1 can be used for the research of lung cancer .
    Cytisine-platinum(IV) prodrug-1
  • HY-183357
    GABAAR/5-HT2AR modulator-1

    		GABA Receptor 5-HT Receptor Reactive Oxygen Species (ROS) TNF Receptor Interleukin Related COX NF-κB IKK NO Synthase Neurological Disease Inflammation/Immunology
    GABAAR/5-HT2AR modulator-1 is an orally active and brain-penetrant GABAAR agonist and 5-HT2AR antagonist with Kd values of 0.89 and 0.78 μM. GABAAR/5-HT2AR modulator-1 blocks 5-HT-stimulated IP1 accumulation, inducing a chloride current, reduces LPS (HY-D1056)-induced increases of ROS, NO, TNF-α, IL-6, IL-1β, iNOS, and COX-2 levels. Antidepressant agent 11 dihydrochloride inhibits NF-κB pathway activation by reducing IκBα and p65 phosphorylation and blocking p65 nuclear translocation. GABAAR/5-HT2AR modulator-1 alleviates depression-like behaviors in LPS-challenged and chronic restraint stress-challenged mice, and protects hippocampal neurons against inflammation-mediated damage .
    GABAAR/5-HT2AR modulator-1

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