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Results for "

reversible activator

" in MedChemExpress (MCE) Product Catalog:

47

Inhibitors & Agonists

1

Peptides

6

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-112472
    S3969

    		Sodium Channel Metabolic Disease
    S3969 is a potent and reversible activator of the human epithelial sodium channel (hENaC). The apparent EC50 for S3969 activation of hENaC is 1.2 μm .
    S3969
  • HY-50662
    A-769662
    25+ Cited Publications

    		 AMPK Cancer
    A-769662 is a potent, reversible AMPK activator with EC50 of 0.8 μM.
    A-769662
  • HY-113221
    Isovalerylcarnitine

    		Proteasome Endogenous Metabolite Metabolic Disease
    Isovalerylcarnitine is a product of the catabolism of L-leucine. Isovalerylcarnitine is also a selective and reversible calpain activator that induces apoptosis .
    Isovalerylcarnitine
  • HY-N0826
    Corynoline
    5 Publications Verification

    		 Cholinesterase (ChE) Keap1-Nrf2 Neurological Disease Inflammation/Immunology Cancer
    Corynoline is a reversible and noncompetitive acetylcholinesterase (AChE) inhibitor with an IC50 of 30.6 μM . Corynoline exhibits anti-inflammatory activity by activating Nrf2 .
    Corynoline
  • HY-144813
    Gü2602

    		Cathepsin Inflammation/Immunology Cancer
    Gü2602 is a potent, reversible cathepsin K (CatK) inhibitor with a Ki of 0.013 nM for mature CatK (mCatK). Gü2602 suppresses the autocatalytic activation of the cathepsin K zymogen .
    Gü2602
  • HY-12809
    Optovin
    1 Publications Verification

    		 TRP Channel Neurological Disease
    Optovin is a reversible photoactivated TRPA1 ligand that enables light-mediated neuronal excitation. Optovin activates TRPA1 via structure-dependent photochemical reactions with redox-sensitive cysteine residues .
    Optovin
  • HY-107301
    Dehydrosoyasaponin I

    Soyasaponin Be; DHS-I

    		 Potassium Channel Neurological Disease
    Dehydrosoyasaponin I (Soyasaponin Be;DHS-I), a triterpene glycoside, is a potent and reversible calcium-activated potassium (maxi-K) channels activator .
    Dehydrosoyasaponin I
  • HY-144812
    Gü1303

    		Cathepsin Inflammation/Immunology Cancer
    Gü1303 is a potent, reversible, slow-binding cathepsin K (CatK) inhibitor with a Ki of 0.91 nM for mature CatK (mCatK). Gü1303 suppresses the autocatalytic activation of the cathepsin K zymogen .
    Gü1303
  • HY-163445
    NAMPT activator-6

    		NAMPT Cancer
    NAMPT activator-6 is a NAMPT activator, a regulatory molecule for the optical control system of NAMPT and NAD+. NAMPT activator-6 can be used to design efficient photoswitchable proteolysis-targeting chimeras (PS-PROTACs) to achieve up-down reversible regulation of NAMPT and NAD+ in a light-dependent manner and reduce the toxicity associated with inhibitor-based PS-PROTACs. PS-PROTAC can be used to achieve antitumor activity, NAMPT, and NAD+ modulation in vivo via optical manipulation .
    NAMPT activator-6
  • HY-113221R
    Isovalerylcarnitine (Standard)

    		Proteasome Endogenous Metabolite Metabolic Disease
    Isovalerylcarnitine (Standard) is the analytical standard of Isovalerylcarnitine. This product is intended for research and analytical applications. Isovalerylcarnitine is a product of the catabolism of L-leucine. Isovalerylcarnitine is also a selective and reversible calpain activator that induces apoptosis .
    Isovalerylcarnitine (Standard)
  • HY-109079A
    Abeprazan hydrochloride

    DWP14012 hydrochloride; Fexuprazan hydrochloride

    		 Proton Pump Metabolic Disease
    Abeprazan hydrochloride (DWP14012 hydrochloride) is a potassium-competitive acid blocker. Abeprazan hydrochloride inhibits H +, K +- ATPase by reversible potassium-competitive ionic binding with no acid activation required. Abeprazan hydrochloride is developed as a potential alternative to proton pump inhibitor for the treatment of acid-related diseases .
    Abeprazan hydrochloride
  • HY-109079
    Abeprazan

    DWP14012; Fexuprazan

    		 Proton Pump Metabolic Disease
    Abeprazan (DWP14012) is a potassium-competitive acid blocker. Abeprazan inhibits H +, K +- ATPase by reversible potassium-competitive ionic binding with no acid activation required. Abeprazan is developed as a potential alternative to proton pump inhibitor for the treatment of acid-related diseases .
    Abeprazan
  • HY-N0826R
    Corynoline (Standard)

    		Cholinesterase (ChE) Keap1-Nrf2 Neurological Disease Inflammation/Immunology Cancer
    Corynoline (Standard) is the analytical standard of Corynoline. This product is intended for research and analytical applications. Corynoline is a reversible and noncompetitive acetylcholinesterase (AChE) inhibitor with an IC50 of 30.6 μM . Corynoline exhibits anti-inflammatory activity by activating Nrf2 .
    Corynoline (Standard)
  • HY-13030
    (+)-JQ-1
    Maximum Cited Publications
    230 Publications Verification

    JQ1

    		 Epigenetic Reader Domain Autophagy Ligands for Target Protein for PROTAC Cancer
    (+)-JQ-1 (JQ1) is a potent, specific, and reversible BET bromodomain inhibitor, with IC50s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)) . (+)-JQ-1 also activates autophagy .
    (+)-JQ-1
  • HY-13520
    Nocodazole
    65+ Cited Publications

    Oncodazole; R17934

    		 Microtubule/Tubulin Bcr-Abl CRISPR/Cas9 Autophagy Apoptosis Cancer
    Nocodazole (Oncodazole) is a rapidly-reversible inhibitor of microtubule. Nocodazole binds to β-tubulin and disrupts microtubule assembly/disassembly dynamics, which prevents mitosis and induces apoptosis in tumor cells. Nocodazole inhibits Bcr-Abl, and activates CRISPR/Cas9.
    Nocodazole
  • HY-W008956
    Myoseverin

    		Microtubule/Tubulin Inflammation/Immunology
    Myoseverina, a microtubule-binding molecule, induces the reversible fission of multinucleated myotubes into mononucleated fragments. Myoseverina affects the expression of a variety of growth factor, immunomodulatory, extracellular matrix-remodeling, and stress response genes, consistent with the activation of pathways involved in wound healing and tissue regeneration .
    Myoseverin
  • HY-18200
    Atopaxar

    E5555; ER-172594-00

    		 Protease Activated Receptor (PAR) JAK Apoptosis Cardiovascular Disease Cancer
    Atopaxar (E5555) is a potent, orally active, selective and reversible thrombin receptor protease-activated receptor-1 (PAR-1) antagonist. Atopaxar, an antiplatelet agent, interferes with platelet signaling. Atopaxar can be used for the research of atherothrombotic disease .
    Atopaxar
  • HY-19837
    BMS-986120

    		Protease Activated Receptor (PAR) Inflammation/Immunology
    BMS-986120 is a first-in-class oral and reversible protease-activated receptor 4 (PAR4) antagonist, with IC50s of 9.5 nM and 2.1 nM in human and monkey blood, respectively. BMS-986120 has potent and selective antiplatelet effects .
    BMS-986120
  • HY-139664
    GSK-3685032
    5 Publications Verification

    		 DNA Methyltransferase Cancer
    GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition .
    GSK-3685032
  • HY-18200B
    Atopaxar hydrobromide

    E5555 hydrobromide; ER 172594-06

    		 Protease Activated Receptor (PAR) JAK Apoptosis Cardiovascular Disease Cancer
    Atopaxar (E5555) hydrobromide is a potent, orally active, selective and reversible thrombin receptor protease-activated receptor-1 (PAR-1) antagonist. Atopaxar hydrobromide, an antiplatelet agent, interferes with platelet signaling. Atopaxar hydrobromide can be used for the research of atherothrombotic disease .
    Atopaxar hydrobromide
  • HY-133233
    Thioetheramide-PC

    1-Palmitylthio-2-palmitoylamido-1,2-dideoxy-sn-glycero-3-phosphorylcholine

    		 Endogenous Metabolite Metabolic Disease
    Thioetheramide-PC is a structurally modified phospholipid that functions as a competitive, reversible inhibitor of secretory phospholipase A2 (sPLA2). The IC50 value for thioetheramide-PC is 2 μM at a substrate concentration of 0.5 mM.1 In addition to binding to the catalytic site of sPLA2, thioetheramide-PC also binds to the activator site of this enzyme. The binding of thioetheramide-PC to the activator site is tighter than its binding to the catalytic site. The result of this dual interaction is that at low concentrations thioetheramide-PC may activate phospholipase activity rather than inhibiting it.
    Thioetheramide-PC
  • HY-19638A
    Cangrelor tetrasodium
    2 Publications Verification

    AR-C69931MX tetrasodium

    		 P2Y Receptor Cardiovascular Disease Inflammation/Immunology
    Cangrelor tetrasodium, an adenosine triphosphate analogue, is a reversible and selective platelet P2Y12 antagonist, with prompt and potent antiplatelet effects. Cangrelor tetrasodium directly blocks adenosine diphosphate (ADP)-induced activation and aggregation of platelets. Cangrelor tetrasodium is also a nonspecific GPR17 antagonist .
    Cangrelor tetrasodium
  • HY-147049
    PAL-4

    		Others Metabolic Disease
    PAL-4 (compound 4) is a potent, selective and reversible Lysophospholipase-like 1 (LYPLAL1) activator with EC50 value of 0.39 μM and 0.49 μM for mice LYPLAL1 and huamn LYPLAL1, respectively. PAL-4 can be used for researching metabolic disorders .
    PAL-4
  • HY-117290
    BMS-962212

    		Factor Xa Cardiovascular Disease
    BMS-962212 is a direct, reversible, selective factor XIa (FXIa) inhibitor . BMS-962212 is well tolerated, with fast onset of pharmacodynamic (PD) responses and rapid elimination. BMS-962212 increases exposure dependently in activated partial thromboplastin time, and decreases exposure dependently in FXI clotting activity .
    BMS-962212
  • HY-162333
    BAL-0028

    		NOD-like Receptor (NLR) Interleukin Related Inflammation/Immunology
    BAL-0028 is a reversible inhibitor of NLRP3 activation with an IC50 value of 25 nM. BAL-0028 binds closely to the NACHT domain of the NLRP3 with KD values of 104-123 nM. BAL-0028 can inhibit the secretion of IL-1β and has anti-inflammatory activity .
    BAL-0028
  • HY-128358
    MR-L2

    		Phosphodiesterase (PDE) Neurological Disease
    MR-L2 is a reversible and noncompetitive allosteric activator of long-isoform phosphodiesterase-4 (PDE4), activates representative PDE4 long-isoform variants (PDE4A4, PDE4B1, PDE4C3, PDE4D5). MR-L2 suppresses PGE2-induced MDCK cell cyst formation with an EC50 of 1.2 μM .
    MR-L2
  • HY-115537
    NAE-IN-M22

    		Apoptosis Cancer
    NAE-IN-M22 is a potent, selective and reversible inhibitor of NEDD8 activating enzyme (NAE), with potency in micromolar range. NAE-IN-M22 inhibits multiple cancer cell lines and induces apoptosis in A549 cells. NAE-IN-M22 also can inhibit tumor growth in vivo .
    NAE-IN-M22
  • HY-19638
    Cangrelor

    AR-C69931MX

    		 P2Y Receptor Cardiovascular Disease Inflammation/Immunology
    Cangrelor (AR-C69931MX), an adenosine triphosphate analogue, is an intravenous, reversible and selective platelet P2Y12 antagonist, with prompt and potent antiplatelet effects. Cangrelor directly blocks adenosine diphosphate (ADP)-induced activation and aggregation of platelets. Cangrelor is also a nonspecific GPR17 antagonist .
    Cangrelor
  • HY-E70028
    UDP-sugar pyrophosphorylase (BlUSP)

    		Endogenous Metabolite Metabolic Disease
    UDP-sugar pyrophosphorylase (BlUSP) is the enzyme capable of activating glucose-1-phosphate (Glc-1-P) to UDP-glucose (UDP-Glc). UDP-sugar pyrophosphorylase (BlUSP) catalyzes a reversible transfer of the uridyl group from UTP to sugar-1-phosphate, producing UDP-sugar and pyrophosphate (PPi) .
    UDP-sugar pyrophosphorylase (BlUSP)
  • HY-118628
    (E/Z)-BML264
    3 Publications Verification

    N-(p-Amylcinnamoyl) anthranilic acid; ACA

    		 Phospholipase TRP Channel Cardiovascular Disease
    (E/Z)-BML264 (N-(p-amylcinnamoyl) Anthranilic Acid) is a broad spectrum Phospholipase A2 (PLA2) inhibitor and TRP channel blocker . (E/Z)-BML264 (N-(p-amylcinnamoyl) Anthranilic Acid) is also an effective reversible inhibitor of calcium-activated chloride channels, has potential to treat arrhythmia .
    (E/Z)-BML264
  • HY-161125
    (+)-JQ1-OH

    		Others Others
    (+)-JQ1-OH is the major metabolite of (+)-JQ1(HY-13030). (+)-JQ-1 (JQ1) is a potent, specific, and reversible BET bromodomain inhibitor, with IC50s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)). (+)-JQ-1 also activates autophagy .
    (+)-JQ1-OH
  • HY-14930A
    Mirodenafil dihydrochloride

    SK-3530 dihydrochloride

    		 Phosphodiesterase (PDE) Glucocorticoid Receptor Wnt β-catenin Apoptosis Neurological Disease Inflammation/Immunology Endocrinology
    Mirodenafil (SK3530) dihydrochloride is an orally active, potent, reversible, and selective phosphodiesterase 5 (PDE5) inhibitor. Mirodenafil dihydrochloride is a glucocorticoid receptor (GR) modulator Mirodenafil dihydrochloride activates the Wnt/β-catenin signaling pathway by downregulating Dkk1 expression. Mirodenafil dihydrochloride can be used for the research of erectile dysfunction (ED), Alzheimer’s disease (AD) and systemic sclerosis (SSc) .
    Mirodenafil dihydrochloride
  • HY-14930
    Mirodenafil

    SK3530

    		 Phosphodiesterase (PDE) Glucocorticoid Receptor Wnt β-catenin Apoptosis Neurological Disease Inflammation/Immunology Endocrinology
    Mirodenafil (SK3530) is an orally active, potent, reversible, and selective phosphodiesterase 5 (PDE5) inhibitor. Mirodenafil is a glucocorticoid receptor (GR) modulator Mirodenafil activates the Wnt/β-catenin signaling pathway by downregulating Dkk1 expression. Mirodenafil can be used for the research of erectile dysfunction (ED), Alzheimer’s disease (AD) and systemic sclerosis (SSc) .
    Mirodenafil
  • HY-139664A
    (R)-GSK-3685032

    		DNA Methyltransferase Cancer
    (R)-GSK-3685032 is the R-enantiomer of GSK-3685032. GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition .
    (R)-GSK-3685032
  • HY-153128
    DOCK2-IN-1

    		DOCK Inflammation/Immunology
    DOCK2-IN-1 (compound 3), a CPYPP (HY-110100) analogue, is an inhibitor of DOCK2 as well (IC50=19.1 μM). DOCK2-IN-1 binds to DOCK2 DHR-2 domain in a reversible manner to inhibits its catalytic activity. DOCK2-IN-1 blocks the activation of both chemokine receptor- and antigen receptor-mediated Rac in lymphocytes. DOCK2-IN-1 significantly suppresses chemotactic response and T cell activation .
    DOCK2-IN-1
  • HY-139664B
    (S)-GSK-3685032

    		Others Cancer
    (S)-GSK-3685032 is the isomer of GSK-3685032 (HY-139664), and can be used as an experimental control. GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition .
    (S)-GSK-3685032
  • HY-100671
    L002

    		Histone Acetyltransferase STAT Cardiovascular Disease Inflammation/Immunology Cancer
    L002 is a potent, cell permeable, reversible and specific acetyltransferase p300 (KAT3B) inhibitor with an?IC50?of 1.98 μM . L002 binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain, blocks histone acetylation and p53 acetylation, and inhibits STAT3 activation . L002 has the potential for hypertension‐induced cardiac hypertrophy and fibrogenesis treatment .
    L002
  • HY-103371
    DCPIB
    5+ Cited Publications

    		 Chloride Channel Potassium Channel Neurological Disease
    DCPIB is a selective, reversible and potent inhibitor of volume-regulated anion channels (VRAC). DCPIB voltage-dependently activates potassium channels TREK1 and TRAAK, and inhibits TRESK, TASK1 and TASK3 (IC50s: 0.14, 0.95, 50.72 μM, respectively). DCPIB is also a selective blocker of swelling-induced chloride current (ICl,swell), with an IC50 of 4.1 μM. DCPIB is a useful tool for investigating structure-function studies of K2P channels .
    DCPIB
  • HY-107146
    PZ-128

    P1pal-7

    		 Protease Activated Receptor (PAR) Cardiovascular Disease Cancer
    PZ-128 (P1pal-7), a cell-penetrating lipopeptide pepducin, is a first-in-class, specific and reversible protease-activated receptor-1 (PAR1) antagonist. PZ-128 targets the cytoplasmic surface of PAR1 and interrupts signaling to internally-located G (PAR1-G) proteins. PZ-128 has antiplatelet, anti-metastatic, anti-angiogenic and anticancer effects .
    PZ-128
  • HY-132831
    Selnoflast
    1 Publications Verification

    Somalix; RO-7486967; IZD334

    		 NOD-like Receptor (NLR) Interleukin Related Neurological Disease Inflammation/Immunology
    Selnoflast (RO7486967), formerly somalix/RG6418/IZD334, is an orally active, potent, selective and reversible small molecule NLRP3 inflammasome inhibitor. Selnoflast is a potent inhibitor of IL-1β release stimulated by NLRP3 activation in human Alzheimer's disease (AD) monocyte-derived macrophages. Selnoflast is promising for research of AD and systemic inflammatory diseases, such as ulcerative colitis and chronic obstructive pulmonary disease
    Selnoflast
  • HY-164002
    PF-303

    		Btk Others
    PF-303 is a potent, oral inhibitor of Bruton's tyrosine kinase (BTK) (IC50=0.64 nM). The melamine portion of PF-303 forms a covalent bond with BTK's Cys481, which is reversible and exhibits a high selectivity compared to irreversible covalent BTK inhibitors. PF-303 can be used to model and study the effects of BTK inhibition on the mature immune system, including effects on B-cell subsets, antibody responses, and T-cell-mediated activation .
    PF-303
  • HY-108548
    Rp-8-Br-PET-cGMPS sodium

    Rp-8-Bromo-PET-cGMPS

    		 Others Inflammation/Immunology
    Rp-8-bromo-PET-Cyclic GMPS (Rp-8-bromo-PET-cGMPS) is an analog of cyclic GMP (cGMP). It is a cell permeable, competitive, and reversible inhibitor of cGMP-dependent protein kinases (cGKs) that blocks activation of cGKI and cGKII by cGMP (Kis=35 and 30 nM). It less potently inhibits protein kinase A (Ki=11 μM) and cGMP-induced activation of cyclic nucleotide-gated channels (IC50=25 μM). In the absence of cGMP stimulation, Rp-8-bromo-PET-cGMPS can act as a partial agonist of cGKI (Ki=1 μM). Rp-8-bromo-PET-cGMPS is resistant to hydrolysis by phosphodiesterase 11.
    Rp-8-Br-PET-cGMPS sodium
  • HY-108464A
    Phenamil methanesulfonate

    		Sodium Channel TRP Channel Metabolic Disease Inflammation/Immunology
    Phenamil methanesulfonate, an analog of Amiloride (HY-B0285), is a more potent and less reversible epithelial sodium channel (ENaC) blocker with an IC50 of 400 nM . Phenamil methanesulfonate is also a competive inhibitor of TRPP3 and inhibits TRPP3-mediated Ca 2+ transport with an IC50 of 140 nM in a Ca 2+ uptake assay . Phenamil methanesulfonate is an intriguing small molecule to promote bone repair by strongly activating BMP signaling pathway . Phenamil methanesulfonate is used for the research of cystic fibrosis lung disease .
    Phenamil methanesulfonate
  • HY-155848
    LYP-IN-4

    		Phosphatase Cancer
    LYP-IN-4 (compound D14) is a reversible and selective inhibitor of lymphotyrosine phosphatase (LYP) (Ki=1.34 μM, IC50=3.52μM). LYP-IN-4 inhibits LYP to regulate TCR signaling, up-regulates PD-1/PD-L1 expression, and enhance anti-tumor immunity. LYP-IN-4 activates T cells and inhibits M2 macrophage polarization, inhibits tumor growth in MC38 isogenic mouse models.
    LYP-IN-4
  • HY-N6789
    KT5720
    3 Publications Verification

    		 PKA Neurological Disease Cancer
    KT5720 is a potent, cell-permeable, specific, reversible and ATP-competitive PKA inhibitor (IC50=3.3 μM). KT5720 is effective in reversing MDR1-mediated multidrug resistance. KT5720 also reduces the excitability of dorsal root ganglion (DRG) neurons by attenuating Hyperpolarization-activated cyclic nucleotide-gated (HCN) channel activity and reducing intracellular Ca2 + concentrations. KT5720 can be used in the study of haematological malignancies as well as HCN and DRG neuron-related diseases .
    KT5720
  • HY-18200A
    Atopaxar hydrochloride

    E5555 hydrochloride; ER-172594-00 hydrochloride

    		 Protease Activated Receptor (PAR) JAK Apoptosis Cardiovascular Disease Cancer
    Atopaxar hydrochloride (E5555 hydrochloride) is the hydrochloride salt form of Atopaxar (HY-18200). Atopaxar hydrochloride is an orally active, selective and reversible antagonist for thrombin receptor protease-activated receptor-1 (PAR-1). Atopaxar hydrochloride is the inhibitor for Janus kinase 1 (JAK1) and JAK2, which inhibits the JAK-STAT with EC50 of 5.90 μM in A549. Atopaxar hydrochloride inhibits the cell viability of A549 (IC50=7.02 μM), arrests the cell cycle at G1 phase and induces apoptosis. Atopaxar hydrochloride exhibits antiplatelet and antitumor activities. Atopaxar hydrochloride can be used for the research of atherothrombotic disease .
    Atopaxar hydrochloride
  • HY-B1167A
    Ajmaline hydrochloride

    Cardiorythmine hydrochloride; (+)-Ajmaline hydrochloride

    		 Others Cardiovascular Disease
    Ajmaline hydrochloride is a Class Ia antiarrhythmic agent. It inhibits HERG potassium channels with IC50s of 1.0 μmol/l and 42.3 μmol/l in HEK cells and moth spider oocytes respectively. The inhibitory effect of Ajmaline hydrochloride is rapid, reversible, and positive frequency dependent. It acts primarily on the open state of the HERG channel and may also be combined with the inactivated state. The inhibitory effect of ajmaline hydrochloride is dependent on aromatic residues in the S6 domain, and the sensitivity is significantly reduced in the inactivation-deficient HERG S620T channel. It can also slightly affect the activation voltage of HERG channels. Ajmaline hydrochloride's inhibitory effect on HERG channels may contribute to both its potent antiarrhythmic effects and its potential proarrhythmic risk.
    Ajmaline hydrochloride

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