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Results for "

reversible activator

" in MedChemExpress (MCE) Product Catalog:

92

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1

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2

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3

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8

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4

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1

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-13030
    (+)-JQ-1
    Maximum Cited Publications
    295 Publications Verification

    JQ1

    		 Epigenetic Reader Domain Autophagy Ligands for Target Protein for PROTAC Neurological Disease Cancer
    (+)-JQ-1 (JQ1), a chemical probe, is a potent, specific, CNS-penetrant 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-139664
    GSK-3685032
    10+ Cited Publications

    		 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-19638A
    Cangrelor tetrasodium
    4 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-118628
    (E/Z)-BML264
    5+ Cited Publications

    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-103371
    DCPIB
    10+ 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-13817
    IU1
    20+ Cited Publications

    		 Deubiquitinase Autophagy Apoptosis Cardiovascular Disease Neurological Disease Endocrinology Cancer
    IU1 is a selective, reversible USP14 inhibitor with an IC50 of 4-5 μM. IU1 binds USP14’s catalytic cleft to block deubiquitinase activity. IU1 induces calpain-dependent Tau cleavage, causes ATP deficits, reduces E1~Ub thioester levels and 26S proteasome assembly. IU1 enhances 26S proteasome chymotrypsin-like activity, modulates LC3B-dependent autophagy flux, reduces cancer cell proliferation and migration, and blocks G0/G1 to S phase cell cycle transition in follicular thyroid cancer cells. IU1 activates autophagy-lysosomal and ubiquitin-proteasome pathways, triggers apoptosis, and reduces cervical cancer cell growth. IU1 enhances degradation of proteasome substrates linked to neurodegenerative disease, accelerates oxidized protein degradation, and increases oxidative stress resistance. IU1 can be used for the research of Alzheimer’s disease, follicular thyroid cancer, ischemic stroke, cervical cancer, and neurodegenerative disease .
    IU1
  • 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-N6789
    KT5720
    4 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-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-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-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-19837
    BMS-986120
    1 Publications Verification

    		 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-W105310A
    Croconic acid disodium

    Nacr

    		 HDAC Sirtuin CDK Bcl-2 Family Apoptosis Others
    Croconic acid disodium (Nacr) is a lysine crotonylation (Kcr) activator and electroactive material. Croconic acid disodium reduces the expression of HDAC2, HDAC3, SIRT1, and SIRT3, and increases the expression of EP300, CITED1, ACSS2, DPF2, CDYL, MLLT3, and YEATS2. Croconic acid disodium elevates intracellular crotonyl-CoA content and global histone lysine crotonylation levels. Croconic acid disodium promotes the growth of bovine fibroblasts, regulates cell cycle progression, and inhibits bovine fibroblast apoptosis (apoptosis). Croconic acid disodium improves the blastocyst development efficiency of bovine somatic cell nuclear transfer embryos. Croconic acid disodium undergoes reversible lithium intercalation/deintercalation reactions via sodium-lithium ion exchange. Croconic acid disodium is applicable to research related to cell growth promotion .
    Croconic acid disodium
  • 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-134356
    AICA-riboside, 5′-phosphate

    AICAR-5'-MP

    		 Endogenous Metabolite Others
    AICA-riboside, 5′-phosphate is AICA riboside with a phosphate group. The functions of AICA riboside include: 1) conversion into AMP mimetic to selectively activate AMPK; 2) competition with adenosine for the uptake of nucleoside transporters, reversible blocking of adenosine reuptake, increasing extracellular adenosine concentration, and indirectly activating adenosine A1 receptors. AICA riboside is involved in metabolic regulation (promoting catabolism and inhibiting anabolism) and adenosine-dependent neuroprotection (inhibiting excitatory synaptic transmission). AICA riboside can be used in the study of metabolic diseases (such as diabetes and obesity) and neurological diseases (such as ischemia and epilepsy), and has central nervous system protective activity .
    AICA-riboside, 5′-phosphate
  • 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-10199A
    Ibutamoren
    5 Publications Verification

    MK-677 free base; MK-0677 free base

    		 GHSR Insulin Receptor Neurological Disease Metabolic Disease
    Ibutamoren (MK-677 free base; MK-0677 free base) is an orally active non-peptide growth hormone secretagogue receptor agonist. Ibutamoren activates signal cascades by mimicking endogenous ligands, triggers pulsatile release of growth hormone from the pituitary gland, and increases serum levels of IGF-1 and insulin-like growth factor-binding protein 3. Ibutamoren not only increases the frequency of growth hormone pulses in male individuals, but also promotes elevated bone formation markers in female individuals with postmenopausal osteoporosis. The combination of Ibutamoren with Alendronate sodium hydrate (HY-11101) significantly increases bone mineral density at the femoral neck. However, Ibutamoren may cause mild, reversible adverse reactions such as increased appetite, fluid retention, and elevated fasting blood glucose. Ibutamoren has been widely used in studies related to idiopathic growth hormone deficiency, sarcopenia, Alzheimer's disease, and osteoporosis .
    Ibutamoren
  • 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-W923198
    Fluorescein O-methacrylate

    Methacryloyloxy fluorescein

    		 Fluorescent Dye Others
    Fluorescein O-methacrylate (Methacryloyloxy fluorescein) is a pH-responsive fluorescent monomeric dye. Fluorescein O-methacrylate exhibits pH-responsive fluorescence properties: its fluorescence is activated under alkaline conditions and quenched under neutral or acidic conditions; reversible switching of fluorescence is achievable by adjusting the pH of the solution. Fluorescein O-methacrylate can be used as a monomer for the synthesis of amphiphilic fluorescein polymers. These polymers can self-assemble into stable polymer nanoparticles with enhanced aqueous-phase fluorescence, and also enable the conjugation of nanoparticles with amine-containing biomolecules to support sensitive optical detection of biomarkers (Ex/Em = 490/520 nm) .
    Fluorescein O-methacrylate
  • HY-B0916
    Propoxur

    		Environmental Pollutants MMP Insecticide Cholinesterase (ChE) ERK Keap1-Nrf2 Reactive Oxygen Species (ROS) Infection Neurological Disease Cancer
    Propoxur is a reversible, competitive, orally active AChE inhibitor that can cross the blood-brain barrier. Propoxur inhibits AChE activity to induce neurotoxicity, while promoting MMP-2 expression and enhancing tumor cell migration and invasion by inducing intracellular ROS generation and activating the ERK/Nrf2 signaling pathway. On the one hand, Propoxur inhibits AChE, leading to acetylcholine accumulation and causing neurological dysfunction; on the other hand, it promotes Nrf2 nuclear translocation through ROS-dependent ERK1/2 phosphorylation, and upregulates MMP-2 and other invasion-related proteins. Propoxur is also a carbamate insecticide used to combat turf, forestry, and household pests .
    Propoxur
  • HY-N0430
    Coptisine

    Coptisin

    		 Indoleamine 2,3-Dioxygenase (IDO) NF-κB p38 MAPK PI3K Akt Apoptosis Reactive Oxygen Species (ROS) Mitochondrial Metabolism DNA/RNA Synthesis ROCK LDLR Cardiovascular Disease Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Coptisine is an orally active and brain-penetrant alkaloid found in Coptis chinensis. Coptisine is a reversible, uncompetitive IDO inhibitor with a Ki of 5.8 μM and an IC50 of 6.3 μM. Coptisine suppresses neuroinflammation, reduces Aβ plaque burden and shows neuroprotective activity. Coptisine shows anti-inflammation activity by blocking NF-κB, MAPK, and PI3K/Akt activation. Coptisine inhibits cancer cells proliferation, induces DNA damage, G2/M phase cell cycle arrest, apoptosis, ROS production and mitochondrial dysfunction. Coptisine inhibits Rho/ROCK pathway activation, reduces arrhythmia, limits cardiac injury marker release, reduces infarct size, and preserves cardiac function in rat myocardial ischemia/reperfusion models. Coptisine downregulates HMGCR and upregulates LDLR and CYP7A1 to modulate cholesterol metabolism, reduces abnormal serum lipid levels, and promotes fecal bile acid excretion. Coptisine can be used for the research of cancer, hypercholesterolemia, Alzheimer’s disease, inflammatory disorders and cardiovascular disease .
    Coptisine
  • HY-N0430A
    Coptisine Sulfate
    5 Publications Verification

    		 Indoleamine 2,3-Dioxygenase (IDO) NF-κB p38 MAPK PI3K Akt Apoptosis Reactive Oxygen Species (ROS) Mitochondrial Metabolism DNA/RNA Synthesis ROCK LDLR Cardiovascular Disease Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Coptisine Sulfate is an orally active and brain-penetrant alkaloid found in Coptis chinensis. Coptisine Sulfate is a reversible, uncompetitive IDO inhibitor with a Ki of 5.8 μM and an IC50 of 6.3 μM. Coptisine Sulfate suppresses neuroinflammation, reduces Aβ plaque burden and shows neuroprotective activity. Coptisine Sulfate shows anti-inflammation activity by blocking NF-κB, MAPK, and PI3K/Akt activation. Coptisine Sulfate inhibits cancer cells proliferation, induces DNA damage, G2/M phase cell cycle arrest, apoptosis, ROS production and mitochondrial dysfunction. Coptisine Sulfate inhibits Rho/ROCK pathway activation, reduces arrhythmia, limits cardiac injury marker release, reduces infarct size, and preserves cardiac function in rat myocardial ischemia/reperfusion models. Coptisine Sulfate downregulates HMGCR and upregulates LDLR and CYP7A1 to modulate cholesterol metabolism, reduces abnormal serum lipid levels, and promotes fecal bile acid excretion. Coptisine Sulfate be used for the research of cancer, hypercholesterolemia, Alzheimer’s disease, inflammatory disorders and cardiovascular disease .
    Coptisine Sulfate
  • 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-107460
    LDN-211904 oxalate
    1 Publications Verification

    		 Ephrin Receptor Cancer
    LDN-211904 oxalate is a potent and reversible EphB3 inhibitor with an IC50 of 79 nM. LDN-211904 oxalate shows good metabolic stability in mouse liver microsomes. LDN-211904 oxalate with Cetuximab (HY-P9905) could be effective in inhibiting STAT3-activated colorectal cancer (CRC) stemness and Cetuximab resistance in CRC .
    LDN-211904 oxalate
  • HY-W134005
    Mg(Ⅱ)-EDTA disodium tetrahydrate

    Ethylenediaminetetraacetic acid magnesium disodium tetrahydrate

    		 Phosphatase Others
    Mg(Ⅱ)-EDTA disodium tetrahydrate is a reversible non-covalent activator of fructose diphosphatase (Km=0.9 μM). Mg(Ⅱ)-EDTA disodium tetrahydrate synergistically activates fructose diphosphatase with free Mg 2+, promotes the hydrolysis of fructose-1,6-bisphosphate at pH≤8, and plays a role in enhancing the activity of key enzymes in gluconeogenesis .
    Mg(Ⅱ)-EDTA disodium tetrahydrate
  • 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
    1 Publications Verification

    		 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-153508
    ANO1-IN-4

    		Chloride Channel Others
    ANO1-IN-4 (Compound 10bm) is a reversible inhibitor for calcium-activated chloride channel transmembrane protein 16A (TMEM16A, also known as ANO1) with an IC50 of 0.030 µM. ANO1-IN-4 exhibits good metabolic stability in rat liver microsomes. ANO1-IN-4 inhibits spontaneous contraction in mouse isolated ileum .
    ANO1-IN-4
  • HY-122236
    UMK57

    		Mitosis Kinesin Microtubule/Tubulin Aurora Kinase Cancer
    UMK57 is a MCAK activator and kinetochore-microtubule destabilizer. UMK57 enhances MCAK-dependent microtubule depolymerization, increases kinetochore-microtubule turnover, reduces chromosome mis-segregation and lagging chromosomes, and inhibits cancer cell proliferation. UMK57 triggers adaptive resistance in Aurora B cancer cells via reversible Aurora B signaling pathway alterations. UMK57 can be used for the research of solid tumors .
    UMK57
  • 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-106901A
    Asoxime dichloride

    HI-6

    		 Cholinesterase (ChE) nAChR Neurological Disease
    Asoxime dichloride (HI-6) is an orally active thiosemicarbazone-based antidote. Asoxime dichloride is a reversible inhibitor of AChE, and its core mechanism of action is to re-activate AChE inhibited by nerve toxins, thereby restoring the cholinergic nerve function. Asoxime dichloride significantly restores the function of poisoned muscles without reactivating AChE. Asoxime dichloride is an antagonist of acetylcholine receptors (AChRs), including nicotinic receptor and α7 nAChR. Asoxime dichloride can serve as an effective immunomodulator, improving the immune effect of the nervous system .
    Asoxime dichloride
  • HY-133178
    Urolithin D

    3,4,8,9-Tetrahydroxy urolithin

    		 Ephrin Receptor PPAR AMPK Metabolic Disease Inflammation/Immunology Cancer
    Urolithin D (3,4,8,9-Tetrahydroxy urolithin) is a colonic metabolite of Ellagitannins and a competitive, reversible, and selective antagonist of the EphA receptor. Urolithin D inhibits EphA2-ephrin-A1 binding with an IC50 of 0.9 μM. Urolithin D is also a potent antioxidant that scavenges free radicals and repairs oxidized DNA damage. Additionally, Urolithin D suppresses triglyceride accumulation and promotes fatty acid oxidation by activating the AMPK signaling pathway. Urolithin D can be used for research on tumors, metabolic, and inflammatory diseases .
    Urolithin D
  • 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-149906
    Trecovirsen

    GEM91

    		 HIV mRNA Infection
    Trecovirsen (GEM91) is an antiviral agent targeting HIV gag mRNA, which hybridizes with complementary HIV gag mRNA at the initiation site. Trecovirsen induces a reversible, dose-dependent prolongation of activated partial thromboplastin time via its polyanionic property. Trecovirsen is applicable to research related to HIV infection .
    Trecovirsen
  • 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-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-177106
    ADT-1004

    		Drug Intermediate Ras Cancer
    ADT-1004 is an orally active prodrug of ADT-007 (HY-157887). ADT-007 is a reversible, highly potent and selective pan-RAS inhibitor that binds to the nucleotide-free conformation of RAS proteins and blocks their GTP activation, thereby inhibiting the downstream MAPK and AKT signaling pathways. ADT-1004 can be used for the research of pancreatic ductal adenocarcinoma .
    ADT-1004
  • 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-W020958
    Ru(acac)3

    Tris(acetylacetonato)ruthenium (III)

    		 Caspase Apoptosis Cancer
    Ru (acac) 3 (Tris (acetylacetonato) ruthenium (III)) is a caspase-3 activator and Apoptosis inducer. Ru (acac) 3 exerts growth inhibitory effects on various cell lines in vitro by inhibiting DNA/RNA synthesis and inducing mild reversible S-phase cell cycle arrest. Ru (acac) 3 is commonly used in research related to ovarian cancer, osteosarcoma, cervical cancer, melanoma, and other fields .
    Ru(acac)3
  • HY-108548
    Rp-8-Br-PET-cGMPS sodium

    Rp-8-Bromo-PET-cGMPS

    		 PKG Inflammation/Immunology
    Rp-8-Br-PET-cGMPS sodium (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-N8852
    6-Methoxyflavanone

    6-MeOF

    		 GABA Receptor Taste Receptor Neurological Disease Metabolic Disease
    6-Methoxyflavanone (6-MeOF) is a flavonoid compound that can cross the blood-brain barrier. 6-Methoxyflavanone is a positive allosteric modulator of GABAA receptors. 6-Methoxyflavanone exhibits positive allosteric regulatory effects on human recombinant α1β2γ2L and α2β2γ2L GABAA receptors, and is relatively inactive on the α1β2 GABAA receptor. 6-Methoxyflavanone showes inhibitory behavior towards the activation of bitter receptor hTAS2R39 and hTAS2R14, demonstrating a reversible and non-overcome antagonistic effect. 6-Methoxyflavanone has the effects of anti-anxiety, analgesia and relief of neuropathic pain .
    6-Methoxyflavanone
  • 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-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-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-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-110067
    VO-OHPic

    		PTEN Apoptosis Autophagy Ferroptosis Reactive Oxygen Species (ROS) Interleukin Related Akt Keap1-Nrf2 Cardiovascular Disease Inflammation/Immunology Cancer
    VO-OHPic is a reversible, noncompetitive PTEN inhibitor with an human IC50 value of 46 nM. VO-OHPic inhibits PTEN signaling, activates Akt-GSK3β and Nrf-2/HO-1 pathways, induces apoptosis resistance and elevates IL-10 levels. VO-OHPic inhibits autophagy, ferroptosis and oxidative stress. VO-OHPic can be used for the research of acute myocardial infarction, intervertebral disc degeneration, cardiomyopathy and cancer .
    VO-OHPic
  • HY-111140
    YS121

    		PGE synthase Lipoxygenase PPAR Inflammation/Immunology
    YS121 is a dual inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1; IC50 = 3.4 μM) and 5-lipoxygenase (5-LOX; IC50 = 6.5 μM). YS121 exhibits direct, reversible, and specific binding to mPGES-1 (KD = 10-14 μM) . YS121 dose-dependently reduces PGE2 production with an EC50 of 12 μM in IL-1β-stimulated A549 cells . YS121 (compound 9) activates PPAR-α and -γ (EC50 = 1 and 3.6 μM, respectively) . YS121 exhibits anti-inflammatory efficiency in human whole blood as well as in vivo. YS121 can be used for pleurisy research .
    YS121
  • HY-W014883
    1,12-Dodecanediamine

    1,12-DD; 1,12-Diamino dodecane

    		 Potassium Channel Metabolic Disease
    1,12-Dodecanediamine (1,12-DD) is a reversible Maxi calcium-activated potassium channel blocker. 1,12-Dodecanediamine can reduce the single-channel current amplitude, mean channel open time, and channel open probability. 1,12-Dodecanediamine is promising for research of cell electrical signal transduction mechanism .
    1,12-Dodecanediamine
  • HY-106901AS
    Asoxime-d4 dichloride
    1 Publications Verification

    HI-6-d4

    		 Isotope-Labeled Compounds Cholinesterase (ChE) nAChR Neurological Disease
    Asoxime-d4 dichloride (HI-6-d4) is the deuterium labeled Asoxime dichloride. Asoxime dichloride is an orally active thiosemicarbazone-based antidote. Asoxime dichloride is a reversible inhibitor of AChE, and its core mechanism of action is to re-activate AChE inhibited by nerve toxins, thereby restoring the cholinergic nerve function. Asoxime dichloride significantly restores the function of poisoned muscles without reactivating AChE. Asoxime dichloride is an antagonist of acetylcholine receptors (AChRs), including nicotinic receptor and α7 nAChR. Asoxime dichloride can serve as an effective immunomodulator, improving the immune effect of the nervous system.
    Asoxime-d4 dichloride

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