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Inhibitory mechanism

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44

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-B0125
    Ofloxacin
    Maximum Cited Publications
    9 Publications Verification

    Hoe-280

    		 Bacterial Antibiotic Endogenous Metabolite Orthopoxvirus Infection Cancer
    Ofloxacin (Hoe-280) is a fluoroquinolone whose primary mechanism of action is inhibition of bacterial DNA gyrase. Ofloxacin shows inhibitory activity against vaccinia virus (VV).
    Ofloxacin
  • HY-158128
    MK-8527

    		HIV Reverse Transcriptase Infection
    MK-8527 is an orally active HIV inhibitor and nucleoside reverse transcriptase translocation inhibitor (NRTTI) with antiviral activity. MK-8527 has a similar inhibitory mechanism to ISL (HY-104012) .
    MK-8527
  • HY-B0125R
    Ofloxacin (Standard)

    Hoe-280 (Standard)

    		 Reference Standards Bacterial Antibiotic Endogenous Metabolite Orthopoxvirus Infection
    Ofloxacin (Standard) is the analytical standard of Ofloxacin. This product is intended for research and analytical applications. Ofloxacin (Hoe-280) is a fluoroquinolone whose primary mechanism of action is inhibition of bacterial DNA gyrase. Ofloxacin shows inhibitory activity against vaccinia virus (VV).
    Ofloxacin (Standard)
  • HY-N15587
    Gostatin

    Gostatine

    		 Aminotransferases (Transaminases) Metabolic Disease
    Gostatin is an inhibitor of aspartate aminotransferase (GOT). Gostatin is found in Streptomyces sumanensis nov. sp. NK-23. Gostatin has a strong inhibitory effect on pig heart GOT, a weak inhibitory effect on wheat germ GOT and GPT, and no significant effect on glutamate dehydrogenase and glutamine synthetase. The inhibitory mechanism of gostatin is similar to substrate competitive inhibition, and aspartate has a protective effect on its inhibitory effect. Gostatin can be used to study the catalytic mechanism of GOT and its role in nitrogen metabolism .
    Gostatin
  • HY-113734
    CM026

    		Aldehyde Dehydrogenase (ALDH) Others
    CM026 is a selective aldehyde dehydrogenase 1A1 inhibitor with submicromolar inhibitory activity against aldehyde dehydrogenase 1A1. Its inhibitory mechanism is related to binding to the aldehyde binding pocket and utilizing a unique glycine residue. It can be used as a chemical tool to study the role of this enzyme in disease.
    CM026
  • HY-158792
    GK241

    		Others Others
    GK241 (compound 31a-c) is a 2-oxoamide-based compound that has inhibitory activity against human and mouse group IIA secretory phospholipase A2 (GIIA sPLA2) (IC50 of 143 nM and 68 nM, respectively), and its inhibitory mechanism was studied by molecular dynamics simulation.
    GK241
  • HY-175303
    Xanthine oxidase-IN-17

    		Xanthine Oxidase Metabolic Disease
    Xanthine oxidase-IN-17 is a potent xanthine oxidase (XOD) inhibitor with an IC50 of 298 nM and a Ki of 167 nM. Xanthine oxidase-IN-17 decreases the formation of O₂ ⁻ radical by inhibiting the catalytic activity of XOD to diminish the production of uric acid. Xanthine oxidase-IN-17 shows no cytotoxicity in AML-12 hepatocytes, while suppressing uric acid production. Xanthine oxidase-IN-17 can be used for the study of hyperuricemia and subsequently to gout .
    Xanthine oxidase-IN-17
  • HY-120577
    BA 41899

    		Calcium Channel Cardiovascular Disease
    BA 41899 is a purely calcium-sensitizing agent. BA 41899 is completely devoid of phosphodiesterase (PDE) III inhibitory activity or any other known inotropic mechanism. BA 41899 can be used for the research of cardiovascular diseases, such as congestive heart failure (CHF) .
    BA 41899
  • HY-P2088
    TANDEM

    Des-N-tetramethyltriostin A

    		 Antibiotic Cancer
    TANDEM (Des-N-tetramethyltriostin A) is a synthetic antibiotic drug that has the activity of inhibiting the growth of tumor cells. TANDEM can be used in combination with chemotherapy to enhance the inhibitory effect. TANDEM has shown significant inhibitory effects on a variety of cancer cell lines in in vitro experiments. The structure of TANDEM allows it to effectively target tumor cells during the inhibition process. TANDEM's mechanism of action involves interfering with cell proliferation and survival pathways .
    TANDEM
  • HY-107302
    Sandosaponin A

    Soyasaponin Bd

    		 Endogenous Metabolite Others
    Sandosaponin A (Soyasaponin Bd) is a saponin with inhibitory activity against human recombinant aldehyde reductase (hAKR1B1). Sandosaponin A can inhibit the reduction of l-idose and 4-hydroxynonenal to varying degrees. The presence of Sandosaponin A reveals the challenges posed by the masking effect of conventional aldehyde reductase inhibitors in mixtures when exploring differential aldehyde reductase inhibitors. The inhibitory mechanism of Sandosaponin A may be related to its mode of action on different substrates .
    Sandosaponin A
  • HY-141468
    β-Chlornaltrexamine dihydrochloride

    β-CNA dihydrochloride

    		 Opioid Receptor Neurological Disease
    β-Chlornaltrexamine dihydrochloride (β-CNA dihydrochloride) is a potent long-term opioid receptor blocker. β-Chlornaltrexamine dihydrochloride can effectively block the inhibitory effect of κ opioid receptor agonists on dopamine release. β-Chlornaltrexamine dihydrochloride can be used to study the mechanism of pain perception .
    β-Chlornaltrexamine dihydrochloride
  • HY-174285
    NAPAP

    		Thrombin Cardiovascular Disease
    NAPAP is a thrombin inhibitor. It has potent antithrombin activity (Ki: 2.1 nM). NAPAP selectively inhibits thrombin via a rapid binding mechanism, and has weaker inhibitory effects on trypsin, factor Xa, and plasmin. NAPAP can be used in the study of thrombotic diseases (e.g., venous thrombosis, myocardial infarction) .
    NAPAP
  • HY-Y0624
    4-Pentenoic acid

    		Endogenous Metabolite Mitochondrial Metabolism Metabolic Disease
    4-Pentenoic acid is a medium-chain unsaturated fatty acid. 4-Pentenoic acid has hypoglycemic and fatty acid oxidation inhibitory activities. 4-Pentenoic acid can affect blood glucose metabolism and energy metabolism through mechanisms such as inhibiting long-chain fatty acid oxidation, reducing gluconeogenesis, and promoting glucose utilization .
    4-Pentenoic acid
  • HY-118931
    EF-1502

    		GABA Receptor Neurological Disease
    EF-1502 is a potent and selective GABA transporter inhibitor with GAT1 and BGT1 inhibitory activity. EF-1502 produces a synergistic anti-epileptic effect when used in combination with Tiagabine (HY-B0696), a compound used to suppress epileptic seizures. The dosing combination of EF-1502 exhibited reduced anti-epileptic efficacy and dyskinesia when used with THIP (HY-10232). The mechanism of EF-1502 differs significantly from Tiagabine, suggesting a unique role in the inhibitory strategy .
    EF-1502
  • HY-147663
    hCAIX-IN-6

    		Carbonic Anhydrase Cancer
    Compounds 6b and 14g showed significant inhibitory effect on tumor related subtype HCA IX with low nanomolar potency, while 6k was effective on HCA XII. Compounds 6b, 14g and 6k can be considered as the leading molecules for the development of future cancer therapeutic drugs based on new mechanisms of action.
    hCAIX-IN-6
  • HY-108351
    IM-54

    		Necroptosis Cardiovascular Disease
    IM-54 is a selective inhibitor of oxidative stress-induced necrosis. IM-54 shows potent inhibitory activity against H2O2-induced necrosis. IM-54 acts as a potential cardioprotective agent and biological tool for investigating the molecular mechanisms of cell death .
    IM-54
  • HY-161922
    Antibacterial agent 235

    		Bacterial Infection
    Antibacterial agent 235 (compound thy2I) shows antibacterial activity with minimum inhibitory concentration (MIC) values ranging from 0.5 μg/mL to 8 μg/mL. Antibacterial agent 235 could kill both gram-positive and gram-negative bacteria via a membrane-targeting mechanism of action with a low frequency of resistance .
    Antibacterial agent 235
  • HY-W338140
    Methionine sulfoximine
    1 Publications Verification

    2-Amino-4-(S-methylsulfonimidoyl)butanoic acid

    		 Endogenous Metabolite Neurological Disease
    Methionine sulfoximine (2-Amino-4-(S-methylsulfonimidoyl)butanoic acid) is an irreversible inhibitor of glutamine synthetase with convulsive effects. Methionine sulfoximine is able to affect the metabolism of glutamate and glutamine, which may provide important insights in neurobiological research. Methionine sulfoximine has also been used to study mechanisms related to epilepsy and its inhibitory potential .
    Methionine sulfoximine
  • HY-W719041
    1,6-Di-O-galloyl-β-D-glucose

    		HIV Reverse Transcriptase Infection
    1,6-Di-O-galloyl-β-D-glucose is a compound found in the fruit of Phyllanthus emblica. 1,6-Di-O-galloyl-β-D-glucose has HIV-1 reverse transcriptase (RT) inhibitory activity with an IC50 value of 270 μM. The inhibitory mechanism of 1,6-Di-O-galloyl-β-D-glucose is competitive inhibition of the template primer and non-competitive inhibition of the substrate (dTTP). 1,6-Di-O-galloyl-β-D-glucose can be used in anti-HIV research .
    1,6-Di-O-galloyl-β-D-glucose
  • HY-P1138
    Scrambled 10Panx

    FSVYWAQADR

    		 Gap Junction Protein Others
    Scrambled 10Panx (FSVYWAQADR) is a random sequence variant of a specific inhibitory peptide 10Panx targeted at the half-channel of Pannexin-1 (Panx1). Scrambled 10Panx is used as a control peptide to determine whether other experimental conditions or peptides act through specific molecular mechanisms. Scrambled 10Panx can be used for research in neurobiology and cell biology .
    Scrambled 10Panx
  • HY-135228
    GZ4

    		Calcium Channel Neurological Disease
    GZ4 is a calcium current inhibitor with direct inhibitory activity on cell surface channels. GZ4 inhibition reverses mechanical hyperalgesia/hyperalgesia in a spinal nerve ligation-induced neuropathic pain model. The mechanism of action of GZ4 is similar to that of gabapentin, but the time course of its biological effects is more rapid, indicating that GZ4 can directly inhibit calcium channel currents .
    GZ4
  • HY-161296
    TH6342

    		Bacterial HIV Infection
    TH6342 is a SAMHD1 modulator that binds to pretetrameric SAMHD1 and prevents its oligomerization and allosteric activation. SAMHD1 is a dNTP triphosphohydrolase and an HIV-1 restriction factor. SAMHD1 can limit the replication of retroviruses and DNA viruses and has antiviral effects. The inhibitory mechanism of TH6342 does not occupy the SAMHD1 nucleotide-binding pocket, gently binds the target, and functions as a chemical probe .
    TH6342
  • HY-115824
    7ETMC

    		Cytochrome P450 Others
    7ETMC is a cytochrome P450 inhibitor with selective inhibition of human cytochrome P450s 1A1 and 1A2. 7ETMC has inhibitory effects on P450s 1A1 and 1A2 with IC?? values of 0.46μM and 0.50μM, respectively, within the first six minutes, and has no inhibitory activity against P450s 2A6 and 2B1. Except for 7-ethynyl-3-methyl-4-phenylcoumarin, the remaining inhibitors show mechanism-based inhibition of P450s 1A1 and 1A2.
    7ETMC
  • HY-N0057
    3,4-Dicaffeoylquinic acid
    4 Publications Verification

    3,4-Di-O-caffeoylquinic acid; Isochlorogenic acid B

    		 Glycosidase Influenza Virus Apoptosis Endogenous Metabolite Infection Cancer
    3,4-Dicaffeoylquinic acid (3,4-Di-O-caffeoylquinic acid), naturally isolated from Laggera alata, has antioxidative, DNA protective, neuroprotective and hepatoprotective properties. 3,4-Dicaffeoylquinic acid exerts apoptosis-mediated cytotoxicity and α-glucosidase inhibitory effects. 3,4-Dicaffeoylquinic acid possesses a unique mechanism of anti-influenza viral activity, that is, enhancing viral clearance by increasing TRAIL .
    3,4-Dicaffeoylquinic acid
  • HY-167920
    Glutathione sulfonate

    S-Sulfoglutathione

    		 Endogenous Metabolite Cancer
    Glutathione sulfonate (S-Sulfoglutathione) is a multifunctional bioactive compound that inhibits angiogenesis and tumor growth. Glutathione sulfonate is a competitive inhibitor of glutathione S-transferase and is involved in the detoxification process and the binding of a variety of exogenous and endogenous compounds. Glutathione sulfonate acts in the substrate binding site of Escherichia coli glutathione S-transferase, affecting the catalytic mechanism. The structural characteristics of Glutathione sulfonate contribute to its inhibitory effect by hydrogen bonding in the active center of the enzyme .
    Glutathione sulfonate
  • HY-Y0624R
    4-Pentenoic acid (Standard)

    		Reference Standards Endogenous Metabolite Mitochondrial Metabolism Metabolic Disease
    4-Pentenoic acid (Standard) is the analytical standard of 4-Pentenoic acid (HY-Y0624). This product is intended for research and analytical applications. 4-Pentenoic acid is a medium-chain unsaturated fatty acid. 4-Pentenoic acid has hypoglycemic and fatty acid oxidation inhibitory activities. 4-Pentenoic acid can affect blood glucose metabolism and energy metabolism through mechanisms such as inhibiting long-chain fatty acid oxidation, reducing gluconeogenesis, and promoting glucose utilization.
    4-Pentenoic acid (Standard)
  • HY-114796
    tHGA

    		Lipoxygenase Inflammation/Immunology
    tHGA is a compound with anti-inflammatory activity and has the activity to inhibit soybean 15-LOX. tHGA showed significant inhibitory effects in experiments on human leukocytes, with an IC50 value of 0.42 μM, which is close to the effect of commonly used standard NDGA. tHGA concentration-dependently inhibits the synthesis of 5-LOX products, especially the cysteine leukotriene LTC(4), with an IC50 value of 1.80 μM. and showed no cytotoxicity. The anti-inflammatory effects of tHGA do not appear to be through redox or metal chelation mechanisms, as the compound was negative in these bioactivity tests. tHGA works through a dual LOX/COX inhibition mechanism and has higher selectivity for 5-LOX and COX-2, with an IC50 value of 0.40 μM .
    tHGA
  • HY-W016473
    Adamantane-carboxylic acid

    		Bacterial Infection
    Adamantane-carboxylic acid is a compound with inhibitory activity against microorganisms. Although its specific target has not been clearly defined, it can inhibit Gram-positive bacteria and some Gram-negative bacteria. It forms a 1-monoacylglycerol derivative through a direct reaction with glycidol, and exerts its antibacterial effect by mechanisms such as altering the permeability of the bacterial cell membrane. This compound can be used in the research of antibacterial agents in the food and cosmetic industries to reduce harmful microbial flora and extend the shelf life of products .
    Adamantane-carboxylic acid
  • HY-167689
    Parethoxycaine hydrochloride

    		Adrenergic Receptor Neurological Disease
    Parethoxycaine hydrochloride is an anesthetic with nerve conduction blocking activity. Parethoxycaine hydrochloride exhibits non-selective inhibitory effects on responses to various stimulants in rat vas deferens and guinea pig ileum muscles. Parethoxycaine hydrochloride has an enhanced effect on the action of norepinephrine, and its methyl bromide derivative also exhibits the same properties on the action of norepinephrine and potassium ions. Derivatives of parethoxycaine hydrochloride have significant effects on calcium dose-response curves, displaying different tissue and stimulant selectivities. The mechanism of action of Parethoxycaine hydrochloride involves the regulation of calcium transport processes .
    Parethoxycaine hydrochloride
  • HY-W010995
    2,5-Dimethylcelecoxib

    		Wnt Survivin β-catenin Cancer
    2,5-Dimethylcelecoxib is an analogue of celecoxib (HY-14398) with anticancer activity but without COX-2 inhibitory activity. 2,5-Dimethylcelecoxib exerts its anti-cancer cell proliferation effect by inhibiting the core mechanism of the Wnt/β-catenin signaling pathway. 2,5-Dimethylcelecoxib also inhibits T-cell factor-dependent transcriptional activity and inhibits expression of the Wnt/β-catenin target gene products cyclin D1 and survivin .
    2,5-Dimethylcelecoxib
  • HY-107717
    MNI-caged-NMDA

    		iGluR Neurological Disease
    MNI-caged-NMDA is a light-sensitive amino acid with rapid release properties suitable for use in the study of fast synaptic receptor mechanisms. MNI-caged-NMDA shows metered release of NMDA receptors, inducing rapid and sustained receptor activation in cerebellar interneurons. MNI-caged-NMDA is able to achieve rapid transient responses and generate large inward currents by local laser photolysis. The use of MNI-caged-NMDA can effectively study neurotransmitter signaling and its inhibitory effects on GABA-A receptors .
    MNI-caged-NMDA
  • HY-171477
    Metahexestrol

    		Estrogen Receptor/ERR Cancer
    Metahexestrol is an estrogen receptor (E2R) inhibitor with antitumor activity. It significantly inhibits the proliferation of estrogen receptor-positive MCF-7 human breast cancer cells (ED50 = 1.0 μM). Additionally, Metahexestrol also exhibits inhibitory effects in estrogen receptor-negative MDA-MB-231 cells, and its antiproliferative activity cannot be reversed by estrogen, suggesting that its mechanism of action may be partially independent of the E2R pathway. Metahexestrol can be used in research on estrogen-dependent breast cancer .
    Metahexestrol
  • HY-168165
    Adefovir diphosphate

    		Endogenous Metabolite Cancer
    Adefovir diphosphate is an antiviral compound with activity against hepatitis B virus (HBV). Adefovir diphosphate blocks the replication of HBV by inhibiting reverse transcriptase. Adefovir diphosphate has also shown activity against other viruses such as herpes viruses and human immunodeficiency virus. Adefovir diphosphate is used as an effective inhibitory option in the suppression of chronic hepatitis B. The mechanism of action of Adefovir diphosphate involves blocking the autophosphorylation of growth factor receptors, thereby potentially reducing the risk of hepatocellular carcinoma (HCC) in patients with chronic hepatitis B .
    Adefovir diphosphate
  • HY-N0057R
    3,4-Dicaffeoylquinic acid (Standard)

    3,4-Di-O-caffeoylquinic acid (Standard); Isochlorogenic acid B (Standard)

    		 Reference Standards Glycosidase Influenza Virus Apoptosis Endogenous Metabolite Infection Cancer
    3,4-Dicaffeoylquinic acid (Standard) is the analytical standard of 3,4-Dicaffeoylquinic acid. This product is intended for research and analytical applications. 3,4-Dicaffeoylquinic acid (3,4-Di-O-caffeoylquinic acid), naturally isolated from Laggera alata, has antioxidative, DNA protective, neuroprotective and hepatoprotective properties. 3,4-Dicaffeoylquinic acid exerts apoptosis-mediated cytotoxicity and α-glucosidase inhibitory effects. 3,4-Dicaffeoylquinic acid possesses a unique mechanism of anti-influenza viral activity, that is, enhancing viral clearance by increasing TRAIL .
    3,4-Dicaffeoylquinic acid (Standard)
  • HY-169412
    MAPK-IN-3

    		MDM-2/p53 CDK Caspase Bcl-2 Family Reactive Oxygen Species (ROS) p38 MAPK ERK JNK Cancer
    MAPK-IN-3 (Compound 4a) is an anti-proliferative agent that shows particularly strong inhibitory effects on KYSE 30, HCT 116, and HGC 27, with IC50 values of 0.57 μM, 3.27 μM, and 2.28 μM, respectively. MAPK-IN-3 blocks the cell cycle via a p53-dependent mechanism and induces cell apoptosis through a p53-independent mechanism. MAPK-IN-3 downregulates the expression of cell cycle-related proteins like Cyclin D1 and cyclin B1, upregulates pro-apoptotic proteins such as cleaved PARP, cleaved caspase-7, and cleaved caspase-9, and reduces the expression of anti-apoptotic proteins like Bcl-2. Additionally, MAPK-IN-3 increases the intracellular level of ROS in KYSE 30 cells and upregulates the expression of members of the MAPK signaling pathway associated with ROS, such as p-ERK, p-p38 and p-JNK .
    MAPK-IN-3
  • HY-129200
    Aspergillomarasmine A

    		Endogenous Metabolite Others
    Aspergillomarasmine A is a natural aminopolycarboxylic acid with potent inhibitory activity against class B metallo-β-lactamases (MBLs). Aspergillomarasmine A inactivates MBLs by removing a catalytic Zn2+ cofactor. Aspergillomarasmine A acts as a selective Zn2+ scavenger, promoting the dissociation of the metal cofactor, thereby indirectly inactivating NDM-1. Aspergillomarasmine A causes the loss of Zn2+ ions from the low-affinity binding site of NDM-1. The action of Aspergillomarasmine A results in the rapid degradation of Zn2+-deficient NDM-1, thereby enhancing its potency as a β-lactam enhancer. The mechanism of Aspergillomarasmine A has broad applicability among different Zn2+ chelators .
    Aspergillomarasmine A
  • HY-155846
    Antileishmanial agent-22

    		Parasite Bacterial Infection
    Antileishmanial agent-22 (compound 15b) is a parasite inhibitor and an antibacterial agent, with antileishmanial, antimalarial, and anti-tubercular activities. Antileishmanial agent-22 inhibits leishmanial (IC50=0.408 μM) based on antifolate mechanism. And, Antileishmanial agent-22 inhibits Folic acid and Folinic acid at 100 μM with inhibitory rates of 88% and 94%, respectively. Antileishmanial agent-22 inhibits P. berghei in vivo and in vitro, with 96.67% suppression under 48.4 μM/kg/day and 0.038 μM (IC50), respectively. Moreover, Antileishmanial agent-22 inhibits M. tuberculosis with MIC of 28.44 μM .
    Antileishmanial agent-22
  • HY-P10977
    Tat-ASIC1a (1-20) (mouse, rat)

    		Sodium Channel RIP kinase Neurological Disease
    Tat-ASIC1a (1-20) (mouse, rat) is a competitive ASIC1a membrane-penetrating peptide. Tat-ASIC1a (1-20) (mouse, rat) has significantly neuroprotection effects, and reduces neuronal damage against acidotoxicity by targeting the ASIC1a-RIPK1 pathway and auto-inhibitory mechanism. Tat-ASIC1a (1-20) (mouse, rat) effectively protects brains from ischemic injury in ischemic stroke mice model. Tat-ASIC1a (1-20) (mouse, rat) can be used for neurodegenerative diseases research, such as Huntington disease and Parkinson’s disease .
    Tat-ASIC1a (1-20) (mouse, rat)
  • HY-136818
    DA 4643 dihydrochloride

    		Histamine Receptor Endocrinology
    DA 4643 (hydrochloride) is an H2 receptor antagonist with the chemical name 2-guanidino-4 (3-methylaminomethyleneiminophenyl) thiazole dihydrochloride. It has a weak interaction with cytochrome P-450 and has a less inhibitory effect on P-450 than cimetidine and tiotidine. DA 4643 (hydrochloride) is able to inhibit both enzymatic and non-enzymatic lipid peroxidation reactions. This inhibition may not be achieved by inhibiting agent metabolizing enzymes, but rather due to the antioxidant properties of the compound itself. Compared with other H2 receptor antagonists such as cimetidine, ranitidine and tiotidine, DA 4643 (hydrochloride) shows a unique effect in lipid peroxidation inhibition. These properties make DA 4643 (hydrochloride) a potential H2 receptor antagonist with multiple mechanisms of action.
    DA 4643 dihydrochloride
  • HY-W010991
    N-[3-(2-Furyl)acryloyl]-Phe-Gly-Gly

    FAPGG

    		 Angiotensin-converting Enzyme (ACE) Others
    N-[3-(2-Furyl)acryloyl]-Phe-Gly-Gly (FAPGG) is a specific substrate of angiotensin converting enzyme (ACE) with a Ki of 2.546×10 -4 M. It is used as a chromogenic probe for quantitative detection of ACE activity. N-[3-(2-Furyl)acryloyl]-Phe-Gly-Gly can be hydrolyzed by ACE to generate N-[3-(2-furyl)acryloyl]-Phe (FAP) and Gly-Gly, and the ACE inhibitory effect is monitored by photometry. FAPGG competitively binds to the active center of ACE and is a key tool for screening ACE inhibitors such as Captopril (HY-B0368) and Dioscorin. Its reversible mechanism of action supports hypertension research and drug development targeting the renin-angiotensin system .
    N-[3-(2-Furyl)acryloyl]-Phe-Gly-Gly
  • HY-173365
    VEGFR-2-IN-67

    		VEGFR Cancer
    VEGFR-2-IN-67 (Compound 6b) is an inhibitor of vascular endothelial growth factor receptor 2 (VEGFR-2). Its IC50 values for MDA-231 and MCF-7 cell lines are 5.91 µM and 7.16 µM respectively, and its inhibitory effect on VEGFR-2 is comparable to that of Sorafenib (HY-10201) (IC50 is 53.63 nM). VEGFR-2-IN-67 exerts significant anti-cancer activity through mechanisms such as inducing Apoptosis (the early apoptosis rate reaches 57.20%), arresting the cell cycle at the G1 phase, upregulating pro-apoptotic markers and downregulating Bcl-2. VEGFR-2-IN-67 can be used for research in the field of cancer .
    VEGFR-2-IN-67
  • HY-12716
    BRL-44408

    		Adrenergic Receptor Endocrinology
    BRL-44408 is a selective adrenergic receptor antagonist of α2A/α2B AR. BRL-44408 can effectively antagonize the inhibitory effects of norepinephrine or adrenergic receptor agonist Clonidine (HY-12721) on K +-induced [3H]norepinephrine and [3H]5-hydroxytryptamine release. BRL-44408 has a higher affinity for human platelet membranes containing α2A-adrenoceptors than BRL-41992 and Imiloxan (HY-101337). BRL-44408 may affect the release of norepinephrine and 5-hydroxytryptamine through a mechanism mediated by α2A-adrenoceptors, and has a potential role in the regulation of neurotransmitter release .
    BRL-44408
  • HY-145939
    BAY-888

    BRD5846

    		 Casein Kinase Cancer
    BAY-888 is a selective CK1α/CSNK1A1 (casein kinase 1α) ATP-competitive inhibitor (IC50: 4 nM@10 μM ATP; 63 nM@1 mM ATP). BAY-888 blocks the negative regulation of p53 and other signaling pathways by CK1α, induces apoptosis and inhibits proliferation of tumor cells. BAY-888 has shown inhibitory efficacy against cancers such as acute myeloid leukemia (AML) in PRISM barcoded cell line screening and can mimic the effects of shRNA-mediated CK1α knockdown. BAY-888 is primarily used for the development of anticancer drugs for p53 wild-type tumors and for the study of the mechanisms of CK1α-related signaling pathways .
    BAY-888
  • HY-172892
    PI3K-IN-59

    		PI3K Reactive Oxygen Species (ROS) Cancer
    PI3K-IN-59 (Compound 3d) is a PI3K inhibitor (IC50: 17.44 μM). PI3K-IN-59 has significant antiproliferative activity and exhibits potent inhibitory effects on breast cancer 4T1 cells (IC50: 3.70 μM) and colon cancer CT26 cells (IC50: 1.98 μM) as well as human breast cancer cells (IC50: 19.72 μM). PI3K-IN-59 exerts a dual anti-tumor mechanism by inhibiting PI3Kα enzymatic activity and triggering the Fenton reaction to generate hydroxyl radicals (•OH). PI3K-IN-59 shows promising anti-4T1 tumor effects and is suitable for synergistic targeting studies in breast and colon cancers .
    PI3K-IN-59

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