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Activity evaluation

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55

Inhibitors & Agonists

1

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4

Fluorescent Dye

2

Biochemical Assay Reagents

4

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6

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-W076971

    Others Others
    Ethyl pivaloylacetate is a β-ketoester. Ethyl pivaloylacetate can be uesd as the substrate to evaluate the activity and stereoselectivity of the ketoreductase tool-box .
    Ethyl pivaloylacetate
  • HY-W019724

    Drug Intermediate Others
    2,2-Dihydroxyacetic acid is a key intermediate used in the synthesis of 3-aminocoumarone derivatives, which exhibit significant activity in chemiluminescence reactions and can be used for detecting hydrogen peroxide and evaluating urease activity .
    2,2-Dihydroxyacetic acid
  • HY-135152

    Reactive Oxygen Species (ROS) Cancer
    CYPMPO is a spin-trapping reagent. CYPMPO, a cyclic DEPMPO-type nitrone, is evaluated for spin-trapping capabilities toward hydroxyl and superoxide radicals. anti-oxidant and anti-tumor?activity .
    CYPMPO
  • HY-103455

    Estrogen Receptor/ERR Others
    ZK164015 is an estrogen-glucocorticoid receptor chimera that can be used as a compound screening tool to evaluate tissue-selective estrogen activity. ZK164015 was used to evaluate its effects on ER function in osteoblasts in studies based on green fluorescent protein (GFP)-receptor chimeras. In osteoblast-like (ROS and U2OS) and breast cancer (MCF7) cells, ZK164015 showed different effects in response to ER agonists, including modulation of ERE-luc activity and effects on nuclear mobility.
    ZK164015
  • HY-B1237

    Na+/K+ ATPase Cardiovascular Disease
    Suloctidil is a new drug that is currently being evaluated in many clinical trials for use in dementia and thrombotic disorders Target: Effect of suloctidil on Na+/K+ ATPase activity and on membrane fluidity in rat brain synaptosomes.
    Suloctidil
  • HY-113327

    Endogenous Metabolite Cancer
    1,3,7-Trimethyluric acid is the metabolite of caffeine. The metabolic ratio 1,3,7-Trimethyluric acid to caffeine can be evaluated as a biomarker to describe variability in CYP3A activity in a cohort .
    1,3,7-Trimethyluric acid
  • HY-175011

    EGFR Apoptosis Cancer
    EGFR-IN-165 is a potent EGFR inhibitor. EGFR-IN-165 demonstrates superior potency with IC50s of 17.18 and 64.74 nM against EGFR L858R/T790M and EGFR WT; 2.17 and 6.2 μM against NCI-H1975 cells and A431 cells. EGFR-IN-165 significantly inhibits the migration and induces G1 phase cell cycle arrest and cell apoptosis. EGFR-IN-165 can be used for the study of cancers such as non-small cell lung cancer, colorectal cancer, and head and neck squamous cell carcinoma .
    EGFR-IN-165
  • HY-B1237A

    Na+/K+ ATPase Cardiovascular Disease
    Suloctidil hydrochloride hydrochloride is an active agent against on Na+/K+ ATPase activity and on membrane fluidity in rat brain synaptosomes. Suloctidil hydrochloride is currently being evaluated in many clinical trials for use in dementia and thrombotic disorders.
    Suloctidil hydrochloride
  • HY-W040156

    Fungal Infection
    Oxadixyl is a fungicide with activity that inhibits the growth of fungi. Oxadixyl was tested during the malic fermentation of red wine, where its concentration may be affected. The biological activity of Oxadixyl helps to evaluate its effect on microorganisms during the winemaking process .
    Oxadixyl
  • HY-119324

    Apoptosis Others
    Anticancer agent 254 (compound 10) is a dichloroacetic acid-loaded compound with enhanced antitumor activity against leukemia cells in vitro and better stability in vivo, and can be considered for preclinical evaluation of cancer inhibition.
    Anticancer agent 254
  • HY-146248B

    Biochemical Assay Reagents Metabolic Disease
    TFMU-ADPr is a universal substrate for monitoring PARG activity. TFMU-ADPr directly reports the total bar number hydrolase activity by releasing fluorophore. TFMU-ADPr is a general tool for evaluating small molecule inhibitors and exploring the regulation of ADP-ribose catabolic enzymes in vitro .
    TFMU-ADPr diammonium
  • HY-D1427

    Fluorescent Dye Neurological Disease
    Di-2-ANEPEQ is a voltage sensitive membrane potential fluorescence dye. Di-2-ANEPEQ can be used for the evaluation of voltage-sensitive fluorescence dyes for monitoring neuronal activity in the embryonic central nervous system .
    Di-2-ANEPEQ
  • HY-B1838

    Herbicide Others
    Asulam is a herbicide with control activity against wild oats. Asulam can be used for bulb production in spinach, tulips, daffodils and lilies. Maximum residue limits (MRLs) for Asulam were evaluated in spinach. The review of Asulam took into account its endocrine disrupting properties .
    Asulam
  • HY-W040156R

    Fungal Reference Standards Infection
    Oxadixyl (Standard) is the analytical standard of Oxadixyl. This product is intended for research and analytical applications. Oxadixyl is a fungicide with activity that inhibits the growth of fungi. Oxadixyl was tested during the malic fermentation of red wine, where its concentration may be affected. The biological activity of Oxadixyl helps to evaluate its effect on microorganisms during the winemaking process .
    Oxadixyl (Standard)
  • HY-101040R

    Q203 (Standard); IAP6 (Standard)

    Reference Standards Bacterial Antibiotic Infection
    Oxadixyl (Standard) is the analytical standard of Oxadixyl. This product is intended for research and analytical applications. Oxadixyl is a fungicide with activity that inhibits the growth of fungi. Oxadixyl was tested during the malic fermentation of red wine, where its concentration may be affected. The biological activity of Oxadixyl helps to evaluate its effect on microorganisms during the winemaking process .
    Telacebec (Standard)
  • HY-101445B

    Drug Isomer Neurological Disease
    (S)-Trolox is an analogue of vitamin E, in which the phytyl chain is replaced with a carboxyl group. (S)-Trolox is frequently used as a model compound for studies of structural features, as well as a standard for evaluation of antioxidant activity. (S)-Trolox has potent and specific neuroprotective and antioxidant effects .
    (S)-Trolox
  • HY-W854392

    Biochemical Assay Reagents
    3-Carboxyumbelliferyl-β-D-glucuronide (dipotassium) is a chromogenic substrate with biological activity for enzyme activity detection. 3-Carboxyumbelliferyl-β-D-glucuronide (dipotassium) can be used to evaluate biological reactions associated with glycosidases. 3-Carboxyumbelliferyl-β-D-glucuronide (dipotassium) shows a wide range of application potentials in compound discovery and biomedical research.
    3-Carboxyumbelliferyl-β-D-glucuronide dipotassium
  • HY-P4202

    Suc-AEPF-pNA

    Biochemical Assay Reagents Others
    Suc-Ala-Glu-Pro-Phe-pNA (Suc-AEPF-pNA) is a chromogenic substrate for the peptidylprolyl isomerase Pin1. Suc-Ala-Glu-Pro-Phe-pNA can be used to evaluate the inhibitory effect of the target compound on Pin1, and catalytic activity of Pin1, etc .
    Suc-Ala-Glu-Pro-Phe-pNA
  • HY-P10609

    Btk Others
    Btk substrate peptide is a peptide substrate corresponding to residues 217-229 of human Bruton’s tyrosine kinase (Btk), of which the tyrosine at residue 223 is the major autophosphorylation site of Btk. Btk substrate peptide is used as a substrate in in vitro kinase assays to evaluate the activity of Btk or other tyrosine kinases .
    Btk substrate peptide
  • HY-E70075

    GDH-TIM; GDH-TPI

    Transketolase Metabolic Disease
    α-Glycerophosphate Dehydrogenase-Triosephosphate (GDH-TIM) is an enzyme mixture composed of glycerol phosphate dehydrogenase (GDH) and triphosphate isomerase (TIM). α-Glycerophosphate Dehydrogenase-Triosephosphate can be used to determine the activity of transketolase (TK) in hemolytic substances of red blood cells to evaluate vitamin B deficiency .
    α-Glycerophosphate Dehydrogenase-Triosephosphate
  • HY-116567A

    Endogenous Metabolite Endocrinology
    (S)-OPC-51803 is an agonist of the vasopressin V2 receptor, with activity in suppressing nocturia and urinary incontinence. (S)-OPC-51803 was evaluated in terms of biological activity and showed a stronger V2 receptor agonist effect compared to its (R)-isomer. The use of (S)-OPC-51803 may improve the patient's ability to control nocturnal polyuria .
    (S)-OPC-51803
  • HY-162602

    EGFR Cancer
    EGFR-IN-115 (H-13) is an EGFR inhibitor, with IC50 of 395.2 nM. EGFR-IN-115 can be used in anti-cancer research .
    EGFR-IN-115
  • HY-P4202A

    Suc-AEPF-pNA TFA

    Biochemical Assay Reagents Others
    Suc-Ala-Glu-Pro-Phe-pNA (Suc-AEPF-pNA ) TFA is a chromogenic substrate for the peptidylprolyl isomerase Pin1. Suc-Ala-Glu-Pro-Phe-pNA TFA can be used to evaluate the inhibitory effect of the target compound on Pin1, and catalytic activity of Pin1, etc .
    Suc-Ala-Glu-Pro-Phe-pNA TFA
  • HY-134308

    Fluorescent Dye Others
    8-NBD-cAMP sodium is a fluorescently labeled cyclic adenosine phosphate (cAMP) analogue. 8-NBD-cAMP sodium retains a similar biological activity to cAMP, regulating their activity by binding to specific proteins such as EPACs or PKA. 8-NBD-cAMP sodium can be used in fluorescent competitive binding experiments to evaluate the binding affinity of newly synthesized EPAC1 agonists to EPAC1 proteins .
    8-NBD-cAMP sodium
  • HY-W749411

    Biochemical Assay Reagents Endogenous Metabolite
    Malondialdehyde tetrabutylammonium is a biomarker with antioxidant activity. Malondialdehyde tetrabutylammonium can be used as an indicator of lipid peroxidation to help assess oxidative stress levels. Malondialdehyde tetrabutylammonium is widely used in the food and cosmetics fields, mainly for monitoring and evaluating product stability and safety. Malondialdehyde tetrabutylammonium has an important role in indicating cell damage and is a potential biomarker for studying a variety of diseases.
    Malondialdehyde tetrabutylammonium
  • HY-146282

    GABA Receptor Neurological Disease
    mGAT-IN-1 (compound 28) is a potent and non-selective GAT inhibitor. mGAT-IN-1 has a high inhibitory potency toward mGAT3, with an IC50 of 2.5 μM and pIC50 of 5.61 .
    mGAT-IN-1
  • HY-130406

    Fungal Infection
    Benthiavalicarb isopropyl is a fungicide with specific activity against downy mildew and blight. Benthiavalicarb isopropyl is evaluated for use where necessary to control a serious threat to plant health that cannot be treated by other methods, including non-chemical methods. The use of Benthiavalicarb isopropyl can be considered representative of field applications in potatoes. Environmental and human exposures of Benthiavalicarb isopropyl are considered to be negligible .
    Benthiavalicarb isopropyl
  • HY-Y0889A

    Endogenous Metabolite Metabolic Disease
    1-(2,3-Dichlorphenyl)piperazine hydrochloride is a potent DHCR7 inhibitor with the activity of inhibiting cholesterol biosynthesis. 1-(2,3-Dichlorphenyl)piperazine hydrochloride is often used in biological research to evaluate the function of cholesterol biosynthesis pathway. The application of 1-(2,3-Dichlorphenyl)piperazine hydrochloride is of great significance for understanding diseases related to cholesterol biosynthesis .
    1-(2,3-Dichlorphenyl)piperazine hydrochloride
  • HY-Y0889

    Endogenous Metabolite Metabolic Disease
    1-(2,3-Dichlorphenyl)piperazine is a potent DHCR7 inhibitor with the activity of inhibiting cholesterol biosynthesis. 1-(2,3-Dichlorphenyl)piperazine is often used in biological research to evaluate the function of cholesterol biosynthesis pathway. The application of 1-(2,3-Dichlorphenyl)piperazine is of great significance for understanding diseases related to cholesterol biosynthesis .
    1-(2,3-Dichlorphenyl)piperazine
  • HY-115514A

    BRK Cancer
    BRK inhibitor P21d hydrochloride is a potent breast tumor kinase (BRK/PTK6) inhibitor with an IC50 of 30 nM. BRK inhibitor P21d hydrochloride inhibits p-SAM68 with an IC50 of 52 nM. BRK inhibitor P21d hydrochloride can be used to evaluate the in vivo activity of BRK inhibitors in xenograft breast tumor models .
    BRK inhibitor P21d hydrochloride
  • HY-W708304

    Isotope-Labeled Compounds Herbicide Others
    Asulam-d3 is the deuterium labeled Asulam (HY-B1838). Asulam is a herbicide with control activity against wild oats. Asulam can be used for bulb production in spinach, tulips, daffodils and lilies. Maximum residue limits (MRLs) for Asulam were evaluated in spinach. The review of Asulam took into account its endocrine disrupting properties .
    Asulam-d3
  • HY-167922

    Endogenous Metabolite Neurological Disease
    (R,R,S)-GAT107 is a fully agonistic positive modulator of α7 nicotinic receptors with significant biological activity. Its activity is entirely present in its (+)-isomer 1b, while (-)-isomer 1a does not affect its activity when used together. Studies have shown that (R,R,S)-GAT107 is the most potent ago-PAM for α7 nicotinic receptors currently known and has the potential for further in vivo evaluation .
    (R,R,S)-GAT107
  • HY-116000
    Glumetinib
    1 Publications Verification

    Gumarontinib; SCC244

    c-Met/HGFR Cancer
    Glumetinib (SCC244) is a highly selective, orally bioavailable, ATP-competitive c-Met inhibitor with an IC50 of 0.42 nM. Glumetinib has greater than 2400-fold selectivity for c-Met over those 312 kinases evaluated, including the c-Met family member RON and highly homologous kinases Axl, Mer, TyrO3. Antitumor activity .
    Glumetinib
  • HY-N8960

    Others Neurological Disease
    1-Hydroxybisabola-2,10-dien-4-one is a compound with potential anti-Alzheimer's disease activity. The activity of 1-Hydroxybisabola-2,10-dien-4-one was evaluated in the Caenorhabditis elegans Alzheimer's disease pathological model. 1-Hydroxybisabola-2,10-dien-4-one has a wide range of applications in life science related research .
    1-Hydroxybisabola-2,10-dien-4-one
  • HY-167824

    Endogenous Metabolite Neurological Disease
    SSR180711 is a potent and subtype-selective α7 agonist with activity in Alzheimer's disease and schizophrenia research. SSR180711 can be used to study subtypes of intracerebral hemorrhage associated with cerebral small vessel disease. SSR180711 shows potential in electrophysiological and behavioral studies to evaluate its effects on cognitive function. SSR180711 also has potential for studying cerebrovascular lesions and their effects .
    SSR180711
  • HY-12172

    ACT-077825

    Renin Cardiovascular Disease
    MK-8141 (ACT-077825) is a renin inhibitor that significantly increases levels of immunoreactive renin (ir-AR) by sevenfold but does not result in sustained reductions in blood renin activity (PRA). This study evaluated the antihypertensive efficacy of MK-8141 in hypertensive disease. Despite its effects on ir-AR, MK-8141 (ACT-077825) did not produce significant blood pressure-lowering effects in the absence of sustained PRA inhibition.
    MK-8141
  • HY-119200

    Endogenous Metabolite Cancer
    LY-195448 hydrochloride is a phenethanolamine that exhibits anti-tumour activity across various murine tumour models. LY-195448 hydrochloride acts by blocking cells at metaphase. LY-195448 hydrochloride has demonstrated a lack of "standard" side effects commonly associated with cancer treatments, such as myelosuppression and gastrointestinal toxicity. LY-195448 hydrochloride was evaluated in a phase I trial, where it showed only mild and reversible side effects like hypotension, tachycardia, and tremor.
    LY-195448 hydrochloride
  • HY-117637

    Oxytocin Receptor Neurological Disease
    ALS-I-41 is a novel, potent and selective oxytocin receptor antagonist with the potential to modulate biological activities related to social behavior and mental disorders. ALS-I-41 is being evaluated for behavioral pharmacology experiments in non-human primates and can be administered via intranasal or intramuscular injection. The central nervous system penetration and metabolic rate of ALS-I-41 were studied by mass spectrometry analysis in cerebrospinal fluid and plasma of macaque monkeys .
    ALS-I-41
  • HY-167922S

    Isotope-Labeled Compounds Endogenous Metabolite Neurological Disease
    Heptadecanoyl L-carnitine-d3 HCl is the deuterium labeled (R,R,S)-GAT107 (HY-167922). (R,R,S)-GAT107 is a fully agonistic positive modulator of α7 nicotinic receptors with significant biological activity. Its activity is entirely present in its (+)-isomer 1b, while (-)-isomer 1a does not affect its activity when used together. Studies have shown that (R,R,S)-GAT107 is the most potent ago-PAM for α7 nicotinic receptors currently known and has the potential for further in vivo evaluation .
    Heptadecanoyl L-carnitine-d3 HCl
  • HY-19145

    CI-992

    Renin Cancer
    PD-134672 (CI-992) is a renin inhibitor containing a 2-amino-4-thiazolyl substituent. PD-134672 potently inhibits monkey renin in vitro and only weakly inhibits the related aspartic protease bovine feline hepsin D. The compound exhibits oral hypotensive activity in hyperreninemic normotensive monkeys. Based on its superior efficacy and long-lasting effects in vitro and in the normotensive macaque model, PD-134672 was selected for further evaluation in renal hypertensive monkeys.
    PD-134672
  • HY-113817

    Phosphatase Inflammation/Immunology
    SHIP1 activator 1 is an SH3 domain-containing inositol 5-phosphatase regulator with SHIP1 activating activity. SHIP1 activator 1 retains its SHIA-1 activating ability by removing unnecessary functional groups. SHIP1 activator 1 is able to activate SHIP1 in vitro, inhibit Akt phosphorylation in MOLT-4 cells, and show dose-dependent activity in a mouse model of inflammation. SHIP1 activator 1 is an important chemical tool for evaluating the potential of SHIP1 activators as inhibitors of hematopoietic diseases involving abnormal PI3K cell signaling .
    SHIP1 activator 1
  • HY-19904A

    (+/-)-LY2409021

    Endogenous Metabolite Metabolic Disease
    (+/-)-Adomeglivant ((+/-)-LY2409021) is a potent and selective glucagon receptor antagonist with hypoglycemic activity. (+/-)-Adomeglivant is effective in lowering blood sugar levels in both healthy people and people with type 2 diabetes. (+/-)-Adomeglivant is well tolerated by glucagon signaling blockade in patients with type 2 diabetes and significantly reduces fasting and postprandial blood glucose with a concomitant reversible elevation of aminotransferases. Glucagon signaling inhibition by (+/-)-Adomeglivant is a promising potential inhibitory approach for patients with type 2 diabetes and warrants further evaluation of its benefits and risks in longer clinical trials .
    (+/-)-Adomeglivant
  • HY-104044A

    BGB-290 maleate

    Apoptosis Neurological Disease
    Pamiparib maleate (BGB-290 maleate) is a highly potent and selective PARP inhibitor with neurotoxicity-inducing activity. Pamiparib maleate can effectively penetrate the blood-brain barrier and cause cerebral hemorrhage, brain atrophy, and movement disorders in zebrafish embryos exposed. Pamiparib maleate exposure downregulates the activities of acetylcholinesterase (AChE) and adenosine triphosphatase (ATPase) and leads to upregulation of oxidative stress, which triggers apoptosis and interferes with the expression of neurodevelopment-related genes. The use of pamiparib maleate is also accompanied by downregulation of the Notch signaling pathway, while activation of the Notch signaling pathway can partially rescue neurodevelopmental toxicity. Therefore, pamiparib maleate provides a reference for evaluating its potential neurotoxicity during embryonic development .
    Pamiparib maleate
  • HY-109014

    CMX-157

    HIV HBV Nucleoside Antimetabolite/Analog Infection
    Tenofovir exalidex (CMX157) is a lipid conjugate of the acyclic nucleotide analog Tenofovir with activity against both wild-type and antiretroviral drug-resistant HIV strains, including multidrug nucleoside/nucleotide analog-resistant viruses. Tenofovir exalidex is active against all major subtypes of HIV-1 and HIV-2 in fresh human PBMCs and against all HIV-1 strains evaluated in monocyte-derived macrophages, with EC50s ranging between 0.2 and 7.2 nM. CMX157 is orally available and has no apparent toxicity. Tenofovir exalidex also shows antiviral activity against HBV .
    Tenofovir exalidex
  • HY-146281

    GABA Receptor Neurological Disease Metabolic Disease
    mGAT3/4-IN-2 (compound 27b) is a potent mGAT3/mGAT4 inhibitor, with pIC50 values of 5.44 and 5.25, respectively .
    mGAT3/4-IN-2
  • HY-146280

    GABA Receptor Neurological Disease Metabolic Disease
    mGAT3/4-IN-1 (compound 19b) is a potent mGAT3/mGAT4 inhibitor, with pIC50 values of 5.31 and 5.24, respectively. mGAT3/4-IN-1 exhibits a significant tactile allodynia reduction in diabetic neuropathic mice .
    mGAT3/4-IN-1
  • HY-129763

    Fluorescent Dye Cardiovascular Disease
    Di-4-ANEPPS is a voltage-sensitive dye that acts on voltage-gated ion channels (such as sodium channels) and inhibits sodium current, significantly reducing sodium current density, although specific values like IC50 remain unclear. It mainly binds to the voltage-sensitive regions on the cell membrane, changing its fluorescence properties to reflect membrane potential changes and thus affecting the function of ion channels to exert its activity. This substance can be used in cardiovascular research, such as the electrophysiology of cardiomyocytes, myocardial ischemia, and the effects of drugs on cardiomyocytes. It is of great value in evaluating drug cardiotoxicity and exploring the mechanisms of arrhythmias .
    Di-4-ANEPPS
  • HY-131909

    Anaplastic lymphoma kinase (ALK) Cancer
    CJ-2360 is a potent and orally active ALK inhibitor with IC50s of 2.2, 4.0, 8.8, 6.3, and 8.9 nM against wild-type ALK and F1197M, G1269A, L1196M, and S1206Y ALK mutants, respectively. CJ-2360 displays potent inhibitory activity against two clinically reported ALK mutants (C1156Y and L1196M) and a few other kinases (LTK, MERTK, CLK1, DAPK1, and DAPK2) among the 468 kinases evaluated .
    CJ-2360
  • HY-155517

    NOD-like Receptor (NLR) Pyroptosis Inflammation/Immunology
    INF200 (compound 5) is a sulfonylurea-based inhibitor of NLRP3 and NLRP3-mediated pyroptosis. INF200 has beneficial cardiometabolic effects in rat model of high-fat diet (HFD)-induced metaflammation,and shows anti-inflammatory activity to (10 μM) decreases IL-1β release in human macrophages. INF200 improves glucose and lipid profiles,and attenuates systemic inflammation and biomarkers of cardiac dysfunction (particularly BNP). INF200 also improves myocardial damage-dependent ischemia/reperfusion injury (IRI) in hemodynamic evaluation .
    INF200
  • HY-109014R

    HIV HBV Nucleoside Antimetabolite/Analog Infection
    Tenofovir exalidex (Standard) is the analytical standard of Tenofovir exalidex. This product is intended for research and analytical applications. Tenofovir exalidex (CMX157) is a lipid conjugate of the acyclic nucleotide analog Tenofovir with activity against both wild-type and antiretroviral drug-resistant HIV strains, including multidrug nucleoside/nucleotide analog-resistant viruses. Tenofovir exalidex is active against all major subtypes of HIV-1 and HIV-2 in fresh human PBMCs and against all HIV-1 strains evaluated in monocyte-derived macrophages, with EC50s ranging between 0.2 and 7.2 nM. CMX157 is orally available and has no apparent toxicity. Tenofovir exalidex also shows antiviral activity against HBV .
    Tenofovir exalidex (Standard)

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