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ICR

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61

Inhibitors & Agonists

1

Biochemical Assay Reagents

3

Peptides

6

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-19336
    BAZ2-ICR
    1 Publications Verification

    Epigenetic Reader Domain Cancer
    BAZ2-ICR is a potent, selective, cell active and orally active BAZ2A/B bromodomains inhibitor with IC50s of 130 nM and 180 nM, and Kds of 109 nM and 170 nM, respectively. BAZ2-ICR shows 10-15-fold selectivity for binding BAZ2A/B over CECR2 and >100-fold selectivity over all other bromodomains. BAZ2-ICR is an epigenetic chemical probe .
    BAZ2-ICR
  • HY-151563A

    Deubiquitinase Cancer
    OTUB1/USP8-IN-1 TFA is the TFA salt form of OTUB1/USP8-IN-1 (HY-151563). OTUB1/USP8-IN-1 TFA is a dual inhibitor for OTUB1/USP8, IC50 for OTUB1 and USP8 is 0.17 and 0.28 nM, respectively. OTUB1/USP8-IN-1 TFA inhibits proliferation of NSCLC cells. OTUB1/USP8-IN-1 TFA exhibits good pharmacokinetic characters in ICR mouse, and exhibits antitumor activity in H1975 xenograft mouse model .
    OTUB1/USP8-IN-1 TFA
  • HY-160926

    Glutathione S-transferase Cancer
    16-Oxocafestol enhances levels of glutathione S-transferase (GST) and tissue sulfhydryl in liver and in small bowel mucosa .
    16-Oxocafestol
  • HY-161539

    Opioid Receptor Neurological Disease
    KOR agonist 1 (Compound 7a) is a selective agonist for opioid receptor, with EC50s of 3.4, 701.2 and 1649 nM, for KOR, MOR and DOR, respectively. KOR agonist 1 binds KOR, MOR and DOR, with Kis of 3.9, 1053 and 4196 nM, respectively. KOR agonist 1 exhibits antinociceptive effect in ICR mouse model (ED50 in hot plate test is 0.3 mg/kg, in abdominal constriction test is 0.2 mg/kg) .
    KOR agonist 1
  • HY-115826

    Others Cancer
    AB-163 is an alkylating agent with anti-tumor activity. AB-163 exerts LD50s of 198 (p.o.) and 159 (i.p.) mg/kg in ICR/Ha male mice and can be utilized in cancer research .
    AB-163
  • HY-163315

    Keap1-Nrf2 AMPK Metabolic Disease
    YPLP is a yeast-derived peptide Tyr-Pro-Leu-Pro, which exhibits activity in anti fatigue mechanisms through the nuclear factor erythroid-2-related factor 2 (Nrf2)- and AMP-activated protein kinase (AMPK) pathway. YPLP is orally active .
    YPLP
  • HY-162485

    Dengue virus Virus Protease Infection
    DV-B-120 is a competitive inhibitor for dengue virus (DENV) with IC50s of 5.35, 7.39, 10.49 and 8.58 μM, for DENV-1, DENV-2, DENV-3 and DENV-4, respectively, by inhibiting NS2B-NS3 protease. DV-B-120 exhibits antiviral activity through inhibition of DENV replication .
    DV-B-120
  • HY-158365

    LRRK2 Neurological Disease
    LRRK2-IN-14 (Compound 8) is an orally active LRRK2 inhibitor. LRRK2-IN-14 has an IC50 of 6.3 nM for LRRK2(G2019S) cell activity.LRRK2-IN-14 has an inhibitory effect on hERG (IC50=22 μM). LRRK2-IN-14 has blood-brain barrier permeability .
    LRRK2-IN-14
  • HY-162408

    Protease Activated Receptor (PAR) Others
    PAR4 antagonist 3 (Compound 36) is a selective antagonist for protease activated receptor 4 (PAR4). PAR4 antagonist 3 exhibits antiplatelet efficacy with IC50 of 26.1 nM. PAR4 antagonist 3 improves metabolic stablility in human liver microsomes with T1/2 of 97.6 min .
    PAR4 antagonist 3
  • HY-162409

    Protease Activated Receptor (PAR) Others
    PAR4 antagonist 4 (Compound 37) is a selective antagonist for protease activated receptor 4 (PAR4). PAR4 antagonist 3 exhibits antiplatelet efficacy with IC50 of 14.2 nM. PAR4 antagonist 3 improves metabolic stablility in human liver microsomes with T1/2 of 42.5 min .
    PAR4 antagonist 4
  • HY-161523

    Xanthine Oxidase URAT1 Metabolic Disease
    XOR/URAT1-IN-1 (Compound II15) is a dual inhibitor for xanthine oxidoreductase (XOR) and uric acid transporter 1 (URAT1), with IC50 of 6 nM and 12.9 μM. XOR/URAT1-IN-1 lowers the levels of uric acid in Potassium oxonate (HY-17511)/Hypoxanthine (HY-N0091)-induced acute hyperuricemia mouse model .
    XOR/URAT1-IN-1
  • HY-161723

    Dopamine Transporter CDK Neurological Disease
    LH2-051 is a lysosome-enhancing lead compound, which promotes the lysosome biogenesis and the Aβ aggregate clearance through dopamine transporter-cyclin-dependent kinase 9-transcription factor EB (DAT-CDK9-TFEB) pathway. LH2-051 exhibits good pharmacokinetic characteristics in mouse models. LH2-051 is potential for ameliorating Aleheimer’s Disease .
    LH2-051
  • HY-19126

    Platelet-activating Factor Receptor (PAFR) Infection
    CL-184005 is an antagonist for platelet-activating factor (PAF), that inhibits the PAF-induced platelet aggregation with IC50 of 600 nM and 510 nM, in human and rabbit platelet-rich plasma. CL-184005 protects the rats from endotoxin-induced gastrointestinal damage and hypotension. CL-184005 exhibits potential attenuating Gram-negative bacterial sepsis .
    CL-184005
  • HY-120843

    Endothelin Receptor Cardiovascular Disease
    WS009A is an antagonist for endothelin receptor (ET Receptor) with IC50 of 5.8 and 6.9 μM for ET-1 receptor and ET-2 receptor. WS009A can be used in research of cardiovascular diseases .
    WS009A
  • HY-W008151

    Mitochondrial Metabolism Metabolic Disease
    Diphenyl Phosphate inhibits growth and energy metabolism in zebrafish and mice in a sex-specific manner. Diphenyl Phosphate can inhibit the activity of SDH (respiratory complex II), reduce the expression of CPT1 and disrupts the integrity of the mitochondrial membrane. Diphenyl Phosphate may be used in research on metabolic diseases .
    Diphenyl Phosphate
  • HY-162407

    Btk Cancer
    I-As-1 is a potent inhibitor of Bruton’s tyrosine kinase (BTK), with the IC50 of 2.35 nM. I-As-1 shows antiproliferative activities among Ramos cells and OCI-LY10 cells with IC50s of 0.52 μM and 0.11 μM, respectively .
    I-As-1
  • HY-163879

    Monoamine Oxidase Reactive Oxygen Species Ferroptosis Neurological Disease
    hMAO-B-IN-9 (Compound 25c) is a non-competitive inhibitor for monoamine oxidase B (MAO-B) with an IC50 of 1.58 µM (hMAO-B). hMAO-B-IN-9 forms complex with iron ions as a chelator, and inhibits Erastin (HY-15763)-induced ferroptosis. hMAO-B-IN-9 exhibits antioxidant activity by downregulating the level of reactive oxygen species (ROS). hMAO-B-IN-9 improves cognitive function in mice, without significant toxicity (30 mg/kg). hMAO-B-IN-9 is blood-brain barrier permeable, according to the in silico prediction .
    hMAO-B-IN-9
  • HY-162764

    Androgen Receptor Cancer
    Androgen receptor degrader-5 (compound 14k) exhibits promising properties, including superior androgen receptor degradation activity and antiproliferative activity .
    Androgen receptor degrader-5
  • HY-118803

    Factor Xa Others
    AS1468240 is an orally active inhibitor for anticoagulant factor Xa (fXa), that inhibits human fXa with IC50 of 8.7 nM. AS1468240 prolongs the coagulation time in mice .
    AS1468240
  • HY-129246

    DNA/RNA Synthesis Cancer
    Cytembena is inhibitor for replicative DNA synthesis, purine synthesis and tetrahydrofolate formylase activity. Cytembena ameliorates ovarian or breast cancer, relieves the pain from skeletal metastases .
    Cytembena
  • HY-146615

    TAM Receptor Cancer
    Axl-IN-6 (compound 14) is an orally active and potent AXL inhibitor. Axl-IN-6 is well tolerated and significantly inhibits the tumor growth in MV-4-11 subcutaneous xenograft model .
    Axl-IN-6
  • HY-152031

    Amyloid-β Neurological Disease
    Glutaminyl Cyclase Inhibitor 5 (Compound 71) is a potent and selective human glutaminyl cyclase (hQC) inhibitor with an IC50 of 3.2 nM .
    Glutaminyl Cyclase Inhibitor 5
  • HY-W012977

    DMB; Neohexanol

    TGF-beta/Smad NF-κB Endogenous Metabolite Cardiovascular Disease Metabolic Disease Inflammation/Immunology
    3,3-Dimethyl-1-butanol (DMB) is an orally active inhibitor of trimethylamine (TMA) and trimethylamine N-oxide (TMAO). 3,3-Dimethyl-1-butanol inhibits the signaling pathway of p65 NF-κB and TGF-β1/Smad3. 3,3-Dimethyl-1-butanol has potential applications in cardiovascular disease (CVD) .
    3,3-Dimethyl-1-butanol
  • HY-161643

    Cholinesterase (ChE) Keap1-Nrf2 Neurological Disease Inflammation/Immunology
    S21-1011 is a selective inhibitor for butyrylcholinesterase (BChE), with IC50 of 0.059 and 0.162 μM, for eqBChE and hBChE, respectively. S21-1011 exhibits good blood-brain barrier (BBB) permeability and good pharmacokinetic characters. S21-1011 exhibits anti-inflammatory activity through activation of keap1-Nrf2-ARE pathway (EC50 is 23.48 μM for antioxidant element ARE activation), ameliorates cognitive impairment in murine Alzheimer’s disease model .
    S21-1011
  • HY-163505

    Bacterial Others
    Anti-MRSA agent 11 suppresses fluoroquinolone-sensitive strain USA500 and -resistant MRSA isolate Mu50 (MIC =0.39 μg/mL). Anti-MRSA agent 11 displayes favorable in vivo half-life and safety profiles .
    Anti-MRSA agent 11
  • HY-139414
    Lysophosphatidylcholines
    1 Publications Verification

    Interleukin Related p38 MAPK ERK Apoptosis Inflammation/Immunology
    Lysophosphatidylcholines is an orally active lysolipid and a component of oxidized low density lipoprotein (LDL). Lysophosphatidylcholines induces cell injury, the production of IL-1β and apoptosis. Lysophosphatidylcholines has a proactive effect on sepsis .
    Lysophosphatidylcholines
  • HY-146619

    Amyloid-β Serotonin Transporter Neurological Disease
    RAGE/SERT-IN-1 is a potent and orally active advanced glycation end products (RAGE) and serotonin transporter (SERT) inhibitor with IC50s of 8.26 μM and 31.09 nM, respectively. RAGE/SERT-IN-1 exhibits significant neuroprotective effect against Aβ25-35-induced neuronal damage and alleviates depressive behavior of mice. RAGE/SERT-IN-1 can be used for researching the comorbidity of Alzheimer's disease and depression .
    RAGE/SERT-IN-1
  • HY-146883A

    Filovirus Infection
    As-358 (hydrochloride) has inhibitory effects against Ebola virus and Marburg virus with IC50s of 9.1 μM and 18.1 μM, as well as exhibits good in vivo safety .
    As-358 hydrochloride
  • HY-147943

    PROTACs Btk Cancer
    PROTAC BTK Degrader-1 is a potent, selective and orally active PROTAC BTK degrader with an IC50 value of 34.51 nM and 64.56 nM for BTK WT and BTK-481S, respectively. PROTAC BTK Degrader-1 effectively reduces BTK protein levels and suppresses tumor growth . PROTAC BTK Degrader-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    PROTAC BTK Degrader-1
  • HY-126383

    Bacterial Infection Others Inflammation/Immunology Cancer
    Spilanthol is an orally active analgesic, neuroprotective, antioxidant, antimutagenic, anti-cancer, anti-inflammatory, antimicrobial and insecticidal compound.pilanthol can induce cAMP to inhibit negative regulation of urinary concentration mechanism. Spilanthol can be use as diuretic research .
    Spilanthol
  • HY-121152

    α-synuclein Apoptosis GABA Receptor Dopamine Receptor Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Chiisanoside exhibits neuroprotective, anticancer, antidepressant, anti-inflammatory, anti-obesity and anti-platelet activities. Chiisanoside inhibits tumor growth in H22 xenograft mouse model, through immunoregulation, induction of apoptosis and inhibition of angiogenesis. Chiisanoside attenuates Parkinson’s disease through regulation of Parkin/ZNF746/PGC-1α axis, and promotion of mitochondrial biogenesis .
    Chiisanoside
  • HY-161627

    NF-κB Inflammation/Immunology
    Anemoside A3-methyl 6-aminohexanoate (Compound A3-6) is a derivative of Pulchinenoside C (Anemoside B4) (HY-N0205). Anemoside A3-methyl 6-aminohexanoate inhibits pyruvate carboxylase (PC) with an IC50 of 0.058 μM, reprograms macrophage function, and alleviates DSS-induced colitis through inhibition of the NF-κB and NLRP3 inflammasome pathway. Anemoside A3-methyl 6-aminohexanoate exhibits a moderate in vivo pharmacokinetic characters compared with Anemoside B4 .
    Anemoside A3-methyl 6-aminohexanoate
  • HY-126876

    Apoptosis AMPK Reactive Oxygen Species Cancer
    GL-V9 inhibits proliferation of HepG2 cell (IC50 is 35.2 μM) through induction of apoptosis and cell cycle arrest at G2/M phase. GL-V9 regulates mitochondrial membrane potential and increases the production of intracellular reactive oxygen species. GL-V9 inhibits the pentose phosphate pathway (PPP), enhances fatty acid oxidation (FAO) through activation of AMPK, and thus inhibits the metastasis of cancer cells. GL-V9 exhibits antitumor efficacy in mouse model .
    GL-V9
  • HY-P10302A

    GLP Receptor Metabolic Disease
    GLP-1R/GIPR agonist-1 soduim is the sodium salt form of GLP-1R/GIPR agonist-1 (HY-P10302). GLP-1R/GIPR agonist-1 soduim is a dual agonist for glucagon-like peptide-1 receptor (GLP-1R, EC50 is 0.57 nM) and glucose-dependent insulin releasing peptide receptor (GIPR, EC50 is 0.75 nM). GLP-1R/GIPR agonist-1 soduim lowers blood sugar by mimicking the action of endogenous hormones GLP-1 and GIP, enhancing insulin secretion while inhibiting glucagon secretion. GLP-1R/GIPR agonist-1 soduim can be used in the study of metabolic diseases such as diabetes, obesity, and non-alcoholic steatohepatitis (NASH) .
    GLP-1R/GIPR agonist-1 (soduim)
  • HY-14849

    Razupenem; SM 216601; SMP 601

    Antibiotic Bacterial Others
    PTZ601 (SMP 601) is an antibiotic, which inhibits the gram-positive bacteria, including the Vancomycin (HY-B0671)-resistant Enterococcus faecium (VREF) and Methicillin (HY-121544)-resistant Staphylococcus aureus (MRSA). PTZ601 exhibits antimicrobial activity in infected mouse models .
    PTZ601
  • HY-159088

    Opioid Receptor Neurological Disease
    KOR agonist 2 (Compound 23p) is an agonist for κ opioid receptor (KOR) with Ki of 1.9 nM. KOR agonist 2 exhibits analgesic effect in mouse models with ED50 of 1.30 mg/kg. KOR agonist 2 exhibits high clearance rate (2 mg/kg, i.v.) in mice, high metabolism and clearance in liver microsomes .
    KOR agonist 2
  • HY-143586

    CDK Cancer
    CDK7-IN-8 is a potent CDK7 inhibitor with IC50 of 54.29 nM. CDK7-IN-8 has inhibitory effect on certain cancer cells and in vivo tumor models .
    CDK7-IN-8
  • HY-146468

    Dipeptidyl Peptidase GPR119 Potassium Channel Metabolic Disease
    DPP-4/GPR119 modulator 1 (Compound 22) is an orally active dipeptidyl peptidase IV (DPP-IV) inhibitor and GPR119 agonist. DPP-4/GPR119 modulator 1 shows blood glucose-lowering effect and moderate inhibition on hERG channel with an IC50 of 4.9 μM. DPP-4/GPR119 modulator 1 can be used for diabetes research . DPP-4/GPR119 modulator 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    DPP-4/GPR119 modulator 1
  • HY-162633

    Deubiquitinase Cancer
    USP1-IN-9 (Compound 1m) is reversible and noncompetitive ubiquitin-specific proteases (USP1) inhibitors with an IC50 of 8.8 nM, which is designed and synthesized to pyrido[2,3-d]pyrimidin-7(8H)-one derivative based on the disclosed structure of ML323(HY-17543) and KSQ-4279(HY-145471). USP1-IN-9 displays excellent USP1/UAF inhibition and exhibits strong antiproliferation effect in breast cancer cells. USP1-IN-9 can generate enhanced cell killing with PARP inhibitor olaparib(HY-10162) in olaparib-resistant MDA-MB-436/OP cells, which is promising for research in the field of cancer .
    USP1-IN-9
  • HY-148013

    Beta-secretase NF-κB Neurological Disease
    K284-6111 is an orally active inhibitor for protein chitinase 3-like 1 (CHI3L1). K284-6111 reduces the expression of inflammatory proteins such as iNOS, COX-2, GFAP, and Iba-1, inhibits β-secretase and NF-κB, and suppresses Aβ production. K284-6111 ameliorates the Aβ1–42-induced mice memory impairment, and can be used in research about Alzheimer’s Diseases .
    K284-6111
  • HY-161893

    Bacterial Infection
    Anti-MRSA agent 15 (Compound 9o10) exhibits antibacterial activity, that inhibits methicillin-resistant Staphylococcus aureus (MRSA) with a MIC of 0.0625 μg/mL. Anti-MRSA agent 15 exhibits low hemolysis and low cytotoxicity. Anti-MRSA agent 15 exhibits anti-infective in mice .
    Anti-MRSA agent 15
  • HY-164384

    PI3K Akt mTOR Apoptosis Cancer
    DFX117 is a selective, orally active inhibitor for PI3Kα and c-Met tyrosine kinase. DFX117 inhibits PI3K/Akt/mTOR pathway, inhibits the proliferation of NCI-H1975, NCI-H1993, and HCC827 with IC50s 0.02-0.08 µM. DFX117 arrests cell cycle at G0/G1 phase, induces apoptosis in A549 and NCI-H1975. DFX117 exhibits antitumor efficacy in mice .
    DFX117
  • HY-163345

    5-HT Receptor Neurological Disease
    5-HT7R antagonist 2 (compound 4h) is a 5-HT7R antagonist that antagonizes the G protein and β-arrestin signaling pathways, with a Ki of 67 nM, the IC50 values in cAMP and Tango tests were 2.59 μM and 39.57 μM, respectively. 5-HT7R antagonist 2 has an effect on neurogenesis and can reduce repetitive behaviors related to autism spectrum disorder (ASD) and restore neurogenesis of ASD impairment .
    Pharmacokinetic Analysis ICR Male Mice

    药代动力学分析
    Plasma Intravenous Administration Intraperitoneal Administration
    Tmax (h) 0.08 0.25
    T1/2 (h) 0.77 1.06
    Cmax (ng/mL) 33.07 156.44
    AUClast (ng·h/mL) 28.31 143.27
    CL (L/h/kg) 41.61 -
    Vss (L/kg) 32.43 -
    MRT (h) 0.79 0.93
    F (%) 50.60
    5-HT7R antagonist 2
  • HY-Y0946

    Biochemical Assay Reagents Inflammation/Immunology Cancer
    Acetamide is used as an intermediate in the synthesis of methylamine, thioacetamide, and insecticides, and as a plasticizer in leather, cloth and coatings. Acetamide has carcinogenicity. Acetamide derivatives may has antioxidant activity and potential anti-inflammatory activity. Acetamide holds promise for research in the fields of anti-inflammatory and cancer studies .
    Acetamide
  • HY-115996

    Others Cancer
    Antitumor agent-51 possesses potent and selective inhibitory for osteosarcoma cell growth and migration with IC50 of 21.9 nM in MNNG/HOS cells. Antitumor agent-51 has a considerable bioavailability and a low toxicity .
    Antitumor agent-51
  • HY-145845

    HDAC Monoamine Oxidase Neurological Disease
    HDAC1/MAO-B-IN-1 is a potent, selective and cross the blood-brain barrier HDAC1/MAO-B inhibitor with IC50 values of 21.4 nM and 99.0 nM for HDAC1 and MAO-B, respectively. HDAC1/MAO-B-IN-1 has the potential for the research of Alzheimer’s disease .
    HDAC1/MAO-B-IN-1
  • HY-158113

    Histone Acetyltransferase PROTACs Cancer
    CBPD-409 is an orally active PROTAC degrader for CBP/p300, with DC50 of 0.2–0.4 nM. CBPD-409 exhibits antiproliferative effects in AR+ prostate cancer cell lines VCaP, LNCaP and 22Rv1, with IC50s of 1.2–2.0 nM. CBPD-409 exhibits antitumor efficacy (Red: CBP inhibitor GNE049 (HY-108435); Blue: CRBN/cullin 4A Thalidomide (HY-14658); Black: Linker) .
    CBPD-409
  • HY-163923

    Apoptosis Cancer
    Apoptosis inducer 24 (Compound 4) inhibits the proliferation of gastric cancer cells with IC50 of 1.2-4.8 μM. Apoptosis inducer 24 arrests cell cycle at G2/M phase, induces apoptosis in cell BGC-823, and causes mitochondrial dysfunction. Apoptosis inducer 24 exhibits antitumor efficacy in mice, without significant toxicity (LD50 is 91.2 mg/kg) .
    Apoptosis inducer 24
  • HY-Y0946R

    Biochemical Assay Reagents Inflammation/Immunology Cancer
    Acetamide (Standard) is the analytical standard of Acetamide. This product is intended for research and analytical applications. Acetamide is used as an intermediate in the synthesis of methylamine, thioacetamide, and insecticides, and as a plasticizer in leather, cloth and coatings. Acetamide has carcinogenicity. Acetamide derivatives may has antioxidant activity and potential anti-inflammatory activity. Acetamide holds promise for research in the fields of anti-inflammatory and cancer studies .
    Acetamide (Standard)
  • HY-146715

    Microtubule/Tubulin Apoptosis Cancer
    IDO/Tubulin-IN-2 (HT2) is a potent TDO and tubulin inhibitor. IDO/Tubulin-IN-2 also shows potent activity against U87, HepG2, A549, HCT-116, and LO2 cancer cell lines, with IC50 values of 0.43, 0.036, 0.041, 0.095 and 1.04 μM, respectively. IDO/Tubulin-IN-2 remarkably promotes the antitumor activity .
    IDO/Tubulin-IN-2

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