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LO2

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42

Inhibitors & Agonists

2

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3

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GMP Molecules

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-107632
    GYY4137
    Maximum Cited Publications
    8 Publications Verification

    		 Apoptosis STAT NF-κB NO Synthase COX TNF Receptor Interleukin Related Cardiovascular Disease Neurological Disease Inflammation/Immunology Cancer
    GY4137 is a sustained-release H2S donor possessing vasodilatory, antihypertensive, and anti-inflammatory activities. GY4137 can inhibit cell growth, induce apoptosis, and cause cell cycle arrest by blocking the STAT3 pathway, demonstrating potent anticancer activity [2] .
    GYY4137
  • HY-P3211A
    Nangibotide TFA
    5+ Cited Publications

    LR12 TFA

    		 TREM receptor NF-κB NOD-like Receptor (NLR) Interleukin Related Apoptosis Cardiovascular Disease Inflammation/Immunology
    Nangibotide TFA (LR12 TFA) is a synthetic peptide and TREM-1 receptor inhibitor. Nangibotide TFA inhibits NF-κB and NLRP3 inflammasome activation and reduces the release of pro-inflammatory factors (such as IL-1β, IL-8). Nangibotide TFA inhibits Apoptosis. Nangibotide TFA reduces excessive inflammatory responses and protects tissues (liver, lung) from damage. Nangibotide TFA can be used in the researches for myocardial ischemia-reperfusion injury, septic shock, acute lung injury, osteoarthritis, and acute liver failure [2] .
    Nangibotide TFA
  • HY-P11099
    Cys-LT7

    		Transferrin Receptor Neurological Disease Cancer
    Cys-LT7 is a transferrin receptor (TfR)-targeting peptide ligand. Cys-LT7 binds to a TfR site distinct from endogenous transferrin, mediates conjugated Doxorubicin (HY-15142A) delivery to TfR-overexpressed tumor cells, and exhibits low toxicity to TfR-low-expressed normal cells. Cys-LT7 is an L-configuration peptide susceptible to proteolytic enzymes, leading to poor biostability in peptide-drug conjugates. Cys-LT7 can be used for the research of glioblastoma, hepatocellular carcinoma, lung carcinoma .
    Cys-LT7
  • HY-13495
    ML281
    2 Publications Verification

    		 STK33 PKA Aurora Kinase Bcl-2 Family Apoptosis Metabolic Disease Cancer
    ML281 is a highly selective inhibitor of serine/threonine kinase 33 (STK33) with an IC50 value of 14 nM. ML281 shows 700-fold selectivity over PKA and 550-fold over AurB. ML281 exerts core mechanism by inhibiting STK33: in small cell lung cancer, ML281 downregulates RPS6/BAD signaling phosphorylation, induces apoptosis, and suppresses proliferation, invasion . ML281 reduces STK33-mediated 4-hydroxyphenylpyruvate dioxygenase (HPD) phosphorylation in tyrosinemia . ML281 is suitable for research on STK33 function, KRAS mutation-related cancers (pancreatic cancer, colon cancer, lung adenocarcinoma, etc.), small cell lung cancer, and tyrosinemia-related damage [2]
    ML281
  • HY-18555
    TMPA
    3 Publications Verification

    		 Nuclear Hormone Receptor 4A/NR4A AMPK Metabolic Disease Inflammation/Immunology Cancer
    TMPA is a high-affinity Nur77 antagonist that binds to Nur77 leading to the release and shuttling of LKB1 in the cytoplasm to activate AMPKα. TMPA effectively lowers blood glucose and attenuates insulin resistance in type II db/db, high-fat diet and streptozotocin-induced diabetic mice. TMPA reduces RICD (restimulation-induced cell death) in human T cells, can also be used in studies of cancer and T-cell apoptosis dysregulation [2].
    TMPA
  • HY-161321
    PTP1B-IN-24

    		Phosphatase Insulin Receptor Akt Metabolic Disease
    PTP1B-IN-24 (Compound 9) is a reversible PTP1B inhibitor with an IC50 value of 1.4 μM, and PTP1B-IN-24 can enhance the thermal stability of PTP1B. PTP1B-IN-24 can restore PA- (HY-N0830) induced insulin resistance by increasing the phosphorylation levels of IRS1 and AKT .
    PTP1B-IN-24
  • HY-130713
    Thalidomide-C2-amido-C2-COOH

    		E3 Ligase Ligand-Linker Conjugates Cancer
    Thalidomide-C2-amido-C2-COOH contains a CRBN ligand and a linker for recruiting E3 ubiquitin ligases. Thalidomide-C2-amido-C2-COOH can be used to design and synthesize PROTAC CDK2/9 Degrader-1 (HY-130709). PROTAC CDK2/9 Degrader-1 is applicable to prostate cancer-related research .
    Thalidomide-C2-amido-C2-COOH
  • HY-146350
    TrxR-IN-4

    		TrxR Reactive Oxygen Species (ROS) Apoptosis Cancer
    TrxR-IN-4 is a thioredoxin reductase (TrxR) inhibitor with a rat IC50 of 0.37 μM. TrxR-IN-4 inhibits TrxR activity, elevates reactive oxygen species (ROS) and induces apoptosis. TrxR-IN-4 mediates endoplasmic reticulum stress and induces mitochondrial dysfunction. TrxR-IN-4 can be used for the research of hepatocellular carcinoma .
    TrxR-IN-4
  • HY-N10426
    (+)-Cembrene A

    		Glycosidase Metabolic Disease
    (+)-Cembrene A (Compound 5) is a α-glucosidase inhibitor with an IC50 of 30.31 μM. (+)-Cembrene A is nontoxic towards human normal hepatocyte (LO2) cells .
    (+)-Cembrene A
  • HY-175033
    BRD4-IN-11

    		Epigenetic Reader Domain Phosphatase c-Myc Apoptosis Inflammation/Immunology
    BRD4-IN-11 is an orally active and selective BRD4 inhibitor (IC50 = 26.35 nM (BD1), IC50 = 72.81 nM (BD2)). BRD4-IN-11 is approximately 3- to 18-fold more potent against BRD4 than againstBRD2, BRD3, and BRDT. BRD4-IN-11 enhances H2S release and inhibits the upregulation of fibrotic markers (α-SMA and fibronectin), c-Myc, and CDC25B. BRD4-IN-11 reduces apoptosis in LO2 hepatocytes. BRD4-IN-11 significantly improves liver and lung function in a hepatopulmonary fibrosis model and can be used to study hepatopulmonary fibrosis .
    BRD4-IN-11
  • HY-176274
    FASN/SCD-IN-1

    		Fatty Acid Synthase (FASN) Stearoyl-CoA Desaturase (SCD) Reactive Oxygen Species (ROS) Interleukin Related TNF Receptor SOD LDLR Glutathione Peroxidase Metabolic Disease Inflammation/Immunology
    FASN/SCD-IN-1 is a Silybin (HY-N0779A) derivative, an orally active inhibitor of Fatty Acid Synthase (FASN)/Stearoyl-CoA Desaturase (SCD). FASN/SCD-IN-1 has shown in vitro activity in inhibiting lipid deposition, reducing FASN and SCD transcriptional levels, and exhibiting antioxidant, anti-inflammatory, and anti-fibrotic activities. FASN/SCD-IN-1 has demonstrated significant hepatoprotective effects in a rat model of acute liver injury. FASN/SCD-IN-1 ameliorates the pathological features of MASH liver, including steatosis, inflammation, and fibrosis in a mouse model of myeloproliferative steatohepatitis (MASH). FASN/SCD-IN-1 can be used to study MASH .
    FASN/SCD-IN-1
  • HY-162564
    Antibacterial agent 221

    		Bacterial Infection
    Antibacterial agent 221 (compound 3k) is a potent inhibitor of Gram-positive Methicillin-resistant Staphylococcus aureus (MRSA). Antibacterial agent 221 shows significant cytotoxicity against human LO2 and HepG2 cells .
    Antibacterial agent 221
  • HY-N7161
    3-O-(2'E,4'E-Decadienoyl)-ingenol

    		Others Others
    3-O-(2'E,4'E-Decadienoyl)-ingenol is a natural diterpenoid that shows cytotoxicity against human normal cell lines L-O2 and GES-1, with IC50s of 8.22 μM and 6.67 μM, respectively .
    3-O-(2'E,4'E-Decadienoyl)-ingenol
  • HY-146715
    IDO/Tubulin-IN-2

    		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
  • HY-170606
    α-Glucosidase-IN-79

    		Glycosidase Metabolic Disease
    α-Glucosidase-IN-79 (Compound 4d9) is a non-competitive α-Glucosidase inhibitor with an IC50 of 2.11 μM, which is more potent than existing α-Glucosidase inhibitors such as Acarbose (HY-B0089) (IC50 of 327.0 μM) and HXH8r (IC50 of 15.32 μM). α-Glucosidase-IN-79 is non-cytotoxic to human normal hepatocyte (LO2) cells and shows good metabolic stability in rat plasma. α-Glucosidase-IN-79 holds promise for research into type 2 diabetes .
    α-Glucosidase-IN-79
  • HY-162429
    Antibacterial agent 205

    		Bacterial Infection
    Antibacterial agent 205 (Compound 10d) is a indolylacryloyl-derived oxacins, which exhibits broad antibacterial spectrum with MIC of 0.25-0.5 μg/mL. Antibacterial agent 205 reduces the exopolysaccharide, eliminates the biofilm, and thus attenuates the drug resistance. Antibacterial agent 205 exhibits antibacterial activity through destory of membrane integrity, accumulation of reactive oxygen species ROS, and inhibition of DNA replication .
    Antibacterial agent 205
  • HY-162430
    Antibacterial agent 206

    		Bacterial Infection
    Antibacterial agent 206 (Compound 10e) is a indolylacryloyl-derived oxacins, which exhibits broad antibacterial spectrum with MIC of 0.25-1 μg/mL. Antibacterial agent 206 reduces the exopolysaccharide, eliminates the biofilm, and thus attenuates the drug resistance. Antibacterial agent 206 exhibits antibacterial activity through destory of membrane integrity, accumulation of reactive oxygen species ROS, and inhibition of DNA replication .
    Antibacterial agent 206
  • HY-146114
    Antitumor agent-67

    		Microtubule/Tubulin Quinone Reductase Cancer
    Antitumor agent-67 (compound 3) is a potent antitumor agent. Antitumor agent-67 has highly selective toxicity to cancer cells and lower damage to normal cells. Antitumor agent-67 can be activated by NQO1 and effectively liberate podophyllotoxin and kill tumor cells. Antitumor agent-67 significantly suppresses cancer growth in HepG2 xenograft models without obvious toxicity .
    Antitumor agent-67
  • HY-147698
    ZLHQ-5f

    		CDK Topoisomerase Apoptosis Cancer
    ZLHQ-5f is a dual CDK2 and Topo I inhibitor with an IC50 of 0.145 μM against CDK2/CycA2. ZLHQ-5f arrests the cell cycle in S-phase, triggers apoptosis in HCT116 cells, and has a good safety profile .
    ZLHQ-5f
  • HY-175047
    Enpp-1-IN-26

    		Phosphodiesterase (PDE) Cancer
    Enpp-1-IN-26 (Compound 4e) is an ENPP1 inhibitor with an IC50 of 0.188 μM. Enpp-1-IN-26 enhances IFN-β expression in vivo by preventing ENPP1 from hydrolyzing cGAMP. Enpp-1-IN-26 can be used in the research of metastatic breast cancer .
    Enpp-1-IN-26
  • HY-172225
    [Ru(phen)2(HMPIP)](PF6)2

    		Apoptosis Autophagy Ferroptosis Cancer
    [Ru(phen)2(HMPIP)](PF6)2 (Compound 6A) is an anti-tumor agent. [Ru(phen)2(HMPIP)](PF6)2 can inhibit the proliferation and migration of HepG2 liver cancer cells, and induce apoptosis, autophagy, cell cycle arrest and ferroptosis of HepG2 liver cancer cells. [Ru(phen)2(HMPIP)](PF6)2 exerts its anti-tumor activity by stimulating immune response to increase CD8+ T cells .
    [Ru(phen)2(HMPIP)](PF6)2
  • HY-161281
    α-Glucosidase-IN-49

    		Glycosidase Metabolic Disease
    α-Glucosidase-IN-49 (compound C23) is a potent inhibitor of α-Glucosidase, with IC50 of 0.52 μM. α-Glucosidase-IN-49 has oral bioactivity that can reduce blood glucose and improve glucose tolerance in mice .
    α-Glucosidase-IN-49
  • HY-161283
    JT21-25

    		MAP3K Others
    JT21-25 (compound 9h) is a potent and selective inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with IC50 of 5.1 nM .
    JT21-25
  • HY-176149
    Fluoxetine-Conjugated Platinum(IV) prodrug-1

    		CaMK MMP AMPK Apoptosis Autophagy Cancer
    Fluoxetine-Conjugated Platinum(IV) prodrug-1 (Compound 8) is an eEF2K inhibitor. Fluoxetine-Conjugated Platinum(IV) prodrug-1 inhibits cancer cell proliferation, induces DNA damage, cell cycle arrest at S phase and apoptosis. Fluoxetine-Conjugated Platinum(IV) prodrug-1 induces ROS accumulation and mitochondrial dysfunction. Fluoxetine-Conjugated Platinum(IV) prodrug-1 inhibits TNBC cell migration and invasion by inhibiting MMP-2 activity. Fluoxetine-Conjugated Platinum(IV) prodrug-1 induces autophagy in TNBC cells by activating AMPK. Fluoxetine-Conjugated Platinum(IV) prodrug-1 has antitumor activity and activates immunosuppression in the 4T1-Luc mouse model. Fluoxetine-Conjugated Platinum(IV) prodrug-1 can be used in triple-negative breast cancer (TNBC) research .
    Fluoxetine-Conjugated Platinum(IV) prodrug-1
  • HY-107632G
    GYY4137

    		Apoptosis STAT NF-κB TNF Receptor NO Synthase Interleukin Related COX Cardiovascular Disease Neurological Disease Inflammation/Immunology Cancer
    GYY4137 (GMP) is the GMP-grade version of GYY4137 (HY-107632). Small molecules of GMP grade can be used as adjuvant reagents in cell therapy. GYY4137 (GMP) is a sustained-release H2S donor possessing vasodilatory, antihypertensive, and anti-inflammatory activities. GYY4137 (GMP) can inhibit cell growth, induce apoptosis, and cause cell cycle arrest by blocking the STAT3 pathway, demonstrating potent anticancer activity [2] .
    GYY4137
  • HY-149844
    S-F24

    		Fungal Infection
    S-F24 is an antifungal agent with excellent broad-spectrum. S-F24 inhibits CYP3A4 with an IC50 value of 0.4 μM. S-F24 displays a good safety profile with high selectivity, low hemolytic effects, and low tendency to induce resistance. S-F24 can be used for research on fungal infections .
    S-F24
  • HY-146347
    MAO-B-IN-10

    		Monoamine Oxidase Amyloid-β Neurological Disease
    MAO-B-IN-10 (compound 4f) is a potent, selective, BBB-penetrated MAO-B (monoamine oxidase-B) inhibitor, with IC50 of 5.3 μM. MAO-B-IN-10 can inhibit (58.2%) and disaggregate (43.3%) self-mediated Aβ (amyloid β) aggregation. MAO-B-IN-10 can be use for Alzheimer’s disease research .
    MAO-B-IN-10
  • HY-173130
    α-Glucosidase-IN-86

    		Glycosidase Metabolic Disease Inflammation/Immunology
    α-Glucosidase-IN-86 (Compound A4) is an orally active α-glucosidase inhibitor with an IC50 of 2.72 μM. α-Glucosidase-IN-86 has high safety in mice. α-Glucosidase-IN-86 can reduce fasting blood glucose levels, improve glucose tolerance, regulate blood lipids, and has antioxidant effects in diabetic mice. α-Glucosidase-IN-86 can be used for the research of diabetes .
    α-Glucosidase-IN-86
  • HY-179613
    D-Leucine amide-CDDO-Me-HMP

    		Drug Intermediate Reactive Oxygen Species (ROS) Apoptosis Keap1-Nrf2 Heme Oxygenase (HO) Bcl-2 Family Caspase Metabolic Disease
    D-Leucine amide-CDDO-Me-HMP is a prodrug composed of CDDO-Me (HY-13324) and ligustrazine (HY-N0264). D-Leucine amide-CDDO-Me-HMP can protect against CCl4-induced liver injury. D-Leucine amide-CDDO-Me-HMP can inhibit ROS production, alleviates mitochondrial damage and inhibits cell apoptosis. D-Leucine amide-CDDO-Me-HMP can be used for the research of liver injury .
    D-Leucine amide-CDDO-Me-HMP
  • HY-179517
    ASK1-IN-12

    		ASK1 JNK p38 MAPK Metabolic Disease Inflammation/Immunology
    ASK1-IN-12 is an ASK1 inhibitor with an IC50 of 6.3 nM. ASK1-IN-12 inhibits TNF-α-induced activation of the ASK1-p38/JNK pathway. ASK1-IN-12 can reduce free fatty acid-induced cholesterol increase, lipid droplet accumulation and improves hepatocellular steatosis. ASK1-IN-12 can be used for the research of non-alcoholic steatohepatitis (NASH) .
    ASK1-IN-12
  • HY-P11592
    KIKIKPWWWPKIKIK-NH2

    		Bacterial Infection
    KIKIKPWWWPKIKIK-NH2 is a β-turn antimicrobial peptide. KIKIKPWWWPKIKIK-NH2 can inhibit bacterial biofilm formation and bind to lipopolysaccharid. KIKIKPWWWPKIKIK-NH2 shows wound-healing ability in mice bacteria-infected full-thickness wound models. KIKIKPWWWPKIKIK-NH2 can be used for the research of bacterial infection .
    KIKIKPWWWPKIKIK-NH2
  • HY-107632R
    GYY4137 (Standard)

    		Reference Standards Apoptosis STAT NF-κB NO Synthase COX TNF Receptor Interleukin Related Cardiovascular Disease Neurological Disease Inflammation/Immunology Cancer
    GYY4137 (Standard) is the analytical standard of GYY4137 (HY-107632). This product is intended for research and analytical applications. GY4137 is a sustained-release H2S donor possessing vasodilatory, antihypertensive, and anti-inflammatory activities. GY4137 can inhibit cell growth, induce apoptosis, and cause cell cycle arrest by blocKing the STAT3 pathway, demonstrating potent anticancer activity [2] .
    GYY4137 (Standard)
  • HY-D3215
    Lyso-Cu(II)

    		Fluorescent Dye Neurological Disease
    Lyso-Cu (II) is a lysosome-targeted divalent copper ion probe. Lyso-Cu (II) is applicable to the research of Wilson's disease, Menkes disease and Alzheimer's disease .
    Lyso-Cu(II)
  • HY-D3167
    HDAC-IN-101

    		Fluorescent Dye HDAC Cancer
    HDAC-IN-101 (compound H6M) is a HDAC1 inhibitor and NTR/pH-activated fluorescent inducer, with an IC50 of 65 nM against human HDAC1. HDAC-IN-101 blocks cancer cell proliferation by inhibiting HDAC1. HDAC-IN-101 is reduced by overexpressed nitroreductase to generate H6AQ, a product that emits fluorescence under low pH conditions. HDAC-IN-101 is applicable for cancer-related research .
    HDAC-IN-101
  • HY-181997
    LDLRAP1-IN-1

    		LDLR SARS-CoV Infection
    LDLRAP1-IN-1 (Compound B19) is a LDLRAP1 inhibitor and antiviral agent, with an IC50 of 4.98 μM for disrupting the interaction between LDLRAP1 and LDLR. LDLRAP1-IN-1 covalently modifies the C119 residue of LDLRAP1 at the LDLRAP1-LDLR binding interface, thereby disrupting the interaction between LDLRAP1 and LDLR. LDLRAP1-IN-1 exhibits antiviral activity against HCoV-OC43 .
    LDLRAP1-IN-1
  • HY-183291
    Antibacterial agent 343

    		Bacterial DNA/RNA Synthesis DNA Alkylator/Crosslinker Reactive Oxygen Species (ROS) Penicillin-binding protein (PBP) Infection
    Antibacterial agent 343 (Compound 47) is an Antibacterial agent. Antibacterial agent 343 binds to the allosteric site of PBP2a to open its active site. Antibacterial agent 343 disrupts bacterial cell membranes, leading to protein leakage. Antibacterial agent 343 interacts with DNA and inhibits replication and transcription. Antibacterial agent 343 induces ROS accumulation. Antibacterial agent 343 exhibits antibacterial activity against MRSA, Staphylococcus aureus, and Enterococcus faecalis. Antibacterial agent 343 can be used for the research of methicillin-resistant Staphylococcus aureus infections .
    Antibacterial agent 343
  • HY-181677
    Antibacterial agent 325

    		Bacterial Reactive Oxygen Species (ROS) Lactate Dehydrogenase Infection
    Antibacterial agent 325 is an antibacterial agent. Antibacterial agent 325 exerts potent broad-spectrum antibacterial activity and shows bactericidal activity. Antibacterial agent induces membrane depolarization, disrupts the membrane integrity, increasess ROS production and lipid peroxidation levels. Antibacterial agent 325 inhibits the metabolic activity and Lactate Dehydrogenase (LDH) activity. Antibacterial agent 325 exhibits low drug resistance development in bacteria, low hemolysis and cytotoxicity. Antibacterial agent 325 can be used for the research of bacterial infection .
    Antibacterial agent 325
  • HY-181082
    Aurora kinase-IN-10

    		Aurora Kinase Cancer
    Aurora kinase-IN-10 is an Aurora kinase inhibitor. Aurora kinase-IN-10 exhibits IC50 values of 5.94 nM and 86.06 nM against Aurora A and Aurora B, respectively. Aurora kinase-IN-10 has anti-tumor activity and can be used in the research of tumors such as triple-negative breast cancer .
    Aurora kinase-IN-10
  • HY-181101
    Antifungal agent 151

    		Fungal Infection
    Antifungal agent 151 is a Prp8 intein inhibitor that inhibits the self-splicing process of the Prp8 intein, preventing maturation of the Prp8 protein. Antifungal agent 151 exerts in vitro antifungal activity against Cryptococcus neoformans and Cryptococcus gattii. Antifungal agent 151 can be used for the research of cryptococcus pneumonia .
    Antifungal agent 151
  • HY-181088
    PDE3/4-IN-4

    		Phosphodiesterase (PDE) Interleukin Related Metabolic Disease
    PDE3/4-IN-4 is an orally active PDE3A and PDE4B inhibitor with IC50 values of 10 nM and 9.4 nM, respectively. PDE3/4-IN-4 shows selective activity relative to most other PDE family members. PDE3/4-IN-4 modulates the cAMP/PKA/CREB signaling pathway. PDE3/4-IN-4 inhibits pro-inflammatory factor IL-6. PDE3/4-IN-4 reduces expression of inflammatory markers in liver tissue. PDE3/4-IN-4 attenuates liver fibrosis. PDE3/4-IN-4 limits liver damage in cholestatic and sepsis-induced liver disease mice models. PDE3/4-IN-4 can be used for the research of liver injury, cholestatic liver diseases, sepsis-induced liver injury .
    PDE3/4-IN-4
  • HY-182346
    FBPase-IN-7

    		FBPase Metabolic Disease
    FBPase-IN-7 is a fructose-1,6-bisphosphatase (FBPase) inhibitor with an IC50 of 0.75 μM. FBPase-IN-7 binds to a cryptic allosteric pocket of FBPase, induces conformational rearrangement of key residues, forms a hydrogen-bond network, and disrupts substrate catalysis. FBPase-IN-7 confirms cellular stabilizes HuFBPase in hepatic cells. FBPase-IN-7 has hypoglycemic activity. FBPase-IN-7 can be used for the research of type 2 diabetes .
    FBPase-IN-7
  • HY-181671
    Antibacterial agent 324

    		Bacterial Infection
    Antibacterial agent 324 is an amphipathic antibacterial agent. Antibacterial agent 324 exhibits selective activity against Gram-positive bacteria, with limited activity against enterococci and weak activity against Gram-negative bacteria .
    Antibacterial agent 324

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