Search Result
Results for "
Murine Inhibitors
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-106382
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HIV
CMV
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Infection
Cancer
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PMEDAP is a potent inhibitor of human immunodeficiency virus (HIV) replication. PMEDAP has anti-murine cytomegalovirus (MCMV) activity. PMEDAP is a very potent inhibitor of Moloney murine sarcoma virus (MSV)-induced tumor formation and associated mortality .
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-
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- HY-132869
-
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HOXA
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Others
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MEIS-IN-1 is a potent myeloid ecotropic viral integration site (MEIS) inhibitor to induce murine and human hematopoietic stem-cell expansion.
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-
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- HY-173472
-
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Bacterial
Beta-lactamase
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Infection
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MBL-IN-5 is a metallo-β-lactamase (MBL) inhibitor. MBL-IN-5 inhibits three clinically relevant B1 subfamily MBLs (NDM-1, VIM-1, and IMP-1) with IC50s of 0.05 nM, 14 nM and 21 nM respectively. MBL-IN-5 remarkably enhances carbapenems’ effectiveness against MBL-producing clinical strains and significantly reduces the bacterial load in a neutropenic murine thigh infection model combined with the IPM antibiotic .
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-
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- HY-120944
-
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MMP
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Inflammation/Immunology
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BAY-7598 is a potent, orally bioavailable, and selective MMP12 inhibitor with IC50s of 0.085, 0.67 and 1.1 nM for human MMP12, murine MMP12, and rat MMP12, respectively .
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-
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- HY-155288
-
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Bcr-Abl
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Cancer
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DosatiLink-1 is an Abelson murine leukemia (ABL) enzyme inhibitor .
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-
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- HY-155289
-
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Bcr-Abl
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Cancer
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DosatiLink-2 is an Abelson murine leukemia (ABL) enzyme inhibitor .
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-
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- HY-155290
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Bcr-Abl
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Cancer
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PonatiLink-1-24 is an Abelson murine leukemia (ABL) enzyme inhibitor .
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-
-
- HY-111749
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-
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- HY-12458
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DNA/RNA Synthesis
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Infection
Cancer
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Pyrindamycin A is an antibiotic that inhibits DNA synthesis. Pyrindamycin A shows antitumor activities against murine leukemia, exhibits stronger cytotoxic activities towards murine and human tumor cell lines and especially towards doxorubicin-resistant cells, inhibits P388 and P388/ADR cells with the same IC50 of 3.9 μg/ml .
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-
-
- HY-122357
-
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Adenylate Cyclase
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Inflammation/Immunology
|
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Bestim is a dipeptide, which exhibits high affinity to murine peritoneal macrophages, thymocytes, and plasma membranes isolated from these cells, with Kds of 3.1, 2.1, 18.6 and 16.7 nM, respectively. Bestim inhibits adenylate cyclase in the membranes of murine macrophages and thymocytes. Bestim exhibits immunomodulatory efficacy .
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-
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- HY-13535
-
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Integrin
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Cancer
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ATN-161 is a novel integrin α5β1 antagonist, which inhibits angiogenesis and growth of liver metastases in a murine model.
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-
-
- HY-N14697
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Antibiotic
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Cancer
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Cytorhodin X is a cytotoxic antibiotic. Cytorhodin X can inhibit the proliferation of L1210 murine leukemia cells, with an ED50 of 0.36 μM .
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-
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- HY-120060
-
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Parasite
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Infection
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GNF6702 is a selective inhibitor of the kinetoplastid proteasome. GNF6702 clears parasites in murine models of leishmaniasis, Chagas disease, and human African trypanosomiasis .
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-
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- HY-13535A
-
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ATN-161 TFA salt
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Integrin
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Cancer
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ATN-161 trifluoroacetate salt is a novel integrin α5β1 antagonist, which inhibits angiogenesis and growth of liver metastases in a murine model.
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-
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- HY-168539
-
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HuR
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Inflammation/Immunology
|
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TM11, a Tanshinone mimic, is a potent HuR inhibitor that can inhibit HuR-RNA complex formation. TM11 reduces LPS-induced inflammatory response in murine macrophages .
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-
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- HY-103028A
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GSK963
1 Publications Verification
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RIP kinase
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Others
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GSK963 is a chiral, highly potent and selective inhibitor of RIP1 kinase, with an IC50 of 29 nM. GSK963 is a selective and potent inhibitor of necroptosis in murine and human cells in vitro .
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- HY-120494
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Epoxide Hydrolase
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Inflammation/Immunology
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sEH inhibitor-1 (compound TCPU ) is a potent and oral active inhibitor of sEH (soluble epoxide hydrolase) with IC50s of 0.4 and 5.3 nM in human and murine, respectively .
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- HY-P99294
-
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AMG 479; Human Anti-IGF1R Recombinant Antibody
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IGF-1R
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Cancer
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Ganitumab (AMG 479) is a recombinant human monoclonal antibody to the human type 1 insulin-like growth factor receptor (IGF1R). Ganitumab recognizes murine IGF1R with sub-nanomolar affinity (KD=0.22 nM) and inhibits the interaction of murine IGF1R with IGF1 and IGF2. Ganitumab can be used in research of cancer .
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- HY-100791
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Others
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Cancer
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NSC23005 sodium is a novel and effective p18 inhibitor (ED50=5.21 nM) in promoting Hematopoietic stem cells (HSCs) expansion in both murine and human models.
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-
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- HY-N10445
-
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CD28
CD3
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Inflammation/Immunology
|
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Maydispenoid A is a potent immunosuppressor. Maydispenoid A can inhibit anti-CD3/anti-CD28 mAbs activated and lipopolysaccharide activated murine splenocyte proliferation .
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-
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- HY-160704
-
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Nucleoside Antimetabolite/Analog
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Infection
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CMX-521, a nucleoside analog, is a potent inhibitor for RNA-dependant RNA polymerase (RdRp) of norovirus. CMX-521 suppresses murine norovirus (MNV) and human norovirus .
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- HY-118704
-
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mTOR
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Inflammation/Immunology
Cancer
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P-2281 is a mTOR inhibitor with anticancer and anti-inflammatory efficacies. P-2281 suppresses dextran sulfate sodium (DSS)-induced colitis by inhibiting T cell function and is efficacious in a murine model of human colitis .
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- HY-123143
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MLN576
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Topoisomerase
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Cancer
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XR11576 (MLN576) is an orally active inhibitor of topoisomerase I and II. XR11576 shows cytotoxicity against human and murine tumor cell lines (IC50: 6-47 nM) .
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- HY-N10446
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CD28
CD3
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Inflammation/Immunology
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Maydispenoid B is a potent immunosuppressor. Maydispenoid B can inhibit anti-CD3/anti-CD28 mAbs activated and lipopolysaccharide activated murine splenocyte proliferation .
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- HY-163181
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Bacterial
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Infection
|
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MSU-43085 is an orally active MmpL3 inhibitor of Mycobacterium tuberculosis (Mtb). MSU-43085 effectively inhibits Mtb in an acute murine tuberculosis infection model. MSU-43085 can be used in tuberculosis research .
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- HY-116212
-
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MAGL
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Cancer
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JCP-170, a substituted chloroisocoumarin, is an ABHD6 inhibitor. JCP-170 robustly and reproducibly inhibits metastatic seeding of the murine cell line 0688M and both human pancreatic ductal adenocarcinoma (PDAC) cell lines .
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- HY-N13898
-
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DNA/RNA Synthesis
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Cancer
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Alldimycin A is an anthracycline compound that inhibits RNA and DNA syntheses. Alldimycin A inhibits the growth, DNA and RNA synthesis of murine leukemic L1210, with IC50 values of 0.05 μg/mL, 0.92 μg/mL, and 0.47 μg/mL, respectively .
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- HY-117365
-
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Epigenetic Reader Domain
|
Cancer
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MI-1481 is a highly potent inhibitor of the Menin-MLL1 interaction with IC50 of 3.6 nM. MI-1481 markedly reduces cell growth of murine bone marrow cells transformed and inhibits leukemia progression .
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- HY-119823
-
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P-glycoprotein
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Cancer
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PGP-4008 is a specific P-glycoprotein (Pgp) inhibitor. PGP-4008 inhibits tumor growth in a murine syngeneic Pgp-mediated multiple agent resistance (MDR) solid tumor model when given in combination with Doxorubicin .
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- HY-125987
-
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Ras
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Cancer
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RBC6 is an inhibitor of GTPases RalA. RBC6 inhibits binding of Ral to its effector RALBP1. RBC6 also inhibits Ral-mediated cell spreading of murine embryonic fibroblasts, as well as anchorage-independent growth of human cancer celllines .
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-
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- HY-115474
-
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Wnt
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Cardiovascular Disease
|
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Cardionogen-2 is a biphasic modulator of cardiogenesis, either promoting or inhibiting heart formation depending on the stage of treatment. Cardionogen-2 inhibits Wnt/β-catenin-dependent transcription in murine embryonic stem (ES) cells and zebrafish embryos .
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- HY-121662
-
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LDK
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Apoptosis
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Inflammation/Immunology
Cancer
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Lenaldekar (LDK) inhibits human and murine T-cell expansiomn. Lenaldekar inhibits autoimmune T cell response. Lenaldekar also induces cancer cell apoptosis. Lenaldekar can be used for T-cell mediated autoimmune diseases research .
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-
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- HY-50935
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CS-045
|
PPAR
Autophagy
Apoptosis
Ferroptosis
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Metabolic Disease
Cancer
|
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Troglitazone is an orally active PPARγ agonist, with EC50s of 550 nM and 780 nM for human and murine PPARγ receptor, respectively. Troglitazone has anticancer activity, prevents and inhibits the development of type 2 diabetes.
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- HY-N14957
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Antibiotic
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Infection
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Clavicoronic acid is an avian myeloblastosis virus and Moloney murine leukemia virus reverse transcriptases inhibitor with Ki values of 130, 68 µM, respectively. Clavicoronic acid inhibits the multiplication of vesicular stomatitis virus by interfering with this virus's RNA-directed RNA-polymerase. Clavicoronic acid shows no cytotoxicity .
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- HY-149347
-
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Bacterial
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Infection
|
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Mtb-IN-3 (compound 10c) is an inhibitor of Mycobacterium tuberculosis (Mtb). Mtb-IN-3 shows selective, potent in vitro antimycobacterial activity without cytotoxicity. Mtb-IN-3 inhibits colony-forming in spleen in the murine tuberculosis model .
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-
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- HY-13598
-
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CKD-516
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Microtubule/Tubulin
|
Cancer
|
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Valecobulin (CKD516) is a valine proagent of (S516) and a vascular disrupting agent (VDA). Valecobulin is a potent β-tubulin polymerization inhibitor with marked antitumor activity against murine and human solid tumors .
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- HY-W097659
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Parasite
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Infection
|
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Antileishmanial agent-32 (Compound 12) exhibits a weak antileishmanial activity that inhibits stationary promastigote forms of L. amazonensis with an IC50 >15 μM. Antileishmanial agent-32 exhibits cytotoxicity towards murine macrophages .
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- HY-W787717
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HIV
|
Infection
Inflammation/Immunology
Cancer
|
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12-Methoxydodecanoic acid, a heteroatom-containing analog of myristic acid, possesses anti-viral activity against HIV, with an IC50 of 6.8 μM. 12-Methoxydodecanoic acid inhibits moloney murine leukemia virus (MoMLV) .
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- HY-123464
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Ras
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Cancer
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RBC10 is an anti-cancer agent. RBC10 inhibits the binding of Ral to its effector RALBP1. RBC10 also inhibits Ral-mediated cell spreading of murine embryonic fibroblasts and anchorage-independent growth of human cancer cell lines .
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- HY-N0589
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NF-κB
COX
Bacterial
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Infection
Inflammation/Immunology
|
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Dehydrodiisoeugenol is isolated from Myristica fragrans Houtt, shows anti-inflammatory and anti-bacterial actions . Dehydrodiisoeugenol inhibits LPS- stimulated NF-κB activation and cyclooxygenase (COX)-2 gene expression in murine macrophages .
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- HY-133850
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Pim
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Cancer
|
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10-DEBC is a selective Akt inhibitor. 10-DEBC shows strong inhibitory activity against Moloney murine leukemia virus (Pim) kinase-1 (IC50=1.28 μM) .
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- HY-P2136
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COG1410
2 Publications Verification
|
Apoptosis
|
Neurological Disease
Inflammation/Immunology
|
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COG1410 is an apolipoprotein E-derived peptide and an apoptosis inhibitor. COG1410 exerts neuroprotective and antiinflammatory effects in a murine model of traumatic brain injury (TBI). COG1410 can be used for the research of neurological disease .
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-
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- HY-N12255
-
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Glyoxalase (GLO)
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Cancer
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COTC is a bacterial metabolite with anticancer activity that is found in S. griseosporeus. COTC inhibits glyoxalase in the presence of glutathione (GSH). COTC also inhibits the proliferation of HeLa cells (IC50 = 18 µg/mL), as well as reduces tumor growth and improves survival in an Ehrlich murine spontaneous adenocarcinoma model .
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- HY-N0859B
-
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NO Synthase
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Neurological Disease
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Schisanchinin D is an NO release inhibitor found in the fruits of Schisandra chinensis. Schisanchinin D can inhibit the release of nitric oxide (NO) by lipopolysaccharide (LPS)-activated microglia in primary murine BV2 microglia cells. Schisanchinin D is promising for research of neurodegenerative diseases such as Alzheimer's disease (AD) .
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- HY-125092
-
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Antibiotic
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Infection
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Drimentine C is a terpenylated diketopiperazine antibiotic originally isolated from Actinomycete bacteria. It inhibits proliferation of NS-1 murine β lymphocyte myeloma cells by 63 and 98% in vitro when used at concentrations of 12.5 and 100 μg/mL, respectively.
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-
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- HY-B1448
-
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KW-3049
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Calcium Channel
Apoptosis
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Cardiovascular Disease
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Benidipine hydrochloride is an orally active calcium channel antagonist. Benidipine hydrochloride can inhibit cell proliferation and apoptosis. Benidipine hydrochloride has antioxidant activity and can increase nitric oxide synthase activity and improve coronary circulation in hypertensive rats .
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-
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- HY-13598A
-
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CKD-516 hydrochloride
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Microtubule/Tubulin
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Cancer
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Valecobulin hydrochloride (CKD-516 hydrochloride) is a valine proagent of S516 (HY-130233) and a vascular disrupting agent (VDA). Valecobulin hydrochloride is a potent β-tubulin polymerization inhibitor with marked antitumor activity against murine and human solid tumors .
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- HY-118079
-
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Endogenous Metabolite
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Infection
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Drimentine B is a terpenylated diketopiperazine originally isolated from Actinomycete bacteria that has anticancer activity. It inhibits the proliferation of NS-1 murine β lymphocyte myeloma cells by 41 and 59% in vitro when used at concentrations of 50 and 100 μg/mL, respectively.
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-
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- HY-120427
-
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NSC 658586
|
CCR
CXCR
HIV
HSV
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Infection
Inflammation/Immunology
|
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Cosalane (NSC 658586) is a CCR7 (IC50 = 2.43 μM) and CXCR2 antagonist (IC50 = 0.66 μM). Cosalane is an inhibitor of HIV replication with a wide range of activity against HIV-1 isolates, HIV-2, Rauscher murine leukemia virus, HSV-1, HSV-2 and human cytomegalovirus. Cosalane inhibits both attachment of gp120 to CD4. Cosalane inhibits human and murine CCR7 in response to both CCL19 and CCL21 agonists. Cosalane can be studied in research for HIV or attenuating acute graft-versus-host disease (aGVHD) in allogeneic hematopoietic stem cell transplantation (HSCT) .
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-
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- HY-N2350
-
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MMP
NF-κB
TNF Receptor
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Cancer
|
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Cynaropicrin is a sesquiterpene lactone which can inhibit tumor necrosis factor (TNF-α) release with IC50s of 8.24 and 3.18 μM for murine and human macrophage cells, respectively. Cynaropicrin also inhibits the increase of cartilage degradation factor (MMP13) and suppresses NF-κB signaling.
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- HY-149202
-
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PGE synthase
|
Inflammation/Immunology
|
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UT-11 is a potent and brain-permeable microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor with IC50s of 0.10 μM and 2.00 μM for inhibiting PGE2 production in human (SK-N-AS) and murine (BV2) cells, respectively .
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- HY-100688
-
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Dihydroorotate Dehydrogenase
|
Cancer
|
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ML390 is a potent dihydroorotate dehydrogenase (DHODH) inhibitor. ML390 is an inducer of myeloid differentiation and causes myeloid differentiation in murine (ER-HoxA9) and human (U937 and THP1) acute myeloid leukemia (AML) models .
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- HY-176434
-
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Sirtuin
|
Neurological Disease
|
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DDL-218 is an orally active and potent SirT1 inhibitor. DDL-218 enhances SirT1 in ApoE4-expressing neurons and a murine AD model. DDL-218 can be used in the study of Alzheimer's disease .
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- HY-151808
-
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Btk
|
Cancer
|
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JS25 is a selective and covalent inhibitor of BTK that inactivates BTK with an IC50 value of 5.8 nM by chelating Tyr551. JS25 inhibits cancer cells proliferation, pronounces cell death, and promotes murine xenograft model of Burkitt’s lymphoma. JS25 effectively crosses the blood-brain barrier .
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- HY-129564
-
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Antibiotic
|
Cancer
|
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Acetomycin is an antibiotic. Acetomycin inhibits the growth of CT-8 human colon adenocarcinoma cells (IC50: 1.5 μg/mL) and L1210 murine leukemia cells (IC50: 2.2 μg/mL). Acetomycin can be isolated from actinomycete WP-2661 .
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- HY-135146
-
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DNA Methyltransferase
|
Cancer
|
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GSK-3484862 is a non-covalent inhibitor for DNA methyltransferase (Dnmt1). GSK-3484862 induces DNA hypomethylation to against cancer. GSK-3484862 mediates dramatic demethylation in murine embryonic stem cells with minimal non-specific toxicity .
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-
- HY-16261
-
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INNO-206; DOXO-EMCH
|
Topoisomerase
ADC Cytotoxin
|
Cancer
|
|
Aldoxorubicin (INNO-206) is an albumin-binding proagent of Doxorubicin (DNA topoisomerase II inhibitor), which is released from albumin under acidic conditions. Aldoxorubicin (INNO-206) has potent antitumor activities in various cancer cell lines and in murine tumor models.
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-
- HY-16261C
-
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INNO-206 hydrochloride; DOXO-EMCH hydrochloride
|
Topoisomerase
ADC Cytotoxin
|
Cancer
|
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Aldoxorubicin (INNO-206) hydrochloride is an albumin-binding proagent of Doxorubicin (DNA topoisomerase II inhibitor), which is released from albumin under acidic conditions. Aldoxorubicin hydrochloride (INNO-206) has potent antitumor activities in various cancer cell lines and in murine tumor models.
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- HY-P1293
-
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iGluR
|
Neurological Disease
|
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Conantokin G, a 17-amino-acid peptide, is a potent, selective and competitive antagonist of N-methyl-D-aspartate (NMDA) receptors. Conantokin G inhibits NMDA-evoked currents in murine cortical neurons with an IC50 of 480 nM. Conantokin G has neuroprotective properties .
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- HY-N1388
-
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Others
|
Inflammation/Immunology
|
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Tussilagone, a major active component in Tussilago farfara, has anti-inflammatory effect. Tussilagone ameliorates inflammatory responses in dextran sulphate sodium-induced murine colitis. Tussilagone inhibits the inflammatory response and improves survival in cecal ligation and puncture (CLP)-induced septic mice .
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- HY-139400
-
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FTX-6058
|
Histone Methyltransferase
|
Cardiovascular Disease
|
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Pociredir (FTX-6058) is a potent and orally active inhibitor of Embryonic Ectoderm Development (EED). Pociredir can induce HbF protein expression in cell and murine models. Pociredir can be used for the research of select hemoglobinopathies, including sickle cell disease and β-thalassemia .
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-
- HY-139400A
-
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FTX-6058 hydrochloride
|
Histone Methyltransferase
|
Cardiovascular Disease
|
|
Pociredir (FTX-6058) hydrochloride is a potent and orally active inhibitor of Embryonic Ectoderm Development (EED). Pociredir hydrochloride can induce HbF protein expression in cell and murine models. Pociredir hydrochloride can be used for the research of select hemoglobinopathies, including sickle cell disease and β-thalassemia .
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- HY-P99336
-
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BI-RR 0001; Anti-Human IL6 Recombinant Antibody
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Integrin
|
Neurological Disease
Inflammation/Immunology
|
|
Enlimomab (BI-RR 0001), a murine IgG2a monoclonal antibody to the human ICAM-1, inhibits leukocyte adhesion to the vascular endothelium, thereby decreasing leukocyte extravasation and inflammatory tissue injury. Enlimomab has anti-inflammatory effects, and can be used for stroke research .
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- HY-111151
-
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APAU
|
Epoxide Hydrolase
|
Infection
Cardiovascular Disease
Metabolic Disease
|
|
AR9281 (APAU) is a potent, selective and orally active soluble epoxide hydrolase (s-EH) inhibitor. AR-9281 can inhibits human sEH (HsEH) and murine sEH (MsEH) with IC50 values of 13.8 nM and 1.7 nM, respectively. AR9281 can be used for the research of inflammation, hypertension and type 2 diabetes .
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-
- HY-111180
-
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Endogenous Metabolite
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Metabolic Disease
|
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ML-262 is an inhibitor of hepatic lipid droplet formation (IC50=6.4 nM in murine AML-12 cells), which is associated with non-alcoholic fatty liver disease.1 ML-262 does not induce cytotoxicity (up to 33 μM) or inhibit fatty acid uptake (up to 50 μM).
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- HY-138869
-
|
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Endogenous Metabolite
|
Cancer
|
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AubipyOMe serves as a potent inhibitor of tartrate-resistant acid phosphatase (TRAP/ACP5), a metalloenzyme found in activated osteoclasts and macrophages, demonstrating IC50 values of 1.3 μM for TRAP5a and 1.8 μM for TRAP5b, while effectively inhibiting TRAP activity in extracts from murine macrophages and human lung tissue.
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- HY-130430
-
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(-)-Neplanocin A
|
Antibiotic
Orthopoxvirus
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Infection
Cancer
|
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Neplanocin A ((-)-Neplanocin A) is an antitumor antibiotic with significant antitumor activity against murine L1210 leukemia. Neplanocin A is also an irreversible inhibitor of AdoHcy hydrolase (Ki=8.39 nM). Neplanocin A also has antiviral activity and is effective against vaccinia virus. Neplanocin A is obtained from Ampulariella regularis .
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- HY-50935R
-
|
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PPAR
Autophagy
Apoptosis
Ferroptosis
|
Metabolic Disease
Cancer
|
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Troglitazone (Standard) is the analytical standard of Troglitazone. This product is intended for research and analytical applications. Troglitazone is an orally active PPARγ agonist, with EC50s of 550 nM and 780 nM for human and murine PPARγ receptor, respectively. Troglitazone has anticancer activity, prevents and inhibits the development of type 2 diabetes.
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-
- HY-P1293A
-
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iGluR
|
Neurological Disease
|
|
Conantokin G TFA, a 17-amino-acid peptide, is a potent, selective and competitive antagonist of N-methyl-D-aspartate (NMDA) receptors. Conantokin G TFA inhibits NMDA-evoked currents in murine cortical neurons with an IC50 of 480 nM. Conantokin G TFA has neuroprotective properties .
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- HY-114766
-
|
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Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
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Pumafentrine is an orally active, potent dual PDE3/PDE4 inhibitor. Pumafentrine dose-dependently ameliorates the clinical score and colonic TNFα production in murine Dextran sulphate sodium (DSS; HY-116282C)-induced colitis in a preventive setting .
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-
- HY-19644
-
|
GSK 2256294
|
Epoxide Hydrolase
|
Cardiovascular Disease
|
|
GSK2256294A (GSK 2256294) is a selective and orally active inhibitor of soluble epoxide hydrolase (sEH). GSK2256294A inhibits recombinant human sEH, rat sEH orthologs and murine sEH orthologs with IC50s of 27, 61 and 189 pM, respectively. GSK2256294A can be used for the research of chronic obstructive pulmonary disease (COPD) and cardiovascular disease .
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- HY-126211
-
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HDAC
|
Inflammation/Immunology
|
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KBH-A42 is a novel histone deacetylase (HDAC) inhibitor with significant anti-inflammatory properties. KBH-A42 against TNF-α and NO production with IC50 values of 1.10 and 2.71 µM, respectively, in the LPS-induced murine macrophage RAW 264.7 cells .
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- HY-120241
-
|
K 251-1
|
Phosphodiesterase (PDE)
|
Cancer
|
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Reticulol (K 251-1) is an inhibitor of cyclic adenosine 3', 5'-monophosphate phosphodiesterase. Reticulol shows antitumor activity independent with cell cycle arrest or apoptosis. Reticulol inhibits cell growth of murine melanoma cells and human lung tumor cells. Reticulol protects its lung metastasis via the bloodstream by inhibiting the growth of B16F10 melanoma .
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- HY-N0589R
-
|
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NF-κB
COX
Bacterial
|
Infection
Inflammation/Immunology
|
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Dehydrodiisoeugenol (Standard) is the analytical standard of Dehydrodiisoeugenol. This product is intended for research and analytical applications. Dehydrodiisoeugenol is isolated from Myristica fragrans Houtt, shows anti-inflammatory and anti-bacterial actions . Dehydrodiisoeugenol inhibits LPS-stimulated NF-κB activation and cyclooxygenase (COX)-2 gene expression in murine macrophages .
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-
- HY-77813S
-
|
|
Isotope-Labeled Compounds
Bacterial
Apoptosis
Antibiotic
|
Endocrinology
Cancer
|
|
Benzyl isothiocyanate-d7 is the deuterium labeled Benzyl isothiocyanate. Benzyl isothiocyanate is a member of natural isothiocyanates with antimicrobial activity . Benzyl isothiocyanate potent inhibits cell mobility, migration and invasion nature and matrix metalloproteinase-2 (MMP-2) activity of murine melanoma cells .
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-
- HY-N2106
-
|
|
NF-κB
COX
PGE synthase
NO Synthase
|
Inflammation/Immunology
|
|
Dehydroevodiamine is a major bioactive quinazoline alkaloid isolated from Evodiae Fructus, has an antiarrhythmic effect in guinea-pig ventricular myocytes . Dehydroevodiamine inhibits LPS-induced iNOS, COX-2, prostaglandin E2 (PGE2) and nuclear factor-kappa B (NF-κB) expression in murine macrophage cells .
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-
- HY-N10337
-
|
(-)-Norjuziphine
|
Drug Derivative
|
Cancer
|
|
Norjuziphine ((-)-Norjuziphine) is an alkaloid found in the lotus flower (Nelumbo nucifera). Norjuziphine inhibits the melanogenesis of murine B16 melanoma 4A5 cells stimulated by Theophylline (HY-B0809) (IC50=14.4 μM). Norjuziphine is promising for research of skin whitening and related skin pigmentation diseases .
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-
- HY-146811
-
|
|
Bacterial
|
Inflammation/Immunology
|
|
HSGN-94 is a potent antimicrobial agent with lipoteichoic acid (LTA) biosynthesis inhibition. HSGN-94 inhibits drug-resistant Gram-positive bacteria with MIC values of 0.25-2 μg/mL. HSGN-94 inhibits biofilm formation of MRSA and Vancomycin-resistant Enterococci. HSGN-94 also inhibits pro-inflammatory cytokines, exhibits in vivo efficacy in an MRSA murine wound infection model .
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-
- HY-N2350R
-
|
|
MMP
NF-κB
TNF Receptor
|
Cancer
|
|
Cynaropicrin (Standard) is the analytical standard of Cynaropicrin. This product is intended for research and analytical applications. Cynaropicrin is a sesquiterpene lactone which can inhibit tumor necrosis factor (TNF-α) release with IC50s of 8.24 and 3.18 μM for murine and human macrophage cells, respectively. Cynaropicrin also inhibits the increase of cartilage degradation factor (MMP13) and suppresses NF-κB signaling.
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-
- HY-108444A
-
|
|
VEGFR
|
Cancer
|
(Z)-FeCP-oxindole is a selective human vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor with an IC50 value of 200 nM. (Z)-FeCP-oxindole can significantly inhibit VEGFR1 and PDGFRa or b at 10 μM. (Z)-FeCP-oxindole has some anticancer activity, acting on B16 murine melanoma lines with IC50 less than 1 μM .
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-
- HY-108444
-
|
|
VEGFR
|
Cancer
|
(Z)-FeCP-oxindole is a selective human vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor with an IC50 value of 200 nM. (Z)-FeCP-oxindole can significantly inhibit VEGFR1 and PDGFRa or b at 10 μM. (Z)-FeCP-oxindole has some anticancer activity, acting on B16 murine melanoma lines with IC50 less than 1 μM .
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-
- HY-P2136F
-
|
|
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Biotin-COG1410 TFA is a biotin labled COG1410 (HY-P2136). COG1410 is an apolipoprotein E-derived peptide and an apoptosis inhibitor. COG1410 exerts neuroprotective and antiinflammatory effects in a murine model of traumatic brain injury (TBI). COG1410 can be used for the research of neurological disease .
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-
- HY-124484
-
|
|
Notch
|
Cancer
|
|
JI130 (JI051 derivative?) is a stabilizer for the?Hes1-PHB2?interaction. JI130 inhibits?the ability of Hes1 to repress transcription. JI130?significantly reduces the tumor growth in a murine pancreatic tumor model and has the potential for ?managing pancreatic cancer .
|
-
- HY-163207
-
|
|
Epoxide Hydrolase
HDAC
|
Neurological Disease
|
|
sEH/HDAC6-IN-1 (compound M9) is a selective, orally active dual inhibitor for sEH and HDAC6, with IC50s of 2 nM, 0.72 nM and 5 nM, for human sEH, murine sEH and HDAC6, respectively. sEH/HDAC6-IN-1 reveals analgesic and anti-inflammatory effects .
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-
- HY-12836A
-
|
|
IFNAR
|
Inflammation/Immunology
|
|
IFN alpha-IFNAR-IN-1 hydrochloride is a nonpeptidic, low-molecular-weight inhibitor of the interaction between IFN-α and IFNAR. IFN alpha-IFNAR-IN-1 hydrochloride inhibits modified Vaccinia virus ankara (MVA)-induced IFN-α responses in murine bone-marrow-derived, Flt3- L-differentiated pDC cultures (BM-pDCs) (IC50=2-8 μM) .
|
-
- HY-108632
-
|
|
PARP
|
Cancer
|
|
BYK204165 is a potent and selective PARP1 inhibitor. BYK204165 inhibits cell-free recombinant human PARP-1 (hPARP-1) with a pIC50 of 7.35 (pKi=7.05), and murine PARP-2 (mPARP-2) with a pIC50 of 5.38, respectively. BYK204165 displays 100-fold selectivity for PARP-1 .
|
-
- HY-169290
-
|
|
JAK
HDAC
|
Inflammation/Immunology
|
|
JAK/HDAC-IN-4 (compound 11 i) is a JAK/HDAC inhibitor with the IC50 values of 0.49 nM and 12 nM for JAK2 and HDAC6, respectively. JAK/HDAC-IN-4 inhibits the cell proliferation and the production of nitric oxide. JAK/HDAC-IN-4 ameliorates psoriasis-like skin lesions in an Imiquimod (HY-B0180)-induced murine model with low toxicity .
|
-
- HY-153200
-
|
|
MDM-2/p53
|
Cancer
|
|
MDM2/XIAP-IN-2 is a dual inhibitor of murine double minute 2 (MDM2) and X-linked inhibitor of apoptosis protein (XIAP). MDM2/XIAP-IN-2 degrades MDM2, and inhibits XIAP mRNA translation to inhibits cancer cells. Particularly, MDM2/XIAP-IN-2 inhibits acute lymphoblastic leukemia cell line EU-1 with an IC50 value of 0.3 μM .
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-
- HY-N1388R
-
|
|
Others
|
Inflammation/Immunology
|
|
Tussilagone (Standard) is the analytical standard of Tussilagone. This product is intended for research and analytical applications. Tussilagone, a major active component in Tussilago farfara, has anti-inflammatory effect. Tussilagone ameliorates inflammatory responses in dextran sulphate sodium-induced murine colitis. Tussilagone inhibits the inflammatory response and improves survival in cecal ligation and puncture (CLP)-induced septic mice .
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-
- HY-114366
-
|
|
CXCR
|
Others
|
|
BC-1485 is a small molecule inhibitor of Fibrosis-inducing E3 ligase 1 (FIEL1). BC-1485 protects PIAS4 from ubiquitin-mediated degradation. BC-1485 decreases α-SMA, BAL and CXCL1. BC-1485 ameliorates fibrotic lung injury in murine models .
|
-
- HY-114374
-
|
|
Cathepsin
|
Inflammation/Immunology
|
|
RO5461111 a highly specific and orally active antagonist of Cathepsin S with IC50s of 0.4 nM (human Cathepsin S) and 0.5 nM (murine Cathepsin S), respectively. RO5461111 can effectively inhibit the activation of antigen-specific T cells and B cells. RO5461111 can improve pulmonary inflammation and lupus nephritis .
|
-
- HY-N2939
-
|
|
Others
|
Others
|
|
Bis-5,5-Nortrachelogenin is isolated from active extract of root of Wikstroemia indica. Bis-5,5-Nortrachelogenin inhibits nitric oxide (NO) production in a lipopolysaccharide (LPS) and recombinant mouse interferon-γ(IFN-γ) activated murine macrophage-like cell line, RAW 264.7 with an IC50 value of 48.6 mM .
|
-
- HY-118037
-
|
|
CXCR
|
Inflammation/Immunology
|
|
VUF10132 is a non-peptide CXCR3 receptor antagonist with anti-inflammatory activity, inhibiting diseases such as rheumatoid arthritis, multiple sclerosis, and psoriasis. VUF10132 has high affinity for the human CXCR3 receptor but slightly lower affinity for the murine CXCR3 receptor. Additionally, VUF10132 exhibits inverse agonist properties at the CXCR3 receptor .
|
-
- HY-112041
-
|
PTC596
|
BMI1
Apoptosis
|
Cancer
|
|
Unesbulin (PTC596) is an orally active and selective B-cell-specific Moloney murine leukemia virus integration site 1 (BMI-1) inhibitor. Unesbulin downregulates MCL-1 and induces p53-independent mitochondrial apoptosis in acute myeloid leukemia (AML) cells. Unesbulin has anti-leukemic activity .
|
-
- HY-15652
-
|
ONO-6818; ONO-PO-736
|
Elastase
|
Inflammation/Immunology
|
|
Freselestat (ONO-6818) is a potent and orally active neutrophil elastase inhibitor with a Ki of 12.2 nM. Freselestat is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat has a potent anti-inflammatory activity .
|
-
- HY-110177
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
SP-100030 is a potent NF-κB and activator protein-1 (AP-1) double inhibitor (IC50s=50 and 50 nM, respectively). SP-100030 inhibits IL-2, IL-8, and TNF-alpha production in Jurkat and other T cell lines. SP-100030 decreases murine collagen-induced arthritis (CIA) .
|
-
- HY-170835
-
|
|
Beta-lactamase
Bacterial
|
Infection
Inflammation/Immunology
|
|
NDM-1 inhibitor-7 (Compound A8) is a NDM-1 inhibitor, with IC50 of 10.284 μM. NDM-1 inhibitor-7 restores the ability of MEM to penetrate the cell wall of gram-negative bacteria. NDM-1 inhibitor-7 effectively restores the antibacterial activity of MEM against NDM-1-positive Escherichia coli. NDM-1 inhibitor-7 demonstrates strong efficacy in both the Galleria mellonella infection model and murine peritonitis infection model .
|
-
- HY-121619
-
|
|
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Jacaric acid is a conjugated linolenic acid, which inhibits viability in cells PC-3 (IC50 is 11.8 μM), LNCaP (IC50 is 2.2 μM) and DLD-1, induces apoptosis and necrosis . Jacaric acid exhibits anticaner activity against prostate cancer and adenocarcinoma . Jacaric acid exhibits immunomodulating activity in murine peritoneal macrophages as an immunopotentiator . Jacaric acid is orally active.
|
-
- HY-167860
-
|
|
Others
|
Cancer
|
|
BE-12406B is an antitumor agent that can be found in the culture broth of a streptomycete. BE-12406B can inhibit the growth of Vincristine (HY-N0488)-resistant or Doxorubicin (HY-15142A)-resistant P388 murine leukemia cell lines as well as their parent sensitive cell line .
|
-
- HY-P10710
-
|
|
IFNAR
Interleukin Related
COX
|
Inflammation/Immunology
|
|
BMP-4 is a penetrating heparin-binding peptide with anti-inflammatory and anti-chondrogenic functions. In murine chondrocytes and macrophages, BMP-4 regulates the iNOS-IFN-IL6 signaling pathway to inhibit the expression of inflammatory proteins such as iNOS, COX2, IFN, and IL6 in a dose-dependent manner, effectively suppressing inflammation and alleviating various arthritis symptoms .
|
-
- HY-118700
-
|
Guanidinobiotin
|
NO Synthase
|
Neurological Disease
|
|
2-Iminobiotin (Guanidinobiotin) is a biotin (vitamin H or B7) analog. 2-Iminobiotin is a reversible nitric oxide synthases inhibitor with Kis of 21.8 and 37.5μM for murine iNOS and rat n-cNOS, respectively . 2-Iminobiotin superimposes on hypothermia protects human neuronal cells from hypoxia-induced cell damage .
|
-
- HY-126052
-
|
|
COX
Tyrosinase
HDAC
|
Metabolic Disease
Cancer
|
|
Gnetol is a phenolic compound isolated from the root of Gnetum montanum . Gnetol potently inhibits COX-1 (IC50 of 0.78 μM) and HDAC. Gnetol is a potent tyrosinase inhibitor with an IC50 of 4.5 μM for murine tyrosinase and suppresses melanin biosynthesis. Gnetol has antioxidant, antiproliferative, anticancer and hepatoprotective activity. Gnetol also possesses concentration-dependent α-Amylase, α-glucosidase, and adipogenesis activities .
|
-
- HY-126037
-
|
|
ROR
|
Inflammation/Immunology
|
|
(±)-ML 209 (compound 4n), a diphenylpropanamide, is a retinoic acid-related orphan receptor RORγ antagonist with an IC50 of 1.1 μM. (±)-ML 209 inhibits RORγt transcriptional activity with an IC50 of 300 nM in HEK293t cells. (±)-ML 209 inhibits the transcriptional activity of RORγt, but not RORα in cells. (±)-ML 209 selectively inhibits murine Th17 cell differentiation without affecting the differentiation of naïve CD4 + T cells into other lineages, including Th1 and regulatory T cells .
|
-
- HY-108062A
-
|
|
Beta-lactamase
Bacterial
|
Infection
|
|
BLI-489 hydrate, a penem β-lactamase inhibitor, is active against class A and class C as well as some class D β-lactamases. The combination of Piperacillin and BLI-489 hydrate is efficacious against murine infections caused by class A (including extended-spectrum β-lactamases), class C (AmpC), and class D β-lactamase-expressing pathogens .
|
-
- HY-112742
-
|
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
CP-195543 is a potent, selective and orally active leukotriene B4 (LTB4) receptor antagonist with IC50s of 6.8, 37.0 nM for human neutrophils and murine spleen membranes, respectively. CP-195543 blocks CD11b up-regulation. CP-195543 inhibits LTB4-mediated neutrophil infiltration .
|
-
- HY-128204
-
AN3661
1 Publications Verification
|
Parasite
|
Infection
|
|
AN3661, a potent antimalarial lead compound, targets a Plasmodium falciparum cleavage and polyadenylation specificity factor homologue subunit 3 (PfCPSF3). AN3661 inhibits Plasmodium falciparum laboratory-adapted strains (mean IC50=32 nM), Ugandan field isolates (mean ex vivo IC50=64 nM), and murine P. berghei and P. falciparum infections .
|
-
- HY-135146A
-
|
|
DNA Methyltransferase
|
Cancer
|
|
(Rac)-GSK-3484862 is the isomer of GSK-3484862 (HY-135146), and can be used as an experimental control. GSK-3484862 is a non-covalent inhibitor for DNA methyltransferase (Dnmt1). GSK-3484862 induces DNA hypomethylation to against cancer. GSK-3484862 mediates dramatic demethylation in murine embryonic stem cells with minimal non-specific toxicity .
|
-
- HY-15652A
-
|
ONO-6818 quarterhydrate; ONO-PO-736 quarterhydrate
|
Elastase
|
Inflammation/Immunology
|
|
Freselestat quarterhydrate (ONO-6818 quarterhydrate) is a potent and orally active neutrophil elastase inhibitor with a Ki of 12.2 nM. Freselestat quarterhydrate is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat quarterhydrate has a potent anti-inflammatory activity .
|
-
- HY-117037
-
|
|
Apoptosis
ERK
|
Cardiovascular Disease
Cancer
|
|
FR900359 is a depsipeptide selective inhibitor of Gαq/11/14 in mammalia, can inhibits ERK pathway. FR900359 suppresses the proliferation of melanoma cells and decreases of blood pressure. FR900359 also protected against airway hyperreactivity in murine models of allergen sensitization in Ovalbumins(HY-W250978)–induced sensitization model of asthma. FR900359 can be used for cancer and cardiovascular disease research .
|
-
- HY-111662
-
|
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
|
Fc 11a-2, a benzimidazole compound, is an orally active and potent NLRP3 inflammasome inhibitor. Fc 11a-2 restrains the formation of NLRP3 inflammasome by inhibiting activation of caspase-1 and thus the activation of IL-1b/IL-18. Fc 11a-2 prevents the development of Dextran sulfate sodium (DSS; HY-116282C)-induced murine experimental colitis .
|
-
- HY-145446
-
|
|
Epigenetic Reader Domain
|
Metabolic Disease
|
|
SGC-SMARCA-BRDVIII is a potent and selective inhibitor of SMARCA2/4 and PB1(5), with Kds of 35 nM, 36 nM, and 13 nM, respectively. SGC-SMARCA-BRDVIII also inhibits PB1(2) and PB1(3), with Kds of 3.7 and 2.0 μM, respectively. SGC-SMARCA-BRDVIII can block adipogenesis of 3T3-L1 murine fibroblasts .
|
-
- HY-10029
-
|
Rebemadlin
|
MDM-2/p53
E1/E2/E3 Enzyme
Autophagy
Apoptosis
|
Cancer
|
|
Nutlin-3a (Rebemadlin), an active enantiomer of Nutlin-3, is a potent murine double minute (MDM2) inhibitor (IC50=90 nM). Nutlin-3a inhibits MDM2-p53 interactions and stabilizes the p53 protein, and induces cell autophagy and apoptosis. Nutlin-3a has the potential for the study of TP53 wild-type ovarian carcinomas .
|
-
- HY-10029A
-
|
(Rac)-Rebemadlin
|
MDM-2/p53
Autophagy
Apoptosis
E1/E2/E3 Enzyme
|
Cancer
|
|
(Rac)-Nutlin-3 (Rebemadlin), an active enantiomer of Nutlin-3, is a potent murine double minute (MDM2) inhibitor (IC50=90 nM). (Rac)-Nutlin-3 inhibits MDM2-p53 interactions and stabilizes the p53 protein, and induces cell autophagy and apoptosis. (Rac)-Nutlin-3 has the potential for the study of TP53 wild-type ovarian carcinomas .
|
-
- HY-P99333
-
|
M200; Eos 200-4
|
Integrin
|
Cardiovascular Disease
Cancer
|
|
Volociximab (M200) is a chimeric human/murine IgG4 antibody IIA1 targeting integrin α5β1 (EC50=0.2 nM). Integrin α5β1 is a major fibronectin receptor involved in angiogenesis. Volociximab has antiangiogenic and antitumor activities and inhibits the proliferation of human umbilical vein vascular endothelial cells (HUVECs) .
|
-
- HY-118700A
-
|
Guanidinobiotin hydrobromide
|
NO Synthase
|
Neurological Disease
|
|
2-Iminobiotin hydrobromide (Guanidinobiotin hydrobromide) is a biotin (vitamin H or B7) analog. 2-Iminobiotin hydrobromide is a reversible nitric oxide synthases inhibitor with Kis of 21.8 and 37.5 μM for murine iNOS and rat n-cNOS, respectively . 2-Iminobiotin hydrobromide superimposes on hypothermia protects human neuronal cells from hypoxia-induced cell damage .
|
-
- HY-114015
-
|
|
Ser/Thr Protease
|
Cancer
|
|
APC-6860 is a trypsin-like serine proteases inhibitor with ki values of 0.21 and 0.44 μM for uPA and trypsin, respectively. APC-6860 has a selectivity ratio for tPA versus uPA of 80. APC-6860 has ki values of 0.1 and 0.082 μM for human and murine urokinases, respectively. APC-6860 can be used for the research of cancer .
|
-
- HY-N9480
-
|
SM-345431
|
Phospholipase
Bacterial
|
Infection
Cancer
|
|
Vinaxanthone (SM-345431) is a potent and selective semaphorin3A, phospholipase C (PLC) and FabI inhibitor, with IC50s of 0.1-0.2 μM and 0.9 mM for semaphorin3A and FabI. Vinaxanthone inhibits the substrate (t-o-NAC thioester) and the cofactor (NADPH) with Kis of 3.1 μM and 1.0 μM, respectively. Vinaxanthone can be used to handle infections caused by multidrug-resistant pathogens .
|
-
- HY-149208
-
|
|
HDAC
Apoptosis
|
Cancer
|
HDAC-IN-53 is an orally active, and selective HDAC1-3 inhibitor with IC50 values of 47 nM, 125 nM, and 450 nM, respectively. HDAC-IN-53 does not inhibit class II HDACs (HDAC4, 5, 6, 7, 9; IC50>10 μM). HDAC-IN-53 induces caspase-dependent apoptosis. HDAC-IN-53 significantly inhibits the growth of human tumor xenografts in nude mice and murine tumor growth in immune-competent mice bearing MC38 colon cancer .
|
-
- HY-13545
-
|
|
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
ABT-510 is an anti-angiogenic TSP peptide (Thrombospondin-1 analogue) that induces apoptosis and inhibits ovarian tumour growth in an orthotopic, syngeneic model of epithelial ovarian cancer. ABT-510 also reduces angiogenesis and inflammatory responses in a murine model of inflammatory bowel disease. ABT-510 can be used in studies of cancer (particularly epithelial ovarian cancer) and inflammatory bowel disease (IBD) .
|
-
- HY-13545B
-
|
|
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
ABT-510 acetate is an anti-angiogenic TSP peptide (Thrombospondin-1 analogue) that induces apoptosis and inhibits ovarian tumour growth in an orthotopic, syngeneic model of epithelial ovarian cancer. ABT-510 acetate also reduces angiogenesis and inflammatory responses in a murine model of inflammatory bowel disease. ABT-510 acetate can be used in studies of cancer (particularly epithelial ovarian cancer) and inflammatory bowel disease (IBD) .
|
-
- HY-W010983
-
SC-236
1 Publications Verification
|
COX
PPAR
Apoptosis
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
SC-236 is an orally active COX-2 specific inhibitor (IC50 = 10 nM) and a PPARγ agonist. SC-236 suppresses activator protein-1 (AP-1) through c-Jun NH2-terminal kinase. SC-236 exerts anti-inflammatory effects by suppressing phosphorylation of ERK in a murine model .
|
-
- HY-115567
-
|
1-(β-D-2-Deoxyribofuranosyl)-5-nitroindole
|
Apoptosis
|
Cancer
|
|
5-NIdR (1-(β-D-2-Deoxyribofuranosyl)-5-nitroindole), an artificial nucleoside, exhibits the ability to inhibit the replication of DNA lesions generated by Temozolomide (HY-17364). 5-NIdR induces cancer cells apoptosis and arrests cell cycle at G0 phase. 5-NIdR enhances Temozolomide anti-tumor efficacy in murine glioblastoma model .
|
-
- HY-120516
-
|
|
PAI-1
|
Cardiovascular Disease
|
|
CDE-096 is a potent inhibitor of PAI-1. CDE-096 prevents PAI-1 from inactivating tPA and uPA with similar potency (IC50=30 and 25 nM, respectively) and is active against glycosylated PAI-1, as well as PAI-1 derived from several species (IC50=19, 22 and 18 nM for murine, rat, and Porcine PAI-1, respectively) .
|
-
- HY-P10793
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
Cyclic(YCDGFYACYMDV) is a HER2 signaling pathway inhibitor with anti-cancer activity. This compound self-assembles into nanoparticles in aqueous solution and transforms into nanofibers upon specific binding to HER2 on cancer cells. This transformation disrupts HER2 dimerization and subsequent downstream signaling events, leading to cancer cell apoptosis (Apoptosis). The inhibitory effects on HER2 positive breast cancer have been demonstrated to be effective in a murine xenograft model .
|
-
- HY-107589A
-
|
|
Integrin
|
Inflammation/Immunology
|
|
BIO5192 hydrate is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 hydrate selectively binds to α4β1 (IC50=1.8 nM) over a range of other integrins. BIO5192 hydrate results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels .
|
-
- HY-107589
-
BIO5192
1 Publications Verification
|
Integrin
|
Inflammation/Immunology
|
|
BIO5192 is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 selectively binds to α4β1 (IC50=1.8 nM) over a range of other integrins. BIO5192 results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels .
|
-
- HY-170585
-
|
|
COX
NF-κB
|
Inflammation/Immunology
|
|
COX-2-IN-51 (E25) is a potent COX-2 inhibitor, with an IC50 of 70.7 nM. COX-2-IN-51 significantly inhibits LPS-induced release of NO and PGE2, expression of COX-2 and iNOS, and activation of NF-κB pathway. COX-2-IN-51 exhibits anti-inflammatory and analgesic effects in diverse murine models through inhibiting NF-κB pathway. COX-2-IN-51 has lower gastrointestinal side effects than Indomethacin (HY-14397) .
|
-
- HY-12534
-
|
|
Arp2/3 Complex
|
Neurological Disease
|
|
Wiskostatin is a potent and selective inhibitor of neuronal Wiskott-Aldrich syndrome protein (N-WASP)-mediated actin polymerization by stabilization of the closed, autoinhibited conformation, thereby preventing Arp2/3 complex activation. Wiskostatin is also a dynamin inhibitor with an IC50 value of 20.7 μM and a potent inhibitor of clathrin-mediated endocytosis with an IC50 value of 6.9 μM. Wiskostatin causes a rapid, profound, and irreversible decrease in cellular ATP levels. Wiskostatin also induces disassembly of podosomes in a murine monocyte cell line .
|
-
- HY-N1401
-
|
|
MMP
Apoptosis
HSV
|
Infection
Inflammation/Immunology
Cancer
|
|
20(R)-Ginsenoside Rh2, a matrix metalloproteinase (MMP) inhibitor, acts as a cell antiproliferator. It has anticancer effects via blocking cell proliferation and causing G1 phase arrest. 20(R)-Ginsenoside Rh2 induces apoptosis, and has anti-inflammatory and antioxidative activity . 20(R)-Ginsenoside Rh2 inhibits the replication and proliferation of mouse and human gammaherpesvirus 68 (MHV-68) with an IC50 of 2.77 μM for murine MHV-68 .
|
-
- HY-163749
-
|
|
STING
|
Inflammation/Immunology
|
|
STING-IN-8 (Compound 15b) emerges as a potent stimulator of interferon gene (STING) inhibitor with an IC50 value of 0.121 μM in human and an IC50 value of 0.033 μM in mouse. STING-IN-8 inhibits MSA-2 (HY-136927) or 2’, 3’ -cGAMP (HY-100564)-stimulated STING signaling and suppresses immune-inflammatory cytokine levels in both human and murine cells. STING-IN-8 is promising for research in the field of STING-associated inflammatory and autoimmune diseases .
|
-
- HY-N10653
-
|
(-)-Altemicidin
|
Others
|
Cancer
|
|
Altemicidin is a monoterpene alkaloid originally isolated from S. sioyaensis with acaricidal and anticancer activities. It is acaricidal to two-spotted spider mites (T. urticae) in a greenhouse pot test at concentrations of 10 and 100 ppm. Altemicidin inhibits the growth of murine L1210 lymphocytic leukemia and IMC carcinoma cells (IC50s=0.84 and 0.82 μg/mL, respectively). It is toxic to mice with an LD50 value of 0.3 mg/kg.
|
-
- HY-N8280
-
|
|
Fungal
|
Infection
|
|
IKD-8344 is a macrocyclic dilactone originally isolated from an actinomycete species and has diverse biological activities, including anticancer, antimicrobial, and anthelmintic properties. It is cytotoxic to L5178Y murine leukemia cells (IC50=0.54 ng/ml).1 IKD-8344 inhibits growth of the mycelial form of C. albicans (MIC=6.25 μg/mL) and potentiates the activity of polymyxin B against the multidrug-resistant pathogenic bacterium B. cenocepacia.
|
-
- HY-147849
-
|
|
Parasite
|
Infection
|
|
JMI-105 is a potent PfFP-2 (Plasmodium falciparum falcipain-2 protease) inhibitor. JMI-105 inhibits the growth of CQ S (3D7; IC50=8.8 µM) and CQ R (RKL-9; IC50=14.3 µM) strains of P. falciparum. JMI-105 significantly decreases parasitemia and prolonged host survival in a murine model with P. berghei ANKA infection. JMI-105 has the potential to be used as an anti-malarial agent .
|
-
- HY-160876
-
|
|
Keap1-Nrf2
E1/E2/E3 Enzyme
|
Inflammation/Immunology
|
|
BC-1901S is a proteasome-independent NRF2 activator and stabilizer. BC-1901S binds to DCAF1 (E3 ligase subunit) and disrupts NRF2/DCAF1 interaction, and activates NRF2 by inhibiting NRF2 ubiquitination in a KEAP1-independent manner. BC-1901S shows anti-inflammatory effect in a murine model of LPS-induced acute lung injury .
|
-
- HY-124586
-
-
- HY-P991243
-
|
|
EGFR
PI3K
Akt
|
Cancer
|
|
MP-RM-1 is a selective murine monoclonal antibody inhibitor targeting human epidermal growth factor receptor 3 (ErbB-3). MP-RM-1 blocks the activation of ErbB-3 induced by neuregulin 1 (NRG-1β) and promotes the internalization and degradation of ErbB-3, inhibiting downstream signaling pathways such as PI3K-Akt. MP-RM-1 is promising for research of ErbB-3 highly expressed solid tumors such as breast cancer, melanoma, and prostate cancer .
|
-
- 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 .
|
-
- HY-12927
-
|
|
CXCR
|
Inflammation/Immunology
|
|
SX-517 is a dual CXCR2/1 antagonist, containing boronic acid. SX-517 inhibits CXCL1-induced Ca 2+ flux (IC50=38 nM), and antagonizes CXCL8-induced [(35)S]GTPγS binding (IC50=60 nM) and ERK1/2 phosphorylation. SX-517 has significant ability for inflammation suppression, in both humanized polymorphonuclear (PMN) cells and in murine model .
|
-
- HY-149523
-
|
|
Apoptosis
NO Synthase
Caspase
|
Inflammation/Immunology
Cancer
|
|
Anticancer agent 157 (compound 15) is a NO inhibitor (IC50=0.62 μg/mL) with anti-inflammatory and anticancer activities. Anticancer agent 157 can bind to iNOS (inducible NO synthase) and caspase 8, causing nuclear fragmentation and chromatin condensation, inducing apoptosis. Anticancer agent 157 inhibits HT29 colon cancer cells (IC50=2.45 μg/mL), Hep-G2 liver cancer cells (IC50=3.25 μg/mL), and B16-F10 murine melanoma cells (IC50=3.84 μg/mL) .
|
-
- HY-100574A
-
|
|
Protein Arginine Deiminase
Apoptosis
MicroRNA
|
Inflammation/Immunology
Cancer
|
|
Cl-amidine hydrochloride is an orally active peptidylarginine deminase (PAD) inhibitor, with IC50 values of 0.8 μM, 6.2 μM and 5.9 μM for PAD1, PAD3, and PAD4, respectively. Cl-amidine hydrochloride induces apoptosis in cancer cells. Cl-amidine hydrochloride induces microRNA (miR)-16 (miRNA-16, microRNA-16) expression and causes cell cycle arrest. Cl-Amidine hydrochloride prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model .
|
-
- HY-W324243
-
|
|
11β-HSD
|
Metabolic Disease
|
|
11β-HSD1-IN-9 (compound c4a) is a potent 11β-HSD1 inhibitor with IC50 values of 0.48 and 1.3 µM for human and murine 11β-HSD1, respectively. 11β-HSD1-IN-9 competitively interacts with rat 11β-HSD1. 11β-HSD1-IN-19 can be used in studies of obesity, hyperglycemia and cognitive impairment .
|
-
- HY-100574
-
|
|
Protein Arginine Deiminase
Apoptosis
MicroRNA
|
Inflammation/Immunology
Cancer
|
|
Cl-amidine is an orally active peptidylarginine deminase (PAD) inhibitor, with IC50 values of 0.8 μM, 6.2 μM and 5.9 μM for PAD1, PAD3, and PAD4, respectively. Cl-amidine induces apoptosis in cancer cells. Cl-amidine induces microRNA (miR)-16 (miRNA-16, microRNA-16) expression and causes cell cycle arrest. Cl-Amidine prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model .
|
-
- HY-P99008
-
|
IC14
|
Toll-like Receptor (TLR)
|
Infection
Neurological Disease
Inflammation/Immunology
|
|
Atibuclimab (IC14), is a chimeric monoclonal antibody directed against CD14 and is composed of murine variable and human IgG4 Fc regions. Atibuclimab attenuates Lipopolysaccharides (HY-D1056) (LPS)-induced symptoms and strongly inhibits LPS-induced proinflammatory cytokine release, while only delaying the release of the anti-inflammatory cytokines soluble TNF receptor type I and IL-1 receptor antagonist. Atibuclimab can be used for the research of amyotrophic lateral sclerosis, sepsis, community-acquired pneumonia, or acute lung injury .
|
-
- HY-10071
-
Y-27632
Maximum Cited Publications
331 Publications Verification
|
Organoid
ROCK
Apoptosis
|
Cancer
|
|
Y-27632 is an orally active, ATP-competitive inhibitor of ROCK-I and ROCK-II, with Kis of 220 and 300 nM, respectively. Y-27632 attenuates Doxorubicin-induced apoptosis of human cardiac stem cells. Y-27632 also suppresses dissociation-induced apoptosis of murine prostate stem/progenitor cells. Y-27632 primes human induced pluripotent stem cells (hIPSCs) to selectively differentiate towards mesendodermal lineage via epithelial-mesenchymal transition-like modulation .
|
-
- HY-164999
-
|
|
Endogenous Metabolite
|
Cancer
|
|
N,N'-Bis(2,3-Dihydroxybenzoyl)-O-L-seryl-L-serine is a enterochelin hydrolyzed product. N,N'-Bis(2,3-Dihydroxybenzoyl)-O-L-seryl-L-serine can inhibit the invasion of murine colon cancer cells 26-L5 with an IC50 of 2.7 μM, and has anti-tumor effect. In addition, N,N'-Bis(2,3-Dihydroxybenzoyl)-O-L-seryl-L-serine has no appreciable antimicrobial activities against Micrococcus luteus, Escherichia coli and Candida albicans .
|
-
- HY-173154
-
|
|
Molecular Glues
NEKs
|
Inflammation/Immunology
|
|
NK7-902 is a CRBN molecular glue degrader of NEK7. NK7-902 fully degrades NEK7 in human primary monocytes and whole blood but only partially inhibits NLRP3-dependent IL-1β production. NK7-902 leads to profound and long-lasting NEK7 degradation but only transiently blocks NLRP3 inflammasome activation in non-human primates by oral administration. NK7-902 shows activity in murine systems .
|
-
- HY-157793
-
|
|
Toll-like Receptor (TLR)
NF-κB
MAPKAPK2 (MK2)
|
Inflammation/Immunology
Cancer
|
|
SMU-L11 is a specific TLR7 agonist (EC50=0.024 μM), which recruits MyD88 adapter protein and activates downstream NF-κB and MAPK signaling pathways. In murine models, SMU-L11 significantly enhances immune cell activation and promotes the proliferation of CD4 + T and CD8 + T cells, thereby directly killing tumor cells and inhibiting tumor growth. SMU-L11 can be used for cancer research, and also has the potential for studying immune system diseases .
|
-
- HY-10071A
-
|
|
Organoid
ROCK
Apoptosis
|
Cancer
|
|
Y-27632 hydrochloride hydrate is an orally active, ATP-competitive inhibitor of ROCK-I and ROCK-II, with Kis of 220 and 300 nM, respectively. Y-27632 hydrochloride hydrate attenuates Doxorubicin-induced apoptosis of human cardiac stem cells. Y-27632 hydrochloride hydrate also suppresses dissociation-induced apoptosis of murine prostate stem/progenitor cells. Y-27632 hydrochloride hydrate primes human induced pluripotent stem cells (hIPSCs) to selectively differentiate towards mesendodermal lineage via epithelial-mesenchymal transition-like modulation .
|
-
- HY-100574B
-
|
|
Protein Arginine Deiminase
Apoptosis
MicroRNA
|
Inflammation/Immunology
Cancer
|
|
Cl-amidine TFA is an orally active peptidylarginine deminase (PAD) inhibitor, with IC50 values of 0.8 μM, 6.2 μM and 5.9 μM for PAD1, PAD3, and PAD4, respectively. Cl-amidine TFA induces apoptosis in cancer cells. Cl-amidine TFA induces microRNA (miR)-16 (miRNA-16, microRNA-16) expression and causes cell cycle arrest. Cl-Amidine TFA prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model .
|
-
- HY-N1401R
-
|
|
MMP
Apoptosis
HSV
|
Infection
Inflammation/Immunology
Cancer
|
|
20(R)-Ginsenoside Rh2 (Standard) is the analytical standard of 20(R)-Ginsenoside Rh2. This product is intended for research and analytical applications. 20(R)-Ginsenoside Rh2, a matrix metalloproteinase (MMP) inhibitor, acts as a cell antiproliferator. It has anticancer effects via blocking cell proliferation and causing G1 phase arrest. 20(R)-Ginsenoside Rh2 induces apoptosis, and has anti-inflammatory and antioxidative activity . 20(R)-Ginsenoside Rh2 inhibits the replication and proliferation of mouse and human gammaherpesvirus 68 (MHV-68) with an IC50 of 2.77 μM for murine MHV-68 .
|
-
- HY-N4075R
-
|
|
Endogenous Metabolite
|
Metabolic Disease
Cancer
|
|
20(R)-Ginsenoside Rh2 (Standard) is the analytical standard of 20(R)-Ginsenoside Rh2. This product is intended for research and analytical applications. 20(R)-Ginsenoside Rh2, a matrix metalloproteinase (MMP) inhibitor, acts as a cell antiproliferator. It has anticancer effects via blocking cell proliferation and causing G1 phase arrest. 20(R)-Ginsenoside Rh2 induces apoptosis, and has anti-inflammatory and antioxidative activity . 20(R)-Ginsenoside Rh2 inhibits the replication and proliferation of mouse and human gammaherpesvirus 68 (MHV-68) with an IC50 of 2.77 μM for murine MHV-68 .
|
-
- HY-124309
-
|
|
Lactate Dehydrogenase
Apoptosis
|
Cancer
|
|
NHI-2 is a lactate dehydrogenase A (LDHA) inhibitor with an IC50 of 14.7 µM. NHI-2 shows selective for LDHA over LDHB (IC50 = 55.8 µM). NHI-2 is an efficient anti-glycolytic agent. NHI-2 enhances apoptosis, induces cell cycle arrest at S and G2 phases. NHI-2 has a broad spectrum anti-proliferative activity in cancer cells. NHI-2 affects extracellular acidification rate and ATP production. NHI-2 suppresses tumor growth in murine B78 melanoma tumor model .
|
-
- HY-137936
-
|
|
Antibiotic
|
Infection
|
|
Terrecyclic acid is a sesquiterpene originally isolated from A. terreus with antibiotic and anticancer activity. It is active against S. aureus, B. subtilis, and M. roseus (MICs=25, 50, and 25 μg/mL, respectively). Terrecyclic acid induces a heat shock response, increases levels of reactive oxygen species (ROS), and inhibits NF-κB activity and cell growth in 3T3-Y9-B12 cells.2 In vivo, terrecyclic acid (0.1, 1, and 10 mg/ml) reduces the number of ascitic fluid tumor cells in a mouse model of P388 murine leukemia.
|
-
- HY-W025074
-
|
|
Sirtuin
Histone Methyltransferase
|
Cancer
|
|
BML-278 is a SIRT1 activator (EC150: 1 μM). BML-278 increases H3K9 methylation and inhibits H3K9 acetylation in both the paternal and maternal pronucleus. BML-278 improves early embryonic development. BML-278 arrests the cell cycle at the G1/S phase, and reduces senescence in primary human mesenchymal cells. BML-278 reduces tubulin acetylation in U937 cells. BML-278 also increases mitochondrial density in murine C2C12 myoblasts .
|
-
- HY-159905
-
|
|
MAP4K
|
Inflammation/Immunology
|
|
HPK1-IN-54 is a potent HPK1 (Hematopoietic Progenitor Kinase 1) inhibitor that enhances T cell activation and proliferation by inhibiting HPK1 activity, thereby exhibiting antitumor effects. Its IC50 value against HPK1 is 2.67 nM, with excellent selectivity over the MAP4K family (>100-fold) and other selected kinases (>300-fold). HPK1-IN-54 displayed moderate in vivo clearance and reasonable oral exposure in mice and rats. Additionally, HPK1-IN-54 demonstrated strong antitumor efficacy in a CT26 murine colon cancer model and synergistic effects when combined with anti-PD-1 (HY-P9902A). HPK1-IN-54 shows promise for research in the field of immunotherapy .
|
-
- HY-P1110
-
AF12198
4 Publications Verification
|
Interleukin Related
|
Inflammation/Immunology
|
|
AF12198 is a potent, selective and specific peptide antagonist for human type I interleukin-1 receptor (IL1-R1) (IC50=8 nM) but not the human type II receptor (IC50=6.7 µM) or the murine type I receptor (IC50>200 µM). AF12198 inhibits IL-1-induced IL-8 production (IC50=25 nM) and IL-1-induced intercellular adhesion molecule-1 (ICAM-1) expression (IC50=9 nM) in vitro. AF12198 has anti-inflammatory activities and blocks responses to IL-1 in vivo .
|
-
- HY-155811
-
|
|
iGluR
|
Neurological Disease
|
|
DQP-997-74 (compound 2i) is a selective negative allosteric modulator of N-methyl-d-aspartate receptor (NMDAR), specifically targeting GluN2C/D (IC50: 0.069 μM and 0.035 μM), with blood-brain barrier penetrability. Where DQP refers to dihydroquinoline-pyrazoline. DQP-997-74 acts synergistically with the agonist glutamate to exhibit time-dependent enhanced potency in inhibiting hypersynchronous activity driven by high-frequency excitatory synaptic transmission. DQP-997-74 reduces the number of epileptogenesis in a murine model of tuberous sclerosis complex (TSC)-induced epilepsy. DQP-997-74 can be used for research on NMDAR-related neurological diseases .
|
-
- HY-111640
-
|
|
HIV
Reverse Transcriptase
|
Infection
|
|
3'-Azido-3'-deoxy-5-methylcytidine (CS-92) is a potent xenotropic murine leukemia-related retrovirus (XMRV) inhibitor with a CC50 of 43.5 μM in MCF-7 cells. 3'-Azido-3'-deoxy-5-methylcytidine also inhibits HIV-1 reverse transcriptase with an EC50 of 0.06 μM in peripheral blood mononuclear (PBM) cells . 3'-Azido-3'-deoxy-5-methylcytidine is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
|
-
- HY-149254
-
|
|
Phosphatase
Aldose Reductase
|
Metabolic Disease
|
|
PTP1B/AKR1B1-IN-1 is a dual inhibitor of protein tyrosine phosphatase 1B (PTP1B) and aldose reductase (AKR1B1), with IC50s of 0.06 μM and 4.3 μM, respectively. PTP1B/AKR1B1-IN-1 also inhibits TC-PTP with an IC50 value of 9 μM. PTP1B/AKR1B1-IN-1 serves as an insulin-mimetic agent in murine myoblasts, and reduces AKR1B1-dependent sorbitol accumulation. PTP1B/AKR1B1-IN-1 inhibits development of type 2 diabetes mellitus (T2DM) to control blood glucose levels .
|
-
- HY-172891
-
|
|
CDK
HDAC
Apoptosis
|
Cancer
|
|
CDK9/HDAC1/HDAC3-IN-1 is dual-functional inhibitor of CDK9 and HDAC. CDK9/HDAC1/HDAC3-IN-1 inhibits the protein activity of CDK9/HDAC/HDAC3 with IC50 s of 0.17 μM, 1.73 μM and 1.11 μM for CDK9, HDAC1, and HDAC3, respectively. CDK9/HDAC1/HDAC3-IN-1 inhibits cancer cells by inducing cell apoptosis and cell cycle arrest in the G2/M phase, as well as tumor growth in a murine TNBC MDA-MB-231 xenograft model. CDK9/HDAC1/HDAC3-IN-1 has a broad-spectrum anti-cancer activity, such as breast cancer, cervical cancer, and liver cancer .
|
-
- HY-146066
-
|
|
nAChR
JAK
STAT
NO Synthase
|
Inflammation/Immunology
|
|
α7 nAchR-JAK2-STAT3 agonist 1 is a potent α7 nAchR-JAK2-STAT3 agonist, with an IC50 value of 0.32 μM for nitric oxide (NO). α7 nAchR-JAK2-STAT3 agonist 1 effectively suppresses the expression of iNOS, IL-1β, and IL-6 in murine RAW264.7 macrophages. α7 nAchR-JAK2-STAT3 agonist 1 can inhibit LPS-induced NO release, NF-κB activation and cytokine production. α7 nAchR-JAK2-STAT3 can be used for researching sepsis .
|
-
- HY-172458
-
|
|
Mas-related G-protein-coupled Receptor (MRGPR)
TNF Receptor
|
Neurological Disease
|
|
Z-3578 is a small-molecule antagonist targeting MrgX2 (Mas-related G protein-coupled receptor X2) with significant anti-pseudoallergic activity and a KD value of 729 nM. Z-3578 effectively inhibits mast cell degranulation induced by substance P (SP) and C48/80, suppressing the release of β-hexosaminidase with IC50 values of 4.90 µM and 6.18 µM, respectively. It also markedly reduces the release of histamine and TNF-α, along with intracellular calcium flux. In a murine pseudoallergy model, Z-3578 significantly alleviates paw swelling and dye extravasation and lowers serum histamine levels, indicating potent in vivo anti-allergic effects. Z-3578 holds promise as a lead compound for the treatment of allergic diseases, especially pseudoallergic reactions .
|
-
- HY-149255
-
|
|
Phosphatase
Aldose Reductase
|
Metabolic Disease
|
|
PTP1B/AKR1B1-IN-2 (Compound 7f) is a dual PTP1B/AKR1B1 inhibitor (IC50s: 3.2 and 2.1 μM, Kis: 4.0 and 0.9μM). PTP1B/AKR1B1-IN-2 is an insulin-mimetic agent. PTP1B/AKR1B1-IN-2 improves glucose uptake in murine C2C12 myoblasts. PTP1B/AKR1B1-IN-2 can be used for research of Type 2 diabetes mellitus (T2DM) .
|
-
- HY-169859
-
|
|
Prostaglandin Receptor
Interleukin Related
|
Inflammation/Immunology
Cancer
|
|
EP4 receptor antagonist 7 (Compound 14) is an antagonist of the prostaglandin E2 (PGE2) receptor subtype EP4 with an IC50 value of 1.1 nM. EP4 receptor antagonist 7 inhibits PGE2-induced β-arrestin recruitment in HEK293 cells with an IC50 value of 0.9 nM. EP4 receptor antagonist 7 decreases PGE2-induced expression of mRNA encoding IL-4, macrophage mannose receptor 1 (Mrc1), chitinase-like protein 3 (Chil3), chemokine (C-X-C) motif ligand 1 (Cxcl1), triggering receptor expressed on myeloid cells 2 (Trem2), and arginase-1 (Arg1), in RAW 264.7 macrophages. EP4 receptor antagonist 7 combined with an anti-PD-1 antibody inhibits tumor growth and increases infiltration of CD 8+ T cells into tumors in a CT26 murine colon cancer model .
|
-
- HY-139090
-
|
28-O-Acetyl-3-Oxobetulin; 3-oxo-28-O-Acetylbetulin
|
Bacterial
HIV
Drug Derivative
|
Cancer
|
|
3-Oxobetulin acetate (28-O-Acetyl-3-Oxobetulin; 3-oxo-28-O-Acetylbetulin) is a derivative of betulin (HY-N0083), a cholesterol biosynthesis inhibitor. 3-Oxobetulin acetate inhibits the growth of P388 murine lymphocytic leukemia cells (EC50=0.12 μg/mL) and human MCF-7 breast cancer, SF-268 CNS cancer, H460 lung cancer, and KM20L2 colon cancer cells (GI50s=8, 10.6, 5.2, and 12.7 μg/mL), but not BxPC-3 pancreatic cancer cells or DU145 prostate cancer cells (GI50s=>10 μg/mL for both). 3-Oxobetulin acetate inhibits the replication of X4-tropic recombinant HIV (NL4.3-Ren) in MT-2 lymphoblastoid cells (IC50=13.4 μM). 3-Oxobetulin acetate is also effective against Listeria donovani amastigotes.
|
-
- HY-15616
-
|
|
Melanocortin Receptor
|
Cancer
|
|
BMS-470539 is a synthetic MC-1R agonist with potent anti-inflammatory properties. BMS-470539 selectively activates human and murine MC-1R with EC50 values ??of 16.8 nM and 11.6 nM, respectively. In vitro studies have shown that BMS-470539 is able to dose-dependently inhibit TNF-alpha-induced NF-kB activation in human melanoma cells expressing MC-1R. In vivo, subcutaneous injection of BMS-470539 into BALB/c mice effectively inhibited LPS-induced TNF-alpha production with an ED50 of approximately 10 μmol/kg and a pharmacodynamic half-life of approximately 8 hours. It also significantly reduced leukocyte infiltration in a lung inflammation model and attenuated paw swelling in a delayed-type hypersensitivity model, highlighting its efficacy as an anti-inflammatory agent through MC-1R modulation .
|
-
- HY-146066A
-
|
|
nAChR
JAK
STAT
NO Synthase
|
Others
|
|
(R)-α7 nAchR-JAK2-STAT3 agonist 1 is the R-enantiomer of α7 nAchR-JAK2-STAT3 agonist 1 (HY-146066). α7 nAchR-JAK2-STAT3 agonist 1 is a potent α7 nAchR-JAK2-STAT3 agonist, with an IC50 value of 0.32 μM for nitric oxide (NO). α7 nAchR-JAK2-STAT3 agonist 1 effectively suppresses the expression of iNOS, IL-1β, and IL-6 in murine RAW264.7 macrophages. α7 nAchR-JAK2-STAT3 agonist 1 can inhibit LPS-induced NO release, NF-κB activation and cytokine production. α7 nAchR-JAK2-STAT3 can be used for researching sepsis .
|
-
- HY-116028
-
|
15-Deoxy-Δ12,14-PGD2
|
Endogenous Metabolite
Prostaglandin Receptor
PPAR
Src
|
Cardiovascular Disease
|
|
15-deoxy-Δ12,14-Prostaglandin D2 (15-Deoxy-Δ12,14-PGD2), a metabolite of PGD2 (HY-101988), is an agonist of prostaglandin receptor 2 (DP2). 15-deoxy-Δ12,14-Prostaglandin D2 binds to DP2 (Ki=50 nM) and induces eosinophil activation (EC50=8 nM). 15-deoxy-Δ12,14-Prostaglandin D2 also stimulates the recruitment of steroid receptor coactivator-1 (SRC-1) to peroxisome proliferator-activated receptor γ (PPARγ), inducing PPARγ-mediated transcription. 15-deoxy-Δ12,14-Prostaglandin D2 (15-Deoxy-Δ12,14-PGD2) is cytotoxic to L1210 murine leukemia cells (IC50=0.3 μg/ml) and inhibits ADP-induced platelet aggregation (IC50=320 ng/mL).
|
-
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P2136
-
COG1410
2 Publications Verification
|
Apoptosis
|
Neurological Disease
Inflammation/Immunology
|
|
COG1410 is an apolipoprotein E-derived peptide and an apoptosis inhibitor. COG1410 exerts neuroprotective and antiinflammatory effects in a murine model of traumatic brain injury (TBI). COG1410 can be used for the research of neurological disease .
|
-
- HY-P2136F
-
|
|
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Biotin-COG1410 TFA is a biotin labled COG1410 (HY-P2136). COG1410 is an apolipoprotein E-derived peptide and an apoptosis inhibitor. COG1410 exerts neuroprotective and antiinflammatory effects in a murine model of traumatic brain injury (TBI). COG1410 can be used for the research of neurological disease .
|
-
- HY-13545B
-
|
|
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
ABT-510 acetate is an anti-angiogenic TSP peptide (Thrombospondin-1 analogue) that induces apoptosis and inhibits ovarian tumour growth in an orthotopic, syngeneic model of epithelial ovarian cancer. ABT-510 acetate also reduces angiogenesis and inflammatory responses in a murine model of inflammatory bowel disease. ABT-510 acetate can be used in studies of cancer (particularly epithelial ovarian cancer) and inflammatory bowel disease (IBD) .
|
-
- HY-P1110
-
AF12198
4 Publications Verification
|
Interleukin Related
|
Inflammation/Immunology
|
|
AF12198 is a potent, selective and specific peptide antagonist for human type I interleukin-1 receptor (IL1-R1) (IC50=8 nM) but not the human type II receptor (IC50=6.7 µM) or the murine type I receptor (IC50>200 µM). AF12198 inhibits IL-1-induced IL-8 production (IC50=25 nM) and IL-1-induced intercellular adhesion molecule-1 (ICAM-1) expression (IC50=9 nM) in vitro. AF12198 has anti-inflammatory activities and blocks responses to IL-1 in vivo .
|
-
- HY-122357
-
|
|
Adenylate Cyclase
|
Inflammation/Immunology
|
|
Bestim is a dipeptide, which exhibits high affinity to murine peritoneal macrophages, thymocytes, and plasma membranes isolated from these cells, with Kds of 3.1, 2.1, 18.6 and 16.7 nM, respectively. Bestim inhibits adenylate cyclase in the membranes of murine macrophages and thymocytes. Bestim exhibits immunomodulatory efficacy .
|
-
- HY-P1293
-
|
|
iGluR
|
Neurological Disease
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Conantokin G, a 17-amino-acid peptide, is a potent, selective and competitive antagonist of N-methyl-D-aspartate (NMDA) receptors. Conantokin G inhibits NMDA-evoked currents in murine cortical neurons with an IC50 of 480 nM. Conantokin G has neuroprotective properties .
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- HY-P1293A
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iGluR
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Neurological Disease
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Conantokin G TFA, a 17-amino-acid peptide, is a potent, selective and competitive antagonist of N-methyl-D-aspartate (NMDA) receptors. Conantokin G TFA inhibits NMDA-evoked currents in murine cortical neurons with an IC50 of 480 nM. Conantokin G TFA has neuroprotective properties .
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- HY-P10710
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IFNAR
Interleukin Related
COX
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Inflammation/Immunology
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BMP-4 is a penetrating heparin-binding peptide with anti-inflammatory and anti-chondrogenic functions. In murine chondrocytes and macrophages, BMP-4 regulates the iNOS-IFN-IL6 signaling pathway to inhibit the expression of inflammatory proteins such as iNOS, COX2, IFN, and IL6 in a dose-dependent manner, effectively suppressing inflammation and alleviating various arthritis symptoms .
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- HY-13545
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Apoptosis
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Inflammation/Immunology
Cancer
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ABT-510 is an anti-angiogenic TSP peptide (Thrombospondin-1 analogue) that induces apoptosis and inhibits ovarian tumour growth in an orthotopic, syngeneic model of epithelial ovarian cancer. ABT-510 also reduces angiogenesis and inflammatory responses in a murine model of inflammatory bowel disease. ABT-510 can be used in studies of cancer (particularly epithelial ovarian cancer) and inflammatory bowel disease (IBD) .
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- HY-P10793
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EGFR
Apoptosis
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Cancer
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Cyclic(YCDGFYACYMDV) is a HER2 signaling pathway inhibitor with anti-cancer activity. This compound self-assembles into nanoparticles in aqueous solution and transforms into nanofibers upon specific binding to HER2 on cancer cells. This transformation disrupts HER2 dimerization and subsequent downstream signaling events, leading to cancer cell apoptosis (Apoptosis). The inhibitory effects on HER2 positive breast cancer have been demonstrated to be effective in a murine xenograft model .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P99294
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AMG 479; Human Anti-IGF1R Recombinant Antibody
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IGF-1R
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Cancer
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Ganitumab (AMG 479) is a recombinant human monoclonal antibody to the human type 1 insulin-like growth factor receptor (IGF1R). Ganitumab recognizes murine IGF1R with sub-nanomolar affinity (KD=0.22 nM) and inhibits the interaction of murine IGF1R with IGF1 and IGF2. Ganitumab can be used in research of cancer .
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- HY-P99336
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BI-RR 0001; Anti-Human IL6 Recombinant Antibody
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Integrin
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Neurological Disease
Inflammation/Immunology
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Enlimomab (BI-RR 0001), a murine IgG2a monoclonal antibody to the human ICAM-1, inhibits leukocyte adhesion to the vascular endothelium, thereby decreasing leukocyte extravasation and inflammatory tissue injury. Enlimomab has anti-inflammatory effects, and can be used for stroke research .
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- HY-P99333
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M200; Eos 200-4
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Integrin
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Cardiovascular Disease
Cancer
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Volociximab (M200) is a chimeric human/murine IgG4 antibody IIA1 targeting integrin α5β1 (EC50=0.2 nM). Integrin α5β1 is a major fibronectin receptor involved in angiogenesis. Volociximab has antiangiogenic and antitumor activities and inhibits the proliferation of human umbilical vein vascular endothelial cells (HUVECs) .
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- HY-P99008
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IC14
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Toll-like Receptor (TLR)
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Infection
Neurological Disease
Inflammation/Immunology
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Atibuclimab (IC14), is a chimeric monoclonal antibody directed against CD14 and is composed of murine variable and human IgG4 Fc regions. Atibuclimab attenuates Lipopolysaccharides (HY-D1056) (LPS)-induced symptoms and strongly inhibits LPS-induced proinflammatory cytokine release, while only delaying the release of the anti-inflammatory cytokines soluble TNF receptor type I and IL-1 receptor antagonist. Atibuclimab can be used for the research of amyotrophic lateral sclerosis, sepsis, community-acquired pneumonia, or acute lung injury .
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- HY-P991243
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EGFR
PI3K
Akt
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Cancer
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MP-RM-1 is a selective murine monoclonal antibody inhibitor targeting human epidermal growth factor receptor 3 (ErbB-3). MP-RM-1 blocks the activation of ErbB-3 induced by neuregulin 1 (NRG-1β) and promotes the internalization and degradation of ErbB-3, inhibiting downstream signaling pathways such as PI3K-Akt. MP-RM-1 is promising for research of ErbB-3 highly expressed solid tumors such as breast cancer, melanoma, and prostate cancer .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
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- HY-77813S
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Benzyl isothiocyanate-d7 is the deuterium labeled Benzyl isothiocyanate. Benzyl isothiocyanate is a member of natural isothiocyanates with antimicrobial activity . Benzyl isothiocyanate potent inhibits cell mobility, migration and invasion nature and matrix metalloproteinase-2 (MMP-2) activity of murine melanoma cells .
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-
| Cat. No. |
Product Name |
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Classification |
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- HY-111640
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Azide
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3'-Azido-3'-deoxy-5-methylcytidine (CS-92) is a potent xenotropic murine leukemia-related retrovirus (XMRV) inhibitor with a CC50 of 43.5 μM in MCF-7 cells. 3'-Azido-3'-deoxy-5-methylcytidine also inhibits HIV-1 reverse transcriptase with an EC50 of 0.06 μM in peripheral blood mononuclear (PBM) cells . 3'-Azido-3'-deoxy-5-methylcytidine is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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| Cat. No. |
Product Name |
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Classification |
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- HY-115567
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1-(β-D-2-Deoxyribofuranosyl)-5-nitroindole
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Nucleosides and their Analogs
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5-NIdR (1-(β-D-2-Deoxyribofuranosyl)-5-nitroindole), an artificial nucleoside, exhibits the ability to inhibit the replication of DNA lesions generated by Temozolomide (HY-17364). 5-NIdR induces cancer cells apoptosis and arrests cell cycle at G0 phase. 5-NIdR enhances Temozolomide anti-tumor efficacy in murine glioblastoma model .
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