Search Result
Results for "
Competitive interactions
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
3
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-17504
-
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Rosuvastatin hemicalcium; ZD 4522 Calcium
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HMG-CoA Reductase (HMGCR)
Autophagy
Potassium Channel
Bacterial
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Cardiovascular Disease
Metabolic Disease
Cancer
|
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Rosuvastatin Calcium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Calcium potently blocks hERG current with an IC50 of 195 nM . Rosuvastatin Calcium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Calcium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
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-
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- HY-16993
-
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Apoptosis
WDR5
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Cancer
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OICR-9429, a chemical probe, is high affinity WD repeat domain 5 (WDR5) inhibitor, competitively blocks WDR5 interaction with MLL protein via binding the central peptide-binding pocket of WDR5. OICR-9429 can suppress histone H3K4 trimethylation and can be used for the research of various cancers including non-MLL-rearranged leukaemia, colon, pancreatic, prostate cancer and bladder cancer (BCa) .
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- HY-P99675
-
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AK112
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PD-1/PD-L1
VEGFR
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Cancer
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Ivonescimab (AK112) is a PD-1/VEGF bispecific antibody. Ivonescimab competitively inhibiting PD-1/PD-L1 interaction, reversing the immunosuppression mediated by it, and blocks the binding of VEGF-A to VEGFR2, inhibiting tumour angiogenesis in the tumour microenvironment. Ivonescimab also has significantly anticancer activity against EGFR-mutated locally advanced or metastatic non-squamous non-small cell lung cancer (NSCL) .
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-
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- HY-17504A
-
Rosuvastatin
Maximum Cited Publications
24 Publications Verification
ZD 4522
|
HMG-CoA Reductase (HMGCR)
Autophagy
Potassium Channel
Bacterial
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Cardiovascular Disease
Metabolic Disease
Cancer
|
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Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin potently blocks hERG current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
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- HY-124817
-
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HSP
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Inflammation/Immunology
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Col003 is a selective and potent inhibitor of Hsp47 and competitively binds to the collagen binding site on Hsp47 (IC50=1.8 μM). Col003 discourages the interaction of Hsp47 with collagen and inhibits collagen secretion by destabilizing the collagen triple helix. Col003 can be used for the investigation of fibrosis
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- HY-P1740
-
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Integrin
Apoptosis
Caspase
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Inflammation/Immunology
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RGD peptide (GRGDNP) is an inhibitor of integrin-ligand interactions. RGD peptide (GRGDNP) competitively inhibits α5β1 binding with extracellular matrice (ECM). RGD peptide (GRGDNP) promotes apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing. RGD peptide (GRGDNP) plays an important role in cell adhesion, migration, growth, and differentiation .
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- HY-P99014
-
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ARGX-110
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Fc Receptor (FcR)
NF-κB
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Inflammation/Immunology
Cancer
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Cusatuzumab (ARGX-110) is a selective competitive blocker targeting CD70 (with an equilibrium dissociation constant of 17 pM for binding to human CD70). Cusatuzumab also possesses enhanced antibody-dependent cell-mediated cytotoxicity (ADCC) activity. It is a humanized IgG1 monoclonal antibody, artificially synthesized through humanization and genetic engineering modifications (CH2 region mutation to enhance effector function). Cusatuzumab has a dual mechanism of action: firstly, it competitively blocks the interaction between CD70 and CD27, inhibiting the CD27-NF-κB signaling pathway, reducing regulatory T cell (Treg) activation and tumor cell proliferation; secondly, by enhancing binding to FcγRIIIa, it mediates ADCC and antibody-dependent cellular phagocytosis (ADCP), directly lysing CD70-positive tumor cells. Cusatuzumab can efficiently eliminate leukemia stem cells (LSCs), induce tumor cell differentiation and apoptosis, restore immune surveillance, and target CD70-positive tumors. Cusatuzumab is used in the study of acute myeloid leukemia (AML) .
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-
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- HY-17504B
-
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ZD 4522 Sodium; X-Plended Sodium; Crestor Sodium
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HMG-CoA Reductase (HMGCR)
Potassium Channel
Autophagy
Bacterial
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Cardiovascular Disease
Metabolic Disease
Cancer
|
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Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Sodium potently blocks hERG current with an IC50 of 195 nM . Rosuvastatin Sodium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Sodium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
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- HY-12583
-
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Histone Methyltransferase
Epigenetic Reader Domain
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Cancer
|
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A-366, a chemical probe, is a potent, highly selective, peptide-competitive histone methyltransferase G9a inhibitor with IC50s of 3.3 and 38 nM for G9a and GLP (EHMT1), respectively. A-366 shows >1000-fold selectivity over 21 other methyltransferases. A-366 is also a potent, nanomolar inhibitor of the Spindlin1-H3K4me3-interaction (IC50=182.6 nM). A-366 displays high affinity at human histamine H3 receptor (Ki=17 nM) and shows subtype selectivity among subsets of the histaminergic and dopaminergic receptor families .
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- HY-108831A
-
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AN100226; BG00002
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Integrin
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Inflammation/Immunology
Cancer
|
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Natalizumab (Anti-CD49d) (AN100226; BG00002) Solution is a humanized monoclonal IgG4 antibody inhibitor that selectively targets α4 integrin (CD49d), blocking the interaction of integrins such as α4β1 (VLA-4) with vascular cell adhesion molecule VCAM-1, intercellular adhesion molecule ICAM-1, and fibronectin by competitively binding to the α4 subunit. Natalizumab solution inhibits the adhesion, retention, and transendothelial migration of immune cells (such as CD4 + T cells), reducing the infiltration of inflammatory cells into the central nervous system or lesion sites, thereby exerting anti-inflammatory and immunomodulatory activity. Natalizumab (Anti-CD49d) solution is used in the study of relapsing-remitting multiple sclerosis (RRMS) and is also applied in the research of autoimmune or inflammation-related diseases such as Crohn's disease, B-cell lymphoma, and non-infectious uveitis. Natalizumab (Anti-CD49d) can also prevent lymphocytes from entering the central nervous system, thus preventing acute demyelinating relapses .
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- HY-111126
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K67
1 Publications Verification
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p62
Keap1-Nrf2
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Cancer
|
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K67 is a selective the interaction between Keap1 and S349 phosphorylated p62 inhibitor, with an IC50 of 1.5 μM. K67 has a weaker inhibitory effect on the interaction between Keap1 and Nrf2 (IC50 is 6.2 μM). K67 competitively binds to the binding site of Keap1 with p-p62, blocking the abnormal activation of the p62-dependent Nrf2 pathway. K67 inhibits tumor cell proliferation and enhances the sensitivity of hepatocellular carcinoma (HCC) to chemotherapeutic drugs by restoring Keap1-mediated ubiquitination and degradation of Nrf2 .
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- HY-N0481
-
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COX
TNF Receptor
NO Synthase
Interleukin Related
NF-κB
Apoptosis
p38 MAPK
JNK
ERK
Keap1-Nrf2
RANKL/RANK
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Neurological Disease
Inflammation/Immunology
Cancer
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Roburic acid acts as an anti-inflammatory, anti-tumor and osteoclastogenesis inhibitor, with a Ki of 7.066 μM against human TNF, an IC50 of 9 μM against human COX-2, and an IC50 of 5 μM against ovine COX-1. Roburic acid reduces the production of inflammatory mediators such as NO and IL-6 in macrophages by inhibiting the NF-κB and MAPK (p38/JNK) pathways. By competitively inhibiting the TNF-TNF-R1 interaction, Roburic acid blocks the downstream NF-κB signaling pathway, thereby inducing cell cycle arrest and apoptosis in cancer cells. Roburic acid specifically inhibits osteoclastogenesis and bone resorption by suppressing the RANKL/TRAF6/NF-κB/NFATc1 axis. Roburic acid can be used in research related to osteolytic diseases such as osteoporosis, colorectal cancer and inflammatory diseases .
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- HY-19541
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-
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- HY-100834
-
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5,7-DCKA
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iGluR
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Neurological Disease
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5,7-Dichlorokynurenic acid (5,7-DCKA) is a selective and competitive antagonist of the glycine site on NMDA receptor with a KB of 65 nM. 5,7-Dichlorokynurenic acid reduces NMDA-induced neuron injury. 5,7-Dichlorokynurenic acid increases social interaction time, increases open arm exploration time, disinhibits suppressed conflict responding in rodent models. 5,7-Dichlorokynurenic acid exhibits anxiolytic-like activity in rodent models and supports exploration of glycine’s role in NMDA receptor-mediated synaptic transmission .
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- HY-107597
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Halicin
2 Publications Verification
SU3327
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JNK
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Metabolic Disease
Inflammation/Immunology
|
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Halicin (SU3327) is a potent, selective and substrate-competitive JNK inhibitor with an IC50 of 0.7 μM. Halicin also inhibits protein-protein interactions between JNK and JNK Interacting Protein (JIP) with an IC50 of 239 nM. Halicin shows less active against p38α and Akt kinase .
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- HY-15222
-
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Epigenetic Reader Domain
Apoptosis
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Cancer
|
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Menin-MLL inhibitor MI-2 is a competitive and selective Menin-MLL interaction inhibitor with an IC50 value of 446 nM and a Ki value of 158 nM. Menin-MLL inhibitor MI-2 downregulates the expression of target genes such as HOXA9 and MEIS1, inhibits proliferation of leukemia cells and induces apoptosis and differentiation. Menin-MLL inhibitor MI-2 is proming for rasearch of MLL-rearranged acute leukemias (e.g., AML, ALL) .
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- HY-19347
-
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WD-Repeat Protein 5-0103
|
WDR5
|
Neurological Disease
Cancer
|
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WDR5-0103 (WD-Repeat Protein 5-0103) is a potent and selective WD repeat-containing protein 5 (WDR5) antagonist with a Kd of 450 nM. WDR5-0103 competitively binds to the peptide-binding pocket of WDR5, blocking the interaction between WDR5 and mixed-lineage leukemia (MLL) protein and inhibiting the methyltransferase activity of MLL. WDR5-0103 is mainly used in the research of cancer and neurodegenerative diseases .
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- HY-100034
-
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DA-3003-1
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Phosphatase
Histone Methyltransferase
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Cancer
|
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NSC 663284 (DA-3003-1) is a potent, cell-permeable, and irreversible Cdc25 dual specificity phosphatase inhibitor, has an IC50 for Cdc25B2 of 0.21 μM. NSC 663284 exhibits mixed competitive kinetics against Cdc25A, Cdc25B(2), and Cdc25C with Ki values of 29, 95, and 89 nM, respectively . NSC 663284 inhibits NSD2 (IC50 of 170 nM) through a direct interaction with the catalytic SET domain (Kd of 370 nM) .
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- HY-100903
-
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nor-Binaltorphimine dihydrochloride; nor-BNI dihydrochloride
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Opioid Receptor
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Neurological Disease
|
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Norbinaltorphimine dihydrochloride (nor-Binaltorphimine dihydrochloride; nor-BNI dihydrochloride) is a selective, long-acting competitive antagonist of the κ-opioid receptor. Norbinaltorphimine dihydrochloride blocks κ-opioid receptor-mediated analgesic effects, and inhibits butorphanol-induced changes in κ-opioid receptor binding kinetics, desensitization and down-regulation. Norbinaltorphimine dihydrochloride suppresses specific opioid withdrawal symptoms, precipitates withdrawal behaviors in butorphanol-dependent rats, and serves as a molecular probe for studying κ-opioid receptor-agonist interactions. Norbinaltorphimine dihydrochloride is applicable to research related to neurological disorders such as pain .
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- HY-117040
-
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Norbinaltorphimine; NorBNI
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Opioid Receptor
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Neurological Disease
|
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nor-Binaltorphimine (Norbinaltorphimine; NorBNI) is a selective, long-acting competitive antagonist of the κ-opioid receptor. nor-Binaltorphimine blocks κ-opioid receptor-mediated analgesic effects, and inhibits butorphanol-induced changes in κ-opioid receptor binding kinetics, desensitization and down-regulation. nor-Binaltorphimine suppresses specific opioid withdrawal symptoms, precipitates withdrawal behaviors in butorphanol-dependent rats, and serves as a molecular probe for studying κ-opioid receptor-agonist interactions. nor-Binaltorphimine is applicable to research related to neurological disorders such as pain .
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- HY-13032B
-
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GSK 525762C; I-BET 762 besylate
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Epigenetic Reader Domain
ERK
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Cancer
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Molibresib besylate (GSK 525762C; I-BET 762 besylate) is an orally active pan-BET inhibitor that targets and binds to BRD2, BRD3, BRD4 and BRDT. By competitively occupying acetylated lysine binding sites, Molibresib besylate disrupts the interaction between BET proteins and chromatin, thereby effectively inhibiting MYC expression and target gene transcription. Molibresib besylate exhibits broad antiproliferative activity, which not only inhibits cancer cell growth and induces growth arrest, but also downregulates mitosis-related genes and upregulates the level of p-ERK1/2. When combined with MEK inhibitors, Molibresib besylate shows a significant synergistic effect, reduces tumor burden in mouse models of leukemia, modulates the immune microenvironment and prolongs survival. Molibresib besylate is widely applicable to research related to acute myeloid leukemia, multiple myeloma, triple-negative breast cancer, small-cell lung cancer and various advanced refractory solid tumors .
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- HY-124828
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CMLD-2
2 Publications Verification
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HuR
|
Cancer
|
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CMLD-2, an inhibitor of HuR-ARE interaction, competitively binds HuR protein disrupting its interaction with adenine-uridine rich elements (ARE)-containing mRNAs (Ki=350 nM). CMLD-2 induces apoptosis exhibits antitumor activity in different cancer cells as colon, pancreatic, thyroid and lung cancer cell lines. Hu antigen R (HuR) is an RNA binding protein, can regulate target mRNAs stability and translation .
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- HY-131592
-
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Apoptosis
Keap1-Nrf2
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Neurological Disease
Inflammation/Immunology
Cancer
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Tricetin is a potent competitive inhibitor of the Keap1-Nrf2 Protein Protein Interaction (PPI). Tricetin protects against 6-OHDA-induced neurotoxicity in Parkinson's disease model by activating Nrf2/HO-1 signaling pathway and preventing mitochondria-dependent apoptosis pathway .
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- HY-122866
-
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Ras
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Cancer
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ZT-12-037-01 is a STK19-targeted inhibitor, has a high-affinity interaction with STK19 protein and inhibits oncogenic NRAS-driven melanocyte malignant transformation. ZT-12-037-01 is an ATP-competitive inhibitor, inhibiting phosphorylation of NRAS (major isoform of Ras family) with an IC50 of 24 nM .
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- HY-P99345
-
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TSR-042; ANB-011; WBP-285
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PD-1/PD-L1
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Cancer
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Dostarlimab (TSR-042) is a humanized anti-PD-1 monoclonal antibody. Dostarlimab binds with high affinity to human PD-1 and competitively inhibits its interaction with its ligands, PD-L1 and PD-L2, with IC50s of 1.8 and 1.5 nM, respectively .
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- HY-113352
-
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Endogenous Metabolite
PARP
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Cancer
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7-Methylguanine is an orally active and competitive PARP-1 inhibitor with a Ki value of 61 μM. 7-Methylguanine is a metabolite of nucleic acids. 7-Methylguanine has anticancer activity against uterine sarcoma and colon adenocarcinoma. 7-Methylguanine is used as a probe for protein-DNA interactions .
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- HY-W012817
-
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Environmental Pollutants
COX
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Inflammation/Immunology
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Methylhydroquinone is an orally active COX inhibitor with IC50s of 480.7 μM and 52.2 μM for ovine COX-1 and human recombinant COX-2, respectively. Methylhydroquinone has potential DNA damaging effects: 1) inhibiting COX-1 to reduce prostaglandin synthesis and exert anti-inflammatory activity; 2) inducing DNA single-strand breaks. Methylhydroquinone exerts its effects by competitively binding to the active sites of COX-1 (such as Tyr385, Met522) and non-covalent interactions .
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- HY-136265
-
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Aminoacyl-tRNA Synthetase
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Cancer
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BC-LI-0186 is a potent and selective inhibitor of Leucyl-tRNA synthetase (LRS; LeuRS) and Ras-related GTP-binding protein D (RagD) interaction (IC50=46.11 nM). BC-LI-0186 competitively binds to the RagD interacting site of LRS (Kd=42.1 nM) and has on effects on LRS-Vps34, LRS-EPRS, RagB-RagD association, mTORC1 complex formation or the activities of 12 kinases. BC-LI-0186 can effectively suppress the activity of cancer-associated?MTOR?mutants and the growth of rapamycin-resistant cancer cells.?BC-LI-0186 is a promising agent for lung cancer research .
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- HY-108831
-
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Integrin
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Inflammation/Immunology
Cancer
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Natalizumab (AN100226; BG00002) is a humanized monoclonal IgG4 antibody inhibitor that selectively targets α4 integrin (CD49d). It blocks the interaction of integrins such as α4β1 (VLA-4) with vascular cell adhesion molecule VCAM-1, intercellular adhesion molecule ICAM-1, and fibronectin by competitively binding to the α4 subunit. Natalizumab inhibits the adhesion, retention, and transendothelial migration of immune cells (such as CD4 + T cells), reducing the infiltration of inflammatory cells into the central nervous system or lesion sites, thus exerting anti-inflammatory and immunomodulatory activity. Natalizumab is used in the study of relapsing-remitting multiple sclerosis (RRMS) and also has applications in the study of autoimmune or inflammation-related diseases such as Crohn's disease, B-cell lymphoma, and non-infectious uveitis. Natalizumab can also prevent lymphocytes from entering the central nervous system, thereby preventing acute demyelinating relapses .
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- HY-138068
-
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Endogenous Metabolite
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Metabolic Disease
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L-Tryptophanylglycine is a dipeptide. L-Tryptophanylglycine exerts its function through competitive substrate interaction with intestinal dipeptide transporters .
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- HY-101503
-
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FABP
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Metabolic Disease
|
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HTS01037 is an inhibitor of fatty acid binding; and a competitive antagonist of protein-protein interactions mediated by AFABP/aP2 with a Ki of 0.67 μM.
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- HY-15716
-
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Ras
Apoptosis
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Cancer
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Kobe0065 is a novel and effective inhibitor of Ras-Raf interaction, competitively inhibiting the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46±13 μM.
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- HY-P2244A
-
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YAP
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Cancer
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YAP-TEAD-IN-1 TFA is a potent and competitive peptide inhibitor of YAP-TEAD interaction (IC50=25 nM). YAP-TEAD-IN-1 TFA is a 17mer peptide and shows a higher the binding affinity to TEAD1 (Kd=15 nM) than YAP (50-171) (Kd= 40 nM) .
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- HY-P2244
-
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YAP
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Cancer
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YAP-TEAD-IN-1 is a potent and competitive inhibitor of?YAP–TEAD interaction (IC50=25 nM). YAP-TEAD-IN-1 is a 17mer peptide and shows a higher the binding affinity to TEAD1 (Kd=15 nM) than YAP (50-171) (Kd=40 nM) .
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- HY-P1740A
-
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Integrin
Apoptosis
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Inflammation/Immunology
Cancer
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RGD peptide (GRGDNP) TFA is an inhibitor of integrin-ligand interactions. RGD peptide (GRGDNP) TFA competitively inhibits α5β1 binding with extracellular matrice (ECM). RGD peptide (GRGDNP) TFA promotes apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing. RGD peptide (GRGDNP) TFA plays an important role in cell adhesion, migration, growth, and differentiation .
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- HY-P99463
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AVB-500; AVB-S6-500
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TAM Receptor
PI3K
Akt
p38 MAPK
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Cancer
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Batiraxcept (AVB-500; AVB-S6-500) is a selective, soluble AXL receptor and GAS6 inhibitor that targets the GAS6-AXL signaling axis. Batiraxcept is orally inactive and does not cross the blood-brain barrier. Batiraxcept competitively binds to GAS6 ((KD <1 nM), preventing its interaction with the AXL receptor tyrosine kinase, thereby inhibiting downstream PI3K/AKT and MAPK signaling pathways, reducing tumor cell glycolysis, angiogenesis, and metastatic potential. Batiraxcept has demonstrated antitumor activity in preclinical models of endometrial, cholangiocarcinoma, and ovarian cancer by inhibiting tumor growth, invasion, and metastasis .
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- HY-132309
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BRD0639
1 Publications Verification
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Histone Methyltransferase
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Cancer
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BRD0639 is a first-in-class inhibitor of the PRMT5-substrate adaptor interaction. BRD0639 is a PRMT5 binding motif (PBM)-competitive agent that can support studies of PBM dependent PRMT5 activities .
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- HY-P3245A
-
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Apoptosis
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Cancer
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HXR9 hydrochloride is a cell-permeable peptide and a competitive antagonist of HOX/PBX interaction. HXR9 hydrochloride antagonizes the interaction between HOX and a second transcrip-tion factor (PBX), which binds to HOX proteins in paralogue groups1 to 8. HXR9 hydrochloride selectively decreases cell proliferation and promotes apoptosis in cells with a high level of expression of the HOXA/PBX3 genes, such as MLL-rearranged leukemic cells .
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- HY-108935
-
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HIV Integrase
GLUT
Tyrosinase
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Cancer
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Lavendustin B is an inhibitor of HIV-1 integrase interaction with LEDGF/p75 with an IC50 of 94.07 μM. Lavendustin B is an ATP-competitive GLUT1 inhibitor with a Ki of 15 μM. Lavendustin B is also a weak inhibitor of tyrosine kinases .
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- HY-P3143
-
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PD-1/PD-L1
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Cancer
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BMSpep-57 is a potent and competitive macrocyclic peptide inhibitor of PD-1/PD-L1 interaction with an IC50 of 7.68 nM. BMSpep-57 binds to PD-L1 with Kds of 19 nM and 19.88 nM in MST and SPR assays, respectively. BMSpep-57 facilitates T cell function by in creasing IL-2 production in PBMCs .
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- HY-127024
-
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Thyroid Hormone Receptor
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Metabolic Disease
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Thyroid hormone receptor antagonist (1-850) is a competitive, selective and high-affinity thyroid hormone receptor (TR) antagonist with an IC50 of 1.5 μM for antagonizing the effect of T3 on TR. Thyroid hormone receptor antagonist (1-850) blocks T3-mediated interaction of TRα and TRβ with nuclear receptor coactivator. Thyroid hormone receptor antagonist (1-850) has no effect on the activity of RARα .
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- HY-161137
-
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Amino acid Transporter
iGluR
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Neurological Disease
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LQFM215 is a proline transporter (PROT) inhibitor. LQFM215 inhibits proline transport by competitively binding to the active site of PROT. LQFM215 effectively reduces hyperlocomotion and enhances social interaction .
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- HY-P11112
-
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β-catenin
Wnt
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Inflammation/Immunology
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PTD-DBM is a competitive peptide that blocks the CXXC5-Dvl interaction and induces the expression of β-catenin, α-SMA, and type I collagen. PTD-DBM has skin wound healing activity .
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- HY-P10886
-
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Gap Junction Protein
Claudin
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Inflammation/Immunology
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Zifogaptide is a gap junction protein channel regulator. Zifogaptide mimics the PDZ-binding motif at the C-terminal of Claudin C and competitively interferes with the interaction between Claudin–TJP1 (ZO-1) scaffold. Zifogaptide can promote epithelial cell migration, reduce scar formation, and accelerate wound healing. Zifogaptide can be used for radiation dermatitis, skin injuries, etc .
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- HY-17504R
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Rosuvastatin hemicalcium (Standard); ZD 4522 Calcium (Standard)
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Reference Standards
HMG-CoA Reductase (HMGCR)
Autophagy
Potassium Channel
Bacterial
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Cardiovascular Disease
Metabolic Disease
Cancer
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Rosuvastatin (Calcium) (Standard) is the analytical standard of Rosuvastatin (Calcium). This product is intended for research and analytical applications. Rosuvastatin Calcium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Calcium potently blocks hERG current with an IC50 of 195 nM . Rosuvastatin Calcium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Calcium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
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- HY-10860
-
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sFRP-1
Wnt
β-catenin
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Metabolic Disease
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WAY-362692 is a secreted frizzled-related protein (sFRP-1) inhibitor (IC50 of 0.02 μM), targeting the netrin domain of sFRP-1. WAY-362692 can competitively inhibit the interaction between sFRP-1 and Wnt proteins, and activate the Wnt/β-catenin signaling pathway (EC50 = 0.03 μM). WAY-362692 can activate osteoblasts and promote bone remodeling. WAY-362692 can be used for the research of metabolic disease, such as osteoporosis .
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- HY-P10582A
-
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MHC
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Inflammation/Immunology
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SIYNFEKL TFA is a variant of major MHC class I-restricted epitope SIINFEKL. SIYNFEKL TFA is an antigenic peptide, that can stimulate specific T cells in experimental settings to study the competitive interaction between T cell. SIYNFEKL TFA exhibits low affinity for the OT-I T cell receptor (TCR), and can be used for detection of CD8+ T cells .
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- HY-P10581A
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MHC
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Inflammation/Immunology
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SIIVFEKL TFA is a variant of the major MHC class I-restricted epitope SIINFEKL. SIIVFEKL TFA is an antigenic peptide, that can stimulate specific T cells in experimental settings to study the competitive interaction between T cells. SIIVFEKL TFA exhibits low affinity for the OT-I T cell receptor (TCR), and can be used for detection of CD8+ T cells .
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- HY-149308
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Macrophage migration inhibitory factor (MIF)
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Infection
|
|
MKA031 (compound 6y) is a non-competitive MIF inhibitor with an IC50 value of 1.7 μM. MKA031 (compound 6y) interferes with MIF/AIF interaction, MIF nuclear translocation, and N-methyl-N'-nitro-N-nitrosoguanidine (MNNG)-induced dependent cell death. MKA031 can be used in the study of chronic hepatitis C virus infection .
|
-
-
- HY-17504AS1
-
|
ZD 4522-d6
|
Isotope-Labeled Compounds
Autophagy
Bacterial
HMG-CoA Reductase (HMGCR)
Potassium Channel
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Rosuvastatin-d6 (ZD 4522-d6) is deuterium labeled Rosuvastatin. Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin potently blocks hERG current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
|
-
- HY-P3245
-
|
|
Apoptosis
|
Cancer
|
|
HXR9 is a cell-permeable peptide and a competitive antagonist of HOX/PBX interaction. HXR9 antagonizes the interaction between HOX and a second transcrip-tion factor (PBX), which binds to HOX proteins in paralogue groups1 to 8. HXR9 selectively decreases cell proliferation and promotes apoptosis in cells with a high level of expression of the HOXA/PBX3 genes, such as MLL-rearranged leukemic cells .
|
-
- HY-19374
-
|
|
GCGR
|
Metabolic Disease
|
|
BAY-27-9955 is an orally active non-peptide glucagon receptor antagonist. Bay 27-9955 competitively blocks the interaction of glucagon with the human glucagonreceptor at an IC50 value of 110 nM. BAY-27-9955 can be used for the study of type 2 diabetes .
|
-
- HY-P2477
-
|
|
PD-1/PD-L1
|
Inflammation/Immunology
|
|
Human PD-L1 inhibitor IV, a polypeptide, is a competitive human PD-1 protein inhibitor with a Kd value of 1.38 μM. Human PD-L1 inhibitor IV inhibits the interaction of hPD-1/hPD-L1 .
|
-
- HY-17504BS1
-
|
|
HMG-CoA Reductase (HMGCR)
Autophagy
|
Cardiovascular Disease
Metabolic Disease
|
|
Rosuvastatin-d6 sodium is deuterium labeled Rosuvastatin sodium (HY-17504B). Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Sodium potently blocks hERG current with an IC50 of 195 nM. Rosuvastatin Sodium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Sodium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.
|
-
- HY-W414334
-
|
|
DNA/RNA Synthesis
Fluorescent Dye
|
Cancer
|
|
ICR-191 dihydrochloride enhances Cisplatin (HY-17394)- DNA binding and sensitizes cells to cisplatin. ICR-191 dihydrochloride induces a significant increase in the expression of phosphorylated H2AX (γH2AX), particularly in DNA-replicating cells. ICR-191 dihydrochloride can be used for the study of leukemia .
|
-
- HY-125146
-
|
|
Wnt
|
Others
|
|
BMD4503-2 is a quinoxaline derivative with inhibitory activity against LRP5/6-sclerostin interactions. BMD4503-2 restores the activity of the Wnt/β-catenin signaling pathway by competitively binding to the LRP5/6-sclerostin complex. BMD4503-2 can be used in the study of Wnt signaling pathways in bone development, maintenance and osteoporosis .
|
-
- HY-P3143A
-
|
|
PD-1/PD-L1
|
Cancer
|
|
BMSpep-57 hydrochloride is a potent and competitive macrocyclic peptide inhibitor of PD-1/PD-L1 interaction with an IC50 of 7.68 nM. BMSpep-57 hydrochloride binds to PD-L1 with Kds of 19 nM and 19.88 nM in MST and SPR assays, respectively. BMSpep-57 hydrochloride facilitates T cell function by in creasing IL-2 production in PBMCs .
|
-
- HY-125916
-
|
|
Endogenous Metabolite
|
Cancer
|
|
Pseurotin A is a secondary metabolite of Aspergillus and other fungi. Pseurotin A is a competitive inhibitor of chitin synthase and a neuritogenic agent. Pseurotin A inhibits IgE production (IC50 = 3.6 μM). Pseurotin A inhibits the PCSK9-LDLr interaction. Pseurotin A shows dose-dependent reduction of PCSK9, along with increased LDLR levels in hormone-dependent breast cancer cell lines. Pseurotin A exhibits antitumor activity .
|
-
- HY-17504BR
-
|
ZD 4522 Sodium (Standard); X-Plended Sodium (Standard); Crestor Sodium (Standard)
|
HMG-CoA Reductase (HMGCR)
Potassium Channel
Autophagy
Bacterial
Reference Standards
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Rosuvastatin (Sodium) (Standard) is the analytical standard of Rosuvastatin (Sodium). This product is intended for research and analytical applications. Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Sodium potently blocks hERG current with an IC50 of 195 nM . Rosuvastatin Sodium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Sodium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
|
-
- HY-17504BS2
-
|
ZD 4522-13C,d3 sodium; X-Plended-13C,d3 sodium; Crestor-13C,d3 sodium
|
Autophagy
Bacterial
HMG-CoA Reductase (HMGCR)
Potassium Channel
Isotope-Labeled Compounds
|
Cardiovascular Disease
Metabolic Disease
|
|
Rosuvastatin- 13C,d3 sodium is 13C and deuterated labeled Rosuvastatin sodium (HY-17504B). Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Sodium potently blocks hERG current with an IC50 of 195 nM . Rosuvastatin Sodium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Sodium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
|
-
- HY-17504D
-
|
|
HMG-CoA Reductase (HMGCR)
Potassium Channel
Autophagy
|
Cardiovascular Disease
Metabolic Disease
|
|
(3S,5R)-Rosuvastatin is the (3S,5R)-enantiomer of Rosuvastatin. Rosuvastatin is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM . Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM . Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin is very effective in lowering low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
|
-
- HY-17504C
-
|
|
HMG-CoA Reductase (HMGCR)
Potassium Channel
Autophagy
|
Cardiovascular Disease
Metabolic Disease
|
|
(3R,5R)-Rosuvastatin is the (3R,5R)-enantiomer of Rosuvastatin. Rosuvastatin is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM . Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM . Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin is very effective in lowering low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
|
-
- HY-P11214
-
|
H-TL1
|
TNF Receptor
Integrin
NF-κB
ERK
p38 MAPK
JNK
Interleukin Related
|
Inflammation/Immunology
|
|
Hydrostatin-TL1 (H-TL1), a nine-amino-acid peptide, is a TNF-α antagonist. Hydrostatin-TL1 can be isolated from the venom gland of sea snake Hydrophis cyanocinctus. H-TL1 competitively inhibits the interaction between TNF-α/TNFR1 and attenuates the cytotoxicity and inflammation of TNF-α. Hydrostatin-TL1 can be used for TNF-α-associated inflammatory diseases, such as rheumatoid arthritis, osteoporosis and inflammatory bowel disease (IBD) research .
|
-
- HY-147879
-
-
- HY-128126
-
-
- HY-122564
-
|
|
Dynamin
|
Others
|
|
Pyrimidyn 7 is an inhibitor of dynamin I/II with IC50 values of 1.1 μM and 1.8 μM, respectively. Pyrimidyn 7 competitively inhibits the interactions between GTP and phospholipids with dynamin I. Additionally, Pyrimidyn 7 reversibly inhibits clathrin-mediated endocytosis (CME) of transferrin and epidermal growth factor (EGF) in various non-neuronal cell linecell [1.
|
-
- HY-19539
-
|
|
SOS1
Ras
|
Cancer
|
|
NSC-658497 is an effective inhibitor of Ras-GEF, SOS1. NSC-658497 binds to SOS1, competitively suppresses SOS1-Ras interaction, and dose-dependently inhibits SOS1 GEF activity. NSC-658497 showed dose-dependent efficacy in inhibiting Ras, downstream signaling activities, and associated cell proliferation .
|
-
- HY-W012817R
-
|
|
COX
Reference Standards
|
Others
|
|
Methylhydroquinone (Standard) is the analytical standard of Methylhydroquinone. This product is intended for research and analytical applications. Methylhydroquinone is an orally active COX inhibitor with IC50s of 480.7 μM and 52.2 μM for ovine COX-1 and human recombinant COX-2, respectively. Methylhydroquinone has potential DNA damaging effects: 1) inhibiting COX-1 to reduce prostaglandin synthesis and exert anti-inflammatory activity; 2) inducing DNA single-strand breaks. Methylhydroquinone exerts its effects by competitively binding to the active sites of COX-1 (such as Tyr385, Met522) and non-covalent interactions[1][2].
|
-
- HY-15222A
-
|
|
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
Menin-MLL inhibitor MI-2 dihydrochloride is a competitive and selective Menin-MLL interaction inhibitor with an IC50 value of 446 nM and a Ki value of 158 nM. Menin-MLL inhibitor MI-2 dihydrochloride downregulates the expression of target genes such as HOXA9 and MEIS1, inhibits proliferation of leukemia cells and induces apoptosis and differentiation. Menin-MLL inhibitor MI-2 dihydrochloride is proming for rasearch of MLL-rearranged acute leukemias (e.g., AML, ALL) .
|
-
- HY-159893
-
|
|
Smo
Hedgehog
Apoptosis
|
Cancer
|
|
SMO-IN-5 ((Compound 25(B31)) is a potent and competitive inhibitor of smoothened (SMO) that can inhibit Hedgehog (Hh) signaling. SMO-IN-5 interacts with Smo through hydrogen bonds, hydrophobic interactions, and electrostatic forces. SMO-IN-5 inhibits PC cell proliferation, migration, and induces apoptosis by suppressing Gli1 expression. SMO-IN-5 exhibits antitumor activity in pancreatic cancer. .
|
-
- HY-172662
-
|
|
Telomerase
|
Cancer
|
|
TRF1-TIN2 PPI-IN-1 (Compound 40) is a TRF1-TIN2 interaction inhibitor. TRF1-TIN2 PPI-IN-1 binds to the TRFH domain of TRF1 (KD = 29 μM) and competitively inhibits the binding of the TIN2 peptide (IC50 = 67 μM). TRF1-TIN2 PPI-IN-1 disrupts the interaction between TRF1 and TIN2 by occupying the hotspot region of the TRF1-TIN2 binding interface. TRF1-TIN2 PPI-IN-1 can expel TRF 1 from the shelterin complex and can be used to study shelterin-related cancers .
|
-
- HY-100834A
-
|
5,7-DCKA sodium
|
iGluR
|
Neurological Disease
|
|
5,7-Dichlorokynurenic acid (5,7-DCKA) sodium is a selective and competitive antagonist of the glycine site on NMDA receptor with a KB of 65 nM. 5,7-Dichlorokynurenic acid sodium reduces NMDA-induced neuron injury. 5,7-Dichlorokynurenic acid sodium increases social interaction time, increases open arm exploration time, disinhibits suppressed conflict responding in rodent models. 5,7-Dichlorokynurenic acid sodium exhibits anxiolytic-like activity in rodent models and supports exploration of glycine’s role in NMDA receptor-mediated synaptic transmission .
|
-
- HY-110196
-
|
|
Histone Methyltransferase
|
Others
|
|
(S)-PFI-2 hydrochloride is an inhibitor of lysine methyltransferase SETD7 and is approximately 500-fold more active than its enantiomer (R)-PFI-2. (R)-PFI-2 is a cofactor-dependent and substrate-competitive inhibitor. (R)-PFI-2 can occupy the substrate peptide binding groove of SETD7 (including the catalytic lysine binding channel) and interact with the cofactor The donor methyl group is in direct contact. However, (S)-PFI-2 was not observed to have the same interaction as (R)-PFI-2 .
|
-
- HY-160478
-
|
|
Bcr-Abl
|
Cancer
|
|
GNF-6 (Compound 14) inhibits the gatekeeper threonine residue mutation of BCR-ABL-T315I with IC50s of 0.25 μM, 0.09 μM and 0.590 μM for c-ABL-T334I, BCR-ABL and BCR-ABL-T315I variants, respectively. GNF-6, an ATP competitive inhibitor, disrupts the assembly of the hydrophobic spine (a network of hydrophobic interactions), thereby locking the kinase in an inactive ‘DFG-out’ conformation .
|
-
- HY-133233
-
|
1-Palmitylthio-2-palmitoylamido-1,2-dideoxy-sn-glycero-3-phosphorylcholine
|
Endogenous Metabolite
Phospholipase
|
Metabolic Disease
|
|
Thioetheramide-PC (1-Palmitylthio-2-palmitoylamido-1,2-dideoxy-sn-glycero-3-phosphorylcholine) is a structurally modified phospholipid that acts as a competitive, reversible inhibitor of secretory phospholipase A2 (sPLA2). Thioetheramide-PC has an IC50 value of 2 μM at a substrate concentration of 0.5 mM. In addition to binding to the catalytic site of sPLA2, Thioetheramide-PC also binds to the activation site of the enzyme. Thioetheramide-PC binds more tightly to the activation site than to the catalytic site. As a result of this dual interaction, at low concentrations, Thioetheramide-PC may activate phospholipase activity rather than inhibit it.
|
-
- HY-100834R
-
|
5,7-DCKA (Standard)
|
Reference Standards
iGluR
|
Neurological Disease
|
|
5,7-Dichlorokynurenic acid (Standard) is the analytical standard of 5,7-Dichlorokynurenic acid (HY-100834). This product is intended for research and analytical applications. 5,7-Dichlorokynurenic acid (5,7-DCKA) is a selective and competitive antagonist of the glycine site on NMDA receptor with a KB of 65 nM. 5,7-Dichlorokynurenic acid reduces NMDA-induced neuron injury. 5,7-Dichlorokynurenic acid increases social interaction time, increases open arm exploration time, disinhibits suppressed conflict responding in rodent models. 5,7-Dichlorokynurenic acid exhibits anxiolytic-like activity in rodent models and supports exploration of glycine’s role in NMDA receptor-mediated synaptic transmission .
|
-
- HY-161547
-
|
|
Antibiotic
Biochemical Assay Reagents
|
Others
|
Tetracycline/BSA is a tetracycline-carrier protein conjugate of Tetracycline (HY-A0107) and bovine serum albumin (BSA). Tetracycline/BSA can be used as an immobilized capture antigen for the detection of tetracycline residues in milk .
|
-
- HY-N0481R
-
|
|
Reference Standards
COX
TNF Receptor
NO Synthase
Interleukin Related
NF-κB
Apoptosis
p38 MAPK
JNK
ERK
Keap1-Nrf2
RANKL/RANK
|
Inflammation/Immunology
|
|
Roburic acid (Standard) is the analytical standard of Roburic acid. This product is intended for research and analytical applications. Roburic acid acts as an anti-inflammatory, anti-tumor and osteoclastogenesis inhibitor, with a Ki of 7.066 μM against human TNF, an IC50 of 9 μM against human COX-2, and an IC50 of 5 μM against ovine COX-1. Roburic acid reduces the production of inflammatory mediators such as NO and IL-6 in macrophages by inhibiting the NF-κB and MAPK (p38/JNK) pathways. By competitively inhibiting the TNF-TNF-R1 interaction, Roburic acid blocks the downstream NF-κB signaling pathway, thereby inducing cell cycle arrest and apoptosis in cancer cells. Roburic acid specifically inhibits osteoclastogenesis and bone resorption by suppressing the RANKL/TRAF6/NF-κB/NFATc1 axis. Roburic acid can be used in research related to osteolytic diseases such as osteoporosis, colorectal cancer and inflammatory diseases.
|
-
- HY-W457608
-
|
|
Drug Derivative
|
Cancer
|
|
CU7218 competitively binds to the phosphopeptide-binding pocket of 14-3-3ε and blocks its interaction with the 9J10 peptide. CU7218 can be used in cancer research .
|
-
- HY-181824
-
|
|
Bacterial
|
Infection
|
|
Cholera toxin-IN-1 is a potent competitive inhibitor of cholera toxin B subunit (CTB) with an IC50 value of 11.78 μM. Cholera toxin-IN-1 forms stable hydrogen bonds and hydrophobic interactions. Cholera toxin-IN-1 competitively blocks the binding of CTB to GM1 ganglioside. Cholera toxin-IN-1 can be used for the research of cholera .
|
-
- HY-101503R
-
|
|
FABP
Reference Standards
|
Metabolic Disease
|
|
HTS01037 (Standard) is the analytical standard of HTS01037 (HY-101503). This product is intended for research and analytical applications. HTS01037 is an inhibitor of fatty acid binding; and a competitive antagonist of protein-protein interactions mediated by AFABP/aP2 with a Ki of 0.67 μM.
|
-
- HY-180222
-
|
|
CDK
|
Cancer
|
|
KGA-4066 is a novel non-ATP-competitive CDK2 inhibitor. KGA-4066 inhibits CDK2/Cyclin A2 with an IC50 value of 236.7 nM, disrupts their interaction, promots CDK2 degradation via the lysosomal pathway. KGA-4066 has anticancer activity against hepatocellular carcinoma .
|
-
- HY-179091
-
|
|
PARP
|
Cancer
|
|
CU-TZD-20 is a PARP-1 inhibitor. CU-TZD-20 has a high affinity for binding to the PARP-1 catalytic domain and good structural stability. CU-TZD-20 competitively occupies NAD + binding sites and forms stable interactions with key catalytic residues. CU-TZD-20 can be used for cancer research .
|
-
- HY-107597R
-
|
SU3327 (Standard)
|
Reference Standards
JNK
|
Metabolic Disease
Inflammation/Immunology
|
|
Halicin (Standard) is the analytical standard of Halicin (HY-107597). This product is intended for research and analytical applications. Halicin (SU3327) is a potent, selective and substrate-competitive JNK inhibitor with an IC50 of 0.7 μM. Halicin also inhibits protein-protein interactions between JNK and JNK Interacting Protein (JIP) with an IC50 of 239 nM. Halicin shows less active against p38α and Akt Kinase .
|
-
- HY-183344
-
|
|
Interleukin Related
|
Inflammation/Immunology
|
|
IL-1β-IN-4 is a selective IL-1β competitive binder. IL-1β-IN-4 interferes with the interaction between IL-1β and its cognate receptor IL-1R1, with an IC50 of 8.3 μM. IL-1β-IN-4 can be used in studies related to inflammatory and immune diseases .
|
-
- HY-N17639
-
|
|
TGF-beta/Smad
TGF-β Receptor
|
Others
|
|
Regiafuran C is a compound with both TGF-βRI inhibitory and anti-fibrotic activities. Regiafuran C effectively inhibits renal fibrosis by binding to TGF-βRI and interfering with the TGF-β/Smad and Wnt/β-catenin signaling pathways. Regiafuran C also exhibits free radical scavenging activity, but shows no anti-inflammatory activity in PGE2 competitive enzyme immunoassays. The ability of Regiafuran C to specifically block the Smad3-TGF-βRII interaction and inhibit fibrotic processes allows its use in renal fibrosis research .
|
-
- HY-181759
-
|
|
Ligands for Target Protein for PROTAC
Epigenetic Reader Domain
Histone Acetyltransferase
|
Cancer
|
|
CBP/p300/BRD4 ligand-1 is a small-molecule inhibitor targeting CBP, p300, and BRD4. CBP/p300/BRD4 ligand-1 competitively binds to the functional domains of target proteins without disrupting key interactions. CBP/p300/BRD4 ligand-1 can be used for the construction of dual-target PROTAC degraders (HY-181758) in studies related to prostate cancer and other cancers .
|
-
- HY-100034R
-
|
DA-3003-1 (Standard)
|
Phosphatase
Reference Standards
Histone Methyltransferase
|
Cancer
|
|
NSC 663284 (Standard) is the analytical standard of NSC 663284 (HY-100034). This product is intended for research and analytical applications. NSC 663284 (DA-3003-1) is a potent, cell-permeable, and irreversible Cdc25 dual specificity phosphatase inhibitor, has an IC50 for Cdc25B2 of 0.21 μM. NSC 663284 exhibits mixed competitive kinetics against Cdc25A, Cdc25B(2), and Cdc25C with Ki values of 29, 95, and 89 nM, respectively . NSC 663284 inhibits NSD2 (IC50 of 170 nM) through a direct interaction with the catalytic SET domain (Kd of 370 nM) .
|
-
- HY-100903R
-
|
nor-Binaltorphimine dihydrochloride (Standard); nor-BNI dihydrochloride (Standard)
|
Opioid Receptor
Reference Standards
|
Neurological Disease
|
|
Norbinaltorphimine dihydrochloride (Standard) is the analytical standard of Norbinaltorphimine dihydrochloride (HY-100903). This product is intended for research and analytical applications. Norbinaltorphimine dihydrochloride (nor-Binaltorphimine dihydrochloride; nor-BNI dihydrochloride) is a selective, long-acting competitive antagonist of the κ-opioid receptor. Norbinaltorphimine dihydrochloride blocks κ-opioid receptor-mediated analgesic effects, and inhibits butorphanol-induced changes in κ-opioid receptor binding kinetics, desensitization and down-regulation. Norbinaltorphimine dihydrochloride suppresses specific opioid withdrawal symptoms, precipitates withdrawal behaviors in butorphanol-dependent rats, and serves as a molecular probe for studying κ-opioid receptor-agonist interactions. Norbinaltorphimine dihydrochloride is applicable to research related to neurological disorders such as pain .
|
-
- HY-180197
-
|
|
PKC
iGluR
Reactive Oxygen Species (ROS)
|
Cardiovascular Disease
Neurological Disease
|
|
PICK1 PDZ-IN-1 (Compound 6b) is a selective and brain-penetrant protein interacting with C kinase 1 (PICK1) PDZ domain inhibitor with a Ki of 27.73 μM. PICK1 PDZ-IN-1 can competitively inhibit the interaction between PICK1 and the GluA2 subunit of AMPA receptors. PICK1 PDZ-IN-1 can increase the survival rate of HT22 cells and primary cortical neuron cells induced by glutamate and inhibit ROS production. PICK1 PDZ-IN-1 exhibits neuroprotective effect and reduces the area of cerebral infarction. PICK1 PDZ-IN-1 can be used for the research of ischemic stroke .
|
-
- HY-171216
-
|
|
Integrin
|
Neurological Disease
|
|
GW559090 is a selective, competitive, and high-affinity α4 integrin antagonist with a Kd of 0.19 nM for α4β1. GW559090 can effectively block the binding of α4β1 to vascular cell adhesion molecule 1 (VCAM-1) and fibronectin with IC50 values of 7.72 and 8.04 nM. GW559090 also inhibits the interaction between α4β7 and mucosal addressin cell adhesion molecule 1 (MAdCAM-1) (IC50 = 23 nM). GW559090 can inhibit inflammatory infiltration in the eyes, repair the corneal barrier and restore the function of goblet cells. GW559090 can be used for research of Sjögren's syndrome associated dry eye .
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-161547
-
|
|
Biochemical Assay Reagents
|
Tetracycline/BSA is a tetracycline-carrier protein conjugate of Tetracycline (HY-A0107) and bovine serum albumin (BSA). Tetracycline/BSA can be used as an immobilized capture antigen for the detection of tetracycline residues in milk .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P1740
-
|
|
Integrin
Apoptosis
Caspase
|
Inflammation/Immunology
|
|
RGD peptide (GRGDNP) is an inhibitor of integrin-ligand interactions. RGD peptide (GRGDNP) competitively inhibits α5β1 binding with extracellular matrice (ECM). RGD peptide (GRGDNP) promotes apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing. RGD peptide (GRGDNP) plays an important role in cell adhesion, migration, growth, and differentiation .
|
-
- HY-P2244A
-
|
|
YAP
|
Cancer
|
|
YAP-TEAD-IN-1 TFA is a potent and competitive peptide inhibitor of YAP-TEAD interaction (IC50=25 nM). YAP-TEAD-IN-1 TFA is a 17mer peptide and shows a higher the binding affinity to TEAD1 (Kd=15 nM) than YAP (50-171) (Kd= 40 nM) .
|
-
- HY-P2244
-
|
|
YAP
|
Cancer
|
|
YAP-TEAD-IN-1 is a potent and competitive inhibitor of?YAP–TEAD interaction (IC50=25 nM). YAP-TEAD-IN-1 is a 17mer peptide and shows a higher the binding affinity to TEAD1 (Kd=15 nM) than YAP (50-171) (Kd=40 nM) .
|
-
- HY-P1740A
-
|
|
Integrin
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
RGD peptide (GRGDNP) TFA is an inhibitor of integrin-ligand interactions. RGD peptide (GRGDNP) TFA competitively inhibits α5β1 binding with extracellular matrice (ECM). RGD peptide (GRGDNP) TFA promotes apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing. RGD peptide (GRGDNP) TFA plays an important role in cell adhesion, migration, growth, and differentiation .
|
-
- HY-P3245A
-
|
|
Apoptosis
|
Cancer
|
|
HXR9 hydrochloride is a cell-permeable peptide and a competitive antagonist of HOX/PBX interaction. HXR9 hydrochloride antagonizes the interaction between HOX and a second transcrip-tion factor (PBX), which binds to HOX proteins in paralogue groups1 to 8. HXR9 hydrochloride selectively decreases cell proliferation and promotes apoptosis in cells with a high level of expression of the HOXA/PBX3 genes, such as MLL-rearranged leukemic cells .
|
-
- HY-P3143
-
|
|
PD-1/PD-L1
|
Cancer
|
|
BMSpep-57 is a potent and competitive macrocyclic peptide inhibitor of PD-1/PD-L1 interaction with an IC50 of 7.68 nM. BMSpep-57 binds to PD-L1 with Kds of 19 nM and 19.88 nM in MST and SPR assays, respectively. BMSpep-57 facilitates T cell function by in creasing IL-2 production in PBMCs .
|
-
- HY-P11112
-
|
|
β-catenin
Wnt
|
Inflammation/Immunology
|
|
PTD-DBM is a competitive peptide that blocks the CXXC5-Dvl interaction and induces the expression of β-catenin, α-SMA, and type I collagen. PTD-DBM has skin wound healing activity .
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-
- HY-P10886
-
|
|
Gap Junction Protein
Claudin
|
Inflammation/Immunology
|
|
Zifogaptide is a gap junction protein channel regulator. Zifogaptide mimics the PDZ-binding motif at the C-terminal of Claudin C and competitively interferes with the interaction between Claudin–TJP1 (ZO-1) scaffold. Zifogaptide can promote epithelial cell migration, reduce scar formation, and accelerate wound healing. Zifogaptide can be used for radiation dermatitis, skin injuries, etc .
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- HY-P10582A
-
|
|
MHC
|
Inflammation/Immunology
|
|
SIYNFEKL TFA is a variant of major MHC class I-restricted epitope SIINFEKL. SIYNFEKL TFA is an antigenic peptide, that can stimulate specific T cells in experimental settings to study the competitive interaction between T cell. SIYNFEKL TFA exhibits low affinity for the OT-I T cell receptor (TCR), and can be used for detection of CD8+ T cells .
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-
- HY-P10581A
-
|
|
MHC
|
Inflammation/Immunology
|
|
SIIVFEKL TFA is a variant of the major MHC class I-restricted epitope SIINFEKL. SIIVFEKL TFA is an antigenic peptide, that can stimulate specific T cells in experimental settings to study the competitive interaction between T cells. SIIVFEKL TFA exhibits low affinity for the OT-I T cell receptor (TCR), and can be used for detection of CD8+ T cells .
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-
- HY-P3245
-
|
|
Apoptosis
|
Cancer
|
|
HXR9 is a cell-permeable peptide and a competitive antagonist of HOX/PBX interaction. HXR9 antagonizes the interaction between HOX and a second transcrip-tion factor (PBX), which binds to HOX proteins in paralogue groups1 to 8. HXR9 selectively decreases cell proliferation and promotes apoptosis in cells with a high level of expression of the HOXA/PBX3 genes, such as MLL-rearranged leukemic cells .
|
-
- HY-P2477
-
|
|
PD-1/PD-L1
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Inflammation/Immunology
|
|
Human PD-L1 inhibitor IV, a polypeptide, is a competitive human PD-1 protein inhibitor with a Kd value of 1.38 μM. Human PD-L1 inhibitor IV inhibits the interaction of hPD-1/hPD-L1 .
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-
- HY-P3143A
-
|
|
PD-1/PD-L1
|
Cancer
|
|
BMSpep-57 hydrochloride is a potent and competitive macrocyclic peptide inhibitor of PD-1/PD-L1 interaction with an IC50 of 7.68 nM. BMSpep-57 hydrochloride binds to PD-L1 with Kds of 19 nM and 19.88 nM in MST and SPR assays, respectively. BMSpep-57 hydrochloride facilitates T cell function by in creasing IL-2 production in PBMCs .
|
-
- HY-P11214
-
|
H-TL1
|
TNF Receptor
Integrin
NF-κB
ERK
p38 MAPK
JNK
Interleukin Related
|
Inflammation/Immunology
|
|
Hydrostatin-TL1 (H-TL1), a nine-amino-acid peptide, is a TNF-α antagonist. Hydrostatin-TL1 can be isolated from the venom gland of sea snake Hydrophis cyanocinctus. H-TL1 competitively inhibits the interaction between TNF-α/TNFR1 and attenuates the cytotoxicity and inflammation of TNF-α. Hydrostatin-TL1 can be used for TNF-α-associated inflammatory diseases, such as rheumatoid arthritis, osteoporosis and inflammatory bowel disease (IBD) research .
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| Cat. No. |
Product Name |
Target |
Research Area |
Image |
-
- HY-P99675
-
|
AK112
|
PD-1/PD-L1
VEGFR
|
Cancer
|
|
Ivonescimab (AK112) is a PD-1/VEGF bispecific antibody. Ivonescimab competitively inhibiting PD-1/PD-L1 interaction, reversing the immunosuppression mediated by it, and blocks the binding of VEGF-A to VEGFR2, inhibiting tumour angiogenesis in the tumour microenvironment. Ivonescimab also has significantly anticancer activity against EGFR-mutated locally advanced or metastatic non-squamous non-small cell lung cancer (NSCL) .
|
-
(5)
-
- HY-P99014
-
|
ARGX-110
|
Fc Receptor (FcR)
NF-κB
|
Inflammation/Immunology
Cancer
|
|
Cusatuzumab (ARGX-110) is a selective competitive blocker targeting CD70 (with an equilibrium dissociation constant of 17 pM for binding to human CD70). Cusatuzumab also possesses enhanced antibody-dependent cell-mediated cytotoxicity (ADCC) activity. It is a humanized IgG1 monoclonal antibody, artificially synthesized through humanization and genetic engineering modifications (CH2 region mutation to enhance effector function). Cusatuzumab has a dual mechanism of action: firstly, it competitively blocks the interaction between CD70 and CD27, inhibiting the CD27-NF-κB signaling pathway, reducing regulatory T cell (Treg) activation and tumor cell proliferation; secondly, by enhancing binding to FcγRIIIa, it mediates ADCC and antibody-dependent cellular phagocytosis (ADCP), directly lysing CD70-positive tumor cells. Cusatuzumab can efficiently eliminate leukemia stem cells (LSCs), induce tumor cell differentiation and apoptosis, restore immune surveillance, and target CD70-positive tumors. Cusatuzumab is used in the study of acute myeloid leukemia (AML) .
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-
(5)
-
- HY-108831A
-
|
AN100226; BG00002
|
Integrin
|
Inflammation/Immunology
Cancer
|
|
Natalizumab (Anti-CD49d) (AN100226; BG00002) Solution is a humanized monoclonal IgG4 antibody inhibitor that selectively targets α4 integrin (CD49d), blocking the interaction of integrins such as α4β1 (VLA-4) with vascular cell adhesion molecule VCAM-1, intercellular adhesion molecule ICAM-1, and fibronectin by competitively binding to the α4 subunit. Natalizumab solution inhibits the adhesion, retention, and transendothelial migration of immune cells (such as CD4 + T cells), reducing the infiltration of inflammatory cells into the central nervous system or lesion sites, thereby exerting anti-inflammatory and immunomodulatory activity. Natalizumab (Anti-CD49d) solution is used in the study of relapsing-remitting multiple sclerosis (RRMS) and is also applied in the research of autoimmune or inflammation-related diseases such as Crohn's disease, B-cell lymphoma, and non-infectious uveitis. Natalizumab (Anti-CD49d) can also prevent lymphocytes from entering the central nervous system, thus preventing acute demyelinating relapses .
|
-
(5)
-
- HY-P99345
-
|
TSR-042; ANB-011; WBP-285
|
PD-1/PD-L1
|
Cancer
|
|
Dostarlimab (TSR-042) is a humanized anti-PD-1 monoclonal antibody. Dostarlimab binds with high affinity to human PD-1 and competitively inhibits its interaction with its ligands, PD-L1 and PD-L2, with IC50s of 1.8 and 1.5 nM, respectively .
|
-
(5)
-
- HY-108831
-
|
|
Integrin
|
Inflammation/Immunology
Cancer
|
|
Natalizumab (AN100226; BG00002) is a humanized monoclonal IgG4 antibody inhibitor that selectively targets α4 integrin (CD49d). It blocks the interaction of integrins such as α4β1 (VLA-4) with vascular cell adhesion molecule VCAM-1, intercellular adhesion molecule ICAM-1, and fibronectin by competitively binding to the α4 subunit. Natalizumab inhibits the adhesion, retention, and transendothelial migration of immune cells (such as CD4 + T cells), reducing the infiltration of inflammatory cells into the central nervous system or lesion sites, thus exerting anti-inflammatory and immunomodulatory activity. Natalizumab is used in the study of relapsing-remitting multiple sclerosis (RRMS) and also has applications in the study of autoimmune or inflammation-related diseases such as Crohn's disease, B-cell lymphoma, and non-infectious uveitis. Natalizumab can also prevent lymphocytes from entering the central nervous system, thereby preventing acute demyelinating relapses .
|
-
(5)
-
- HY-P99463
-
|
AVB-500; AVB-S6-500
|
TAM Receptor
PI3K
Akt
p38 MAPK
|
Cancer
|
|
Batiraxcept (AVB-500; AVB-S6-500) is a selective, soluble AXL receptor and GAS6 inhibitor that targets the GAS6-AXL signaling axis. Batiraxcept is orally inactive and does not cross the blood-brain barrier. Batiraxcept competitively binds to GAS6 ((KD <1 nM), preventing its interaction with the AXL receptor tyrosine kinase, thereby inhibiting downstream PI3K/AKT and MAPK signaling pathways, reducing tumor cell glycolysis, angiogenesis, and metastatic potential. Batiraxcept has demonstrated antitumor activity in preclinical models of endometrial, cholangiocarcinoma, and ovarian cancer by inhibiting tumor growth, invasion, and metastasis .
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-
(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N0481
-
-
-
- HY-131592
-
-
-
- HY-113352
-
-
-
- HY-W012817
-
-
-
- HY-125916
-
-
-
- HY-W012817R
-
|
|
Natural Products
Microorganisms
Source Classification
|
COX
Reference Standards
|
|
Methylhydroquinone (Standard) is the analytical standard of Methylhydroquinone. This product is intended for research and analytical applications. Methylhydroquinone is an orally active COX inhibitor with IC50s of 480.7 μM and 52.2 μM for ovine COX-1 and human recombinant COX-2, respectively. Methylhydroquinone has potential DNA damaging effects: 1) inhibiting COX-1 to reduce prostaglandin synthesis and exert anti-inflammatory activity; 2) inducing DNA single-strand breaks. Methylhydroquinone exerts its effects by competitively binding to the active sites of COX-1 (such as Tyr385, Met522) and non-covalent interactions[1][2].
|
-
-
- HY-N0481R
-
|
|
Triterpenes
Structural Classification
Gentiana macrophylla Pall.
Terpenoids
Gentianaceae
Plants
Source Classification
|
Reference Standards
COX
TNF Receptor
NO Synthase
Interleukin Related
NF-κB
Apoptosis
p38 MAPK
JNK
ERK
Keap1-Nrf2
RANKL/RANK
|
|
Roburic acid (Standard) is the analytical standard of Roburic acid. This product is intended for research and analytical applications. Roburic acid acts as an anti-inflammatory, anti-tumor and osteoclastogenesis inhibitor, with a Ki of 7.066 μM against human TNF, an IC50 of 9 μM against human COX-2, and an IC50 of 5 μM against ovine COX-1. Roburic acid reduces the production of inflammatory mediators such as NO and IL-6 in macrophages by inhibiting the NF-κB and MAPK (p38/JNK) pathways. By competitively inhibiting the TNF-TNF-R1 interaction, Roburic acid blocks the downstream NF-κB signaling pathway, thereby inducing cell cycle arrest and apoptosis in cancer cells. Roburic acid specifically inhibits osteoclastogenesis and bone resorption by suppressing the RANKL/TRAF6/NF-κB/NFATc1 axis. Roburic acid can be used in research related to osteolytic diseases such as osteoporosis, colorectal cancer and inflammatory diseases.
|
-
-
- HY-N17639
-
|
|
Structural Classification
Phenols
Polyphenols
Plants
Moraceae
Morus alba Linn.
Source Classification
|
TGF-beta/Smad
TGF-β Receptor
|
|
Regiafuran C is a compound with both TGF-βRI inhibitory and anti-fibrotic activities. Regiafuran C effectively inhibits renal fibrosis by binding to TGF-βRI and interfering with the TGF-β/Smad and Wnt/β-catenin signaling pathways. Regiafuran C also exhibits free radical scavenging activity, but shows no anti-inflammatory activity in PGE2 competitive enzyme immunoassays. The ability of Regiafuran C to specifically block the Smad3-TGF-βRII interaction and inhibit fibrotic processes allows its use in renal fibrosis research .
|
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-17504AS1
-
|
|
|
Rosuvastatin-d6 (ZD 4522-d6) is deuterium labeled Rosuvastatin. Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin potently blocks hERG current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
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-
-
- HY-17504BS1
-
|
|
|
Rosuvastatin-d6 sodium is deuterium labeled Rosuvastatin sodium (HY-17504B). Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Sodium potently blocks hERG current with an IC50 of 195 nM. Rosuvastatin Sodium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Sodium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.
|
-
-
- HY-17504BS2
-
|
|
|
Rosuvastatin- 13C,d3 sodium is 13C and deuterated labeled Rosuvastatin sodium (HY-17504B). Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Sodium potently blocks hERG current with an IC50 of 195 nM . Rosuvastatin Sodium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Sodium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
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