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Competitive interactions

" in MedChemExpress (MCE) Product Catalog:

91

Inhibitors & Agonists

1

Biochemical Assay Reagents

14

Peptides

6

Inhibitory Antibodies

8

Natural
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3

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-17504
    Rosuvastatin Calcium
    Maximum Cited Publications
    24 Publications Verification

    Rosuvastatin hemicalcium; ZD 4522 Calcium

    HMG-CoA Reductase (HMGCR) Autophagy Potassium Channel Bacterial Cardiovascular Disease Metabolic Disease Cancer
    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 .
    Rosuvastatin Calcium
  • HY-16993
    OICR-9429
    10+ Cited Publications

    Apoptosis WDR5 Cancer
    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) .
    OICR-9429
  • HY-P99675
    Ivonescimab
    1 Publications Verification

    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) .
    Ivonescimab
  • HY-17504A
    Rosuvastatin
    Maximum Cited Publications
    24 Publications Verification

    ZD 4522

    HMG-CoA Reductase (HMGCR) Autophagy Potassium Channel Bacterial Cardiovascular Disease Metabolic Disease Cancer
    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 .
    Rosuvastatin
  • HY-124817
    Col003
    5+ Cited Publications

    HSP Inflammation/Immunology
    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
    Col003
  • HY-P1740
    RGD peptide (GRGDNP)
    Maximum Cited Publications
    7 Publications Verification

    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 .
    RGD peptide (GRGDNP)
  • HY-P99014
    Cusatuzumab
    1 Publications Verification

    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) .
    Cusatuzumab
  • HY-17504B
    Rosuvastatin Sodium
    Maximum Cited Publications
    24 Publications Verification

    ZD 4522 Sodium; X-Plended Sodium; Crestor Sodium

    HMG-CoA Reductase (HMGCR) Potassium Channel Autophagy Bacterial Cardiovascular Disease Metabolic Disease Cancer
    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 .
    Rosuvastatin Sodium
  • HY-12583
    A-366
    5+ Cited Publications

    Histone Methyltransferase Epigenetic Reader Domain Cancer
    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 .
    A-366
  • HY-108831A
    Natalizumab (Anti-CD49d)
    3 Publications Verification

    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 .
    Natalizumab (Anti-CD49d)
  • HY-111126
    K67
    1 Publications Verification

    p62 Keap1-Nrf2 Cancer
    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 .
    K67
  • HY-N0481
    Roburic acid
    1 Publications Verification

    COX TNF Receptor NO Synthase Interleukin Related NF-κB Apoptosis p38 MAPK JNK ERK Keap1-Nrf2 RANKL/RANK Neurological Disease Inflammation/Immunology Cancer
    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 .
    Roburic acid
  • HY-19541
    I-CBP112
    5 Publications Verification

    Histone Acetyltransferase Epigenetic Reader Domain Cancer
    I-CBP112, a chemical probe, is a specific and potent acetyl-lysine competitive protein-protein interaction inhibitor, that inhibits the CBP/p300 bromodomains, enhances acetylation by p300.
    I-CBP112
  • HY-100834
    5,7-Dichlorokynurenic acid
    1 Publications Verification

    5,7-DCKA

    iGluR Neurological Disease
    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 .
    5,7-Dichlorokynurenic acid
  • HY-107597
    Halicin
    2 Publications Verification

    SU3327

    JNK Metabolic Disease Inflammation/Immunology
    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 .
    Halicin
  • HY-15222
    Menin-MLL inhibitor MI-2
    4 Publications Verification

    Epigenetic Reader Domain Apoptosis Cancer
    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) .
    Menin-MLL inhibitor MI-2
  • HY-19347
    WDR5-0103
    1 Publications Verification

    WD-Repeat Protein 5-0103

    WDR5 Neurological Disease Cancer
    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 .
    WDR5-0103
  • HY-100034
    NSC 663284
    5+ Cited Publications

    DA-3003-1

    Phosphatase Histone Methyltransferase Cancer
    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) .
    NSC 663284
  • HY-100903

    nor-Binaltorphimine dihydrochloride; nor-BNI dihydrochloride

    Opioid Receptor Neurological Disease
    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 .
    Norbinaltorphimine dihydrochloride
  • HY-117040
    nor-Binaltorphimine
    5+ Cited Publications

    Norbinaltorphimine; NorBNI

    Opioid Receptor Neurological Disease
    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 .
    nor-Binaltorphimine
  • HY-13032B
    Molibresib besylate
    20+ Cited Publications

    GSK 525762C; I-BET 762 besylate

    Epigenetic Reader Domain ERK Cancer
    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 .
    Molibresib besylate
  • HY-124828
    CMLD-2
    2 Publications Verification

    HuR Cancer
    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 .
    CMLD-2
  • HY-131592
    Tricetin
    1 Publications Verification

    Apoptosis Keap1-Nrf2 Neurological Disease Inflammation/Immunology Cancer
    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 .
    Tricetin
  • HY-122866
    ZT-12-037-01
    1 Publications Verification

    Ras Cancer
    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 .
    ZT-12-037-01
  • 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 .
    Dostarlimab
  • HY-113352

    Endogenous Metabolite PARP Cancer
    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 .
    7-Methylguanine
  • HY-W012817

    Environmental Pollutants COX Inflammation/Immunology
    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 .
    Methylhydroquinone
  • HY-136265
    BC-LI-0186
    1 Publications Verification

    Aminoacyl-tRNA Synthetase Cancer
    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 .
    BC-LI-0186
  • HY-108831
    Natalizumab
    3 Publications Verification

    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 .
    Natalizumab
  • HY-138068

    Endogenous Metabolite Metabolic Disease
    L-Tryptophanylglycine is a dipeptide. L-Tryptophanylglycine exerts its function through competitive substrate interaction with intestinal dipeptide transporters .
    L-Tryptophanylglycine
  • HY-101503
    HTS01037
    1 Publications Verification

    FABP Metabolic Disease
    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.
    HTS01037
  • HY-15716
    Kobe0065
    4 Publications Verification

    Ras Apoptosis Cancer
    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.
    Kobe0065
  • HY-P2244A
    YAP-TEAD-IN-1 TFA
    2 Publications Verification

    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) .
    YAP-TEAD-IN-1 TFA
  • HY-P2244
    YAP-TEAD-IN-1
    2 Publications Verification

    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) .
    YAP-TEAD-IN-1
  • HY-P1740A
    RGD peptide (GRGDNP) TFA
    Maximum Cited Publications
    7 Publications Verification

    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 .
    RGD peptide (GRGDNP) TFA
  • HY-P99463
    Batiraxcept
    2 Publications Verification

    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 .
    Batiraxcept
  • HY-132309
    BRD0639
    1 Publications Verification

    Histone Methyltransferase Cancer
    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 .
    BRD0639
  • 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 .
    HXR9 hydrochloride
  • HY-108935

    HIV Integrase GLUT Tyrosinase Cancer
    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 .
    Lavendustin B
  • 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 .
    BMSpep-57
  • HY-127024

    Thyroid Hormone Receptor Metabolic Disease
    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 .
    Thyroid hormone receptor antagonist (1-850)
  • HY-161137

    Amino acid Transporter iGluR Neurological Disease
    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 .
    LQFM215
  • 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 .
    PTD-DBM
  • 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 .
    Zifogaptide
  • HY-17504R
    Rosuvastatin Calcium (Standard)
    10+ Cited Publications

    Rosuvastatin hemicalcium (Standard); ZD 4522 Calcium (Standard)

    Reference Standards HMG-CoA Reductase (HMGCR) Autophagy Potassium Channel Bacterial Cardiovascular Disease Metabolic Disease Cancer
    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 .
    Rosuvastatin Calcium (Standard)
  • HY-10860

    sFRP-1 Wnt β-catenin Metabolic Disease
    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 .
    WAY-362692
  • 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 .
    SIYNFEKL TFA
  • 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 .
    SIIVFEKL TFA
  • HY-149308

    Macrophage migration inhibitory factor (MIF) 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 .
    MKA031
  • 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 .
    Rosuvastatin-d6

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