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Results for "

1A9 cells

" in MedChemExpress (MCE) Product Catalog:

79

Inhibitors & Agonists

1

Biochemical Assay Reagents

3

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6

Natural
Products

1

Isotope-Labeled Compounds

3

Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-402410
    TETi76
    1 Publications Verification

    TET Protein Cancer
    TETi76 is an orally active TET family inhibitor with IC50 values ??of 1.5, 9.4 and 8.8 μM for TET1, TET2 and TET3, respectively. TETi76 competitively binds to the active site of TET enzymes, reduces cytosine hydroxymethylation and restricts clonal growth of TET2 mutants in vitro and in vivo, but does not affect the growth of normal hematopoietic precursor cells. TETi76 can be used for leukemia research .
    TETi76
  • HY-50101A
    Mavorixafor trihydrochloride
    Maximum Cited Publications
    8 Publications Verification

    AMD-070 trihydrochloride; AMD-11070 trihydrochloride

    CXCR HIV Infection Endocrinology Cancer
    Mavorixafor trihydrochloride (AMD-070 trihydrochloride) is a potent, selective and orally available CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding, and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC50 of 1 and 9 nM, respectively.Mavorixafor trihydrochloride can be used for the study of WHIM syndrome .
    Mavorixafor trihydrochloride
  • HY-50101
    Mavorixafor
    Maximum Cited Publications
    8 Publications Verification

    AMD-070; AMD-11070

    CXCR HIV Infection Endocrinology Cancer
    Mavorixafor (AMD-070) is a potent, selective and orally available CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding, and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC50 of 1 and 9 nM, respectively. Mavorixafor can be used for the study of WHIM syndrome .
    Mavorixafor
  • HY-13631J

    (1R,9R)-DX8951f

    Drug Derivative Topoisomerase Apoptosis Cancer
    (1R,9R)-Exatecan mesylate ((1R,9R)-DX8951f) is a non-prodrug camptothecin derivative and a potent topoisomerase I inhibitor (IC50=0.975 μg/mL in mice and 0.82 μg/mL in humans). (1R,9R)-Exatecan mesylate blocks enzyme activity and induces apoptosis by stabilizing the enzyme-DNA cleavable complex. (1R,9R)-Exatecan mesylate not only effectively inhibits the proliferation of various malignant tumor cells and tumor growth, but also circumvents P-glycoprotein-mediated multidrug resistance. (1R,9R)-Exatecan mesylate is widely used in preclinical studies of multiple cancers including pancreatic cancer, lung cancer, breast cancer, and leukemia . The low-activity isomer of (1R,9R)-Exatecan mesylate is (1S,9R)-Exatecan mesylate (HY-13631I).
    (1R,9R)-Exatecan mesylate
  • HY-W011696

    cis-1-Amino-9-octadecene, 80-90%

    Environmental Pollutants Biochemical Assay Reagents Cancer
    Oleylamine, 80-90% (cis-1-Amino-9-octadecene, 80-90%) is a multifunctional reagent used for metal ion coordination and nanoparticle surface modification, and acts as a solvent, surfactant and reducing agent in the synthesis of metal oxide nanoparticles. Oleylamine, 80-90% regulates nanoparticle morphology, magnetization intensity and water proton relaxation rate via thiol-ene "click" reaction, and enhances the colloidal stability of nanoparticles in organic reagents. Oleylamine, 80-90% is mainly used in research and applications in fields such as nanomaterial synthesis, biomedical imaging (MRI contrast agents, fluorescent probes), cancer cell targeting and drug delivery .
    Oleylamine, 80-90%
  • HY-134884
    INCB086550
    2 Publications Verification

    PD-1/PD-L1-IN-8

    PD-1/PD-L1 Cancer
    INCB086550 is a potent, oral, small-molecule PD-L1 inhibitor with IC50s value of 3.1, 4.9 and 1.9 nM for human, cynomolgus, and rat, respectively. INCB086550 promotes the dimerization of cell-surface PD-L1 and induces PD-L1 entry into Golgi vesicles then traffick to the nucleus. INCB086550 can be used for multiple cancers research .
    INCB086550
  • HY-13631I

    (1S,9R)-DX8951f

    Drug Derivative Topoisomerase Apoptosis Cancer
    (1S,9R)-Exatecan mesylate ((1S,9R)-DX8951f) is a non-prodrug camptothecin derivative and a topoisomerase I inhibitor (IC50=0.975 μg/mL in mice and 0.82 μg/mL in humans). (1S,9R)-Exatecan mesylate blocks enzyme activity and induces apoptosis by stabilizing the enzyme-DNA cleavable complex. (1S,9R)-Exatecan mesylate not only effectively inhibits the proliferation of various malignant tumor cells and tumor growth, but also circumvents P-glycoprotein-mediated multidrug resistance. (1S,9R)-Exatecan mesylate is widely used in preclinical studies of various cancers such as pancreatic cancer, lung cancer, breast cancer, and leukemia .
    The chiral isomer of (1S,9R)-Exatecan mesylate is (1R,9R)-Exatecan mesylate (HY-13631J).
    (1S,9R)-Exatecan mesylate
  • HY-N0762
    Isobavachin
    5 Publications Verification

    Cytochrome P450 UGT p38 MAPK NF-κB NO Synthase COX Fc Receptor (FcR) RANKL/RANK Keap1-Nrf2 Reactive Oxygen Species (ROS) Apoptosis Autophagy Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Isobavachin is an orally active, blood-brain barrier-penetrating prenylated flavonoid present in Psoralea corylifolia. Isobavachin inhibits human CYP2B6, CYP2C9, CYP2C19, UGT1A1, UGT1A9, and UGT2B7. Isobavachin suppresses MAPK activation, NF-κB nuclear translocation, overexpression of iNOS/COX-2, FcεRI-mediated signaling pathways, and RANKL-induced osteoclastogenesis. Isobavachin induces autophagy, cytotoxicity, neuronal differentiation, and NRF2 activation; it alleviates oxidative damage, inflammatory responses, apoptosis, iron accumulation, mitochondrial biogenesis, and mast cell degranulation. Isobavachin is applicable to research related to liver injury, inflammatory diseases, osteoporosis, liver cancer, prostate cancer, glioma, periodontitis-induced bone loss, and Alzheimer's disease .
    Isobavachin
  • HY-B0927

    (-)-β-Hydrastine; (1R,9S)-β-Hydrastine

    Tyrosine Hydroxylase Dopamine Receptor OAT Neurological Disease
    Hydrastine ((-)-β-Hydrastine; (1R,9S)-β-Hydrastine) is a selective competitive inhibitor of tyrosine hydroxylase (TH), inhibiting dopamine biosynthesis (IC50=20.7 μM, PC12 cells). Hydrastine also inhibits the organic cation transporter OCT1 (IC50=6.6 μM). Hydrastine may cause neuronal toxicity through mitochondrial dysfunction rather than oxidative stress damage, and can aggravate cell apoptosis when combined with L-DOPA. Hydrastine can be used to study Parkinson's disease-related dopaminergic neuronal damage .
    Hydrastine
  • HY-100738

    NSC144303

    Apoptosis Cancer
    Ubiquitin Isopeptidase Inhibitor I, G5 (NSC 144303) is an apoptosome-independent caspase and apoptosis activator with IC50 values of 1.76 and 1.6 μM in E1A and E1A/C9DN cells, respectively.
    Ubiquitin Isopeptidase Inhibitor I, G5
  • HY-12954

    NCH-51

    HDAC HIV Infection Cancer
    PTACH (NCH-51) is a potent HDAC inhibitor with IC50s of 48 nM, 32 nM, and 41 nM for HDAC1, HDAC4, and HDAC6, respectively. PTACH exerts potent growth inhibition against various cancer cells (EC50s of 1.1-9.1 μM) .
    PTACH
  • HY-129035

    Vanin-1-IN-1

    Pantetheinase Metabolic Disease Inflammation/Immunology
    PFI-653 (Vanin-1-IN-1, compound 3), a chemical probe, is a vanin-1 inhibitor that binds to plasma vanin-1 from mouse, rat, dog, and human. Vanin-1 is a cell surface-associated inositol (GPi) -anchored protein that plays important roles in metabolism and inflammation. PFI-653 inhibits vanin-1 from different species with IC50s of 6.85 nM (human recombinant plasma vanin-1), 9.0 nM (human plasma vanin-1), 24.5 nM (mouse recombinant vanin-1), and 53.4 nM (mouse plasma vanin-1) .
    PFI-653
  • HY-132192
    PD-1/PD-L1-IN-9
    2 Publications Verification

    PD-1/PD-L1 Cancer
    PD-1/PD-L1-IN-9 is a potent and orally active inhibitor of PD-1/PD-L1 interaction, with an IC50 of 3.8 nM. PD-1/PD-L1-IN-9 can enhance the killing activity of tumor cells by immune cells. PD-1/PD-L1-IN-9 also exhibits significant in vivo antitumor activity in a CT26 mouse model .
    PD-1/PD-L1-IN-9
  • HY-146320
    ANO1-IN-1
    2 Publications Verification

    Chloride Channel Cancer
    ANO1-IN-1 (Compound 9c) is a selective ANO1 channel blocker with an IC50 of 2.56 μM and 15.43 μM against ANO1 and ANO2, respectively. ANO1-IN-1 suppresses strongly proliferation of glioblastoma cells .
    ANO1-IN-1
  • HY-118052

    PKD HDAC Cardiovascular Disease
    BPKDi is an inhibitor of PKD. BPKDi inhibits three members of the PKD family, PKD1, PKD2, and PKD3, with IC50 values of 1 nM, 9 nM, and 1 nM, respectively. BPKDi blocks signal-dependent phosphorylation and nuclear export of class IIa HDACs in cardiomyocytes and concomitantly suppresses hypertrophy of these cells .
    BPKDi
  • HY-153803

    PROTACs Molecular Glues Btk Cancer
    GBD-9 is a degrader based on the E3 ubiquitin ligase CRBN that targets BTK and the G1 to S phase transition protein GSPT1. GBD-9 has both PROTAC and molecular glue properties by inducing ubiquitination and proteasomal degradation of target proteins. GBD-9 can efficiently degrade wild-type and mutant BTK (such as C481S mutation) and GSPT1. GBD-9 significantly inhibits tumor cell proliferation by inducing G1 phase arrest in cancer cells, downregulating anti-apoptotic proteins (BCL-2, MCL-1) and activating Caspase-3 to induce apoptosis. GBD-9 is mainly used in the research of hematological tumors such as diffuse large B-cell lymphoma (DLBCL) and acute myeloid leukemia (AML) .
    GBD-9 is composed of E3 ubiquitin ligase ligand (pink part) 5-Aminothalidomide (HY-W023573), target protein ligand (blue part) Btk Inhibitor: IBT6A (HY-13036A), and PROTAC linker (black part) Nonanoic acid (HY-N7057).
    GBD-9
  • HY-146805

    MNK Eukaryotic Initiation Factor (eIF) Apoptosis Cancer
    EB1 is the inhibitor of kinases MNK with IC50s of 0.69 μM (MNK1) and 9.4 μM (MNK2). EB1 selectively inhibits the growth of cancer cells, but not normal cells. EB1 also increases cell apoptosis and suppresses eIF4E phosphorylation .
    EB1
  • HY-111844

    PROTACs SNIPERs RAR/RXR Neurological Disease Metabolic Disease Cancer
    PROTAC RAR degrader-1 (Compound 9) is a potent and selective RAR PROTAC Degrader consisting of apoptotic protein inhibitors (IAPs) ligands. IAPs-based degraders are also known as SNIPERs. PROTAC RAR Degrader-1 reduces RARα levels in HT1080 cells in a concentration-dependent manner but is blocked by the proteasome inhibitor MG132 (HY-13259). PROTAC RAR Degrader-1 can be used in the study of nuclear receptor-related diseases. (Pink: RAR ligand 1 (HY-111843); Black: Linker (HY-140189); Blue: IAPs Ligand (HY-B0134)) .
    PROTAC RAR Degrader-1
  • HY-162161

    Fluorescent Dye Microtubule/Tubulin Cancer
    Flutax-2 is an active fluorescent derivative of Paclitaxel (HY-B0015) that binds to polymerized αβ-tubulin dimers. Flutax-2 is applicable for imaging microtubules in live cells, isolated cytoskeletons and parasites (Ex/Em=496/526 nm) .
    Flutax-2
  • HY-16668
    Tyrphostin A1
    1 Publications Verification

    Tyrphostin 1; AG9

    Interleukin Related Inflammation/Immunology
    Tyrphostin A1(AG9) inhibits CD40L-stimulated IL-12 production in macrophage cultures and antigen-induced generation of Th1 cells.
    Tyrphostin A1
  • HY-173155

    Akt Cancer
    AKT1-IN-9 (4) is a selective mutant AKT1(E17K) inhibitor, with EC50 values of 9 nM and 995 nM in LAPC4-CR and SkBr3 cells, respectively .
    AKT1-IN-9
  • HY-155582

    Src Cancer
    BLK degrader 1 (compound 9) is a selective degrader of B-lymphoid tyrosine kinase (BLK). BLK degrader 1 shows anticancer activity in several B-lymphoid cell lines .
    BLK degrader 1
  • HY-160267

    HIV DNA/RNA Synthesis Infection Neurological Disease Cancer
    iPAF1C is a inhibitor of the polymerase-associated factor 1 complex (PAF1C) with specific targeting to the PAF1 binding groove of CTR9 (a key subunit of PAF1C). iPAF1C disrupts PAF1C assembly by interfering with the PAF1-CTR9 interaction. iPAF1C selectively impairs BRD4-mediated recruitment of PAF1 to chromatin at hypoxia-responsive genes and inhibits RNA polymerase II (RNAPII) pause release. iPAF1C increases the population of HIV-1 NL4.3 Nef-IRES-GFP infected primary human CD4 +T cells in a dose-dependent manner. PAF1C can be used for the study of infection and diseases associated with abnormal hypoxic adaptation (e.g., cancers, neurological disorders) .
    iPAF1C
  • HY-153893

    Mitochondrial Metabolism Metabolic Disease
    Magmas-IN-1 (compound 9) is a small molecule Magmas inhibitor (SMMI). Magmas is mitochondria associated,granulocyte-macrophage colony stimulating factor signaling molecule,as well as a GM-CSF inducible gene in myeloid cells. Magmas-IN-1 inhibits Magmas and modulates mitochondrial function. Magmas-IN-1 also inhibits proliferation in yeast at 4 μM .
    Magmas-IN-1
  • HY-15843

    MicroRNA Apoptosis Cancer
    MIR96-IN-1 targets the Drosha site in the miR-96 (miRNA-96, microRNA-96) hairpin precursor, inhibiting its biogenesis, derepressing downstream targets, and triggering apoptosis in breast cancer cells. MIR96-IN-1 binds to RNAs with Kds of 1.3, 9.4, 3.4, 1.3 and 7.4 μM for RNA1, RNA2, RNA3, RNA4 and RNA5, respectively . MIR96-IN-1 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
    MIR96-IN-1
  • HY-132192A
    PD-1/PD-L1-IN-9 hydrochloride
    2 Publications Verification

    PD-1/PD-L1 Cancer
    PD-1/PD-L1-IN-9 hydrochloride is a potent and orally active inhibitor of PD-1/PD-L1 interaction, with an IC50 of 3.8 nM. PD-1/PD-L1-IN-9 hydrochloride can enhance the killing activity of tumor cells by immune cells. PD-1/PD-L1-IN-9 hydrochloride also exhibits significant in vivo antitumor activity in a CT26 mouse model .
    PD-1/PD-L1-IN-9 hydrochloride
  • HY-148203

    Bcl-2 Family Cancer
    Mcl-1 inhibitor 9 (example 2) is a myeloid cell leukemia 1 (Mcl-1) inhibitor with IC50 value of 0.21889 nM. Mcl-1 inhibitor 9 shows anti-tumor activity .
    Mcl-1 inhibitor 9
  • HY-N12726

    p38 MAPK MMP Infection Inflammation/Immunology Cancer
    Halociline, a derivative of alkaloids, that can be isolated from the marine fungus Penicillium griseofulvum. Halociline targets MAPK1, MMP-9, and PIK3CA in gastric cancer cells, potentially mediated by diverse pathways including cancer, lipid metabolism, atherosclerosis, and EGFR tyrosine kinase inhibitor resistance. Halociline possesses antimicrobial, antioxidant and biofilm inhibitory activities .
    Halociline
  • HY-149001

    PARP Cancer
    PARP1-IN-9 (Compound 5c) is a PARP1 inhibitor with an IC50 of 30.51 nM. PARP1-IN-9 induces cell apoptosis and shows anticancer activity. PARP1-IN-9 has higher potency than Olaparib (HY-10162) .
    PARP1-IN-9
  • HY-161383

    Checkpoint Kinase (Chk) Cancer
    CHK1-IN-9 (compound 11) is an orally active CHK1 inhibitor with an IC50 value of 0.55 nM. CHK1-IN-9 can enhance the effect of DNA-damaging drugs on tumor cells. CHK1-IN-9 has synergistic anticancer effects with Gemcitabine (HY-17026) .
    CHK1-IN-9
  • HY-162633

    Deubiquitinase Cancer
    USP1-IN-9 (Compound 1m) is reversible and noncompetitive ubiquitin-specific proteases (USP1) inhibitors with an IC50 of 8.8 nM, which is designed and synthesized to pyrido[2,3-d]pyrimidin-7(8H)-one derivative based on the disclosed structure of ML323(HY-17543) and KSQ-4279(HY-145471). USP1-IN-9 displays excellent USP1/UAF inhibition and exhibits strong antiproliferation effect in breast cancer cells. USP1-IN-9 can generate enhanced cell killing with PARP inhibitor olaparib(HY-10162) in olaparib-resistant MDA-MB-436/OP cells, which is promising for research in the field of cancer .
    USP1-IN-9
  • HY-145035

    MAP4K Inflammation/Immunology Cancer
    HPK1-IN-9 is potent inhibitor of HPK1. HPK1 is a serine/threonine protein kinase cloned from hematopoietic progenitor cells and belongs to the MAP4K family of mammalian Ste-20-related protein kinases. HPK1-IN-9 has the potential for the research of HPK1 related diseases (extracted from patent WO2021213317A1, compound 112) .
    HPK1-IN-9
  • HY-161407

    Aurora Kinase Cancer
    AURKA-IN-1 (compound 9) is an cell-active covalent AURKA inhibitor. AURKA-IN-1 is a lysine-reactive activity probe .
    AURKA-IN-1
  • HY-163801

    Nuclear Hormone Receptor 4A/NR4A Neurological Disease
    Nurr1 agonist 9 (Compound 36) is an agonist for Nurr1 with an EC50 of 0.090 µM and a Kd of 0.17 µM. Nurr1 agonist 9 activates the Nurr1 homodimer (NurRE, EC50=0.094 µM) and the Nurr1-RXR heterodimer (DR5, EC50=0.165 µM). Nurr1 agonist 9 induces the expression of Nurr1-regulated tyrosine hydroxylase (TH) in organoid Parkinson's Disease model. Nurr1 agonist 9 is human brain endothelial cell barrier prmeable .
    Nurr1 agonist 9
  • HY-156502

    MAP4K Cancer
    TINK-IN-1 (Compound 9) is a potent and selective Traf2- and Nck-interacting kinase (TNIK) inhibitor with an IC50 of 8 nM. TINK-IN-1 inhibits colorectal cancer cells viability .
    TINK-IN-1
  • HY-159609

    Molecular Glues Cancer
    GSPT1 degrader-9 (Compound F) is a cereblon-based molecular glue degrader for G1 to S phase transition protein 1 (GSPT1) that degrades GSPT1 with a rate of 95% (1 μM) GSPT1 and 86% (0.1 μM). GSPT1 degrader-9 inhibits the cell viability of HL-60 with an IC50 of 9.2 nM .
    GSPT1 degrader-9
  • HY-101329S

    9-Anthracenecarboxylic acid-d9

    Chloride Channel Others
    Anthracene-9-carboxylic acid-d9 is the deuterium labeled Anthracene-9-carboxylic acid [1]. Anthracene-9-carboxylic acid (9-Anthracenecarboxylic acid) is an anthracene derivative traditionally used to block and identify Ca2+-activated Cl- currents (CaCCs) in various cell types, like diverse smooth muscle cells, epithelial cells and salivary gland cells .
    Anthracene-9-carboxylic acid-d9
  • HY-162762

    Protease Activated Receptor (PAR) Cancer
    PAR-2 antagonist 1 (Compound 9a) is a protease-activated receptor 2 (PAR2) antagonist with an IC50 value of 0.9 μM. PAR-2 antagonist 1 can effectively inhibit the proliferation and migration of breast cancer cells .
    PAR-2 antagonist 1
  • HY-136340

    Glucocorticoid Receptor NF-κB Metabolic Disease Inflammation/Immunology
    21-Acetoxypregna-1,4,9(11),16-tetraene-3,20-dione is an intermediate of delta 9,11 steroids synthesis, for example, Vamorolone (HY-109017). The delta 9,11 steroids are modifications of glucocorticoids and has anti-inflammatory properties. The delta 9,11 steroids are agents for protection against cell damage (lipid peroxidation) and inhibition of neovascularization .
    21-Acetoxypregna-1,4,9(11),16-tetraene-3,20-dione
  • HY-179003

    mTOR Glutaminase Reactive Oxygen Species (ROS) Autophagy Apoptosis Ferroptosis Glutathione Peroxidase Cancer
    mTOR/GLS1-IN-1 (Compoud 9d) is a potent dual targeted mTOR/GLS1 inhibitor. Has anti proliferative activity against various tumor cells. mTOR/GLS1-IN-1 dose dependently induces ROS accumulation, induces autophagosome formation, and induces apoptosis. mTOR/GLS1-IN-1 can increase Fe 2+, decrease GPX4, and induce ferroptosis. mTOR/GLS1-IN-1 can inhibit cell migration, invasion, and angiogenesis. mTOR/GLS1-IN-1 can be used in the research of cancer, such as breast cancer .
    mTOR/GLS1-IN-1
  • HY-156401

    PROTACs Epigenetic Reader Domain Cancer
    BRD9 c-1 (Compound 13-7) is a PROTAC BRD9 degrader [1]. BRD9 Degrader-1 has a micromolar binding affinity for BRD9 and a nanomolar affinity for the BRD9-VCB ternary complex. BRD9 Degrader-1 induces BRD9 proteasome degradation in HEK293T cells, which can be reversed by MLN4924 (HY-70062). (Blue: VH032-cyclopropane-F (HY-125905); Black: linker (HY-W763939); Pink: HY-168695) .
    BRD9 Degrader-1
  • HY-171837

    Caspase Cancer
    c9,t11,c15-CLNA is a conjugated linolenic acid (CLNA) isomer produced by Lactobacillus plantarum ZS2058. c9,t11,c15-CLNA has significant anti-proliferation activity against colon cancer cells (IC50: 18.26 μM). c9,t11,c15-CLNA induces pyroptosis by activating the canonical pyroptosis pathway mediated by caspase-1. c9,t11,c15-CLNA can be used in the study of colon cancer .
    c9,t11,c15-CLNA
  • HY-179013

    Virus Protease Flavivirus Dengue Virus Infection
    NS2B/NS3-IN-9 (Compound 73) is a broad-spectrum, non-competitive anti-Orthoflavivirus lipopeptide inhibitor targeting the NS2B-NS3 protease. NS2B/NS3-IN-9 exhibits IC50 values for Dengue virus DENV2 NS2B-NS3, West Nile virus WNV NS2B-NS3, and Zika virus ZIKV NS2B-NS3 of 2.4, 7.2, and 1.9 μM, respectively. NS2B/NS3-IN-9 also exhibits antiviral activity at the cellular level against DENV2, WNV, and ZIKV, with EC50 values of 4.1, 4.9, and 5.0 μM, respectively. NS2B/NS3-IN-9 has no significant toxicity to cells. NS2B/NS3-IN-9 can be used for the study of anti-Orthoflavivirus .
    NS2B/NS3-IN-9
  • HY-178172

    Histone Methyltransferase c-Myc Epigenetic Reader Domain HOXA Cancer
    AF9/ENL-DOT1L/AF4 PPI-IN-1 is a potent AF9/ENL and histone methyltransferase DOT1L/AF4 protein-protein interactions (PPI) inhibitor. AF9/ENL-DOT1L/AF4 PPI-IN-1 can inhibit the AF9-DOT1L (IC50 = 1.5 μM), AF9-AF4 (IC50 = 1 μM), ENL-AF4 (IC50 = 1.2 μM) interactions. AF9/ENL-DOT1L/AF4 PPI-IN-1 can suppress the expression of Mixed lineage leukemia (MLL) target genes Myc and Meis1 and selectively block the proliferation of MLL-r and several other leukemia cells. AF9/ENL-DOT1L/AF4 PPI-IN-1 exhibits significant antitumor activities in a mouse model of MLL-r leukemia without overt toxicities. AF9/ENL-DOT1L/AF4 PPI-IN-1 can be used for the study of MLL-r leukemia .
    AF9/ENL-DOT1L PPI-IN-1
  • HY-143727

    RIP kinase Inflammation/Immunology
    RIPK1-IN-9 (example 45), a dihydronaphthyridone compound, is a potent and selective RIPK1 inhibitor. RIPK1-IN-9 inhibits U937 cell (IC50=2 nM) and L929 cell (IC50=1.3 nM) .
    RIPK1-IN-9
  • HY-128607

    Bcl-2 Family Cancer
    Mcl1-IN-9 is a potent myeloid cell leukemia-1 (Mcl-1) Inhibitor with an IC50 of 446 nM in reengineered BCR-ABL+ B-ALL cells and a Ki of 0.03 nM .
    Mcl1-IN-9
  • HY-143427

    MALT1 Cancer
    MALT1-IN-9 is a potent MALT1 protease inhibitor with a IC50 of <500 nM in Raji MALT1-GloSensor cells. MALT1-IN-9 has anticancer effects (WO2021000855A1; Compound 5) .
    MALT1-IN-9
  • HY-P3608

    GCGR Metabolic Disease
    [Des-His1,Glu9] Glucagon is a potent glucagon receptor system peptide antagonist. [Des-His1,Glu9] Glucagon enhances the glucose-stimulated release of insulin from pancreatic islet cells. [Des-His1,Glu9] Glucagon can be used to research diabetes .
    [Des-His1,Glu9] Glucagon
  • HY-174425

    Cytochrome P450 Cancer
    CYP1B1-IN-9 is a highly selective and competitive CYP1B1 Inhibitor with IC50 values of 1.48 nM, > 100 μM, and > 80 μM for CYP1B1, CYP1A1, and CYP1A2, respectively. CYP1B1-IN-9 significantly inhibits the migration and invasion of A549/T cells. CYP1B1-IN-9 has the ability to resensitize Paclitaxel (HY-B0015)-resistant cells, and good metabolic stability and safety, and shows favorable pharmacokinetic parameters. CYP1B1-IN-9 can be used for the study of tumor-drug resistance .
    CYP1B1-IN-9
  • HY-170966

    HDAC Cancer
    HDAC1-IN-9 (13c) is a HDAC1 inhibitor. HDAC1-IN-9 inhibits HDAC1 enzyme with an IC50 of 1.07 µM. HDAC1-IN-9 exhibits the highest anti-proliferative effect against HT-29 (human colon adenocarcinoma), with anIC50 of 1.78 μM. HDAC1-IN-9 induces substantial Apoptosis in HCT-116 (human colon cancer) cells. HDAC1-IN-9 possesses antiangiogenic property. HDAC1-IN-9 reduces the expression levels of VEGFR-2 and phosphorylated VEGFR-2 (pVEGFR-2) by approximately 80 % .
    HDAC1-IN-9

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