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HK2 inhibitor

" in MedChemExpress (MCE) Product Catalog:

13

Inhibitors & Agonists

1

Fluorescent Dyes

1

Biochemical Assay Reagents

3

Natural
Products

1

GMP Molecules

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-155008
    PROTAC HK2 Degrader-1
    2 Publications Verification

    PROTACs Hexokinase Cancer
    PROTAC HK2 Degrader-1 is a PROTAC consisting of Lonidamine (HY-B0486) as a target protein Hexokinase 2 (HK2) inhibitor and Thalidomide (HY-14658) as a CRBN ligand-linked PROTAC. PROTAC HK2 Degrader-1 selectively inhibits the proliferation of breast cancer cells by forming a ternary complex through the ubiquitin-proteasome system to degrade Hexokinase 2 (HK2) protein leading to mitochondrial damage and cell death. PROTAC HK2 Degrader-1 effectively inhibits breast tumor growth and reduces the colonic side effects of cisplatin for breast cancer research .
    PROTAC HK2 Degrader-1
  • HY-N7675

    NF-κB TGF-beta/Smad Syk Cardiovascular Disease Neurological Disease Metabolic Disease
    Flavanomarein is a substance with cytoprotective, anti-inflammatory and antioxidant activities, with a Ka of 3.064e-5 M against human Syk. Flavanomarein enhances the phosphorylation level of AKT, regulates the expression of PKC-δ, P85α, PKC-β1, Sirt1, Bcl-2 and ICAD, and inhibits the nuclear translocation of NF-κB p65. Flavanomarein regulates EMT marker proteins, promotes the proliferation of HK-2 cells, and protects neuronal cells from 6-OHDA-induced neurotoxic damage. Flavanomarein can be used in studies related to Parkinson's disease and diabetic nephropathy.
    Flavanomarein
  • HY-175035

    Hexokinase Inflammation/Immunology Cancer
    HK-2-IN-1 is a Hexokinase 2 (HK-2) inhibitor. HK-2-IN-1 exhibits a non-activating effect on human recombinant HK-2 enzyme. HK-2-IN-1 has anti-tumor activity, affecting immune cells in the tumor microenvironment. HK-2-IN-1 has immunomodulatory effects and is potentially useful in the study of cancers such as colon cancer, liver cancer, and breast cancer .
    HK-2-IN-1
  • HY-N2445
    Flavokawain C
    4 Publications Verification

    Apoptosis Akt JNK PERK Caspase PARP MDM-2/p53 IAP Reactive Oxygen Species (ROS) SOD FABP Autophagy AMPK mTOR GLUT EGFR PI3K HSP VEGFR FAK Cancer
    Flavokawain C is an orally active natural chalcone. Flavokawain C inhibits the proliferation of various cancer cells. Flavokawain C upregulates GADD153 in cancer cells, inhibits the phosphorylation of Akt and JNK, suppresses early ERK phosphorylation, activates late ERK phosphorylation, activates caspase related subtypes, induces PARP-1 cleavage, causes upregulation of p21 and p27, downregulation of mutant p53 and anti-apoptotic IAP proteins, elevates intracellular ROS levels, reduces SOD activity, and induces apoptosis. Flavokawain C downregulates FABP4, induces autophagy in cancer cells, and activates the AMPK/mTOR pathway . Flavokawain C decreases the expression of glycolysis-related proteins GLUT1 and HK2, and inhibits glycolysis in nasopharyngeal carcinoma cells. Flavokawain C inhibits the activation of the EGFR/PI3K/Akt/mTOR signaling pathway and reduces the expression of HSP90B1. Flavokawain C inhibits angiogenesis by decreasing the expression of angiogenic proteins Ang-1 and VEGF in human umbilical vein endothelial cells. Flavokawain C increases γ-H2AX levels in cells, inhibits the phosphorylation of FAK, PI3K and AKT in cells, and induces DNA damage in cells. Flavokawain C exerts anti-tumor activity in multiple tumor xenograft mouse models. Flavokawain C is applicable to research related to colorectal cancer, colon adenocarcinoma, nephroblastoma, nasopharyngeal carcinoma and liver cancer .
    Flavokawain C
  • HY-125938
    Cycloartenyl ferulate
    1 Publications Verification

    Cycloartenol ferulate; Cycloartenol ferulic acid ester

    Drug Derivative Apoptosis Reactive Oxygen Species (ROS) JAK STAT Inflammation/Immunology Cancer
    Cycloartenyl ferulate (Cycloartenol ferulate; Cycloartenol ferulic acid ester) is a derivative of γ-oryzanol (HY-B2194) with multiple biological activities including antioxidant, anti-inflammatory, and anti-tumor properties. Cycloartenyl ferulate selectively binds to IFNγR1 (binding affinity Kd = 0.5 μM) to activate the canonical JAK1/2-STAT1 signaling pathway. Cycloartenyl ferulate inhibits paraquat (PQ)-triggered apoptosis and ROS in HK2 cells. Cycloartenyl ferulate enhances the activation and cytolytic activity of natural killer (NK) cells by upregulating the expression of NK cell activation receptors (NKG2D, NKp30, NKp44) and the release of cytotoxic molecules and cytokine IFNγ. Cycloartenyl ferulate exerts anti-cancer effects in tumor mice models. Cycloartenyl ferulate can be used for the study of cancer and allergic inflammation intervention .
    Cycloartenyl ferulate
  • HY-168717

    Hexokinase Microtubule/Tubulin Reactive Oxygen Species (ROS) Cancer
    HK2-IN-2 (Compound 26) is a Hexokinase 2 inhibitor that demonstrates significant anti-tumor activity by targeting microtubules and Hexokinase 2, with an IC50 value of 0.764 μM against MD-MBA-231 cells. HK2-IN-2 effectively inhibits the activity of Hexokinase 2, leading to the accumulation of Reactive Oxygen Species and dysfunction of the mitochondrial membrane potential (MMP), thereby promoting apoptosis and blocking the cell cycle .
    HK-2-IN-2
  • HY-130437

    MDM-2/p53 TGF-β Receptor Caspase Infection Metabolic Disease
    p-nitro-Pifithrin-α, a cell-permeable analog of pifithrin-α, is a potent p53 inhibitor. p-nitro-Pifithrin-α suppresses p53-mediated TGF-β1 expression in HK-2 cells. p-nitro-Pifithrin-α inhibits the activation of caspase-3 by Zika virus (ZIKV) strains. p-nitro-Pifithrin-α attenuates steatosis and liver injury in mice fed a high-fat diet [4]. non-alcoholic fatty liver disease .
    p-nitro-Pifithrin-α
  • HY-182243

    Hexokinase VDAC Apoptosis AMPK Bcl-2 Family Cancer
    HK2-IN-4 is a selective hexokinase 2 (HK2) inhibitor with an IC50 value of 0.79 μM and a Kd value of 0.41 μM. HK2-IN-4 blocks the interaction between HK2 and voltage-dependent anion channel 1 (VDAC1). HK2-IN-4 reduces lactate and ATP levels in cancer cells. HK2-IN-4 induces the production of apoptosis (apoptosis) markers in cancer cells, including increased p-AMPK/AMPK ratio and Bax levels, as well as decreased Bcl2 levels. HK2-IN-4 inhibits the proliferation of cancer cells with high HK2 expression. HK2-IN-4 can be used in research related to colorectal cancer and non-small cell lung cancer .
    HK2-IN-4
  • HY-156368

    RIP kinase Inflammation/Immunology
    RIPK3-IN-4 (Compound 42) is a RIPK3 inhibitor. RIPK3-IN-4 inhibits HK-2 cell damage, necroptosis and inflammatory responses. RIPK3-IN-4 reduces Cisplatin (HY-17394)- and I/R-induced kidney damage, inflammatory response and necroptosis in acute kidney injury .
    RIPK3-IN-4
  • HY-179378

    DYRK TGF-beta/Smad NF-κB Wnt β-catenin MDM-2/p53 Notch Inflammation/Immunology
    XRF-1021 is an orally active HIPK2 inhibitor (IC50 = 0.18 μM). XRF-1021 reduces the expression of fibrotic markers in TGF-β1 stimulated NRK-49F and HK-2 cells, including Fibronectin, Collagen I and α-SMA. XRF-1021 blocks TGF-β, NF-κB, p53, Wnt/β-catenin, and Notch signaling. XRF-1021 reduces renal injury and fibrosis in vivo. XRF-1021 can be used for the research of chronic kidney disease .
    XRF-1021
  • HY-180805

    Hexokinase Mitophagy Apoptosis GLUT Cancer
    HK2-IN-3 (compound 12) is a potent hexokinase 2 (HK2) inhibitor with an IC50 of 56.4 nM. HK2-IN-3 reduces glucose uptake and downregulated GLUT1/GLUT4 in oral squamous cell carcinoma (OSCC). HK2-IN-3 induces mitophagy and apoptosis. HK2-IN-3 suppresses tumor growth and angiogenesis in OSCC xenograft mouse models. HK2-IN-3 can be used for OSCC research .
    HK2-IN-3
  • HY-183809

    Hexokinase Inflammation/Immunology
    ZSW is a hexokinase 2 (HK2) inhibitor with human HK2 IC50 of 0.48 μM, human HK2 Ka of 252.00 μM, and selectivity over HK3 and GCK. ZSW binds directly to HK2, inhibits its enzymatic activity, modulates macrophage phenotypes through glycolysis inhibition, and inhibits NF-κB nuclear translocation by preventing IκBα phosphorylation and degradation. ZSW alleviates inflammatory bowel disease (IBD) and improves the intestinal inflammatory state of IBD mice. ZSW can be used for the research of inflammatory bowel disease .
    ZSW
  • HY-15947G

    GDC-0994

    ERK c-Myc Hexokinase Lactate Dehydrogenase Cancer
    Ravoxertinib GMP is Ravoxertinib (HY-15947) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Ravoxertinib (GDC-0994) is an orally active ERK1/2 inhibitor. Ravoxertinib inhibits the ERK1/2 MAPK signaling pathway and reduces the expression levels of c-Myc, HK2 and LDHA. Ravoxertinib decreases mammosphere formation, and exerts additive and/or superadditive cytotoxicity when combined with Ipatasertib (HY-15186) in 3D tumor sphere models. Ravoxertinib can be used in research related to various cancers including breast cancer, melanoma, head and neck cancer, non-small cell lung cancer, ovarian cancer and Merkel cell carcinoma .
    Ravoxertinib

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