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RKO

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16

Inhibitors & Agonists

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-113803

    4-HNE alkyne

    Biochemical Assay Reagents Cancer
    4-Hydroxynonenal alkyne (4-HNE alkyne) is a click chemical reagent containing alkynes. 4-Hydroxynonenal alkyne induces heme oxygenase and cell apoptosis in colon cancer (RKO) cells .
    4-Hydroxynonenal alkyne
  • HY-151623
    ACBI2
    1 Publications Verification

    PROTACs Epigenetic Reader Domain Cancer
    ACBI2 is a highly potent and orally active VHL PROTAC SMARCA2 degrader (EC50: 7 nM), which selectively degrades SMARCA2 with a DC50 value of 1 nM in RKO cells. ACBI2 can be used in the research of lung cancer .
    ACBI2
  • HY-B1139
    Tolperisone hydrochloride
    1 Publications Verification

    Apoptosis Neurological Disease
    Tolperisone hydrochloride is a centrally acting muscle relaxant studied in neurological disorders causing pathological rhabdomyosclerosis (pyramidal tract injury, multiple sclerosis, myelopathy, encephalomyelitis), spastic paralysis, and other muscle dystonia-related Encephalopathy. Tolperisone hydrochloride also has antiviral activity .
    Tolperisone hydrochloride
  • HY-170390

    PROTACs Epigenetic Reader Domain Cancer
    AB3067 is a PROTAC degrader for BET protein, that recruits two different E3 ligase Cereblon and VHL with good affinity (IC50=559 nM for VHL in live HEK293; IC50=190 nM for CRBN in live HEK293), and degrades BRD2, BRD3, BRD4 and CRBN with DC50 of 2.1~2.3, 1.6, 15 and 75 nM, respectively. AB3067 inhibits the proliferation of RKO cell with an EC50 of 111 nM . (Pink: ligand for target protein (HY-131633A); Black: linker (HY-170391); Blue: ligand for E3 ligase VHL (HY-112078) and CRBN(HY-W998346))
    AB3067
  • HY-154973

    Oxidative Phosphorylation Mitochondrial Metabolism AMPK Metabolic Disease Cancer
    AMPK activator 11 is an AMP-activated protein kinase (AMPK) activator with nanomolelevel antiproliferation activities against several CRCs. AMPK activator 11 selectively inhibits the RKO xenograft growth along by activating AMPK and upregulating oxidative phosphorylation (OXPHOS) ( mitochondrial metabolism ) and can be used for anti-tumor and metabolic disease research .
    AMPK activator 11
  • HY-155073

    Microtubule/Tubulin Apoptosis Cancer
    Tubulin inhibitor 35 (compound 6b) is a dual inhibitor of topoisomerase I (IC50=~50 μM) and tubulin polymerization (IC50=5.69 μM). Tubulin inhibitor 35 inhibits migration and invasion of MGC-803 and RKO cell lines,and induces apoptosis via arresting cell cycle at G2/M phase. Tubulin inhibitor 35 exhibis potent efficacy in gastrointestinal tumor inhibiton (inhibits MGC-803 (IC50=0.09 μM) and RKO (IC50=0.2 μM) cell lines) .
    Tubulin inhibitor 35
  • HY-155972

    CRM1 Cancer
    CRM1-IN-1 (Compound KL1) is a noncovalent CRM1 inhibitor. CRM1-IN-1 induces nuclear CRM1 degradation (IC50: 0.27 μM). CRM1-IN-1 inhibits CRM1-mediated nuclear export and cell proliferation, and triggers apoptosis in colorectal cancer cells .
    CRM1-IN-1
  • HY-B1139R

    Apoptosis Neurological Disease
    Tolperisone (hydrochloride) (Standard) is the analytical standard of Tolperisone (hydrochloride). This product is intended for research and analytical applications. Tolperisone hydrochloride is a centrally acting muscle relaxant studied in neurological disorders causing pathological rhabdomyosclerosis (pyramidal tract injury, multiple sclerosis, myelopathy, encephalomyelitis), spastic paralysis, and other muscle dystonia-related Encephalopathy. Tolperisone hydrochloride also has antiviral activity .
    Tolperisone (hydrochloride) (Standard)
  • HY-150755

    Topoisomerase COX Apoptosis Reactive Oxygen Species Cancer
    Topo I/COX-2-IN-2 (Compound W10) is a potent dual-target inhibitor of Topo I and COX-2 with IC50 values of 0.90 μM and 2.31 μM, respectively. Topo I/COX-2-IN-2 induces cancer cell apoptosis through the mitochondrial pathway .
    Topo I/COX-2-IN-2
  • HY-155972A

    CRM1 Apoptosis Cancer
    CRM1-IN-2 (Compound KL2) is a noncovalent CRM1 inhibitor. CRM1-IN-2 localizes CRM1 in the nuclear periphery, depletes nuclear CRM1, and inhibits CRM1-mediated nuclear export. CRM1-IN-2 inhibits growth of colorectal cancer cells, and induces apoptosis .
    CRM1-IN-2
  • HY-135533

    Aburamycin A

    Autophagy Cancer
    Chromomycin A2 (Aburamycin A) has cytotoxicity and induces autophagy. Chromomycin A2 has anti-tumor activity and can be used in cancer research .
    Chromomycin A2
  • HY-163767

    β-catenin Inflammation/Immunology Cancer
    Antitumor agent-171 (Compound 35) is an inhibitor for β-catenin/BCL9 interaction with IC50 of 1.61 μM. Antitumor agent-171 exhibits high affinity to β-catenin with Kd of 0.63 μM. Antitumor agent-171 inhibits the gene expression of axin2 with IC50 of 0.84 μM. Antitumor agent-171 inhibits cell viability of HCT116 with IC50 of 4.39 μM. Antitumor agent-171 activates T cells, promotes antigen presentation, and exhibits antitumor efficacy and good pharmacokinetic characteristics in mouse models .
    Antitumor agent-171
  • HY-163768

    β-catenin Inflammation/Immunology Cancer
    Antitumor agent-172 (Compound 28) is an inhibitor for β-catenin/BCL9 interaction with IC50 of 3.92 μM. Antitumor agent-172 exhibits high affinity to β-catenin with Kd of 82 nM. Antitumor agent-172 activates T cells, promotes antigen presentation, and exhibits antitumor efficacy and good pharmacokinetic characteristics in mouse models .
    Antitumor agent-172
  • HY-12580

    MDM-2/p53 Cancer
    RO5353 is an orally active inhibitor for p53-MDM2 with an IC50 of 7 nM for MDM2. RO5353 inhibits the proliferation of wild-type p53 cancer cells with an average IC50 of 7 nM. RO5353 exhibits antitumor efficacy and good pharmacokinetic characteristics in mice .
    RO5353
  • HY-18964
    MG-101
    Maximum Cited Publications
    10 Publications Verification

    Calpain inhibitor I; Ac-LLnL-CHO; ALLN

    Proteasome Apoptosis Cancer
    MG-101 (ALLN) is an inhibitor of cysteine proteases which inhibits calpain I, calpain II, cathepsin B and cathepsin L with Kis of 190, 220, 150 and 500 pM, respectively. MG-101 induces apoptosis and inhibits tumor growth, it can be used for the research of colon cancer .
    MG-101
  • HY-122626

    Epigenetic Reader Domain Cancer
    BRPF1B/TRIM24-IN-1 (compound 34) is a potent TRIM24/BRPF1/BRPF2 inhibitor, with IC50 values of 0.43, 0.34, 1.75 μM, respectively. BRPF1B/TRIM24-IN-1 binds the TRIM24 bromodomain with a KD of 222 nM and has a KD for the BRPF1 bromodomain of 137 nM and for BRD1 of 1130 nM .
    BRPF1B/TRIM24-IN-1

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