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RKO

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20

Inhibitors & Agonists

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Peptides

1

Natural
Products

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Click Chemistry

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

    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-168925
    EXQ-2d

    		Wnt PARP β-catenin Cancer
    EXQ-2d is the inhibitor for tankyrase and inhibits TNKS1 and TNKS2 with an IC50 of 48.8 nM and 13.8 nM (pIC50=7.31 and 7.86). EXQ-2d inhibits WNT/β-catenin signaling pathway with IC50 of 515 nM. EXQ-2d exhibits anti-proliferative activity in cancer cells COLO 320DM and RKO with GI50 of 4.9 μM and 77 μM .
    EXQ-2d
  • HY-170390
    AB3067

    		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-170877
    SHP2-IN-35

    		SHP2 PI3K Akt Autophagy Cancer
    SHP2-IN-35 (Compound 3f) is the inhibitor for SHP2. SHP2-IN-35 exhibits antiproliferative activity in cancer cells RKO, SW480 and CT26 with IC50 of 5.72 μM, 3.71 μM and 1.42 μM, respectively. SHP2-IN-35 inhibits the PI3K-Akt signaling pathway, regulates the cell cycle associated gene expressions, and induces mitochondrial-related autophagy. SHP2-IN-35 inhibits the expression of certain cytokines and chemokines in the tumor microenvironment (TME), thereby regulating the tumor progression .
    SHP2-IN-35
  • HY-154973
    AMPK activator 11

    		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-P10914
    D-CopA3

    		MDM-2/p53 Autophagy Inflammation/Immunology Cancer
    D-CopA3 is the inhibitor for MDM2 and the activator for p53 signaling pathway. D-CopA3 exhibits cytotoxicity in colorectal cancer cells HCT-116, LoVo, and RKO (IC50=15-18 μM), induces JNK/Beclin-1 mediated autophagy. D-CopA3 downregulates the expression of cell cycle inhibitory protein p21Cip1/Waf1, enhances the mucosal barrier function and reduces penetration of inflammatory mediators. D-CopA3 exhibits anti-inflammtory activity in mouse C. difficile toxin A-induced acute enteritis models and DSS (HY-116282)-induced chronic colitis models. D-CopA3 exhibits antitumor efficacy in mouse HCT-116 xenograft models .
    D-CopA3
  • HY-155073
    Tubulin inhibitor 35

    		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-IN-1

    		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
    Tolperisone hydrochloride (Standard)

    		Reference Standards 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-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-155972A
    CRM1-IN-2

    		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-150755
    Topo I/COX-2-IN-2

    		Topoisomerase COX Apoptosis Reactive Oxygen Species (ROS) 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-135533
    Chromomycin A2

    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-12580
    RO5353

    		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-176727
    WRN inhibitor 19

    		DNA/RNA Synthesis Cancer
    WRN inhibitor 19 (Compound 40) is a WRN helicase inhibitor (IC50: 3.7 nM). WRN inhibitor 19 exhibits selective antiproliferative activity in WRN-dependent cancer cells. WRN inhibitor 19 inhibits WRN helicase function by competitively binding to the ATP site and induces DNA damage and cell cycle arrest. WRN inhibitor 19 can be used in the study of WRN-dependent cancers .
    WRN inhibitor 19
  • HY-163767
    Antitumor agent-171

    		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
    Antitumor agent-172

    		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-18964
    MG-101
    Maximum Cited Publications
    11 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
    BRPF1B/TRIM24-IN-1

    		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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