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CRC

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64

Inhibitors & Agonists

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8

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-N2146
    Combretastatin A4
    2 Publications Verification

    CRC 87-09

    Microtubule/Tubulin Cancer
    Combretastatin A4 is a microtubule-targeting agent that binds β-tubulin with Kd of 0.4 μM.
    Combretastatin A4
  • HY-N5014
    Liensinine perchlorate
    Maximum Cited Publications
    8 Publications Verification

    Apoptosis Inflammation/Immunology Cancer
    Liensinine Perchlorate is a constituent of Nelumbo nucifera Gaertn, with ani-hypertension and anti-cancer activities. Liensinine Perchlorate induces colorectal cancer (CRC) cell apoptosis .
    Liensinine perchlorate
  • HY-123772

    CDK Cancer
    CDK5 inhibitor 20-223 is a potent CDK2 and CDK5 inhibitor with IC50s of 6.0 and 8.8 nM, respectively. CDK5 inhibitor 20-223 is an effective anti-colorectal cancer (CRC) agent .
    CDK5 inhibitor 20-223
  • HY-100190

    Amphetinile; CRC 82-07

    Microtubule/Tubulin Cancer
    Amphethinile is an anti-tubulin agent. The affinity constant for the association (Ka) of Amphethinile with tubulin is 1.3 μM.
    Amphethinile
  • HY-161102

    Autophagy Cancer
    [Ru(phen)2(xant)] hexafluorophosphate is an inducer of Autophagy. [Ru(phen)2(xant)] hexafluorophosphate eliminates CRC stem cells by targeting the chaperone Hsp90. [Ru(phen)2(xant)] hexafluorophosphate reduces cell migration and invasion .
    [Ru(phen)2(xant)] hexafluorophosphate
  • HY-108695B

    Apoptosis Endogenous Metabolite Cancer
    (±)-Enterodiol is the racemate of Enterodiol (HY-108695). Enterodiol is transformed by human intestinal bacteria from lignans contained in various whole-grain cereals, nuts, legumes, flaxseed, and vegetables. Enterodiol has an apoptotic effect in colorectal cancer (CRC) cells. Enterodiol has anti-cancer activities .
    (±)-Enterodiol
  • HY-108695

    Apoptosis Endogenous Metabolite Cancer
    Enterodiol is transformed by human intestinal bacteria from lignans contained in various whole-grain cereals, nuts, legumes, flaxseed, and vegetables. Enterodiol has an apoptotic effect in colorectal cancer (CRC) cells. Anti-cancer activities .
    Enterodiol
  • HY-161140

    PI3K Wnt Cancer
    PI3Kα-IN-16 (Z86) is a novel PI3Kα inhibitor with an IC50 value of 4.28 μM. PI3Kα-IN-16 has potent inhibitory efficiency on PI3K-mediated CRCs growth and migration. PI3Kα-IN-16 also inhibits the Wnt signaling pathway .
    PI3Kα-IN-16
  • HY-139065

    Others Cancer
    AMPC is a potent and effective TFF3 inhibitor. AMPC inhibits cell proliferation, survival, oncogenicity, and CSC-like behaviour in TFF3-positive CMS4 CRC cells. AMPC acts as a potential anti-cancer agent alone or in combination with 5-FU, and can be used for cancer research .
    AMPC
  • HY-155068

    Reactive Oxygen Species Apoptosis Microtubule/Tubulin Cancer
    FC-11 is a Tubulin inhibitor that effectively inhibits tumor growth in mice. FC-11 can also induce endoplasmic reticulum (ER) stress to generate excess reactive oxygen species (ROS), leading to mitochondrial damage, thereby promoting apoptosis in colorectal cancer (CRC) cells by targeting microtubules. FC-11 can be used in cancer research .
    FC-116
  • HY-160493

    Wnt β-catenin Cancer
    PTK7/β-catenin-IN-6 (Compound 03653) is an inhibitor for PTK7/β-catenin interaction, which inhibits the Wnt signaling pathway, and exhibits an anticancer activity against colorectal cancer (CRC) .
    PTK7/β-catenin-IN-6
  • HY-107460

    Ephrin Receptor Cancer
    LDN-211904 oxalate (compound 32) is a potent and selective EphB3 inhibitor with an IC50 of 0.079 µM. LDN-211904 oxalate shows good metabolic stability in mouse liver microsomes. LDN-211904 oxalate with cetuximab could be effective in inhibiting STAT3-activated CSC stemness and cetuximab resistance in CRC .
    LDN-211904 oxalate
  • HY-108433

    Carnitine palmitoyltransferase 2

    Apoptosis MDM-2/p53 Metabolic Disease Cancer
    CPT2 (Carnitine palmitoyltransferase 2), an enzyme that participates in fatty acid oxidation, also is a colorectal cancer (CRC) prognostic biomarker. CPT2 overexpression can activate p-p53 to increase p53 expression, thereby inhibiting tumor proliferation and promoting apoptosis. CPT2 deficiency results in the most common inherited disorder of long-chain fatty acid oxidation affecting skeletal muscle. Downregulation of CPT2 is also highly correlated with the progression of various cancers and has potential for cancer research .
    CPT2
  • 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-122347A

    GW823296 maleate

    Neurokinin Receptor Neurological Disease
    Orvepitant maleate (GW823296 maleate) is potent, selective, orally active and well-tolerated neurokinin-1 receptor (NK-1) antagonist with a pKi of 10.2 for human neurokinin-1 receptor. Orvepitant maleate can across the blood-brain barrier. Orvepitant maleate has the potential for depressive disorder and chronic refractory cough (CRC) treatment .
    Orvepitant maleate
  • HY-147949

    Microtubule/Tubulin Apoptosis Cancer
    SKLB0565 is a potent tubulin inhibitor. SKLB0565 shows significant anti-proliferative activity against CRC (colorectal carcinoma) cell lines, with IC50 values ranging from 0.012 μM to 0.081 μM. SKLB0565 causes G2/M phase arrest and mitochondria-mediated intrinsic apoptosis. SKLB0565 inhibits cell migration and disrupted the tube formation of HUVECs .
    SKLB0565
  • HY-P99613

    MK-4280

    LAG-3 Cancer
    Favezelimab (MK-4280) is a humanized anti-LAG-3 monoclonal antibody that blocks the interaction between LAG-3 and its ligand MHC class II. Favezelimab has the potential for colorectal cancer (CRC) research combined with the PD-L1 inhibitor Pembrolizumab (HY-P9902) .
    Favezelimab
  • HY-P99406

    MCLA 158

    EGFR Cancer
    Petosemtamab (MCLA 158) is an anti- EGFR (Kd: 0.22 nM) and anti-LGR5 (Kd: 0.86 nM) monoclonal antibody (mAb). Petosemtamab leads to EGFR signaling blockade and receptor degradation in LGR5+ cancer cells. Petosemtamab can be used in the research of solid tumors, such as head and neck squamous cell carcinoma (HNSCC), metastatic colorectal cancer (CRC) .
    Petosemtamab
  • HY-B0294
    Flubendazole
    5+ Cited Publications

    Parasite Microtubule/Tubulin STAT MDM-2/p53 Apoptosis Autophagy Infection Cancer
    Flubendazole is an anthelmintic drug based on altering microtubule structure, inhibition of tubulin polymerization and disruption of microtubule function. Flubendazole induces apoptosis in human colorectal cancer (CRC) by blocking the STAT3 signaling axis and activation of autophagy. Flubendazole induces P53 expression and reduced Cyclin B1 and p-cdc2 expression. Flubendazole is an antitumor agent. Flubendazole can be used for worm and intestinal parasites .
    Flubendazole
  • HY-151939

    DNA/RNA Synthesis Apoptosis Cancer
    BLM-IN-2 is a Bloom's Syndrome Protein (BLM) inhibitor with an IC50 value of 0.8 μM. BLM-IN-2 effectively suppresses the proliferation, invasion, cell cycle arrest and apoptosis of CRC cells. BLM-IN-2 can be used for the reserarch of colorectal cancer (CRC) .
    BLM-IN-2
  • HY-162285

    Akt Cancer
    Anticancer agent 189 (compound 4) is an anticancer agent that antagonizes CRC effects by targeting AKT1 .
    Anticancer agent 189
  • HY-158050

    c-Fms
    PXB17 can inhibit CSF1R (IC50 = 1.7 nM) by blocking the activation of PI3K/ AKT/mTORC1 signaling. PXB17 is orally effective. PXB17 significantly inhibits the growth of CRC, improves PD-1 mAb efficacy and reduces tumor recurrence in CRC .
    PXB17
  • HY-113264

    Apoptosis Cancer
    PGD2 ethanolamide is the COX-2 dependent metabolite of Anandamide that induces apoptosis in colorectal carcinoma (CRC) cells .
    PGD2 ethanolamide
  • HY-N11777

    NHAP

    NF-κB Cancer
    (−)-N-Hydroxyapiosporamide (NHAP), an alkaloid, is an NF-κB inhibitor with potent antitumor activity in vitro and in vivo. (−)-N-Hydroxyapiosporamide can be used for the research of colorectal cancer (CRC) .
    (−)-N-Hydroxyapiosporamide
  • HY-153833

    KVA-E-23A

    Others Cancer
    PDS-0330 is a specific and potent Claudin-1 inhibitor. PDS-0330 interferes with claudin-1/Src association and inhibits colorectal cancer (CRC) progression and metastasis .
    PDS-0330
  • HY-P1201

    Somatostatin Receptor Cancer
    Cyclosomatostatin is a potent somatostatin (SST) receptor antagonist. Cyclosomatostatin can inhibit somatostatin receptor type 1 (SSTR1) signaling and decreases cell proliferation, ALDH+ cell population size and sphere-formation in colorectal cancer (CRC) cells .
    Cyclosomatostatin
  • HY-W181530

    CDK Cancer
    NCT02 is a cyclin K degrader. NCT02 induces ubiquitination of cyclin K (CCNK) and proteasomal degradation of CCNK and its complex partner CDK12. NCT02 has the potential for the research of metastatic colorectal cancer (CRC) .
    NCT02
  • HY-B0008

    MK-231

    NF-κB PD-1/PD-L1 Inflammation/Immunology Cancer
    Sulindac (MK-231) is an orally active nonsteroidal anti-inflammatory agent. Sulindac also is an immunomodulatory agent. Sulindac can be used for the research of arthritis of the spine, gouty arthritis and kinds of cancer including colorectal cancer (CRC) and lung cancer .
    Sulindac
  • HY-P1201A

    Somatostatin Receptor Cancer
    Cyclosomatostatin TFA is a potent somatostatin (SST) receptor antagonist. Cyclosomatostatin TFA can inhibit somatostatin receptor type 1 (SSTR1) signaling and decreases cell proliferation, ALDH+ cell population size and sphere-formation in colorectal cancer (CRC) cells .
    Cyclosomatostatin TFA
  • HY-116572A

    Others Cancer
    TASIN-1 is a selective inhibitor of truncated APC gene (adenomatous polyposis coli gene) and exerts cytotoxic effects through inhibition of cholesterol biosynthesis. TASIN-1 represents a potential therapeutic strategy for prevention and intervention in CRC with mutant APC .
    TASIN-1
  • HY-B0008A

    MK-231 sodium

    NF-κB PD-1/PD-L1 Infection Inflammation/Immunology Cancer
    Sulindac (MK-231) is an orally active nonsteroidal anti-inflammatory agent. Sulindac also is an immunomodulatory agent. Sulindac can be used for the research of arthritis of the spine, gouty arthritis and kinds of cancer including colorectal cancer (CRC) and lung cancer .
    Sulindac sodium
  • HY-N3913

    STAT Bcl-2 Family Cancer
    Furowanin A is a flavonoid with anti-neoplastic effects. Furowanin A inhibits STAT3/Mcl-1 axis to suppress proliferation, block cell cycle progression, induce apoptosis and promote autophagy. Furowanin A potently inhibits colorectal cancer (CRC) cells .
    Furowanin A
  • HY-162148

    EGFR Cancer
    HNPMI is an inhibitor of EGFR and has cytotoxic effects on tumor cells. HNPMI can downregulate the protein levels of osteopontin, survivin and cathepsin S, leading to apoptosis. HNPMI also regulates BCL-2/BAX and p53 in CRC cell lines to inhibit tumorigenesis .
    HNPMI
  • HY-136541
    YB-0158
    2 Publications Verification

    Wnt pathway inhibitor 2

    Wnt Apoptosis Cancer
    YB-0158 (Wnt pathway inhibitor 2) is a reverse-turn peptidomimetic and a potent colorectal cancer stem cell (CSC) targeting agent. YB-0158 disrupts Sam68-Src interactions and induces apoptosis in CRC cells. Anti-cancer activities .
    YB-0158
  • HY-135103
    Tauro-β-muricholic acid sodium
    1 Publications Verification

    T-βMCA sodium

    FXR Cancer
    Tauro-β-muricholic Acid sodium (T-βMCA sodium), a endogenous metabolite, is a competitive and reversible farnesoid X receptor (FXR) antagonist, with an IC50 of 40 μM .
    Tauro-β-muricholic acid sodium
  • HY-139611B

    Histone Methyltransferase Cancer
    (S)-MRTX-1719 (example 16-7) is the S-enantiomer of MRTX-1719. (S)-MRTX-1719 is a PRMT5/MTA complex inhibitor, with an IC50 of 7070 nM .
    (S)-MRTX-1719
  • HY-146254

    Carbonic Anhydrase Apoptosis Reactive Oxygen Species Cancer
    hCAIX-IN-12 is a potent hCAIX inhibitor with IC50 values of 0.74, 10.78 µM for CAIX and CAII, respectively. hCAIX-IN-12 shows antiproliferative effect and induces apoptosis. hCAIX-IN-12 increases ROS production. hCAIX-IN-12 has the potential for the research of colorectal cancer (CRC) .
    hCAIX-IN-12
  • HY-163090

    HDAC Reactive Oxygen Species Apoptosis Cancer
    HR488B is an efficient HDAC1 inhibitor. HR488B specifically suppressed the growth of CRC cells by inducing cell cycle G0/G1 arrest and apoptosis. HR488B causes mitochondrial dysfunction, reactive oxygen species (ROS) generation, and DNA damage accumulation .
    HR488B
  • HY-B1414

    p-chloro-m-xylenol

    Bacterial Influenza Virus Parasite Infection
    Chloroxylenol is a broad-spectrum antibacterial agent that can be used to control bacteria, algae, fungi and viruses .
    Chloroxylenol
  • HY-139611

    Histone Methyltransferase Cancer
    MRTX-1719 is a potent, orally active, selective PRMT5•MTA complex inhibitor, with IC50 of 3.6 and 20.5 nM for PRMT5•MTA and PRMT5. MRTX-1719 binds to the PRMT5•MTA complex, with KD value of 0.14 pM. MRTX-1719 shows antineoplastic activity in vitro and in vivo, and can be used for cancer study .
    MRTX-1719
  • HY-151628

    Others Cancer
    MRV03-068 (Compound 2) is a selective colibactin-activated peptidase (ClbP) inhibitor that blocks the genotoxic effect of Colibactin (HY-145930) on eukaryotic cells. MRV03-068 can be used in colorectal cancer research .
    MRV03-068
  • HY-151629

    Others Cancer
    MRV03-069 (Compound 3) is a selective colibactin-activated peptidase (ClbP) inhibitor that blocks the genotoxic effect of Colibactin (HY-145930) on eukaryotic cells. MRV03-069 can be used in colorectal cancer research .
    MRV03-069
  • HY-156375

    Pyruvate Kinase PDK-1 Cancer
    PKM2 activator 6 (Compound Z10) is a PKM2 activator and PDK1 inhibitor (KD: 121 and 19.6 μM respectively). PKM2 activator 6 induces colorectal cell apoptosis, and inhibits cell proliferation and migration . PKM2 activator 6 inhibits glycolysis. PKM2 activator 6 inhibits proliferation of DLD-1, HCT-8, HT-29, MCF-10A cells (IC50: 10.04, 2.16, 3.57, 66.39 μM) .
    PKM2 activator 6
  • HY-155391

    Carbonic Anhydrase P-glycoprotein Wnt β-catenin Cancer
    hCA/Wnt/β-catenin-IN-1 (Compd 15) is an inhibitor of hCA (Ki: 33.6, 24.1, 6.8 nM for hCA II, hCA IX, hCA XII). hCA/Wnt/β-catenin-IN-1 reduces P-gp activity. hCA/Wnt/β-catenin-IN-1 also inhibits Wnt/β-catenin signaling pathway. hCA/Wnt/β-catenin-IN-1 inhibits cancer cell viability, including the NCI/ADR-RES DOX-resistant cell line .
    hCA/Wnt/β-catenin-IN-1
  • HY-114491

    ERK Raf Cancer
    Rineterkib (compound B) is an orally available ERK1 and ERK2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer. Rineterkib hydrochloride can also inhibit RAF .
    Rineterkib
  • HY-114491A

    ERK Raf Cancer
    Rineterkib hydrochloride (compound B) is an orally available ERK1 and ERK2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer. Rineterkib hydrochloride can also inhibit RAF .
    Rineterkib hydrochloride
  • HY-161027

    Apoptosis Cancer
    DHP-B possesses anti-cancer activity and induces apoptosis. DHP-B covalently binds to Cys96 of CPT1A, blocks FAO, and disrupts the mitochondrial CPT1A-VDAC1 interaction, leading to increased mitochondrial permeability and reduced oxygen consumption and energy metabolism in CRC cells. DHP-B can be isolated from the plant Peperomia dindygulensis .
    DHP-B
  • HY-144256

    Others Cancer
    CHD1Li 6.11 is a potent oncogenic CHD1L inhibitor (IC50=3.3 µM for cat-CHD1L recombinant protein). CHD1Li 6.11 is an orally bioavailable antitumor agent, significantly reducing the tumor volume of CRC xenografts generated from isolated quasi mesenchymal cells (M-phenotype), which possess enhanced tumorigenic properties .
    CHD1Li 6.11
  • HY-157088

    Caspase Apoptosis Others
    C105SR is a cyclophilin D (CypD) inhibitor targeting to peptidyl-prolylcis-trans isomerase (PPIase). C105SR inhibits mitochondrial permeability transition opening (mPTP) with an IC 50 of 5 nM. C105SR inhibits hypoxia and reoxygenation inudced hepatocyte apoptosis and increases the level of calcium retention capacity (CRC). C105SR exhibits hepaprotective effect in ischaemia-reperfusion injury (IRI) mouse model .
    C105SR
  • HY-155491

    Bacterial Cancer
    Antibacterial agent 166 (Compound 19q), a derivative of Nitisinone (HY-B0607), is a selective and orally active Fusobacterium nucleatum inhibitor with a MIC50 of 1 μg/mL. Antibacterial agent 166 effectively attenuates the migratory ability of MC-38 cells induced by Fusobacterium nucleatum. Antibacterial agent 166 is a promising anti-F. nucleatum lead compound and can be used for colorectal cancer (CRC) research .
    Antibacterial agent 166

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