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colorectal cancer and melanoma

" in MedChemExpress (MCE) Product Catalog:
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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-149380
    Vem-L-Cy5

    		Raf Cancer
    Vem-L-Cy5 (compound 3)，modified with the NIR fluorophore cyanine-5 (Cy5)，is a Vemurafenib (HY-12057)-based inhibitor of BRAF. Vem-L-Cy5 targets to BRAF V600E，and also inhibits MEK phosphorylation. Vem-L-Cy5 has cell permeability，and inhibits cell growth of many types of cancer .
    Vem-L-Cy5
  • HY-153863
    MS934

    		PROTACs MEK Raf Cancer
    MS934 is a novel improved VHL-recruiting MEK 1/2 PROTAC degrader. MS934 also degrades CRAF. MS934 can be used for the research of variety of human cancers, such as melanoma, nonsmall cell lung cancer (NSCLC), colorectal cancer, primary brain tumors, and hepatocellular carcinoma (Pink: Target protein ligand (HY-168288); Black: linker (HY-168289); Blue: E3 ligase ligand (HY-112078)) .
    MS934
  • HY-150510A
    MS8511 hydrochloride

    		Histone Methyltransferase Neurological Disease Cancer
    MS8511 (hydrochloride) is a selective G9a/GLP covalent irreversible inhibitor by targeting a cysteine residue at the substrate binding site, with IC50 values of 100 nM (G9a) and 140 nM (GLP), and Kd values of 44 nM (G9a) and 46 nM (GLP). MS8511 (hydrochloride) reduces the cellular H3K9me2 level and enhances antiproliferation activity. MS8511 (hydrochloride) can be used for the research of several types of cancers including brain, breast, ovarian, lung, bladder, melanoma, colorectal cancer, and other disease such as Alzheimer’s disease (AD), sickle cell disease, Prader−Willi syndrome (PWS) .
    MS8511 hydrochloride
  • HY-177081
    Envometinib

    		MEK Cancer
    Envometinib (Compound B) is a dual-MEK inhibitor that works through Deep Cyclic Inhibition (DCI). Envometinib has antitumor activity in various in vivo models. Envometinib can be studied in RAS and RAF mutated cancer such as colorectal cancer and melanoma .
    Envometinib
  • HY-119261
    Ruboxyl

    		Antibiotic Cancer
    Ruboxyl is an anthracycline antibiotic with antitumor activity. Ruboxyl inhibits colorectal cancer (CRC) liver metastasis in mice by 84%, suppresses B16 melanoma growth, and increases the survival rate of mice with L1210 or L5178Y leukemia .
    Ruboxyl
  • HY-175034
    Topoisomerase I/II-IN-1

    		Topoisomerase Apoptosis MDM-2/p53 Bcl-2 Family Caspase Cancer
    Topoisomerase I/II-IN-1 is a dual inhibitor of topoisomerase I/II. Topoisomerase I/II-IN-1 induces G2/M arrest and apoptosis in cancer cells by upregulating p53, p21, and Bax mRNA levels, caspase-3 protein levels, and the Bax/Bcl-2 ratio, while downregulating Bcl-2. Topoisomerase I/II-IN-1 is useful in the study of various cancers, including melanoma, renal cancer, colorectal cancer, and breast cancer .
    Topoisomerase I/II-IN-1
  • HY-155240
    Tyrosinase-IN-13

    		Tyrosinase Cancer
    Tyrosinase-IN-13 (compound 3c), a derivative of Flurbiprofen (HY-10582), is a potent, non-competitive tyrosinase inhibitor (IC50=68 μM; Ki=36.3 μM). Tyrosinase-IN-13 is cytotoxic against hepatocellular carcinoma (HepG2), colorectal cancer (HT-29), and melanoma (B16F10) .
    Tyrosinase-IN-13
  • HY-106435
    Cystemustine

    		DNA/RNA Synthesis DNA Alkylator/Crosslinker Cancer
    Cystemustine is a DNA inhibitor (a chloroethyl nitrosourea, CENU). Cystemustine can cause DNA cross-linking, thereby inhibiting the proliferation of tumor cells. Cystemustine can also exert cytotoxic effects by interfering with the cell cycle, inducing cell re-differentiation, and altering phospholipid metabolism. Cystemustine exhibits high anti-tumor activity and a relatively short plasma half-life in mice. Cystemustine can be used for the study of various malignant tumors, including melanoma, glioma, renal cancer, head and neck cancer, and colorectal cancer, etc .
    Cystemustine
  • HY-173178
    LNS8801

    		Estrogen Receptor/ERR Cancer
    LNS8801 is an orally active agonist of the G protein-coupled estrogen receptor (GPER). By activating GPER, LNS8801 mediates downstream signaling pathways, such as promoting the production of cyclic adenosine monophosphate (cAMP) and activating the cAMP response element-binding protein (CREB) signaling, thereby exerting anti-tumor activities including inhibiting tumor cell proliferation, inducing cell differentiation, and enhancing tumor immunogenicity. LNS8801 can be used in the research of various cancers (e.g., melanoma, pancreatic cancer, colorectal cancer, lung cancer, etc.) and relevant studies exploring the roles of GPER in normal physiological and pathological processes .
    LNS8801
  • HY-150510
    MS8511

    		Histone Methyltransferase Neurological Disease Cancer
    MS8511 is a selective G9a/GLP covalent irreversible inhibitor by targeting a cysteine residue at the substrate binding site, with IC50 values of 100 nM (G9a) and 140 nM (GLP), and Kd values of 44 nM (G9a) and 46 nM (GLP). MS8511 reduces the cellular H3K9me2 level and enhances antiproliferation activity. MS8511 can be used for the research of several types of cancers including brain, breast, ovarian, lung, bladder, melanoma, colorectal cancer, and other disease such as Alzheimer’s disease (AD), sickle cell disease, Prader−Willi syndrome (PWS) .
    MS8511
  • HY-173149
    CDD-2789

    		Anaplastic lymphoma kinase (ALK) TGF-beta/Smad TGF-β Receptor Cancer
    CDD-2789 is a highly selective small-molecule inhibitor targeting Activin receptor type 1 (ALK2, also known as ACVR1). It blocks the SMAD1/5 signaling pathway mediated by ALK2/ALK1, thereby effectively suppressing downstream phosphorylation events induced by BMP and activin A. In the NanoBRET cellular model, CDD-2789 exhibits an inhibitory IC50 of 0.54 µM against ALK2. CDD-2789 holds promise for research on ALK2-related diseases, including diffuse intrinsic pontine glioma (DIPG), ependymoma, endometrial cancer, melanoma, non–small cell lung cancer, colorectal cancer, and pancreatic cancer .
    CDD-2789
  • HY-132844
    Tunlametinib

    HL-085

    		 MEK Cancer
    Tunlametinib is a highly selective, orally active MEK1/2 inhibitor (IC50=1.9 nM, MEK1). Tunlametinib blocks the RAS-RAF-MEK-ERK signaling pathway, arrests tumor cell cycle and promotes apoptosis. Tunlametinib potently inhibits the proliferation of RAS/RAF mutant cancer cells (such as BRAF V600E, KRAS G12C mutant cells). Tunlametinib shows synergistic anti-tumor effects with BRAF/KRAS G12C/SHP2 inhibitors, Docetaxel (HY-B0011). Tunlametinib can be used to study targeted therapy for RAS/RAF mutation-driven malignancies (such as melanoma, colorectal cancer, and non-small cell lung cancer) .
    Tunlametinib
  • HY-176219
    Bcl-2-IN-23

    		Bcl-2 Family Apoptosis Necroptosis Cancer
    Bcl-2-IN-23 (compound 5) is a selective inhibitor targeting Bcl-2. The IC50 of Bcl-2-IN-23 in HTB-140, HeLa and SW620 cells is 25.7-33.7 μM. Bcl-2-IN-23 can non-covalently competitively bind to Bcl-2 protein, significantly reduce its expression, and induce late apoptosis and necroptosis of cancer cells. Bcl-2-IN-23 enhances the sensitivity of cancer cells to apoptosis and reduces the release of IL-6 inflammatory factors by disrupting the Bcl-2-mediated mitochondrial apoptosis inhibition pathway. Bcl-2-IN-23 can be used for anti-apoptosis research of malignant tumors such as melanoma, cervical cancer, and colorectal cancer .
    Bcl-2-IN-23
  • HY-202699
    SHOC2–RAS PPI-IN-1

    		Ras Apoptosis Cancer
    SHOC2–RAS PPI-IN-1 (compound 6) is a non-covalent competitive inhibitor targeting the interaction between SHOC2 and RAS proteins. SHOC2–RAS PPI-IN-1 has an IC50 of 0.048 μM and a KD of 0.065 μM for NRAS Q61R. SHOC2–RAS PPI-IN-1 can inhibit the activity of the SMP phosphatase complex, leading to increased CRAF S259 phosphorylation levels, thereby blocking the MAPK signaling pathway (such as reducing the levels of pMEK and pERK), inducing tumor cell cycle arrest and apoptosis. SHOC2–RAS PPI-IN-1 can be used for targeted research on malignant tumors such as melanoma and colorectal cancer with NRAS Q61R mutations .
    SHOC2–RAS PPI-IN-1

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