1. Signaling Pathways
  2. Apoptosis
  3. c-Myc

c-Myc

Myc

The transcription factor c-Myc is a member of the basic helix-loop-helix leucinezipper (bHLHZip) protein family. The target genes of the c-MYC protein participate in different cellular functions, including cell cycle, survival, protein synthesis, cell adhesion, and micro-RNA expression. c-Myc is also one of the four factors used in reprogramming somatic cells to induce pluripotent stem (iPS) cells and is implicated in maintaining cancer stem-like cells (CSCs). Most biological functions of c-Myc require heterodimerization with its activation partner Max.

c-Myc is also part of a dynamic network whose members interact selectively with one another and with various transcriptional coregulators and histone-modifying enzymes. Deregulated expression of c-MYC caused by gene amplification, retroviral insertion, or chromosomal translocation is associated with tumorigenesis. c-Myc has been identified as a highly promising target for cancer therapy.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-16291A
    APTO-253 hydrochloride
    Inhibitor
    APTO-253?(LOR-253) hydrochloride is a small molecule that inhibits c-Myc expression, stabilizes G-quadruplex DNA and induces cell cycle arrest and apoptosis in acute myeloid leukemia cells. APTO-253?hydrochloride mediates anticancer activity via induction of Kruppel-like factor 4?(KLF4)?tumor suppressor. APTO-253?hydrochloride exhibits antiarthritic activity.
    APTO-253 hydrochloride
  • HY-125636
    Mycro1
    Inhibitor
    Mycro1 is an inhibitor of c-Myc/Max dimer and DNA binding, with an IC50 value of 30 μM for the inhibition of Myc/Max DNA binding activity. Mycro1 can inhibit c-myc-dependent cell proliferation, gene transcription and oncogenic transformation.
    Mycro1
  • HY-178039
    CDK9-IN-42
    Inhibitor
    CDK9-IN-42 is a potent and selective CDK9 inhibitor with an IC50of 3.8 nM. CDK9-IN-42 can inhibit the growth of cancer cells and induce apoptosis by downregulating Myc-1 and c-Myc. CDK9-IN-42 can be used for the research of cancer, such as breast and lungcancer.
    CDK9-IN-42
  • HY-W013724S
    Inosine-5'-diphosphate-15N4 dilithium
    Inhibitor
    Inosine-5'-diphosphate-15N4 dilithium (IDP-15N4 dilithium) is 15N labeled Inosine-5'-diphosphate dilithium. Inosine-5'-diphosphate (IDP) is a decoy substrate of NM23-H2. Inosine-5'-diphosphate has a superior bond capacity on GDP-binding pocket of NM23-H2 (KD: 5.0 μM). Inosine-5'-diphosphate abrogates c-MYC transcription, induces apoptosis and G2/M cell cycle arrest by disrupting NM23-H2-Pu27-GQ interactions without affecting NM23-H2-mediated kinase properties. Inosine-5'-diphosphate has antihypoxic, antihyperthermic and antiarrhythmic activity and protects animals against the noxious effects of γ-irradiation. Inosine-5'-diphosphate can be used for cancers like Burkitt's lymphoma and cardiovascular diseases research.
    Inosine-5'-diphosphate-<sup>15</sup>N<sub>4</sub> dilithium
  • HY-178045
    MYC-IN-4
    Inhibitor
    MYC-IN-4 is a MYC inhibitor. MYC-IN-4 impairs MYC/MAX protein-protein interaction (IC50 = 3.06 μM). MYC-IN-4 inhibits MYC-aberrant PC-3 prostate cancer cells with an IC50 of 0.440 μM. MYC-IN-4 demonstrates potent antitumor efficacy in FVB mice bearing Myc-CaP prostate tumor allografts. MYC-IN-4 can be used for the study of prostate cancer.
    MYC-IN-4
  • HY-169348
    β-catenin-IN-8
    Inhibitor
    β-catenin-IN-8 (Compound 25) is a β-catenin inhibitor. β-catenin-IN-8 inhibits β-catenin and c-Myc protein levels, and inhibits Wnt-target genes level (Fgf20 and Sall4). β-catenin-IN-8 has colorectal cancer anticancer activities, and has metabolic stability.
    β-catenin-IN-8
  • HY-175771
    STAT3-IN-46
    Inhibitor
    STAT3-IN-46 is a selective and orally active inhibitor of signal transducer and activator of transcription 3 (STAT3) (KD = 323.3 nM). STAT3-IN-46 directly binds to the SH2 domain of the STAT3 and inhibits IL-6/JAK/STAT3 signaling pathway (IC50 = 0.87 μM) and downregulates c-Myc and Bcl-2 levels. STAT3-IN-46 can be used for the research of cancer, such as triple-negative breast cancer.
    STAT3-IN-46
  • HY-125718
    MLS-2384 free base
    Inhibitor
    MLS-2384 free base is a dual JAK/Src kinase inhibitor. MLS-2384 free base downregulates STAT3 downstream proteins c-Myc and Mcl-1. MLS-2384 free base induces Apoptosis. MLS-2384 free base exhibits anticancer activity against prostate cancer, breast cancer, skin cancer, ovarian cancer, lung cancer, and liver cancer.
    MLS-2384 free base
  • HY-P10418
    VGN50
    Inhibitor
    VGN50 is a bioactive molecule that mimics the function of K-Rta and down-regulates MYC-mediated gene transcription. VGN50 has antitumor activity.
    VGN50
  • HY-160549
    c-Myc inhibitor 14
    Inhibitor
    c-Myc inhibitor 14 (Compound 13A) is a c-Myc protein inhibitor. The IC50 value of HL60 inhibitor is <100 nM. c-Myc inhibitor 14 shows antitumor activity.
    c-Myc inhibitor 14
  • HY-170595
    PROTAC LZK degrader 1
    Inhibitor
    PROTAC LZK degrader 1 (Compound 21A) is a PROTAC that targets the degradation of LZK (Leucine Zipper Kinase, encoded by MAP3K13). PROTAC LZK degrader 1 (10 μM) promotes the degradation of LZK and inhibits the expression of p53 and c-MYC, leading to reduced viability of global head and neck squamous cell carcinoma (HNSCC) cell lines. PROTAC LZK degrader 1 can be used in cancer research. PROTAC LZK degrader 1 consists of an E3 ligase ligand (blue part, HY-112078), a target protein ligand (red part, HY-170596), and a linker (black part, HY-W019543)[1].
    PROTAC LZK degrader 1
  • HY-169921
    c-Myc inhibitor 15
    Inhibitor
    c-Myc inhibitor 15 (Compound A5) is a selective c-Myc inhibitor that exerts anticancer effects by disrupting the interaction between c-Myc and Max, leading to the degradation of c-Myc protein and the induction of apoptosis. Its IC50 values are 4.08 μM and 7.86 μM in A549 and NCI-H1299 lung cancer cell lines, respectively, demonstrating strong cytotoxic activity. In a syngeneic tumor model, c-Myc inhibitor 15 exhibited outstanding antitumor efficacy, achieving a tumor growth inhibition rate of 76.4% and significantly reducing c-Myc protein expression levels. c-Myc inhibitor 15 holds promise for research related to c-Myc-driven lung cancers.
    c-Myc inhibitor 15
  • HY-125090
    PHA-680626
    Inhibitor
    PHA-680626 is an effective inhibitor of the interaction between Aurora-A and N-Myc. PHA-680626 inhibits kinase activity of AURKA and Bcr-Abl, and induces N-Myc degradation. PHA-680626 decreases phosphorylation of CrkL and histone H3. PHA-680626 shows anti-proliferative and pro-apoptotic activity on Imatinib (HY-15463)-resistant chronic myeloid leukemia cell lines and primary CD34+ cells.
    PHA-680626
  • HY-143471
    WNY0824
    Inhibitor
    WNY0824 (PLK1/BRD4-IN-1) is an orally active dual inhibitor of PLK1 and BET protein families, with IC50 values ​​of 22, 402.5, 150.7, 103.9, and 311.9 nmol/L for PLK1, BRD2, BRD3, BRD4, and BRDT, respectively. WNY0824 induces cell cycle arrest and apoptosis by inhibiting AR- and MYC-mediated transcriptional processes. In addition, WNY0824 also inhibits tumor growth in Enzalutamide (HY-70002) resistant CRPC xenograft tumor models.
    WNY0824
  • HY-154839
    c-Myc inhibitor 10
    Inhibitor
    c-Myc inhibitor 10 (compound 17), a c-Myc inhibitor, exhibits increased cellular potency, consistent with an increase in permeability with methylation of the morpholine nitrogen.
    c-Myc inhibitor 10
  • HY-121444
    MYRA-A
    Inhibitor
    MYRA-A is a potent apoptosis inducer in a Myc-dependent manner. MYRA-A inhibits Myc transactivation and interferes with the DNA-binding activity of Myc family proteins. MYRA-A inhibits cell viability.
    MYRA-A
  • HY-181729
    PROTAC BET Degrader-15
    Inhibitor
    PROTAC BET Degrader-15 is a BET PROTAC degrader with DC50 values of <0.10 nM, <0.01 nM, and <0.01 nM against BRD2, BRD3, and BRD4, respectively. PROTAC BET Degrader-15 induces significant G2/M phase cell cycle arrest and triggers apoptosis. PROTAC BET Degrader-15 causes marked downregulation of c-Myc, accompanied by upregulation of the cell cycle inhibitory protein p21, downregulation of CDK6, and an increase in the apoptosis marker cleaved PARP. PROTAC BET Degrader-15 is applicable to the research of hematologic malignancies and lung cancer.
    PROTAC BET Degrader-15
  • HY-180124
    CDK8-IN-20
    Inhibitor
    CDK8-IN-20 (Compound 67j) is a selective, potent and orally active type I CDK8 inhibitor with an IC50 of 70.5 nM. CDK8-IN-20 shows IC50 values of 147.8, 726.9 and 217.4 nM for homologous kinase CDK19, CDK7 and CDK9. CDK8-IN-20 can inhibit the Wnt/β-catenin pathway and downregulate the expression of β-catenin, Cyclin D1, and c-Myc. CDK8-IN-20 can induce ROS production and cause G2/M and S phase arrest. CDK8-IN-20can be used for the research of cancer, such as colon cancer.
    CDK8-IN-20
  • HY-183770
    LCI40
    Inhibitor
    LCI40 is an orally active dual PI3K/BRD4 inhibitor (PI3Kα IC50 = 0.071 μM, PI3Kβ IC50 = 0.17 μM, PI3Kγ IC50 = 0.66 μM, PI3Kδ IC50 = 0.072 μM, BRD4 BD1 IC50 = 0.19 μM, and BRD4 BD2 IC50 = 1.88 μM. LCI40 inhibits phosphorylation of pAKT (S473) and suppresses c-MYC levels in mantle cell lymphoma cells. LCI40 displays immunomodulatory capacity with minimal toxicity to normal mouse immune cells. LCI40 can be used for the research of mantle cell lymphoma.
    LCI40
  • HY-178909
    Y502-2304
    Inhibitor
    Y502-2304 is a c-Myc G-quadruplex stabilizer. Y502-2304 exhibits potent antiproliferative activity in multiple myeloma (MM) cells. Y502–2304 downregulates c-Myc mRNA and protein expression. Y502-2304 induces apoptosis in MM cells, characterizes by elevated γH2AX levels, increases reactive oxygen species (ROS) generation, and mitochondrial dysfunction. Y502-2304 significantly inhibits tumor growth in a xenograft MM model. Y502-2304 can be used for the study of multiple myeloma.
    Y502-2304
Cat. No. Product Name / Synonyms Application Reactivity