10058-F4 is a c-Myc inhibitor that specificallly inhibits the c-Myc-Max interaction and prevents transactivation of c-Myc target gene expression.

10074-G5 is a c-Myc Max interaction inhibitor.

A rocaglate (flavagline) derivative that acts a highly specific inhibitor of the oncogenic translation program supporting MM, including key oncoproteins such as MYC, MDM2, CCND1, MAF, and MCL-1.

APTO-253 is a novel small molecule with potent anti-tumor activity in cancer cells via induction of the gene that expresses the Krüppel-like factor 4 (KLF4) master transcription factor, leading to cell cycle inhibition and programmed cell death.

CBL0137 is a metabolically stable curaxin that activates p53 with an EC50 value of 0.37 µM and inhibits NF-κB with an EC50 of 0.47 µM.

MYCMI-6 (NSC354961) is a selective, high affinity inhibitor of MYC-MAX interaction, blocks MYC-driven transcription and binds selectively to the MYC bHLHZip domain with Kd of 1.6 uM in SPR assay.

Mycro 3 is potent and selective for c-Myc in whole cell assays.

sAJM-589 is a novel, potent small molecule Myc inhibitor that disrupts the Myc-Max leucine-zipper heterodimer with IC50 of 1.8 uM.

Lusianthridin, a pure compound from Dendrobium venustum, have an anti-migratory effect. Lusianthridin enhances c-Myc degradation through the inhibition of Src-STAT3 signaling.

EN4, a covalent ligand that targets cysteine 171 (C171) of MYC, is selective for c-MYC over N-MYC and L-MYC. EN4 inhibits MYC transcriptional activity, downregulates MYC targets, and impairs tumorigenesis.

NY2267 is a disruptor of Myc-Max interaction, with an IC50 of 36.5 μM.

MYC-IN-2 is a MYC protein-protein inhibitor. MYC-IN-2 can be used for the research of cancer.

c-Myc inhibitor 4 is a potent, orally bioavailable c-MYC-reducing compound.

c-Myc inhibitor 5 (DA3) is a fluorescent, long chain-bridged bispurine that selectively targets the c-MYC G-quadruplex (KD of 16 μM). c-Myc inhibitor 5 shows inhibition on c-MYC expression rather than other G4-driven oncogenes.

3JC48-3 is a potent, cellularly active and stable c-Myc inhibitor, inhibits c-Myc-max dimerization with IC50 of 34 uM, 5 times more potent than 10074-G5, exhibits an approximate twofold selectivity for c-Myc-Max heterodimers over Max-Max homodimers.3JC48-3 inhibited the proliferation of c-Myc-over-expressing HL60 and Daudi cells with single-digit micromolar IC50 values by causing growth arrest at the G0 /G1 phase.3JC48-3 inhibited c-Myc-Max dimerization in cells validated by CoIP.3JC48-3 decreased prostate cancer cells' growth and viability in a dose-dependent fashion in vitro, upregulated PrKD1 expression and phosphorylation of known PrKD1 substrates: the threonine 120 (Thr-120) residue in beta-catenin and the serine 216 (Ser-216) in Cell Division Cycle 25 (CDC25C).3JC48-3 (1 g/kg, i.p.) decreased the rate of tumor growth in mice with patient-derived prostate cancer xenografts (PDX), without dose-limiting toxicity.

F0909-0360 is a novel small molecule inhibitor of c-Myc, causes the functional repression of c-Myc target gene, shows appreciable anticancer activity against c-Myc expressing cell lines (HT29, IC50=0.2 uM).F0909-0360 showed c-Myc dependent apoptotic cell death, efficiently inhibited the functionality of c-Myc, suppressed the expression of c-Myc target genes (CAD, ODC1, NOP58, and NOP56) both at the transcriptional and translational levels.F0909-0360 showed considerable in vitro efficacy against cancer stem cells (CSCs), inhibited sphere forming capacity of D341-CSCs with IC50 of 4.06 uM.

F1021-0686 is a novel small molecule inhibitor of c-Myc, causes the functional repression of c-Myc target gene, shows appreciable anticancer activity against c-Myc expressing cell lines (HT29, IC50=1.55 uM).F1021-0686 showed c-Myc dependent apoptotic cell death, efficiently inhibited the functionality of c-Myc, suppressed the expression of c-Myc target genes (CAD, ODC1, NOP58, and NOP56) both at the transcriptional and translational levels.F1021-0686 showed considerable in vitro efficacy against cancer stem cells (CSCs), inhibited sphere forming capacity of D341-CSCs with IC50 of 5.27 uM.

MYCMI-7 is a small molecule MYC-binding compound (Kd=4 uM) that inhibits MYC-MAX interaction.MYCMI-7 efficiently and selectively inhibits MYC:MAX and MYCN:MAX interactions in cells, binds directly to recombinant MYC, and reduces MYC-driven transcription.MYCMI-7 induces degradation of MYC and MYCN proteins.MYCMI-7 potently induces growth arrest/apoptosis in tumor cells in a MYC/MYCN-dependent manner and downregulates the MYC pathway on a global level.MYCMI-7 downregulates MYC/MYCN, inhibits tumor growth, and prolongs survival through apoptosis in mouse tumor models of MYC-driven AML, breast cancer, and MYCN-amplified neuroblastoma.

PKUMDL-YC-1205 is a specific small molecule that can specifically bind to the disordered bHLH-LZ domain of c-Myc (SPR kd=18 uM).PKUMDL-YC-1205 abrogates cell proliferation of HL-60 cells with IC50 of 40 uM, blocks the interaction between c-Myc370–409 and Max.

WBC100 (WBC-100) is a novel potent, oral active that selectively degrades c-Myc protein over other proteins and potently kills c-Myc overexpressing cancer cell.selectively kills c-Myc overexpressing cancer cells Mia-paca2 (PDAC), H9 (T-cell lymphoma), andMOLM-13 (acute myeloid leukemia) with IC5 of 61, 17 and 16 nM, respectively.WBC100 targets the nuclear localization signal 1 (NLS1)-Basic-nuclear localization signal 2 (NLS2) region of c-Myc and induces c-Myc protein degradation through ubiquitin E3 ligase CHIP mediated 26S proteasome pathway, leading to apoptosis of cancer cells.WBC100 potently regresses multiple lethal c-Myc overexpressing tumors such as acute myeloid leukemia, pancreatic, and gastric cancers with good tolerability in multiple xenograft mouse models.

IZTZ-1, an imidazole-benzothiazole conjugate, is a c-MYC G4 ligand. IZTZ-1 is able to downregulate the c-MYC expression by stabilizing c-MYC G4. IZTZ-1 induces cell cycle arrest, apoptosis, thereby inhibiting cell proliferation in B16 cells. IZTZ-1 shows antitumor activity, and can be used for melanoma research.

D089 is a selective small molecule stabilizer of the MYC G4-quadruplex, not only inhibits MYC expression in myeloma cell lines, but also selectively induces G1 arrest in MYC-driven cancer cell lines containing the MYC-G4 sequence.