| E4750New |
Cpd. 37
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MYC-IN-3 (Cpd. 37) is an alkynyl-substituted phenylpyrazole derivative and an inhibitor of MYC function by disrupting MYC/MAX interaction with an IC50 of 1.27 μM in PC3 cells and preventing MYC/MAX binding to DNA. It exhibits antiproliferative activity against multiple malignant cell lines and demonstrates enhanced therapeutic efficacy in a mouse allograft model of prostate cancer.
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| S0103 |
ML327
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ML327 is an isoxazole compound that blocks MYC expression and tumor formation in neuroblastoma. This compound also restores E-cadherin expression with In-Cell Western EC50 of 1.0 μM. It induces apoptosis.
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| S0987 |
MYCMI-6
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MYCMI-6 (NSC354961) is a potent and selective endogenous inhibitor of MYC:MAX protein interactions. This compound blocks MYC-driven transcription and binds to the MYC bHLHZip domain with Kd of 1.6 μM. It inhibits tumor cell growth in a MYC-dependent manner with IC50 of <0.5 μM. This chemical induces apoptosis.
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| S9871 |
BTYNB
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BTYNB (BTYNB IMP1 Inhibitor, MDK6620) is a potent and selective inhibitor of IMP1 binding to c-Myc mRNA. This compound downregulates β-TrCP1 mRNA and reduces activation of nuclear transcriptional factors-kappa B (NF-κB). It disrupts this enhancer function by impairing IGF2 mRNA-binding protein 1 (IGF2BP1)-RNA association.
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| S1109 |
BI 2536
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BI-2536 is a potent Plk1 inhibitor with IC50 of 0.83 nM in a cell-free assay. BI-2536 inhibits Bromodomain 4 (BRD4) with Kd of 37 nM and potently suppresses c-Myc expression. BI-2536 induces apoptosis and attenuates autophagy. Phase 2.
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Gut, 2025, gutjnl-2024-334274
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Nat Commun, 2025, 16(1):1599
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Genome Biol, 2025, 26(1):204
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| S8961 |
Alobresib (GS-5829)
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Alobresib (GS-5829) is a novel BET inhibitor that represents a highly effective therapeutics agent against recurrent/chemotherapy-resistant USC-overexpressing c-Myc. This compound inhibits CLL cell proliferation and induces leukemia cell apoptosis through deregulation of key signaling pathways, such as BLK, AKT, ERK1/2, and MYC. It also inhibits NF-κB signaling.
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| E1882 |
THZ1
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THZ1 is a potent and covalent inhibitor of CDK7 with an IC50 of 3.2 nM. It also inhibits the CDK12 and CDK13 and downregulates MYC expression. It exhibits strong anti proliferative effect across a broad range of cancer cell lines including human T-cell acute lymphoblastic leukaemia (T-ALL) cancer.
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