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Catalog No. Product Name Information Product Use Citations Product Validations
S1109 BI 2536 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.
Leukemia, 2024, 38(5):969-980
Clin Transl Med, 2024, 14(5):e1703
Clin Transl Med, 2024, 14(5):e1703
S7153 10058-F4 10058-F4 is a c-Myc inhibitor that specificallly inhibits the c-Myc-Max interaction and prevents transactivation of c-Myc target gene expression. 10058-F4 promotes a caspase-3-dependent apoptosis and modulates autophagy.
Cell Metab, 2024, S1550-4131(24)00284-5
Cell Stem Cell, 2024, S1934-5909(24)00041-9
Sci Rep, 2024, 14(1):4060
S8762 dBET6 dBET6 is a highly cell-permeable PROTAC degrader of BET bromodomains with an IC50 of 14 nM for BRD4 binding. dBET6 also induces c-MYC downregulation and apoptosis.
J Pathol, 2024, 262(1):37-49
Genes Cancer, 2023, 10.18632/genesandcancer.233
Genes Cancer, 2023, 14:56-76
S8426 10074-G5 10074-G5 is a c-Myc inhibitor that binds to and distorts the bHLH-ZIP domain of c-Myc (Kd = 2.8 µM), thereby inhibiting c-Myc/Max heterodimer formation and inhibiting its transcriptional activity (IC50 = 146 µM).
Exp Mol Med, 2023, 10.1038/s12276-023-01062-5
J Exp Clin Cancer Res, 2023, 42(1):25
Cell Rep, 2023, 10.1016/j.celrep.2023.113347
S8906 MYCi975 MYCi975 (NUCC-0200975) is a potent, selective and orally active inhibitor of MYC that disrupts MYC/MAX interaction, promotes MYC T58 phosphorylation and MYC degradation, and impairs MYC driven gene expression. MYCi975 exhibits potent anti-tumor activities.
Cell Rep, 2023, 42(2):112023
Cancer Res, 2022, 82(7):1174-1192
Clin Transl Med, 2022, 12(12):e1146
S8905 MYCi361 MYCi361 is a MYC inhibitor that engages MYC inside cells, disrupts MYC/MAX dimers, and impairs MYC-driven gene expression. MYCi361 binds to MYC with Kd of 3.2 μM. MYCi361 suppresses in vivo tumor growth, increases tumor immune cell infiltration, upregulates PD-L1 on tumors, and sensitizes tumors to anti-PD1 immunotherapy.
Cell Mol Biol Lett, 2024, 29(1):103
Oncotarget, 2023, 14:879-889
Oncotarget, 2023, 10.18632/oncotarget.28517
S9807 EN4 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.
Nat Commun, 2024, 15(1):3905
Cell Rep, 2023, 42(11):113198
S6963 APTO-253

APTO-253 (LOR-253, LT-253) inhibits c-Myc expression and selectively induces CDKN1A (p21), promotes G0-G1 cell-cycle arrest, and triggers apoptosis in acute myeloid leukemia (AML) cells. APTO-253 is also an inducer of KLF4 (Krüppel-like factor 4).
Cell Commun Signal, 2023, 21(1):94
S8961 Alobresib (GS-5829) Alobresib (GS-5829) is a novel BET inhibitor that represents a highly effective therapeutics agent against recurrent/chemotherapy-resistant USC-overexpressing c-Myc. Alobresib (GS-5829) inhibits CLL cell proliferation and induces leukemia cell apoptosis through deregulation of key signaling pathways, such as BLK, AKT, ERK1/2, and MYC. Alobresib (GS-5829) also inhibits NF-κB signaling.
S0103 ML327 ML327 is an isoxazole compound that blocks MYC expression and tumor formation in neuroblastoma. ML327 also restores E-cadherin expression with In-Cell Western EC50 of 1.0 μM. ML327 induces apoptosis.
S0987New MYCMI-6 MYCMI-6 (NSC354961) is a potent and selective endogenous inhibitor of MYC:MAX protein interactions. MYCMI-6 blocks MYC-driven transcription and binds to the MYC bHLHZip domain with Kd of 1.6 μM. MYCMI-6 inhibits tumor cell growth in a MYC-dependent manner with IC50 of <0.5 μM. MYCMI-6 induces apoptosis.
S9667 Inobrodib (CCS-1477) Inobrodib (CCS1477; CBP-IN-1; CBP/p300-IN-4）is a potent and selective inhibitor of p300/CBP bromodomain. CCS1477 works by inhibiting the expression and function of the androgen receptor (AR), as well as inhibiting c-Myc.
bioRxiv, 2024, 2024.03.29.587346
PLoS Pathog, 2023, 19(8):e1011598
S9871 BTYNB BTYNB (BTYNB IMP1 Inhibitor, MDK6620) is a potent and selective inhibitor of IMP1 binding to c-Myc mRNA. BTYNB downregulates β-TrCP1 mRNA and reduces activation of nuclear transcriptional factors-kappa B (NF-κB). BTYNB disrupts this enhancer function by impairing IGF2 mRNA-binding protein 1 (IGF2BP1)-RNA association.
S0249 Mycro 3 Mycro 3 is a potent and selective inhibitor of c-Myc in whole cell assays. Mycro 3 also shows weak inhibitory activity against AP-1.
S1109 BI 2536 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.
Leukemia, 2024, 38(5):969-980
Clin Transl Med, 2024, 14(5):e1703
Clin Transl Med, 2024, 14(5):e1703
S7153 10058-F4 10058-F4 is a c-Myc inhibitor that specificallly inhibits the c-Myc-Max interaction and prevents transactivation of c-Myc target gene expression. 10058-F4 promotes a caspase-3-dependent apoptosis and modulates autophagy.
Cell Metab, 2024, S1550-4131(24)00284-5
Cell Stem Cell, 2024, S1934-5909(24)00041-9
Sci Rep, 2024, 14(1):4060
S8426 10074-G5 10074-G5 is a c-Myc inhibitor that binds to and distorts the bHLH-ZIP domain of c-Myc (Kd = 2.8 µM), thereby inhibiting c-Myc/Max heterodimer formation and inhibiting its transcriptional activity (IC50 = 146 µM).
Exp Mol Med, 2023, 10.1038/s12276-023-01062-5
J Exp Clin Cancer Res, 2023, 42(1):25
Cell Rep, 2023, 10.1016/j.celrep.2023.113347
S8906 MYCi975 MYCi975 (NUCC-0200975) is a potent, selective and orally active inhibitor of MYC that disrupts MYC/MAX interaction, promotes MYC T58 phosphorylation and MYC degradation, and impairs MYC driven gene expression. MYCi975 exhibits potent anti-tumor activities.
Cell Rep, 2023, 42(2):112023
Cancer Res, 2022, 82(7):1174-1192
Clin Transl Med, 2022, 12(12):e1146
S8905 MYCi361 MYCi361 is a MYC inhibitor that engages MYC inside cells, disrupts MYC/MAX dimers, and impairs MYC-driven gene expression. MYCi361 binds to MYC with Kd of 3.2 μM. MYCi361 suppresses in vivo tumor growth, increases tumor immune cell infiltration, upregulates PD-L1 on tumors, and sensitizes tumors to anti-PD1 immunotherapy.
Cell Mol Biol Lett, 2024, 29(1):103
Oncotarget, 2023, 14:879-889
Oncotarget, 2023, 10.18632/oncotarget.28517
S9807 EN4 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.
Nat Commun, 2024, 15(1):3905
Cell Rep, 2023, 42(11):113198
S6963 APTO-253

APTO-253 (LOR-253, LT-253) inhibits c-Myc expression and selectively induces CDKN1A (p21), promotes G0-G1 cell-cycle arrest, and triggers apoptosis in acute myeloid leukemia (AML) cells. APTO-253 is also an inducer of KLF4 (Krüppel-like factor 4).
Cell Commun Signal, 2023, 21(1):94
S0103 ML327 ML327 is an isoxazole compound that blocks MYC expression and tumor formation in neuroblastoma. ML327 also restores E-cadherin expression with In-Cell Western EC50 of 1.0 μM. ML327 induces apoptosis.
S0987New MYCMI-6 MYCMI-6 (NSC354961) is a potent and selective endogenous inhibitor of MYC:MAX protein interactions. MYCMI-6 blocks MYC-driven transcription and binds to the MYC bHLHZip domain with Kd of 1.6 μM. MYCMI-6 inhibits tumor cell growth in a MYC-dependent manner with IC50 of <0.5 μM. MYCMI-6 induces apoptosis.
S9667 Inobrodib (CCS-1477) Inobrodib (CCS1477; CBP-IN-1; CBP/p300-IN-4）is a potent and selective inhibitor of p300/CBP bromodomain. CCS1477 works by inhibiting the expression and function of the androgen receptor (AR), as well as inhibiting c-Myc.
bioRxiv, 2024, 2024.03.29.587346
PLoS Pathog, 2023, 19(8):e1011598
S9871 BTYNB BTYNB (BTYNB IMP1 Inhibitor, MDK6620) is a potent and selective inhibitor of IMP1 binding to c-Myc mRNA. BTYNB downregulates β-TrCP1 mRNA and reduces activation of nuclear transcriptional factors-kappa B (NF-κB). BTYNB disrupts this enhancer function by impairing IGF2 mRNA-binding protein 1 (IGF2BP1)-RNA association.
S0249 Mycro 3 Mycro 3 is a potent and selective inhibitor of c-Myc in whole cell assays. Mycro 3 also shows weak inhibitory activity against AP-1.
S8762 dBET6 dBET6 is a highly cell-permeable PROTAC degrader of BET bromodomains with an IC50 of 14 nM for BRD4 binding. dBET6 also induces c-MYC downregulation and apoptosis.
J Pathol, 2024, 262(1):37-49
Genes Cancer, 2023, 10.18632/genesandcancer.233
Genes Cancer, 2023, 14:56-76
S8961 Alobresib (GS-5829) Alobresib (GS-5829) is a novel BET inhibitor that represents a highly effective therapeutics agent against recurrent/chemotherapy-resistant USC-overexpressing c-Myc. Alobresib (GS-5829) inhibits CLL cell proliferation and induces leukemia cell apoptosis through deregulation of key signaling pathways, such as BLK, AKT, ERK1/2, and MYC. Alobresib (GS-5829) also inhibits NF-κB signaling.
S0987New MYCMI-6 MYCMI-6 (NSC354961) is a potent and selective endogenous inhibitor of MYC:MAX protein interactions. MYCMI-6 blocks MYC-driven transcription and binds to the MYC bHLHZip domain with Kd of 1.6 μM. MYCMI-6 inhibits tumor cell growth in a MYC-dependent manner with IC50 of <0.5 μM. MYCMI-6 induces apoptosis.

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