c-Myc

Signaling Pathway Map

Research Area

Inhibitory Selectivity

c-Myc Products

Catalog No. 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.

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.

S0103New

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.

S8905New

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.

S8906New

MYCi975

MYCi975 is an 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.

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).

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.

S8961New

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.

Catalog No. 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.

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.

S0103New

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.

S8905New

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.

S8906New

MYCi975

MYCi975 is an 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.

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).

Catalog No. Information Product Use Citations Product Validations
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.

Catalog No. Information Product Use Citations Product Validations
S8961New

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.