c-Myc 选择性抑制剂 | 调节剂
| 目录号 | 产品名 | 产品描述 | Selective / Pan | IC50 / Ki |
|---|---|---|---|---|
| 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. | Selective | |
| 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. | Selective | |
| 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). |
Selective | |
| 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. | Selective | |
| 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. | Selective | |
| 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. | Selective | |
| 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). | Selective | c-Myc, Kd: 2.8 μM |
| 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. | Selective | MYC, Kd: 3.2 μM |
| 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. | Selective | |
| 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. | Selective | |
| 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. | Selective | |
| 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. | Selective |
