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Table 1 Properties of small molecules, peptides and proteins that inhibit Myc activity

From: Taking the Myc out of cancer: toward therapeutic strategies to directly inhibit c-Myc

Inhibitor type Inhibitor Mechanism of action (A, B or C)a Inhibitor of Myc/Max binding to DNA in vitro Activity in vitro Reduction of cancer cell growth/proliferation Tumor reduction in animal models Reference
Small Molecules IIA6B17 B Yes IC50 = 50 ± 25 μM (EMSA, inhibition of E-box binding) Yes [73, 74]
NY2267 B Yes IC50 = 36.5 μM (EMSA, inhibition of E-box binding) [75]
10,058-F4 B Yes KD = 42 μM (Binding to c-Myc) 15 μM (SPR) Yes No [76,77,78,79,80,81]
10,074-G5 B Yes IC50 = 146.8 μM (EMSA, inhibition of E-box binding)
KD = 20 μM (Binding to c-Myc) 18 μM (SPR)
Yes No [76, 77, 82, 83]
JY-3-094 B Yes IC50 = 33 μM (EMSA, inhibition of E-box binding) Yes [84, 85]
3jc48–3 B Yes IC50 = 34.8 μM (EMSA, inhibition of E-box binding) Yes [86]
Mycro1, Mycro2 B Yes IC50 = 30 ± 5 μM (Mycro1) and 23 ± 4 μM (EMSA, inhibition of dimerization and E-box binding) Yes [87, 88]
Mycro3 B Yes IC50 = 40 ± 13 μM (FP competition assay, inhibition of E-box binding and dimerization) Yes [88,89,90]
MYCMI-6 B KD = 1.6 ± 0.5 μM (SPR, binding to c-Myc) Yes Yes [91]
KJ-Pyr-9 B Yes KD = 6.5 ± 1.0 nM (Backscattering Interferometry, binding to c-Myc) Yes [62, 92, 93]
MYCi361 B, C Yes KD = 3.2 μM (FP competition assay, binding to c-Myc) Yes Yes [94]
MYCi975 B, C KD = 2.5 μM (FP competition assay, binding to c-Myc) Yes Yes [94]
Celastrol and analogues A,C Yes IC50 = 67 ± 2 μM (Celastrol) (EMSA, inhibition of E-box binding) Yes Yes b [95]
JKY-2-169 A Yes IC50 = 11.6 ± 2.3 μM (EMSA, inhibition of E-box binding) [94, 96, 97]
EN4 B Yes IC50 = 6.7 ± 2.3 μM (inhibition of E-box binding) Yes Yes [98]
(Poly)peptide/mini-protein Omomyc A, B, C Yes KD of Omomyc homodimer = nM range (Circular Dichroism spectroscopy, binding to E-box) Yes Yes [43,44,45, 48, 49, 99,100,101,102,103,104,105]
Max bHLHZ A, B Yes [5]
Mad1 A, B Yes Yes [106]
ME47 A Yes KD = 15.3 ± 1.6 nM (EMSA, binding to E-box) Yes c Yes c [107,108,109,110]
Monoclonal antibody B Yes [111]
H1 peptide B Yes Yes Yes [112,113,114,115,116,117]
aMax/aMip B Yes KD = 460 μM (aMax), 250 μM (aMip) (Thermal denaturation monitored by CD, binding c-Myc in absence of DNA) [118,119,120]
Linked basic regions A [121,122,123]
  1. a Mechanisms of action: A) E-box inhibitor, B) Inhibitor of c-Myc/Max binding, C) c-Myc degradation promoter
  2. b Shown to inhibit tumor growth but likely due to another mechanism [124]
  3. c Transgene, not as a peptide alone
  4. - indicates that this is currently unknown