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

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

K_D = 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)

K_D = 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

–

K_D = 1.6 ± 0.5 μM (SPR, binding to c-Myc)

Yes

Yes

[91]

KJ-Pyr-9

B

Yes

K_D = 6.5 ± 1.0 nM (Backscattering Interferometry, binding to c-Myc)

Yes

–

[62, 92, 93]

MYCi361

B, C

Yes

K_D = 3.2 μM (FP competition assay, binding to c-Myc)

Yes

Yes

[94]

MYCi975

B, C

–

K_D = 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

K_D 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

K_D = 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

K_D = 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]