Table 1.
Inhibitors used in the study.
| Inhibitor | Mechanism | IC50 in MV411, μM |
Concentration used, μM |
References |
|---|---|---|---|---|
| ATRA | ↓MYB expression | 0.27 | 1 | 43 |
| Celastrol | MYB::p300 (KIX domain) | 0.12 | 0.1 | 34 |
| Mebendazole | MYB degradation | 0.71 | 10 | 41,42,62 |
| MYBMIM | MYB::CBP/p300 (KIX domain) | 1.5 | 20 | 31 |
| Naphthol AS-E phosphate | MYB::p300 (KIX domain) | 13.2 | 10 | 40 |
| Plumbagin | MYB::p300 (MYB TAD) | 0.58 | 0.5 | 33 |
| JQ1 | BET bromodomain inhibition → ↓MYB functional output | 0.41 | 1 | 44,45 |
| KI-MS2-008 | Stabilization of MAX homodimer → MYC inhibition | 22.4 | 50 | 46 |
| MYCi361 | Dissociation of MYC/MAX heterodimer → MYC inhibition | 2.22 | 10 | 47 |