Table 3. Biochemical IC50 values for norleucine peptide inhibitors derived from the H4K44 and H3K36 sequencesa.
| Peptide | Peptide Sequence | WHSC1 941–1240 Biochemical IC50 (μM) | WHSC1L1 1054–1285 Biochemical IC50 (μM) |
|---|---|---|---|
| PTD1 | Ac-RLARRGGV[Nle]RISGLI-NH2 | 0.088 ± 0.005 | 1.1 ± 0.1 |
| PTD2 | Ac-GV[Nle]RI-NH2 | 22 ± 2 | 3.2 ± 0.2 |
| PTD3 | Ac-GVARI-NH2 | 640 ± 70 | > 1000 |
| PTD4 | Ac-GGV[Nle]R-NH2 | 180 ± 20 | 320 ± 30 |
| PTD5 | Ac-RGGV[Nle]-NH2 | 190 ± 20 | 110 ± 10 |
| PTD6 | Ac-V[Nle]RIS-NH2 | 110 ± 20 | 3.0 ± 0.3 |
| PTD7 | Ac-[Nle]RISG-NH2 | 200 ± 40 | > 1000 |
| PTD8 | Ac-SAPATGGV[Nle]KPHRYR-NH2 | 13 ± 1 | 190 ± 30 |
| PTD9 | Ac-GV[Nle]KP-NH2 | 130 ± 20 | 370 ± 40 |
aIC50 values were calculated from three independent replicates