Approved antilymphoma agents and experimental inhibitors of key regulatory pathway with a median IC50 below 1 µM in B-cell and T-cell lymphoma cell lines
| Compound . | IC50, nM . | 95% CI, nM . | Mechanism of action . |
|---|---|---|---|
| B-cell lymphomas | |||
| Bortezomib | 5 | 5-7 | Proteasome inhibitor |
| Roniciclib | 23 | 18-29 | CDK inhibitor |
| Romidepsin | 34 | 2-94 | Class I HDAC inhibitor |
| Panobinostat | 161 | 11-1263 | Class I and II HDAC inhibitor |
| MI2 | 490 | 224-1000 | MALT1 inhibitor |
| BAY 1238097 | 684 | 463-1356 | BET inhibitor |
| Atuveciclib | 716 | 395-1020 | PTEFb/CDK9 inhibitor |
| Ibrutinib | 788 | 31-1000 | BTK inhibitor ibrutinib |
| T-cell lymphomas | |||
| Romidepsin | 2 | 2-5 | Class I HDAC inhibitor |
| Bortezomib | 3 | 2-6 | Proteasome inhibitor |
| Panobinostat | 10 | 5-14 | Class I and II HDAC inhibitor |
| Roniciclib | 21 | 16-42 | CDK inhibitor |
| BAY 1238097 | 410 | 282-690 | BET inhibitor |
| Atuveciclib | 567 | 324-1952 | PTEFb/CDK9 inhibitor |
| Compound . | IC50, nM . | 95% CI, nM . | Mechanism of action . |
|---|---|---|---|
| B-cell lymphomas | |||
| Bortezomib | 5 | 5-7 | Proteasome inhibitor |
| Roniciclib | 23 | 18-29 | CDK inhibitor |
| Romidepsin | 34 | 2-94 | Class I HDAC inhibitor |
| Panobinostat | 161 | 11-1263 | Class I and II HDAC inhibitor |
| MI2 | 490 | 224-1000 | MALT1 inhibitor |
| BAY 1238097 | 684 | 463-1356 | BET inhibitor |
| Atuveciclib | 716 | 395-1020 | PTEFb/CDK9 inhibitor |
| Ibrutinib | 788 | 31-1000 | BTK inhibitor ibrutinib |
| T-cell lymphomas | |||
| Romidepsin | 2 | 2-5 | Class I HDAC inhibitor |
| Bortezomib | 3 | 2-6 | Proteasome inhibitor |
| Panobinostat | 10 | 5-14 | Class I and II HDAC inhibitor |
| Roniciclib | 21 | 16-42 | CDK inhibitor |
| BAY 1238097 | 410 | 282-690 | BET inhibitor |
| Atuveciclib | 567 | 324-1952 | PTEFb/CDK9 inhibitor |
BTK, Bruton tyrosine kinase; CDK, cyclin-dependent kinase; HDAC, histone deacetylase; MALT1, mucosa-associated lymphoid tissue lymphoma translocation protein 1.