Table 2.
Combination of I-BET151 and other drugs in cancer.
| Types of Combination | Cell lines | Molecular target | Effect | References |
|---|---|---|---|---|
| I-BET151 and trametinib | In vitro in SUM-159PT and MDA-MB-231 cell lines. In vivo in mice. | Inhibit trametinib-induced PDGFRB and DDR1 (SUM-159PT) and FGFR2 and DDR1 (SUM-229PE). | Inhibit trametinib-induced growth and prevent or reverse adaptive drug resistance of cancer cells to trametinib. | (91) |
| I-BET151 and TMZ | In vitro in U87MG and U251 cell lines. In vivo in mice. | Upregulate PUMA. | Promote TMZ-induced apoptosis, oxidative stress and suppress migration, invasion, and formation of colony. | (92) |
| I-BET151 and S63845 | In vitro in 11 melanoma cell lines such as A06M, C002M, C025M1, etc. In vivo in mice. | Inhibit BCL2A1, upregulate BIM and induce caspase‐dependent death. | Synergistically induce apoptosis and expansion of the range of action of I-BET151 and S63845. | (93) |
| I-BET151 and alisertib | In vitro in NB-1643, SK-N-SH, NB-SD and SK-N-AS cell lines. In vivo in mice. | Inhibit reflexive upregulation of AURKA, MYC and MYCN in response to alisertib. | Synergistically inhibit neuroblastoma viability in vitro and vivo. | (94) |
| I-BET151 and IKK inhibitor VII | In vitro in U937 and I-BET151-resistant U937 cell lines. | Inhibit NF-κBp65. | Enhance or restore the sensitivity to I-BET151 in U937 cells. | (13) |
| I-BET151 and THZ1 | In vitro in K562, Jurkat and murine I-BET151-resistant AF9 AML cells. | Synergistically inhibit of the re-activated MYC, MYB, TAL1 and LMO2. | Synergistically induce anticancer effect toward I-BET151-resistant leukemia. | (95) |
| I-BET151 and Vitamin C | In vitro in MDA-MB-231, BT-549 and HCC1937 cell lines. | Upregulate HDAC1 and inhibit H3ac and H4ac. | Sensitize TNBC to I-BET151. | (96) |
| I-BET151 and Vitamin C | In vitro in 1205Lu, C8161, SK-MEL-28, A2058 and SK-MEL-2 cell lines. | Inhibit HAT1 and the acetylation of H4. | Sensitize melanoma to I-BET151. | (97) |
| I-BET151 and LBH589 |
In vitro in KMJR138, Me1007, Mel-RM cell lines and cells from patients. In vivo in mice. |
Inhibit the AKT and Hippo/YAP signaling pathways. Upregulate BIM. | Synergistically induce caspase-dependent apoptosis. | (98) |
| I-BET151 and LBH589 | In vivo in mice. | Upregulate antileukemic activity. | (36) | |
| I-BET151 and romidepsin | In vivo in mice. | Increase IL-6 production and enhance CD8+ T cell proliferation. | Upregulate vaccine-elicited Ab responses. | (99) |
| I-BET151, Forskolin, ISX9, CHIR99021 and DAPT | In vitro in U87MG and glioblastoma stem cells. | Upregulate Ngn2, Ascl1, Brn2 and MAP2. | Reprogram of glioblastoma cells into Neurons. | (100) |
| I-BET151, forskolin and rapamycin | In vitro in U87MG and C6. | Inhibit pdgfra, pdgfrb, pdgfrl, met, vegfa and colla1. | Suppress proliferation and reprogram malignant gliomas to differentiate into glial cells. | (101) |