Skip to main content
. 2021 Sep 2;11:716830. doi: 10.3389/fonc.2021.716830

Table 1.

Anticancer activity of I-BET151 against various cancer cells.

Cancer type Cell lines Molecular target Effect References
Acute myeloid leukemia In vitro in MV4;11, MOLM13 and NOMO1 cell lines. In vivo in mice. Inhibit BCL2, C-MYC and CDK6. Cause G0/G1 arrest and induce cell apoptosis (7)
Acute myeloid leukemia In vitro SEM, RS4; 11 and ALL-PO cell lines. In vivo in mice. Inhibit HOXA7/9 and RUNX1. Inhibit proliferation, cause G0/G1 arrest, block cell division and induce cell apoptosis. (36)
Acute myeloid leukemia In vitro in MOLM13 and THP1 cell lines. In vivo in humanized bone marrow xenograft model of secondary MLL-AF9-driven B-ALL. Inhibit Bax, BCL2 and C-MYC. Upregulate CDKN1A and CDKN1B. Inhibit proliferation, cause G0/G1 arrest and induce cell apoptosis. (37)
Acute myeloid leukemia In vitro in OCI-AML3, KG-1, SKM1, Kasumi, ME-1 cell lines. In vivo in mice. Inhibit BCL2, C-MYC and IRF8. Cause cell cycle arrest and induce cell apoptosis. (38)
Acute myeloid leukemia In vitro in AML lines with dual DNMT3AR882H and RAS mutations. In vivo in mice. Inhibit Mn1, Mycn and Bcl2. Cause cell cycle arrest and induce cell apoptosis. (39)
Acute myeloid leukemia In vitro in U937, HL-60, R-U937 and R-HL-60 cell lines. Inhibit HP1γ. Inhibit proliferation. (40)
Myeloma In vitro in H929, KMS12PE, KMS12BM, KMS18, KMS11 and RPMI8226 cell lines. In vivo in mice. Downregulate MYC. Upregulate HEXIM1. Cause cell cycle arrest and induce cell apoptosis. (41)
Myeloma In vitro in U266, RPMI8226, MM1 and KMS11 cell lines. Inhibit MYCL1 in U266. Inhibit c-MYC in RPMI8226, MM1 and KMS11. Inhibit proliferation and cause cell cycle arrest. (42)
Myeloma In vitro in SKO-007(J3), CD138+ multiple myeloma cells and NK cells isolated from the bone marrow of multiple myeloma patients. Inhibit IRF4 and upregulate MICA. Promote NK cell degranulation. (29)
Myeloma In vitro in RAW 264.7 cell lines and in mononuclear cells isolated from healthy donors and patients with multiple myeloma. Inhibit TRACP, MMP9, Ctsk and c-Src. Upregulate OPG. Suppress IκB-α degradation and p65 nuclear translocation. Inhibit osteoclast formation and inflammatory cytokine secretion. (11)
Primary effusion lymphoma In vitro in BC1, BC3 and BCBL1 cell lines. In vivo in mice. Inhibit c-Myc. Inhibit proliferation and cause G0/G1 arrest. (43)
Mantle cell lymphoma In vitro in JVM-2, MINO, Z138 and KPUM-YY1 cell lines Inhibit PAX5, IKZF1, BTK, SYK, EBF1 and MYC. Cause G1/S arrest and induce cell apoptosis. (44)
Myeloproliferative neoplasms In vitro in a human erythroleukemic cell line. Inhibit LMO2. Inhibit proliferation and induce cell apoptosis. (45)
Triple-negative breast cancer In vitro in MDA-MB-231, MDA-MB-468 and BT549 cell lines. Inhibit IKBKE. Inhibit proliferation and induce cell apoptosis. (12)
Breast cancer In vitro in MB-231, MB-468 and SK-BR-3 cell lines. Upregulate GSSG and MDA levels. Induce ferroptosis. (46)
Breast cancer In vivo in mice implanted with Mvt1 and 6DT1. Inhibit proliferation. (47)
Glioma In vitro in U87MG, A172, SW1783 cell lines and glioblastoma stem cells derived from patients. In vivo in mice. Inhibit proliferation and cause G1/S arrest. (48)
Glioma In vitro in U87MG, A172, LN18, T98G cell lines and in patient derived xenograft cells. Inhibit HOTAIR, TUG1 and H19. Inhibit proliferation. (49)
Glioma In vitro in U87MG, U251 cell lines and Primary cells obtained from GBM patients. In vivo in mice. Inhibit Notch1/NICD/Hes1. Reduce self‐renewal and proliferation of glioma-initiating cells. (6)
Melanoma In vitro in Me1007, SK-Mel-28, Mel-RMu, Mel-JD, Mel-RM and the resistant (post) cell lines from patients. In vivo in mice. Inhibit p50, p105 and CDK6. Upregulate of CDKN1A. Inhibit cytokine/chemokine production, cause cell cycle arrest and induce cell apoptosis. (4)
Melanoma In vitro in Mel-RMU, Sk-Mel-28, Mel-RM, Mel-JD and Me1007 cell lines. In vivo in mice. Inhibit XIAP. Upregulate of BIM and p21. Cause cell cycle arrest and induce cell apoptosis. (50)
Neuroblastoma In vitro in SK-N-BE (2) and Kelly cell lines. Inhibit NCYM and N-Myc. Upregulate of TP53INP1. Induce cell apoptosis. (51, 52)
Ovarian cancer In vitro in 28 ovarian cancer cell lines. In vivo in mice. Inhibit FoxM1, AURKB, survivin, cyclinB and PLK1. Inhibit proliferation, cause G0/G1 arrest. (5)
Ovarian cancer In vitro in SK-OV-3, CaoV-3 and ID8 cell lines.
In vivo in mice.
Upregulate BIM and Cleaved caspase-3. Inhibit MMP2, MMP9 and p-Stat3. Inhibit proliferation, invasion and migration, induce cell apoptosis and antitumor immune response. (30)
Ovarian cancer In vitro in A2780CP, OVCAR3 and SKOV3 cell lines. Inhibit FoxM1, AURKB, cyclinB1, ZEB2, N-cadherin, Survivin and Bcl-2. Inhibit proliferation, invasion, migration and induce cell apoptosis. (53)
Colorectal cancer In vitro in HCT116 transduced with SLUG or SNAIL retroviruses. Suppress EMT and inhibit SP cell production. (54)
Castration-resistant prostate cancer In vitro in LNCaP95 and VCaP cell lines. Inhibit AR-V7, C-MYC, PSA and TMPRSS2. Inhibit proliferation and AR signaling. (55)
Pancreatic ductal adenocarcinoma In vitro in human primary pancreatic stellate cells. Inhibit COL1A1, COL1A2 and collagen I. Attenuate fibrosis. (56)
Non-small cell lung carcinoma In vitro in Calu-1, H460 and A549 cell lines. Inhibit c-Myc, eIF4E and cyclin D1. Inhibit proliferation. (57)
HHS Vulnerability Disclosure