Table 1. BET bromodomain inhibitors in cancer.

name	Cancer type	Target	Mechanism/pathway	Reference
JQ1	Tam-R breast cancer	BRD3/4	Suppresses the classic estrogen receptor-α signaling pathway and the growth of Tam-R breast cancer cells in culture	[53]
	NUT midline carcinoma (NMC)	BRD3/4	Suppresses different BRD4-NUT translocations	[73]
	AML cells	BRD4	Reduce binding of BRD4 and RNA polymerase II to the DNA of c-MYC and BCL2	[62]
	OCI-AML3 cell line	BRD4	Trigger caspase 3/7-mediated apoptosis and DNA damage response.	[63]
	Erythroleukemia cell line UT7	BRD4	Inhibit Epo-induced UT7 proliferation and restoring terminal erythroid differentiation	[95]
	B-cell non-Hodgkin lymphoma	BRD4	Induce cell death through MYC-CYCLON pathway	[96]
	Neuroblastoma	BRD4	Induce cell death through targeting MYCN	[67]
	Primary glioblastoma xenograft lines	BRD4	Induced marked G1 cell-cycle arrest and apoptosis through Bcl-xL and p21(CIP1/WAF1).	[97]
	Osteosarcoma cells	BRD4	Trigger transcriptional silencing of MYC and RUNX2, resulting from the depletion of BRD4	[98]
		BRD2	Decrease STAT5-dependent transcription of both heterologous reporter genes and endogenous STAT5 target genes	[64]
I-BET151	Myeloma cell	BRD2/3/4	Induce apoptosis and exerts strong anti-proliferative effect associating with contrasting effects on oncogenic MYC and HEXIM1, and inhibit transcriptional activator PTEFb	[77]
	AML	BRD4	Suppress cell growth in a HOX gene independent manner, but relieving upon NPM1c mutation and cytosplasmic dislocation.	[79]
	Erythroleukemic (HEL) cell	BRD4	Suppress myeloproliferative neoplasms by constitutively active JAK2 kinase	[78]
I-BET762	Myeloma cell	BRD2/3/4	Inhibit myeloma cell proliferation, resulting in survival advantage in a systemic myeloma xenograft model.	[77]
	neuroblastoma tumor models	BRD2/3/4	Suppress cell growth in apoptosis signaling, and N-Myc-driven pathways, including the direct suppression of BCL2 and MYCN.	[76]
CPI203	Mantle cell lymphoma (MCL)	BRD2/3/4;	Decreased tumor burden, involving simultaneous MYC and IRF4 downregulation and apoptosis induction.	[81]
RVX2135	Myc-induced murine lymphoma	BRD2/3/4	Exhibit broad transcriptional effects in Myc-transgenic lymphoma cells affecting many transcription factor networks.	[82]
Dinaciclib	leukemia	BRDT,CDKs;	Interact with the acetyl-lysine recognition site of the bromodomain testis-specific protein BRDT	[94]
PFI-1	Leukemia	BRD2/4	Induce G1 cell-cycle arrest, downregulation of MYC expression, downregulation of Aurora B kinase	[84]
RVX-208	;	BRD3(BD2);	Raise apoA-I and increase preβ-HDL particles. Displace BET proteins from chromatin modestly affecting BET-dependent gene transcription.	[90]