Table 2 the inhibitors of SEs

JQ1

BRD4

PAAD, SCC, HCC, Lymphoma, OV,

CRC, Gliomas,

BRCA,

LUAD, NPC

MicroRNAs, NOTCH signaling,

NF-κB signaling, ALDH, KDM6A,

MYC, FoxM1, MAPK signaling,

SE-lncRNA DSCAM-AS1,LINC01004,

LINC01977, LOC100506178

58–66, 27

17,25

36,46

AZD5153

BET

HCC, Leukemia

NAD + synthesis, MYC, MYB, b-catenin

67–68

OTX015

(MK-8628, Birabresib)

BET

Solid tumors,

LUAD,

Hematologic Malignancies,

MYCN, c-MYC, MAP3K8,

SE-LINC00880

69–74

18

I-BET726

BRD4

Skin SCC,

NB, Melanoma

c-Myc, Bcl-2, and cyclin D1,SphK1

Akt signaling, SE-LINC00857

75–76

PLX2853

BET

OV, Lymphomas

ARID1A, MYC

77–79

NHWD-870

BET

Solid tumor

CSF1, c-MYC

80

BMS986158

BET

PDAC, Rhabdomyosarcoma

Mitochondrial metabolism

CRTFs

81–83

THZ1

CDK7

NPC, OSCC,

Leukemia,

SCC

PAK4, RUNX1, DNAJB1, SREBF2, YAP1, SE-lncRNA LIMD1-AS1,

SE-LINC00094

91–95,

45,

23

THZ2

CDK7

Osteosarcoma

TNBC

SE associated oncogenes

“Achilles cluster”

96

97

SY-1365

CDK7

Leukemia, TNBC

MCL1

98

LDC4297

CDK7

PDAC

Transcription rates

89

BS-181

CDK7

Synovial sarcoma

3D spheroid formation and migration

99

ICEC0942

CDK7

BRCA

Synthetic lethality with tamoxifen

100

SY-5609

CDK7

Solid tumor

ClinicalTrials: NCT04247126

101

LY3405105

CDK7

Solid tumor

Stop at phase I trial

102

AZD4573

CDK9

Lymphoma

MYC, Mcl-1, JunB, PIM3

103

Alvocidib

CDK9

Leukemia/

Lymphoma

IRF4

105