Table 2 Small-molecule inhibitors targeting SE

TF

KLF5

SR18662

Colorectal Cancer [221]

–-

–-

–-

ML264

Colorectal Cancer [221]

–-

–-

–-

Breast Cancer [222]

–-

–-

–-

TCF4

LF3

Colon Cancer [223]

–-

–-

–-

MYC

MYCi361

Prostate Cancer [224]

–-

–-

–-

MYCi975

Glioma [117]

–-

–-

–-

EN4

Breast Cancer [225]

–-

–-

–-

HMEs

HDAC3

RGFP966

Hepatocellular Carcinoma [226]

–-

–-

–-

HDAC1, HDAC2, HDAC3

Domatinostat (4SC-202)

Merkel Cell Carcinoma [227]

–-

–-

–-

Advanced Hematologic Malignancies

Completed

1

NCT01344707

Tucidinostat

Non Small Cell Lung Cancer

Recruiting

2

NCT05141357

Cervical Cancer

Recruiting

1/2

NCT04651127

PCI-24781

Lymphoma Follicular

Recruiting

2

NCT03934567

Metastatic Solid Tumors

Recruiting

1

NCT01543763

Sarcoma

Completed

1/2

NCT01027910

Largazole

Colorectal Cancer [228]

–-

–-

–-

HDAC1, HDAC3, HDAC7

MS-275 (Entinostat)

Melanoma

Recruiting

2

NCT03765229

Breast Cancer

Recruiting

1

NCT03473639

MGCD0103

Rhabdomyosarcoma

Recruiting

1

NCT04299113

Urothelial Carcinoma

Completed

2

NCT02236195

Vorinostat

Non-small Cell Lung Cancer

Terminated

1/2

NCT00503971

Lymphoma

Completed

3

NCT01728805

Multiple Myeloma

Completed

1/2

NCT01502085

Panobinostat

Mesothelioma

Completed

1

NCT00535951

Non Small Cell Lung Cancer

Completed

1

NCT00535951

JMJD2A

Z-JIB-04

Breast Cancer [229]

–-

–-

–-

KDM6A

GSK J1

Glioblastoma [230]

–-

–-

–-

Neck Squamous Cell Carcinoma [231]

–-

–-

–-

EP300

CPI-637

Prostate Cancer [232]

–-

–-

–-

Y08197

Prostate Cancer [232]

–-

–-

–-

Cofactors

BRD4

AZD5153

Malignant Solid Tumor

Completed

1

NCT03205176

Lymphadenoma

Completed

1

NCT03205176

ABBV-075

Prostate Cancer

Completed

1

NCT02391480

Breast Cancer

Completed

1

NCT02391480

Multiple Myeloma

Completed

1

NCT02391480

BMS-986158

Advanced Cancer

Completed

1/2

NCT02419417

Solid Tumor Childhood

Recruiting

1

NCT03936465

Lymphoma

Recruiting

1

NCT03936465

Brain Tumor

Recruiting

1

NCT03936465

CPI-0610

Myelofifibrosis

Recruiting

2

NCT02158858

PLX51107

Sarcoma

Terminated

2

NCT02683395

Breast Cancer

Terminated

2

NCT02683395

Uveal Melanoma

Terminated

2

NCT02683395

INCB054329

Ovarian Cancer

Terminated

1/2

NCT02431260

Lymphoma

Terminated

1/2

NCT02431260

FT-1101

Acute myeloid leukemia

Completed

1

NCT02543879

iBET151

Gastric cancer [233]

–-

–-

–-

JQ1

Prostate Cancer [234]

–-

–-

–-

Ovarian Cancer [235]

–-

–-

–-

Multiple Myeloma Cells [236]

–-

–-

–-

BRD2, BRD4

CC-90010

Glioblastoma

Recruiting

1

NCT04324840

Astrocytoma

Active not recruiting

1

NCT04047303

BRD2, BRD3, BRD4

GSK525762

NUT Carcinoma

–-

1

NCT01597703

OTX-015

Acute Leukemia

Completed

1

NCT01713582

Lymphoma

Completed

1

NCT01713582

NUT Midline Carcinoma

Completed

1

NCT02259114

Adenocarcinoma

Completed

1

NCT02259114

Triple Negative Breast Cancer

Completed

1

NCT02259114

BRDT, BRD2, BRD3, BRD4

ODM-207

CRPC

–-

1

NCT03035591

Melanoma

–-

1

NCT03035591

Non-Medullary Carcinoma

–-

1

NCT03035591

Cofactors

CDK7

SY-1365

Ovarian Cancer

Recruiting

1

NCT03134638

Breast Cancer

Recruiting

1

NCT03134638

CT7001

Advanced Solid Malignancies

Recruiting

2

NCT03363893

THZ1

Neuroblastoma [40]

–-

–-

–-

Glioma [237]

–-

–-

–-

CDK9

Dinaciclib

Hepatocellular carcinoma [238]

–-

–-

–-

Acute Myeloid Leukemia

Active not recruiting

1

NCT03484520

Malignant Solid Neoplasm

Recruiting

1

NCT01434316

Wogonin

Lung Epithelial Cancer [239]

–-

–-

–-

Hepatocellular Carcinoma [240]

–-

–-

–-

BAY 1143572

Leukemia

Completed

1

NCT02345382

Neoplasms

Completed

1

NCT01938638

CDK4, CDK6

Trilaciclib

Small cell lung cancer

Completed

1/2

NCT02499770

PD-0332991

Lung cancer

Recruiting

1

NCT03170206

Metastatic Pancreatic Ductal Adenocarcinoma

Completed

1

NCT02501902

Ribociclib (LEE011)

Non-small cell lung cancer

Completed

1

NCT02292550

Breast Cancer

Recruiting

4

NCT04657679

Ovarian Carcinoma

Recruiting

1

NCT04315233

SPH3643

Colon Cancer [241]

–-

–-

–-

Glioblastoma [241]

–-

–-

–-

CDK12, CDK13

THZ531

Prostate Cancer [242]

–-

–-

–-

CDK8, CDK19

BCD-115

Breast Cancer

Completed

1

NCT03065010