Table 2 Histone lysine methyltransferases (KMTs) and their selective inhibitors

H3K4

MLL1

KMT2A

TRX1

SET/PHD/FYRC/BD

MM102*

MM-401*

WDR5-0103*

[66,67,68]

MLL2

KMT2B

MLL4

SET/PHD/FYRC/BD

MLL3

KMT2C

HALR

SET/PHD/FYRC

MLL4

KMT2D

MLL2

SET/PHD/FYRC

MLL5

KMT2E

SET/PHD

SET1A

KMT2F

SETD1A

SET/RRM

SET1B

KMT2G

SETD1B

SET/RRM

ASH1L

KMT2H

ASH1

SET/PHD

SET7/SET9

KMT7

SETD7

SET

H3K9

G9A

KMT1C

EHMT2

SET/TAD/ANK

BIX01294

UNC0321

[83, 85]

GLP

KMT1D

EHMT1

SET/TAD/ANK

SUV39H1

KMT1A

H3-K9-HMTase 1

SET/CD

Chaetocin

[82]

SUV39H2

KMT1B

H3-K9-HMTase 2

SET/CD

SETDB1

KMT1E

H3-K9-HMTase 4

SET/Tudor/MBD

RIZ1

KMT8

PRDM2

PR/ZF

H3K27

EZH2

KMT6

SET/SANT

EPZ-6438 (Tazemetostat)

EPZ011989

GSK126

GSK503

GSK343

EPZ005687

CPI-1205

CPI-169

EI1

EED226**

[96,97,98,99, 101,102,103,104]

H3K36

SET2

KMT3A

SETD2

SET/SRI

N-propyl sinefungin

(Pr-SNF)

[124]

NSD1

KMT3B

STO

SET/PHD

BIX01294

[125]

SMYD2

KMT3C

ZMYND14

SET/MYND

ASH1L

KMT2H

ASH1

SET/PHD/BD

H3K79

DOT1L

KMT4

LRR

EPZ5676 (Pinometostat)

EPZ004777

SGC 0946

[129,130,131,132,133]

H4K20

PR-Set7

KMT5A

SETD8

SET

SUV420H1

KMT5B

CGI85

SET

A-196

[142]

SUV420H2

KMT5C

SET

NSD1

KMT3B

STO

SET/PHD