Table 1 Summary of chemical probes and their chemotype-matched controls for protein methyltransferases. Related to Fig. 1a–c, Supplementary Figs. 1 and 2

WDR5^a

OICR-9429¹⁴

64

HEK293: disrupt interaction of WDR5^b with MLL1 & RbBP5

223 & 458

OICR-0547

EED^a

A-395³⁵

34

RD: ↓ H3K27me3

90

A-395N

EZH2

GSK343⁶³

4

HCC1806: ↓ H3K27me3

250

EZH2,H1

UNC1999¹¹

10,45

MCF10A: ↓ H3K27me3

124

UNC2400

DOT1L

SGC0946¹²

0.3

MCF10A,A431: ↓ H3K79me2

10,3

SGC0649

G9a & GLP

A-366²⁶

4 & 38

PC3: ↓ H3K9me2

300

Use UNC0642

G9a & GLP

UNC0642¹⁰

<3

PC3: ↓ H3K9me2

130

Use A-366

SUV420H1/2

A-196¹³

21

U2OS: ↓ H4K20me2/3

262/370 (SUV420H1)

A-197, SGC2043

SMYD2

BAY-598²⁹

27

HEK293, SMYD2^b:↓ p53K370me

58

BAY-369

SMYD3

BAY-6035^c

88

HeLa, SMYD3^b:

↓ MEKK2K260me3

70

BAY-444

SETD7

(R)-PFI-2²⁷

2

MEFs and MCF7:

↑ nuclear YAP

sub-μM

(S)-PFI-2

Type 1 PRMTs

MS023³⁷

30,8 (PRMT1,6)

MCF7 (PRMT1), HEK293 (PRMT6^b): ↓ H4R3me2a,

↓ H3R2me2a

9,56 (PRMT1,6)

MS094

PRMT3

SGC707³⁴

31

HEK293, PRMT3^b:

↓ H4R3me2a

91

XY1

PRMT4

TP-064⁶⁴

<10

HEK293: ↓ Med12me2a,

↓ Baf155me2a

43, 340

TP-064N

PRMT4

SKI-73^d,e

11

MCF-7: ↓ Med12me2a

540

SKI-73N

PRMT4,6

MS049⁶⁵

44,63

HEK293:

↓ Med12me2a (PRMT4),

↓ H3R2me2a (PRMT6^b)

1400, 970

MS049N

PRMT5

GSK591²⁸

11

Z138: ↓ SmD3me2s

56

SGC2096

PRMT5

LLY-283³¹

22

MCF7: ↓ SmBB'Rme2s

30

LLY-284

PRMT7

SGC3027^d,f

<2.5

C2C12, PRMT7^b:

↓ HSP70R469me

2400

SGC3027N