Lysine Methyltransferase Inhibitors Small Molecules and Peptides

(3S,3'S,5aR,5aR,10bR,10'bR,11aS,11'aS)-2,2',3,3',5a,5'a,6,6'-octahydro-3,3'-bis(hydroxymethyl)-2,2'-dimethyl-[10b,10'b(11H,11'H)-bi3,11a-epidithio-11aH-pyrazino[1',2':1,5]pyrrolo[2,3-b]indole]-1,1',4,4'-tetrone

Purity:

≥95%

UNC 1999

Catalog #: 4904

Citations (17)

Product Documents

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Potent and selective EZH2/EZH1 inhibitor

Chemical Name:

N-[(1,2-Dihydro-6-methyl-2-oxo-4-propyl-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[6-[4-(1-methylethyl)-1-piperazinyl]-3-pyridinyl]-1H-indazole-4-carboxamide

Purity:

≥98%

DZNep HCl

Catalog #: TB4703-RMU

Product Documents

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3-Deazaneplanocin A hydrochloride synthesized to Ancillary Material Grade

Chemical Name:

(1S,2R,5R)-5-(4-Amino-1H-imidazo[4,5-c]pyridin-1-yl)-3-(hydroxymethyl)-3-cyclopentene-1,2-diol hydrochloride

Purity:

≥98%

Ryuvidine

Catalog #: 2609

Citations (3)

Product Documents

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SETD8 inhibitor; also CDK4 inhibitor

Chemical Name:

2-Methyl-5-[(4-methylphenyl)amino]-4,7-benzothiazoledione

Purity:

≥98%

BIX 01294

Catalog #: 3364

Citations (17)

Product Documents

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GLP and G9a inhibitor

Chemical Name:

2-(Hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6,7-dimethoxy-N-[1-(phenylmethyl)-4-piperidinyl]-4-quinazolinamine trihydrochloride

Purity:

≥98%

(R)-PFI 2 hydrochloride

Catalog #: 4892

Citations (4)

Product Documents

Images (1)

Potent and selective SETD7 inhibitor

Chemical Name:

8-Fluoro-1,2,3,4-tetrahydro-N-[(1R)-2-oxo-2-(1-pyrrolidinyl)-1-[[3-(trifluoromethyl)phenyl]methyl]ethyl]-6-isoquinolinesulfonamide hydrochloride

Purity:

≥97%

A 366

Catalog #: 5163

Citations (7)

Product Documents

Images (1)

Potent and selective G9a/GLP inhibitor

Chemical Name:

5'-Methoxy-6'-[3-(1-pyrrolidinyl)propoxy]spiro[cyclobutane-1,3'-[3H]indol]-2'-amine

Purity:

≥98%

UNC 0224

Catalog #: 3861

Citations (2)

Product Documents

Images (1)

Potent G9a and GLP inhibitor

Chemical Name:

7-[3-(Dimethylamino)propoxy]-2-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6-methoxy-N-(1-methyl-4-piperidinyl)-4-quinazolinamine

Purity:

≥98%

UNC 0638

Catalog #: 4343

Citations (20)

Product Documents

Images (1)

Selective G9a and GLP inhibitor

Chemical Name:

2-Cyclohexyl-6-methoxy-N-[1-(1-methylethyl)-4-piperidinyl]-7-[3-(1-pyrrolidinyl)propoxy]-4-quinazolinamine

Purity:

≥98%

UNC 0638

Catalog #: 4343

Citations (20)

Product Documents

Images (1)

Selective G9a and GLP inhibitor

Chemical Name:

2-Cyclohexyl-6-methoxy-N-[1-(1-methylethyl)-4-piperidinyl]-7-[3-(1-pyrrolidinyl)propoxy]-4-quinazolinamine

Purity:

≥98%

(S)-PFI 2 hydrochloride

Catalog #: 5400

Citations (1)

Product Documents

Images (1)

Negative control of (R)-PFI 2 hydrochloride (Cat. No. 4892)

Chemical Name:

8-Fluoro-1,2,3,4-tetrahydro-N-[(1S)-2-oxo-2-(1-pyrrolidinyl)-1-[[3-(trifluoromethyl)phenyl]methyl]ethyl]-6-isoquinolinesulfonamide hydrochloride

Purity:

≥97%

EPZ 004777

Catalog #: 5567

Citations (8)

Product Documents

Images (1)

Highly potent DOT1L inhibitor

Chemical Name:

7-[5-Deoxy-5-[[3-[[[[4-(1,1-dimethylethyl)phenyl]amino]carbonyl]amino]propyl](1-methylethyl)amino]-β-D-ribofuranosyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine

Purity:

≥98%

SGC 0946

Catalog #: 4541

Citations (5)

Product Documents

Images (1)

Highly potent and selective DOT1L inhibitor; cell permeable

Chemical Name:

1-[3-[[[(2R,3S,4R,5R)-5-(4-Amino-5-bromo-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-3,4-dihydroxytetrahydrofuran-2-yl]methyl](isopropyl)amino]propyl]-3-[4-(2,2-dimethylethyl)phenyl]urea

Purity:

≥98%

GSK 343

Catalog #: 6128

Citations (7)

Product Documents

Images (1)

Potent and selective SAM-competitive EZH2 inhibitor

Chemical Name:

N-[(1,2-Dihydro-6-methyl-2-oxo-4-propyl-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[2-(4-methyl-1-piperazinyl)-4-pyridinyl]-1H-indazole-4-carboxamide

Purity:

≥98%

JQEZ5

Catalog #: 6153

Product Documents

Images (1)

Potent and selective SAM-competitive EZH2 inhibitor

Chemical Name:

N-[(1,2-Dihydro-6-methyl-2-oxo-4-propyl-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[6-(4-methyl-1-piperazinyl)-3-pyridinyl]-1H-pyrazolo[3,4-b]pyridine-4-carboxamide

Purity:

≥98%

A 196

Catalog #: 6167

Citations (2)

Product Documents

Images (1)

Potent and selective SUV420H1/H2 inhibitor

Chemical Name:

6,7-Dichloro-N-cyclopentyl-4-(4-pyridinyl)-1-phthalazinamine

Purity:

≥98%

PF 06726304 acetate

Catalog #: 6169

Citations (1)

Product Documents

Images (1)

Highly potent and SAM-competitive EZH2 inhibitor

Chemical Name:

5,8-Dichloro-2-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-7-(3,5-dimethyl-4-isoxazolyl)-3,4-dihydro-1(2H)-isoquinolinone acetate

Purity:

≥97%

BAY 6035

Catalog #: 6561

Product Documents

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Potent and selective SMYD3 inhibitor

Chemical Name:

(2S)-1-(3-Azabicyclo[3.1.0]hex-3-ylcarbonyl)-N-(2-cyclopropylethyl)-2,3,4,5-tetrahydro-2-methyl-4-oxo-1H-1,5-benzodiazepine-7-carboxamide

Purity:

≥98%

BI 9321

Catalog #: 6665

Product Documents

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Nuclear receptor-binding SET domain (NSD) 3 antagonist; selectively binds PWWP1 domain

Chemical Name:

(4-(5-(7-Fluoroquinolin-4-yl)-1-methyl-1H-imidazol-4-yl)-3,5-dimethylphenyl)methanamine trihydrochloride

Purity:

≥98%

UNC 6934

Catalog #: 7183

Citations (1)

Product Documents

Images (1)

Antagonizes PWWP1 interaction with nucleosomal H3K36me2, alters NSD2 nucleolar localization

Chemical Name:

N-Cyclopropyl-3,4-dihydro-3-oxo-N-[[4-[(4-pyrimidinylamino)carbonyl]phenyl]methyl]-2H-1,4-benzoxazine-7-carboxamide

Purity:

≥98%

AS 99

Catalog #: 7648

Product Documents

Images (1)

Selective ASH1L histone methyltransferase inhibitor

Chemical Name:

N-[[3-[3-(Aminothioxomethyl)phenyl]-1-[1-[(trifluoromethyl)sulfonyl]-4-piperidinyl]-1H-indol-6-yl]methyl]-1-methyl-3-azetidinecarboxamide

Purity:

≥98%

EED 226

Catalog #: 7762

Citations (2)

Product Documents

Images (1)

Potent and selective EED inhibitor

Chemical Name:

N-(2-Furanylmethyl)-8-[4-(methylsulfonyl)phenyl]-1,2,4-triazolo[4,3-c]pyrimidin-5-amine

Purity:

≥98%

MS 159

Catalog #: 8079

Product Documents

Images (1)

NSD2 Degrader (PROTAC®)

Chemical Name:

N-Cyclopropyl-N-(4-((5-(3-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)acetamido)propoxy)pyridin-2-yl)-carbamoyl)benzyl)-3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazine-7-carboxamide

Purity:

≥98%

Lysine Methyltransferase Inhibitors Small Molecules and Peptides

3-Deazaneplanocin A hydrochloride

GSK 126

Chaetocin

UNC 1999

DZNep HCl

Ryuvidine

BIX 01294

(R)-PFI 2 hydrochloride

A 366

UNC 0224

UNC 0638

UNC 0638

(S)-PFI 2 hydrochloride

EPZ 004777

SGC 0946

GSK 343

JQEZ5

A 196

PF 06726304 acetate

BAY 6035

BI 9321

UNC 6934

AS 99

EED 226

MS 159

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