Lysine Methyltransferase Inhibitors: Small Molecules and Peptides
Lysine methyltransferases are type of enzyme. They catalyze the transfer of methyl groups from S-adenosylmethionine (SAM) to the lysine residues on histones, particularly histones H3 and H4. The dysregulation of this methylation is critical in the development of cancer.
25 results for "Lysine Methyltransferase Inhibitors Small Molecules and Peptides" in Products
25 results for "Lysine Methyltransferase Inhibitors Small Molecules and Peptides" in Products
Lysine Methyltransferase Inhibitors: Small Molecules and Peptides
Lysine methyltransferases are type of enzyme. They catalyze the transfer of methyl groups from S-adenosylmethionine (SAM) to the lysine residues on histones, particularly histones H3 and H4. The dysregulation of this methylation is critical in the development of cancer.
EZH2 histone methyltransferase inhibitor
| Alternate Names: | DZNep,NSC 617989 |
| 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% (HPLC) |
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% (HPLC) |
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% (HPLC) |
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% (HPLC) |
SETD8 inhibitor; also CDK4 inhibitor
| Chemical Name: | 2-Methyl-5-[(4-methylphenyl)amino]-4,7-benzothiazoledione |
| Purity: | ≥98% (HPLC) |
Very high affinity and selective EZH2 inhibitor
| Chemical Name: | N-[(1,2-Dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-3-methyl-1-[(1S)-1-methylpropyl]-6-[6-(1-piperazinyl)-3-pyridinyl]-1H-indole-4-carboxamide |
| Purity: | ≥98% (HPLC) |
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% (HPLC) |
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% (HPLC) |
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: | ≥99% (HPLC) |
SUV39H1 inhibitor
| Chemical Name: | (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% (HPLC) |
Potent and selective SUV420H1/H2 inhibitor
| Chemical Name: | 6,7-Dichloro-N-cyclopentyl-4-(4-pyridinyl)-1-phthalazinamine |
| Purity: | ≥98% (HPLC) |
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% (HPLC) |
Potent and selective G9a and GLP inhibitor
| Chemical Name: | 2-(4,4-Difluoro-1-piperidinyl)-6-methoxy-N-[1-(1-methylethyl)-4-piperidinyl]-7-[3-(1-pyrrolidinyl)propoxy]-4-quinazolinamine |
| Purity: | ≥99% (HPLC) |
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% (HPLC) |
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: | ≥99% (HPLC) |
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% (HPLC) |
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% (HPLC) |
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% (HPLC) |
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% (HPLC) |
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% (HPLC) |
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% (HPLC) |
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% (HPLC) |
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% |
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% (HPLC) |
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% (HPLC) |
