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
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% |
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) |
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) |
SETD8 inhibitor; also CDK4 inhibitor
Chemical Name: | 2-Methyl-5-[(4-methylphenyl)amino]-4,7-benzothiazoledione |
Purity: | ≥98% |
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% |
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% |
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 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) |
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) |
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% |
Potent and selective SUV420H1/H2 inhibitor
Chemical Name: | 6,7-Dichloro-N-cyclopentyl-4-(4-pyridinyl)-1-phthalazinamine |
Purity: | ≥98% |
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/GLP inhibitor
Chemical Name: | 5'-Methoxy-6'-[3-(1-pyrrolidinyl)propoxy]spiro[cyclobutane-1,3'-[3H]indol]-2'-amine |
Purity: | ≥98% |
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) |
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) |
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% |
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% |
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% |
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) |
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% |
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% |
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) |
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% |
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) |