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A cell-permeable compound that is shown (at 1uM concentrations) to inhibit EZH2-mediated trimethylation of K27 on histone H3 and induces the expression of cell-cycle regulatory genes, p21 and p27, as well as the cell death regulator, FBXO32, in OCI-AML3 and HL-60 cells, whereby treatment with inhibitor increases p16 levels in the former, but not the latter of the two cultures. At concentrations between 200nM and 2000nM, this compound is found to dose-dependently deplete the expression of polycomb group proteins EZH2, SUZ12, and EED in cultured and primary AML cell extracts. At concentrations up to ≥ 1000nM, DZNep dose-dependently increases the percentage of apoptotic cells up to > ~ 38%, with greater potency against OCI-AML3 than HL-60 cultures and inhibits colony growth up to > ~ 85% for both cell lines. In OCI-AML3 cultures, 1000nM of treatment demonstrates a significant increase in the accumulation of cells in the G0/G1 phase (58.5%) with a concomitant decrease in the number of c Group: Biochemicals. Grades: Highly Purified. CAS No. 102052-95-9. Pack Sizes: 2mg. Molecular Formula: C??H??N?O?; HCl; H?O. US Biological Life Sciences.
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histone-lysine N-methyltransferase
One of a group of enzymes methylating proteins; see also EC 2.1.1.59, [cytochrome-c]-lysine N-methyltransferase and EC 2.1.1.60, calmodulin-lysine N-methyltransferase. Group: Enzymes. Synonyms: protein methylase III; protein methylase 3; protein (lysine) methyltransferase; protein methyltransferase II; protein-lysine N-methyltransferase; histone H1-specific S-adenosylmethionine:protein-lysine N-methyltransferase; S-adenosyl-L-methionine:histone-L-lysine 6-N-methyltransferase. Enzyme Commission Number: EC 2.1.1.43. CAS No. 9055-8-7. Storage: Store it at +4 ?C for short term. For long term storage, store it at -20 ?C?-80 ?C. Form: Liquid or lyophilized powder. EXWM-1947; histone-lysine N-methyltransferase; EC 2.1.1.43; 9055-08-7; protein methylase III; protein methylase 3; protein (lysine) methyltransferase; protein methyltransferase II; protein-lysine N-methyltransferase; histone H1-specific S-adenosylmethionine:protein-lysine N-methyltransferase; S-adenosyl-L-methionine:histone-L-lysine 6-N-methyltransferase. Cat No: EXWM-1947.
HMTase Inhibitor IX, MM-102 (Histone Methyltransferase Inhibitor IX, MM102, (S) -N- (bis (4-Fluoro phenyl ) methy l )-1- (2- (2-ethyl -2-isobutyramidobutanamid o)-5-guanidinopentanamido) cyclopentane carboxami de , TFA)
A cell-permeable peptidomimetic that prevents MLL1 (Mixed Lineage Leukemia 1) from complex assembling with WDR5 (Trp-Asp Repeat Domain 5), RbBP5 (Retinoblastoma Binding Protein 5), and ASH2L (Absent Small or Homeotic-2-Like) for enhanced H3K4 methyltransferase activity (IC50 = 0.4nM). Shown to reduce HoxA9 and Meis-1 mRNA expression in myeloblasts derived from MLL1-AF9-transduced murine bone marrow cells (50uM for 96 h) and preferentially inhibit the growth of MLL1-AF4-harboring MV4;11 and MLL1-ENL-harboring KOPN8 leukemia cultures (GI50 in 7 days = 25uM) via apoptosis induction, while exhibiting much reduced potency against BCR-ABL-dependent K562 cells (GI50 in 7 days = 84uM). Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. Molecular Formula: C??H??F?N?O? · CF?CO?H. US Biological Life Sciences.
A quinazolinamine compound that acts as a potent, reversible and SAM (S-adenosylmethionine) non-competitive inhibitor of methyltransferases G9a (H3K9 HMT/EHMT2; IC50=15nM; =23nM) and GLP (G9a-like protein/EHMT1; IC50=20nM). Displays 1,000-fold greater selectivity for G9a over SET7/9 (H3K4 HMTase), SET8/PreSET7 (H4K20 HMTase), PRMT3 (MTase) and JMJD2E (demethylase), and minimally affects the activities of a broad range of GPCRs, ion-channels and transporters in a 30-target selectivity panel, with the exception of muscarinic M2 receptor and histamine H1 receptors (82% and 31% inhibition at 1uM, respectively). Group: Biochemicals. Grades: Highly Purified. CAS No. 1197196-48-7. Pack Sizes: 5mg. US Biological Life Sciences.
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Monoclonal Anti-SUV39H1 Histone Methyltransferase antibody produced in mouse
1-Chloro-3-iodopropane is used as reagent in the synthesis of several organic compounds including that of (-)-Terengganensine A which is a complex heptacyclic monoterpene indole alkaloid. Also used in the synthesis of A-366 which is a potent inhibitor of histone methyltransferase G9a. Group: Biochemicals. Grades: Highly Purified. CAS No. 6940-76-7. Pack Sizes: 1g, 5g. Molecular Formula: C3H6ClI. US Biological Life Sciences.
1-Methyl-4-[5-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)pyridin-2-yl]piperazine is used to prepare yrazolopyridine and indazoles as histone lysine methyltransferase EZH2 inhibitors. It is also used to synthesize tetrahydropyrido pyrazines as anaplastic lymphoma kinase inhibitors. Group: Biochemicals. Grades: Highly Purified. CAS No. 918524-63-7. Pack Sizes: 50mg, 100mg. Molecular Formula: C16H26BN3O2, Molecular Weight: 303.209999999999. US Biological Life Sciences.
2-(Benzoylamino)-1-(3-phenylpropyl)-1H-benzimidazole-5-carboxylic Acid is a small molecule that has been reported as a novel histone methyltransferase inhibitor. Group: Biochemicals. Grades: Highly Purified. CAS No. 1374601-41-8. Pack Sizes: 1mg, 5mg. Molecular Formula: C24H21N3O3, Molecular Weight: 399.44. US Biological Life Sciences.
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3-(Aminomethyl)-4,6-dimethylpyridin-2(1H)-one
3-(Aminomethyl)-4,6-dimethylpyridin-2(1H)-one is a reactant in the preparation of pyrazolopyridine and indazoles as histone lysine methyltransferase EZH2 inhibitors. Group: Biochemicals. Grades: Highly Purified. CAS No. 771579-27-2. Pack Sizes: 50mg, 250mg. Molecular Formula: C8H12N2O, Molecular Weight: 152.19. US Biological Life Sciences.
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3-Bromo-4- (methoxymethoxy) benzaldehyde
3-Bromo-4- (methoxymethoxy) benzaldehyde is an intermediate in synthesizing CARM1-IN-1 Hydrochloride (C183610), a mixed Histone/Protein Methyltransferase, Acetyltransferase, and Class III Deacetylase (Sirtuin) inhibitor. Group: Biochemicals. Grades: Highly Purified. CAS No. 162269-90-1. Pack Sizes: 50mg, 100mg. Molecular Formula: C9H9BrO3. US Biological Life Sciences.
Worldwide
3-Deazaneplanocin A
3-Deazaneplanocin A (DZNep) is a potent histone methyltransferase EZH2 inhibitor [1] [2]. 3-Deazaneplanocin A is a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor. 3-Deazaneplanocin A shows anti-orthopoxvirus activity [6] [7]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: DZNep; 3-Deazaneplanocin. CAS No. 102052-95-9. Pack Sizes: 1 mg; 5 mg. Product ID: HY-10442.
3-Deazaneplanocin A (DZNep, NSC 617989)
A lysine methyltransferase EZH2 (KMT63) inhibitor. DZNep is a selective inhibitor of trimethylation of lysine 27 on histone H3 (H3K27me3) and lysine 20 on histone H4 (H4K20me3). DZNep treatment of cultured human AML cells induces increased expression of the cell-cycle regulators p21, p27, and FBXO32, leading to cell cycle arrest and apoptosis. Group: Biochemicals. Alternative Names: 5R-(4-amino-1H-imidazo[4, 5-c]pyridin-1-yl)-3-(hydroxymethyl)-3-cyclopentene-1S, 2R-diol). Grades: Highly Purified. CAS No. 102052-95-9. Pack Sizes: 250ug, 1mg. US Biological Life Sciences.
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3-Deazaneplanocin A hydrochloride
3-Deazaneplanocin A hydrochloride (DZNep hydrochloride) is a potent histone methyltransferase EZH2 inhibitor [1] [2]. 3-Deazaneplanocin A hydrochlorideis a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor [6]. 3-Deazaneplanocin A hydrochloride also has anti- orthopoxvirus and anti-variola activities [7]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: DZNep hydrochloride; NSC 617989 hydrochloride; 3-Deazaneplanocin hydrochloride. CAS No. 120964-45-6. Pack Sizes: 1 mg; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-12186.
A 196
A 196 is a potent and selective inhibitor of SUV420H1/H2 (IC50 = 25 and 144 nM, respectively) with 100-fold selectivity over other histone methyltransferases and non-epigenetic targets. It was shown to inhibit the di- and tri-methylation of H4K20me in multiple cell lines (IC50 < 1 μM). Synonyms: SGC A-196; SGC A 196; SGC A196; SGC-A-196; SGCA196; A-196; A 196; A196; 6,7-Dichloro-N-cyclopentyl-4-(4-pyridinyl)-1-phthalazinamine. Grades: ≥98% by HPLC. CAS No. 1982372-88-2. Molecular formula: C18H16Cl2N4. Mole weight: 359.25.
A-366
A-366 is a peptide-competitive inhibitor of the G9a/GLP histone lysine methyltransferase (IC50 = 3.3 nM) and is approximately 1000-fold selective over other methyltransferases. Synonyms: A 366; A366. CAS No. 1527503-11-2. Molecular formula: C19H27N3O2. Mole weight: 329.44.
AS-85
AS-85 is a potent ASH1L histone methyltransferase inhibitor ( IC 50 =0.6 μM) with anti-leukemic activity. AS-85 strongly binds to the ASH1L SET domain, with the K d value of 0.78?μM [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 2323623-80-7. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-141430.
BAY-598
BAY-598 is a potent, peptide-competitive chemical probe for SET and MYND domain-containing protein 2 (SMYD2), IC50 values of 27 nM and 58 nM for biochemical and cellular activity, respectively. BAY 598 exhibits 100-fold selectivity for SMYD2 over other histone methyltransferases and non-epigenetic enzymes. Synonyms: (S, E) -N- (1- (N'-cyano-N- (3- (difluoromethoxy) phenyl) carbamimidoyl) -3- (3, 4-dichlorophenyl) -4, 5-dihydro-1H-pyrazol-4-yl) -N-ethyl-2-hydroxyacetamide; BAY-598; BAY 598; BAY598. CAS No. 1906919-67-2. Molecular formula: C22H20Cl2F2N6O3. Mole weight: 525.33.
BAY-598 R-isomer
BAY-598 R-isomer is the R-isomer of BAY589 which is a potent, peptide-competitive chemical probe for SET and MYND domain-containing protein 2 (SMYD2), IC50 values of 27 nM and 58 nM for biochemical and cellular activity, respectively. BAY 598 exhibits 100-fold selectivity for SMYD2 over other histone methyltransferases and non-epigenetic enzymes. Synonyms: (R, E) -N- (1- (N'-cyano-N- (3- (difluoromethoxy) phenyl) carbamimidoyl) -3- (3, 4-dichlorophenyl) -4, 5-dihydro-1H-pyrazol-4-yl) -N-ethyl-2-hydroxyacetamide; BAY-598 R-isomer; BAY 598 R-isomer; BAY598 R-isomer. CAS No. 1906920-28-2. Molecular formula: C22H20Cl2F2N6O3. Mole weight: 525.33.
BAY-6035
BAY-6035 is an inhibitor of SET and MYND domain-containing protein 3 (SMYD3) with IC50 of 70 nMm, which exhibits >100-fold selectivity for SMYD3 over other histone methyltransferases. BAY-6035 inhibits methylation of MEKK2 peptide in a cell-free assay and in cell. Synonyms: (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. Grades: ≥95%. CAS No. 2247890-13-5. Molecular formula: C22H28N4O3. Mole weight: 396.48.
BIX 01294
Selective and cell permeable G9a histone lysine methyltransferase (HMTase) inhibitor. Pluripotent stem cell inducer. Group: Biochemicals. Alternative Names: 2-(Hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6,7-dimethoxy-N-4-quinazolinamine. Grades: Highly Purified. CAS No. 935693-62-2. Pack Sizes: 1mg, 5mg, 25mg. Molecular Formula: C28H38N6O2. US Biological Life Sciences.
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BIX01294 hydrochloride hydrate
Histone methyltransferases (HMT) are histone-modifying enzymes (e.g., histone-lysine N-methyltransferases and histone-arginine N-methyltransferases) that catalyze the transfer of one, two, or three methyl groups to lysine and arginine residues of histone proteins. BIX 01294 is a diazepin-quinazolinamine derivate and G9a histone methyltransferase inhibitor with IC50 of 1.9 μM and GLP inhibitor with IC50 of 0.7 μM. It less effectively inhibits the HMTase G9a-like protein and has no effect on other known HMTases. BIX 01294 was reported to function by blocking the histone binding sites. It modulates the epigenetic status of chromatin and has been used to improve the reprogramming efficiency of iPSC generation. Synonyms: BIX 01294; BIX-01294. Grades: ≥98%. CAS No. 1808255-64-2. Molecular formula: C28H38N6O2·3HCl·xH2O. Mole weight: 600.
BIX 01294 trihydrochloride
BIX 01294 is a G9a histone methyltransferase inhibitor. It enhances the induction of pluripotent stem cells from somatic cells in vitro. BIX-01294 trihydrochloride induces necroptosis and autophagy. Synonyms: BIX 01294 trihydrochloride; BIX-01294; N-(1-benzylpiperidin-4-yl)-6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)quinazolin-4-amine trihydrochloride. Grades: >98%. CAS No. 1392399-03-9. Molecular formula: C28H41Cl3N6O2. Mole weight: 600.02.
BIX 01294 Trihydrochloride
G9a-like protein and G9a histone lysine methyltransferase (HMTase) inhibitor that H3K9me2 chromatin levels modulates H3K9me2 levels in mammalian cells and potentiates induction of pluripotent stem cells from somatic cells in vitro. Group: Biochemicals. Alternative Names: 2-(Hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6,7-dimethoxy-N-[1-(phenylmethyl)-4-piperidinyl]-4-quinazolinamine Trihydrochloride. Grades: Highly Purified. Pack Sizes: 25mg. US Biological Life Sciences.
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BIX-01338 hydrate
BIX-01338 hydrate is a histone lysine methyltransferase inhibitor. Uses: Scientific research. Group: Signaling pathways. CAS No. 1228184-65-3. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-12991A.
BRD4770
BRD4770 is a novel histone methyltransferase inhibitor. BRD4770 reduced cellular levels of di- and trimethylated H3K9 without inducing apoptosis, induced senescence, and inhibited both anchorage-dependent and -independent proliferation in the pancreatic cancer cell line PANC-1. ATM-pathway activation, caused by either genetic or small-molecule inhibition of G9a, may mediate BRD4770-induced cell senescence. BRD4770 may be a useful tool to study G9a and its role in senescence and cancer cell biology. Synonyms: BRD4770; BRD-4770; BRD 4770. Grades: 0.98. CAS No. 1374601-40-7. Molecular formula: C25H23N3O3. Mole weight: 413.477.
BRD9539
BRD9539 is an inhibitor of euchromatin histone methyltransferase 2 (EHMT2) with an IC50 value of 6.3 μM. It is selective for G9a and PRC2 over SU39H1 and NDMT1 up to a concentration of 40 μM. BRD9539 is a more potent biochemical inhibitor than its methyl-ester analogue BRD4770, with 20% remaining G9a activity compared to 45% of BRD4770 at screening concentration. Synonyms: BRD-9539; BRD 9539. Grades: ≥98%. CAS No. 1374601-41-8. Molecular formula: C24H21N3O3. Mole weight: 399.4.
calmodulin-lysine N-methyltransferase
One of a group of enzymes methylating proteins; see also EC 2.1.1.43 histone-lysine N-methyltransferase and EC 2.1.1.59 [cytochrome-c]-lysine N-methyltransferase. Group: Enzymes. Synonyms: S-adenosylmethionine:calmodulin (lysine) N-methyltransferase; S-adenosyl-L-methionine:calmodulin-L-lysine 6-N-methyltransferase. Enzyme Commission Number: EC 2.1.1.60. CAS No. 75603-20-2. Storage: Store it at +4 ?C for short term. For long term storage, store it at -20 ?C?-80 ?C. Form: Liquid or lyophilized powder. EXWM-1962; calmodulin-lysine N-methyltransferase; EC 2.1.1.60; 75603-20-2; S-adenosylmethionine:calmodulin (lysine) N-methyltransferase; S-adenosyl-L-methionine:calmodulin-L-lysine 6-N-methyltransferase. Cat No: EXWM-1962.
Chaetocin
Chaetocin is a specific inhibitor of the histone methyltransferase ( HMT ) SU(VAR)3-9 with an IC 50 of 0.6 μM for SU(VAR)3-9. It also inhibits thioredoxin reductase ( TrxR ) with an IC 50 of 4 μM. Uses: Scientific research. Group: Natural products. CAS No. 28097-03-2. Pack Sizes: 10 mM * 1 mL; 1 mg; 5 mg; 10 mg. Product ID: HY-N2019.
CID-2818500
CID-2818500 is an inhibitor of protein arginine methyltransferase 1 (PRMT1). It also inhibits histone H4 methylation by PRMT8, but not histone H3.1 methylation by CARM1 or Set7/9, when used at concentrations of 10 and 100 μM. Synonyms: α-Nitrostilbene; NSC 385; 1,1'-(1-nitro-1,2-ethenediyl)bis-benzene. Grades: ≥98%. CAS No. 1215-07-2. Molecular formula: C14H11NO2. Mole weight: 225.2.
CMP-5
CMP-5 is a potent, specific, and selective PRMT5 inhibitor, while displays no activity against PRMT1, PRMT4, and PRMT7 enzymes. CMP-5 selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. CMP-5 prevents Epstein-Barr virus (EBV)-driven B-lymphocyte transformation but leaving normal B cells unaffected [1] [2]. Uses: Scientific research. Group: Signaling pathways. CAS No. 880813-42-3. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-120137.
[cytochrome c]-lysine N-methyltransferase
One of a group of enzymes methylating proteins; see also EC 2.1.1.43 histone-lysine N-methyltransferase and EC 2.1.1.60 calmodulin-lysine N-methyltransferase. Group: Enzymes. Synonyms: cytochrome c (lysine) methyltransferase; cytochrome c methyltransferase; cytochrome c-specific protein methylase III; cytochrome c-specific protein-lysine methyltransferase; S-adenosyl-L-methionine:[cytochrome c]-L-lysine 6-N-methyltransferase. Enzyme Commission Number: EC 2.1.1.59. CAS No. 82047-78-7. Storage: Store it at +4 ?C for short term. For long term storage, store it at -20 ?C?-80 ?C. Form: Liquid or lyophilized powder. EXWM-1960; [cytochrome c]-lysine N-methyltransferase; EC 2.1.1.59; 82047-78-7; cytochrome c (lysine) methyltransferase; cytochrome c methyltransferase; cytochrome c-specific protein methylase III; cytochrome c-specific protein-lysine methyltransferase; S-adenosyl-L-methionine:[cytochrome c]-L-lysine 6-N-methyltransferase. Cat No: EXWM-1960.
DC-S239
DC-S239 is a potent and selective histone methyltransferase SET7 inhibitor. Uses: Designed for use in research and industrial production. Additional or Alternative Names: DC-S239; DC S239; DCS239. Product Category: Inhibitors. Appearance: Solid powder. CAS No. 303141-21-1. Molecular formula: C15H15N3O5S. Mole weight: 349.36. Purity: >98%. IUPACName: Ethyl 2-Amino-4-methyl-5-((3-nitrophenyl)carbamoyl)-thiophene-3-carboxylate. Canonical SMILES: O=C(C1=C(N)SC(C(NC2=CC=CC([N+]([O-])=O)=C2)=O)=C1C)OCC. Product ID: ACM303141211. Alfa Chemistry ISO 9001:2015 Certified.
EPZ005687
EPZ005687 is a selective EZH2 enzyme inhibitor with Ki of 24 nM. It is 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases. EPZ005687 can block trimethylation of the PRC2 target histone 3 lysine 27 with IC50 value of 80 nM, decreasing the proliferation of lymphoma cells carrying mutant, but not wild-type, EZH2. No development of preclinical research for the treatment of Cancer, Lymphoma and Solid tumours was reported. Uses: Cancer; lymphoma; solid tumours. Synonyms: EPZ005687; EPZ 005687; EPZ-005687; 1-Cyclopentyl-N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-6-[4-(4-morpholinylmethyl)phenyl]-1H-indazole-4-carboxamide; 1-Cyclopentyl-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-6-(4-(morpholinomethyl)phenyl)-1H-indazole-4-carboxamide. Grades: 98%. CAS No. 1396772-26-1. Molecular formula: C32H37N5O3. Mole weight: 539.67.
EPZ020411
EPZ020411, with potent anticancer activity, is an orally bioactive, selective inhibitor of PRMT6/8/1 with over 100-fold selective for other histone methyltransferases including four arginine methyltransferases (PRMT3, PRMT4, PRMT5, and PRMT7). Synonyms: N,N'-dimethyl-N'-[[5-[4-[3-[2-(oxan-4-yl)ethoxy]cyclobutyl]oxyphenyl]-1H-pyrazol-4-yl]methyl]ethane-1,2-diamineEPZ020411; EPZ 020411; EPZ-020411CHEMBL3589039GTPL9243SCHEMBL17 62195749LN, N'-Di methyl -N- ( {3- [4- ( {trans-3- [2- (Tetra hydro-2h-Pyran-4-yl ) ethoxy] cyclobutyl } oxy) pheny l. CAS No. 1700663-41-7. Molecular formula: C25H38N4O3. Mole weight: 442.59.
EPZ-5676
EPZ-5676 is a small molecule inhibitor of histone methyltransferase with potential antineoplastic activity. Upon intravenous administration, EPZ-5676 specifically blocks the activity of the histone lysine-methyltransferase DOT1L, thereby inhibiting the methylation of nucleosomal histone H3 on lysine 79 (H3K79) that is bound to the mixed lineage leukemia (MLL) fusion protein which targets genes and blocks the expression of leukemogenic genes. This eventually leads to an induction of apoptosis in the leukemic cells bearing the MLL gene translocations. DOT1L, a non-SET domain-containing histone methyltransferase, specifically methylates H3K79 and plays a key role in normal cell differentiation and in the development of leukemia with MLL gene rearrangement on chromosome 11 and promotes the expression of leukemia-causing genes. Synonyms: EPZ-5676; EPZ5676; EPZ 5676. CAS No. 1380288-87-8. Molecular formula: C30H42N8O3. Mole weight: 562.719.
EZH2-IN-14
EZH2-IN-14 is a selective EZH2 ( Histone Methyltransferase ) inhibitor with an IC 50 of 12 nM. EZH2-IN-14 inhibits the methyltransferase activity of EZH2/PRC2 (that is, reducing H3K27me3). EZH2-IN-14 shows >200-fold selective for EZH2 over the highly homologous H3K27 methyltransferase EZH1 [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 1979157-17-9. Pack Sizes: 5 mg; 10 mg; 25 mg; 50 mg. Product ID: HY-148458.
Gliotoxin
Gliotoxin is a sulfur-containing mycotoxin produced by species of fungi and pathogens of humans. Gliotoxin exhibits inhibitory activities against histone H3K9 methyltransferase, a key enzyme in the regulation of transcriptional activity by writing epigenetic marks. Gliotoxin also exhibits immunosuppressive properties by causing apoptosis of cells of the immune system. In addition, various studies suggests Gliotoxin may also be a potential anti-inflammatory, antibiotic, antifungal and antiviral agent. Group: Biochemicals. Alternative Names: (3R,5aS,6S,10aR)-2,3,5a,6-Tetrahydro-6-hydroxy-3-(hydroxymethyl)-2-methyl-10H-3,10a-epidithiopyrazino[1,2-a]indole-1,4-dione. Grades: Highly Purified. CAS No. 67-99-2. Pack Sizes: 1mg. US Biological Life Sciences.
Worldwide
GSK591
GSK591, also known as EPZ015866 and GSK3203591, is a chemical probe for PRMT5. In an in vitro biochemical assay, GSK591 potently inhibits the PRMT5/MEP50 complex from methylating (histone) H4 with IC50=11 nM. In Z-138 cells, GSK591 inhibits the symmetric arginine methylation of SmD3 with EC50=56 nM. Further, GSK591 is selective for PRMT5 (up to 50 micromolar) relative to a panel of methyltransferases. (http://www.thesgc.org/chemical-probes/GSK59). Uses: Designed for use in research and industrial production. Additional or Alternative Names: GSK591; GSK-591; GSK 591; EPZ015866; EPZ-015866; EPZ 015866; GSK 3203591; GSK-3203591; GSK3203591. Product Category: Others. Appearance: Solid powder. CAS No. 1616391-87-7. Molecular formula: C22H28N4O2. Mole weight: 380.49. Purity: >98%. IUPACName: (S)-2-(cyclobutylamino)-N-(3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)isonicotinamide. Canonical SMILES: O=C(NC[C@H](O)CN1CCC(C=CC=C2)=C2C1)C3=CC(NC4CCC4)=NC=C3. Product ID: ACM1616391877. Alfa Chemistry ISO 9001:2015 Certified. Categories: GSK-598809.
Histone H3 (1-34)
Histone H3 (1-34) is a histone peptide that acts as a substrate for methyltransferase/demethylase enzymes. Synonyms: Ala-Arg-Thr-Lys-Gln-Thr-Ala-Arg-Lys-Ser-Thr-Gly-Gly-Lys-Ala-Pro-Arg-Lys-Gln-Leu-Ala-Thr-Lys-Ala-Ala-Arg-Lys-Ser-Ala-Pro-Ala-Thr-Gly-Gly. Molecular formula: C144H260N54O44. Mole weight: 3451.98.
Histone H3 (21-44)
Histone H3 (21-44) is a histone fragment that is used as a substrate for the protein arginine methyltransferase PRMT4. Synonyms: H3 (21-44); H-Ala-Thr-Lys-Ala-Ala-Arg-Lys-Ser-Ala-Pro-Ala-Thr-Gly-Gly-Val-Lys-Lys-Pro-His-Arg-Tyr-Arg-Pro-Gly-OH; L-Alanyl-L-threonyl-L-lysyl-L-alanyl-L-alanyl-L-arginyl-L-lysyl-L-seryl-L-alanyl-L-prolyl-L-alanyl-L-threonylglycylglycyl-L-valyl-L-lysyl-L-lysyl-L-prolyl-L-histidyl-L-arginyl-L-tyrosyl-L-arginyl-L-prolylglycine. Grades: ≥95%. CAS No. 1373516-71-2. Molecular formula: C109H185N39O29. Mole weight: 2505.91.
HMTase Inhibitor IV, UNC0638 (2-Cyclohexyl-N-(1-isopropylpiperidin-4-yl)-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazolin-4-amine)
A cell-permeable quinazolinamine compound that acts as a potent and reversible inhibitor of G9a and GLP HMTases (histone methyltransferases) (IC50=<15 and 19nM for G9a and GLP, respectively) and displays ~15-fold greater selectivity over DNMT1 and minimally blocks the activities of JMJD2E (IC50=4.66uM) and SETD7, SETD8, PRMT3 and SUV39H2 (IC50>10uM). Shown to lower H3K9Me2 levels in MDA-MB231 cells (IC50=81nM; EC50=11.2uM for cell toxicity) and 6-fold more potent than the HMTase Inhibitor, BIX-01294. Also, affects the activities of adrenergic a1A, adrenergic a and muscarinicM2 by 90%, 69% and 64% and a panel of 26-receptors and ion-channels by <30% at 1uM. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 2mg. US Biological Life Sciences.
A cell-permeable analog of the amino-benzimidazolo BIX-01338 and the methylester prodrug of BRD9539 that acts as an SAM-competitive inhibitor against PRC2 and G9a (IC50<6.3uM) histone methyltransferase activities, displaying little effect toward 10 other HMTases, 9 HDACs, and 100 cellular kinases. Selectively reduces H3K9me2 and H3K9me3 (EC50=5uM) histone methylation levels in pancreatic cancer cells (PANC-1) with much less or little effect toward H3K36me3, H3K4me3, H3K27me3, or H3K6me3 levels. Inhibits both anchorage-dependent and -independent PANC-1 proliferation via ATM activation and G2/M cell-cycle arrest, but not apoptosis induction (no caspase3/7 activation; 10uM, 72h). Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences.
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MAK683
MAK683 is an inhibitor of embryonic ectoderm development protein (EED) with potential antineoplastic activity. MAK683 binds to the domain of EED that interacts with trimethylated lysine 27 on histone 3 (H3K27me3), leading to a conformational change in the EED H3K27me3-binding pocket and preventing the interaction of EED with the histone methyltransferase enhancer zeste homolog 2 (EZH2). MAK683 is undergoing phase II clinical trials for the identification of antitumor activity. Synonyms: MAK-683; MAK 683; MAK683; EED inhibitor-1; N-[(5-fluoro-2,3-dihydro-1-benzofuran-4-yl)methyl]-8-(2-methylpyridin-3-yl)-[1,2,4]triazolo[4,3-c]pyrimidin-5-amine. Grades: 98%. CAS No. 1951408-58-4. Molecular formula: C20H17FN6O. Mole weight: 376.395.
Methylation Compound Library
125 methylation-related compounds that can be used for high-throughput and high-content screening. - Targets include DNA Methyltransferase, Histone Methyltransferase, etc. - Can be used for studies on epigenetics, differentiation, aging, cancer, etc. - Detailed instructions, compound structure, target information, activity description, etc. - NMR and HPLC analytical techniques to ensure high product purity and quality. - All compounds are available in stock. Uses: Scientific use. Product Category: L3510. Categories: Methylation Compounds Libraries.
Nicotinamide N-Methyltransferase from Human, Recombinant
Nicotinamide N-Methyltransferase (NNMT) methylates nicotinamide and other pyridine containing compounds. NNMT transfers a methyl group from S-adenosylmethionine (SAM) to nitrogen N1 of nicotinamide to produce 1-methylnicotinamide (MNA) and S-adenosylhomocysteine. MNA is a messenger molecule that increases neurite branching, serves as an anti-thrombotic, and has anti-inflammatory properties. The role of NNMT overexpression in cancers may be to alter epigenetic methylation patterns in two ways: by lowering the intracellular concentration of SAM, required by methyltransferase enzymes, and by depleting the available NAD+ by transforming nicotinamide to MNA. Sirtuins use NAD+ as a substrate to alter protein acetylation and ribosylation, including histone targets. Group: Enzymes. Synonyms: NNMT. Enzyme Commission Number: E.C. 2.1.1.1. Purity: > 95% by SDS-PAGE. Mole weight: 42.6 kDa. Stability: As supplied, 6 months from the QC date provided on the Certificate of Analysis, when stored properly. Storage: Store at -80°C. Form: Liquid. Source: recombinant N-terminal His- and SUMO-tagged protein expressed in E. coli. Species: Human. NNMT; Nicotinamide N-Methyltransferase. Cat No: NATE-1656.
A cell-permeable phenyl sulfonyl oxyimi nocyclohexadienone compound that acts as a potent, selective, and reversible inhibitor of p300 histone acetyl transferase (IC50 = 1.98uM). Shown to occupy Ac-CoA binding pocket of p300, and less potent to CBP, PCAF, GCN5 and GNAT. Suppresses Histone H3 and H4 acetylation in triple negative breast cancer cell line MDAMB-468 as well as in HCT116 cell line and blocks p300-mediated STAT3 phosphorylation in pancreatic cancer cell line MIA Paca-2. Does neither inhibit the activities of histone deacetylases 1, 6, and 11 nor 8-diverse histone methyltransferases tested (DOT1, EZH1, G9a, PRMT1, SETD2, SET7-9, SMYD2, and SUV39H2). Reported to suppress tumor growth in mice bearing tumor xenografts of MDAMB-468 cell line (at 500ug/100ul, i.p. twice a week). Group: Biochemicals. Grades: Highly Purified. CAS No. 321695-57-2. Pack Sizes: 10mg. Molecular Formula: C??H??NO?S. US Biological Life Sciences.
Worldwide
Pinometostat
Pinometostat (EPZ-5676) is a potent DOT1L histone methyltransferase inhibitor with a K i of 80 pM. Uses: Scientific research. Group: Signaling pathways. Alternative Names: EPZ-5676. CAS No. 1380288-87-8. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-15593.
Procyanidin B3
Procyanidin B3 is a natural product, acts as a specific HAT inhibitor, binds to the other site of p300 instead of the active site, selectively inhibits p300-mediated androgen receptor acetylation. Procyanidin B3 has no effect on HDAC or HMT (histone methyltransferase). Uses: Designed for use in research and industrial production. Additional or Alternative Names: PROCYANIDIN B3;CATECHIN-(4ALPHA->8)-CATECHIN;CATECHIN-(4ALPHA->8)-CATECHIN B3;procyanidin B3 from barley;(2R,2R,3S,3S,4S)-2,2-Bis(3,4-dihydroxyphenyl)-4,8-bichroman-3,3,5,5,7,7-hexol;(2R,2R,3S,3S,4α)-3,3,4,4-Tetrahydro-2α,2α-bis(3,4-dihydroxyphenyl)-4,8-bi[2H-1-benzopyran]-3,3,5,5,7,7-hexol;3,3,4,4-Tetrahydro-2α,2α-bis(3,4-dihydroxyphenyl)-4α,8-bi[2H-1-benzopyran]-3β,3β,5,5,7,7-hexol;(2R,2R,3S,3S,4S)-2,2-Bis(3,4-dihydroxyphenyl)-3,3,4,4-tetrahydro-[4,8-bi-2H-1-benzopyran]-3,3,5,5,7,7-hexol. Product Category: Inhibitors. Appearance: Solid. CAS No. 23567-23-9. Molecular formula: C30H26O12. Mole weight: 578.52. Purity: 0.9963. Canonical SMILES: O[C@@H]1[C@@H](C2=CC=C(O)C(O)=C2)OC3=CC(O)=CC(O)=C3[C@H]1C4=C5C(C[C@H](O)[C@@H](C6=CC=C(O)C(O)=C6)O5)=C(O)C=C4O. Density: 1.705. Product ID: ACM23567239. Alfa Chemistry ISO 9001:2015 Certified.
Psammaplin A
Antibiotic. Caffeine-like Ca2+ releaser in heavy sarcoplasmic reticulum (HSR). Antifungal. Chitinase inhibitor. DNA methyltransferase inhibitor. Histone deacetylase (HDAC) inhibitor. Anticancer compound. Angiogenesis suppressor. Group: Biochemicals. Alternative Names: (α E, α 'E) -N, N'- (Dithiodi-2, 1-ethanediyl) bis[3-bromo-4-hydroxy-α - (hydroxyimino) benzenepropanamide]; (E,E)-Psammaplin A; Bisprasin; Psammaplin A; UVI 5000; (E,E)-N,N'-(Dithiodi-2,1-ethanediyl)bis[3-bromo-4-hydroxy-α-(hydroxyimino)-benzenepropanamide]. Grades: Highly Purified. CAS No. 110659-91-1. Pack Sizes: 100ug, 500ug. Molecular Formula: C??H??Br?N?O?S?. US Biological Life Sciences.
Potent DOT1L methyltransferase inhibitor (KD = 0.06nm, IC50 = 0.3nm in a radioactive assay); blocks H3K79 methylation in A431 cells and MCF10A cells (IC50 values are 2.65 and 8.8nm respectively). Inactive at 12 histone methyltransferases and DNMT1. Selectively kills cells transformed with the MLL-AF9 fusion oncogene in an in vitro model of leukemia; lowers levels of MLL target genes HOXA9 and Meis1. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences.
Worldwide
Tanshindiol C
Tanshindiol C is a S-adenosylmethionine-competitive EZH2 (Histone Methyltransferase) inhibitor with an IC50 of 0.55 μM for inhibiting the methyltransferase activity. Tanshindiol C is also an activator of both Nrf2 and Sirtuin 1 (Sirt1) in macrophages. Tanshindiol C possesses anti-cancer activity, and can be used for atherosclerosis research. Uses: Designed for use in research and industrial production. Product Category: Inhibitors. Appearance: Red powder. CAS No. 97465-71-9. Molecular formula: C18H16O5. Mole weight: 312.3. Purity: 0.98. IUPACName: (6R,7R)-6,7-dihydroxy-1,6-dimethyl-8,9-dihydro-7H-naphtho[1,2-g][1]benzofuran-10,11-dione. Canonical SMILES: CC1=COC2=C1C(=O)C(=O)C3=C2C=CC4=C3CCC(C4(C)O)O. Product ID: ACM97465719. Alfa Chemistry ISO 9001:2015 Certified.
TP 064
TP 064 is a potent and selective PRMT4 inhibitor with >100-fold selectivity over other histone methyltransferases and non-epigenetic targets. TP 064 inhibits methylation of H3 (1-25) and MED12 in cellular assays (IC50 values are <10 and 43 nM, respectively). Synonyms: TP-064; TP064; N-Methyl-N-((2-(1-(2-(methylamino)ethyl)piperidin-4-yl)pyridin-4-yl)methyl)-3-phenoxybenzamide. Grades: ≥98% by HPLC. CAS No. 2080306-20-1. Molecular formula: C28H34N4O2. Mole weight: 458.6.
Trichostatin A
Potent, reversible inhibitor of histone deacetylase. Mediates the activation of O6-methylguanine-DNA methyltransferase (MGMT). May be involved in cell cycle progression of several cell types, induces cell growth arrest at both G1 and G2/M phases. In some cases induces apoptosis. Group: Biochemicals. Grades: Highly Purified. CAS No. 58880-19-6. Pack Sizes: 1mg. US Biological Life Sciences.
Worldwide
Trichostatin A (TSA, A300, R-(E,E)-7-(4-(dimethylamino)phenyl)-N-hydroxy- 4,6-dimethyl-7-oxo-2,4-heptadienamide)
Antibiotic. Antifungal. Antiprotozoal. Potent and reversible, cell permeable inhibitor of histone deacetylase (HDAC). Immunosuppressive. Anticancer compound. Antifibrogenic. Apoptosis inducer. Induces cell growth arrest at both G1 and G2/M phases. Enhances the efficacy of anticancer agents that target DNA. Inactivates mitotic spindle checkpoint. Smooth muscle cell proliferation inhibitor. Telomerase inhibitor. Downregulates DNA methyltransferase DNMT1 and affects DNA methylation. Anti-inflammatory. Inhibits osteoclastogenesis and bone resorption. Group: Biochemicals. Alternative Names: TSA, A300, R-(E,E)-7-(4-(dimethylamino)phenyl)-N-hydroxy- 4,6-dimethyl-7-oxo-2,4-heptadienamide. Grades: Highly Purified. CAS No. 58880-19-6. Pack Sizes: 1mg, 5mg. Molecular Formula: C17H22N2O3, Molecular Weight: 302.4. US Biological Life Sciences.
Worldwide
UNC0224
The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression. The histone methyltransferase (HMTase) G9a can mono- or dimethylate lysine 9 on histone 3 (H3), contributing to early embryogenesis, genomic imprinting, and lymphocyte development. UNC0224 is a potent and selective G9a HMTase inhibitor, exhibiting an IC50 value of 15 nM. Isothermal titration calorimetry revealed UNC0224 binds to G9a with a Kd value of 29 nM. UNC0224 also inhibits GLP, a closely-related H3K9 HMTase, with assay-dependent IC50 values of 20-58 nM, but is more than 1,000-fold selective against SET7/9 (a H3K4 HMTase) and SET8 (a H4K20 HMTase). Synonyms: UNC0224; UNC-0224; UNC 0224; 7-[3-(Dimethylamino)propoxy]-2-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6-methoxy-N-(1-methyl-4-piperidinyl)-4-quinazolinamine. Grades: >98%. CAS No. 1197196-48-7. Molecular formula: C26H43N7O2. Mole weight: 485.67.
UNC0321
UNC0321 is the first G9a inhibitor with picomolar potency and the most potent G9a inhibitor to date. Protein lysine methyltransferase G9a, which catalyzes methylation of lysine 9 of histone H3 (H3K9) and lysine 373 (K373) of p53, is overexpressed in human cancers. Genetic knockdown of G9a inhibits cancer cell growth, and the dimethylation of p53 K373 results in the inactivation of p53. Synonyms: UNC0321, UNC-0321, UNC 0321, CHEMBL1214066, CHEBI:785916, UNC0321 (trifluoroacetate salt), NCGC0018778901, KB81388. Grades: >98%. CAS No. 1238673-32-9. Molecular formula: C27H45N7O3. Mole weight: 515.69.
UNC0321 (TFA Salt)
UNC0321 (trifluoroacetate salt) is a selective histone lysine methyltransferase (HMTase) inhibitor for G9a and GLP (also known as EHMT1), with IC50 of 6nM and 15nM, respectively. It is more than 40,000-fold more selective for G9a and GLP vs. SET7/9, SET8, PRMT3, or JMJD2E. Group: Biochemicals. Alternative Names: 4-Quinazolinamine, 7-[2-[2- (dimethylamino) ethoxy]ethoxy]-2- (hexahydro-4-methyl-1H-1, 4-diazepin-1-yl) -6-methoxy-N- (1-methyl-4-piperidinyl) -, trifluoroacetate. Grades: Highly Purified. CAS No. 1238673-32-9 (free base). Pack Sizes: 50mg. US Biological Life Sciences.
Worldwide
UNC0638
UNC0638 selectively inhibits G9a and GLP histone methyltransferases with IC 50 of 15 nM and 19 nM, respectively. UNC0638 inhibits TNBC cell invasion and migration in vitro. UNC0638 is also an inhibitor of EHMT1/2 and induces fetal hemoglobin ( HbF ) expression in human erythroid progenitor cell culture. In addition, UNC0638 has anti- FMDV (foot-and-mouth disease virus) and anti- VSV (vesicular stomatitis virus) activities, with excellent potency and selectivity against multiple epigenetic and non-epigenetic targets [1] [2] [3] [4] [5]. Uses: Scientific research. Group: Signaling pathways. CAS No. 1255580-76-7. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-15273.
UNC0638 hydrate
UNC 0638 is a selective inhibitor of G9a/EHMT2 and GLP histone lysine methyltransferases (IC50 values are < 15 nM and 19 nM for G9a and GLP respectively, and> 10000 nM for a panel of other histone methyltransferases). UNC 0638 inhibits dimethylation of H3K9 in MCF-7 cells (IC50 = 70 nM). Synonyms: UNC 0638; UNC0638; UNC-0638; 2-Cyclohexyl-6-methoxy-N-[1-(1-methylethyl)-4-piperidinyl]-7-[3-(1-pyrrolidinyl)propoxy]-4-quinazolinamine. Grades: ≥99% by HPLC. CAS No. 1255517-77-1. Molecular formula: C30H49N5O3. Mole weight: 527.7.
WDR5-0103
WDR5-0103 is a small molecule that binds a peptide-binding pocket on WDR5 with Kd of 450 nM. It inhibits MLL catalytic activity with an IC50 value of 39±10 μM in vitro. It is a WD40-repeat antagonist that binds to WDR55 central cavity. It inhibits MLL1 histone methyltransferase activity in vitro through disruption of the interaction of MLL with WDR5. It is an essential componet of the human trithorax-like famliy of SET1 methyltransferase complexes that carry out trimethylation of histone 3 Lys4. Uses: Wdr5-0103 inhibits mll1 histone methyltransferase activity. it is an essential componet of the human trithorax-like famliy of set1 methyltransferase complexes that carry out trimethylation of histone 3 lys4. Synonyms: 3-[(3-Methoxybenzoyl)aMino]-4-(4-Methyl-1-piperazinyl)benzoic Acid Methyl Ester;Methyl 3-(3-methoxybenzamido)-4-(4-methylpiperazin-1-yl)benzoate;WDR5-0103; WDR 5-0103; WDR-5-0103; WDR50103; WDR-50103; WDR 50103; WD-Repeat Protein 5-0103. Grades: >98 %. CAS No. 890190-22-4. Molecular formula: C21H25N3O4. Mole weight: 383.44.
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