Epigenetics

Covalent modifications to DNA or histone proteins with various chemical groups can determine whether genes are turned on or off and can thus influence the production of proteins in a cell. This genetic control without altering DNA sequences is crucial in many normal cellular functions. Aberrant epigenetic alterations are present in myriad disease states. Pharmacological manipulation of the various enzymes involved in epigenetic changes in pathological states is an important new target in drug discovery. Writers (methyl and acetyl transferases) are enzymes capable of modifying nucleotide bases and amino acid residues on histones. Erasers (demethylases and deacetylases) remove these same modifications. Readers (bromodomains) are enzymes capable of recognizing specific epigenetic marks that direct a particular transcriptional outcome.

Bromodomains

  • GSK620 | BD2 selective BET inhibitor
    CAS:
    2088410-46-0
    Catalog Number:
    10-4180
  • CPI203 | BET bromodomain inhibitor
    CAS:
    1446144-04-2
    Catalog Number:
    10-4048
  • BI 9564 | BRD9 bromodomain inhibitor
    CAS:
    1883429-22-8
    Catalog Number:
    10-4320
  • BZ1 | BPTF inhibitor
    CAS:
    2766623-38-3
    Catalog Number:
    10-4037
    Activity:
    BPTF inhibitor
    Chemical Names:
    5-((4-(2-Aminoethyl)phenyl)amino)-4-chloro-2-methylpyridazin-3(2H)-one
    Molecular Weight:
    278.74
    Molecular Formula:
    C13H15ClN4O
    Solubility:
    Soluble in DMSO (>50 mg/ml); ethanol (>50 mg/ml)
    Physical Properties:
    Yellow solid
    Purity:
    98% HPLC
    NMR (Conforms)
    Storage Temperature:
    -20°C
    Stability:
    Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month.
    Shipping Code:
    RT
  • GSK6853 | BRPF1 inhibitor
    CAS:
    1910124-24-1
    Catalog Number:
    10-4016
    Activity:
    BRPF1 inhibitor
    Chemical Names:
    N-[1,3-Dimethyl-6-[(2R)-2-methylpiperazin-1-yl]-2-oxobenzimidazol-5-yl]-2-methoxybenzamide
    Molecular Weight:
    409.49
    Molecular Formula:
    C22H27N5O3
    Solubility:
    Soluble in DMSO (25 mg/ml); ethanol (25 mg/ml)
    Physical Properties:
    White solid
    Purity:
    98% HPLC
    NMR (Conforms)
    Storage Temperature:
    -20°C
    Stability:
    Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
    Shipping Code:
    RT
View All Bromodomains Products

Deubiquitinase

  • OTUDin3 | OTUD3 inhibitor
    CAS:
    441290-65-9
    Catalog Number:
    10-4981
  • iBAP-II | BAP1 inhibitor
    CAS:
    1013813-81-4
    Catalog Number:
    10-4038
    Activity:
    BAP1 inhibitor
    Chemical Names:
    4-(8-Nitro-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4-yl)phenol
    Molecular Weight:
    308.33
    Molecular Formula:
    C18H16N2O3
    Solubility:
    Soluble in DMSO (25 mg/ml)
    Physical Properties:
    Yellow solid
    Purity:
    >98% HPLC
    NMR (Conforms)
    Storage Temperature:
    -20°C
    Stability:
    Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
    Shipping Code:
    RT
  • Thiolutin | Inhibitor of the DUB PSMD14
    CAS
    87-11-6
    Catalog Number:
    10-2106
    Activity:
    Inhibitor of the DUB PSMD14
    Chemical Names:
    N-(4,5-Dihydro-4-methyl-5-oxo-1,2-dithiolo[4,3-b]pyrrol-6-yl)acetamide;
    Acetopyrrothin
    Molecular Weight:
    228.29
    Molecular Formula:
    C8H8N2O2S2
    Solubility:
    Soluble in DMSO (up to 15 mg/ml)
    Physical Properties:
    Yellow solid
    Purity:
    >98% HPLC
    NMR (Conforms)
    Storage Temperature:
    -20°C
    Stability:
    Stable for 3 years as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
    Shipping Code:
    RT
  • P22077 | Selective USP7 inhibitor
    CAS:
    1247819-59-5
    Catalog Number:
    10-4125
    Activity:
    Selective USP7 inhibitor
    Chemical Name:
    1-(5-((2,4-Difluorophenyl)thio)-4-nitrothiophen-2-yl)ethanone
    Molecular Weight:
    315.32
    Molecular Formula:
    C12H7F2NO3S2
    Solubility:
    Soluble in DMSO (up to 25 mg/ml)
    Physical Properties:
    Off-white solid
    Purity:
    98% by HPLC
    NMR (Conforms)
    Storage Temperature:
    -20°C
    Stability:
    Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
    Shipping Code:
    RT
  • PR-619 | DUB inhibitor
    CAS:
    2645-32-1
    Catalog Number:
    10-1485
    Activity:
    DUB inhibitor
    Alternate Names:
    3,5-Dithiocyanatopyridine-2,6-diamine
    Chemical Name:
    2,6-Diaminopyridine-3,5-bis(thiocyanate)
    Molecular Weight:
    223.28
    Molecular Formula:
    C7H5N5S2
    Solubility:
    Soluble in DMSO (up to 5 mg/ml).
    Physical Properties:
    Yellow solid
    Purity:
    98% by TLC
    NMR (Conforms)
    Storage Temperature:
    -20°
    Stability:
    Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month.
    Shipping Code:
    RT
View All Deubiquitinase Products

DNA Demethylation

View All DNA Demethylation Products

DNA Methylation

  • DBIC | DNMT3B S-nitrosylation inhibitor
    CAS:
    487026-67-5
    Catalog Number:
    10-5161
  • DBIC-neg2 | DBIC negative control
    CAS:
    N/A
    Catalog Number:
    10-5162
    Activity:
    DBIC negative control
    Chemical Names:
    (E)-N’-(3,4-Dihydroxybenzylidene)acetohydrazide
    Molecular Weight:
    194.19
    Molecular Formula:
    C9H10N2O3
    Solubility:
    Soluble in DMSO (40 mg/ml)
    Physical Properties:
    Pale yellow solid
    Purity:
    >98% TLC
    NMR (Conforms)
    Storage Temperature:
    -20°C
    Stability:
    Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
    Shipping Code:
    RT
  • SGI-1027 | DNA methyl transferase inhibitor
    CAS:
    1020149-73-8
    Catalog Number:
    10-5488
    Activity:
    DNA methyl transferase inhibitor
    Chemical Names:

    N-[4-[(2-Amino-6-methyl-4-pyrimidinyl)amino]phenyl]-4-(4-quinolinylamino)benzamide

    Molecular Weight:
    461.52
    Molecular Formula:
    C27H23N7O
    Solubility:
    Soluble in DMSO (up to 35 mg/ml)
    Physical Properties:
    Off-white solid
    Purity:
    98% TLC
    NMR (Conforms)
    Storage Temperature:
    -20°C
    Stability:
    Stable for 2 years as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
    Shipping Code:
    RT
  • PF-9366 | Methionine adenosyltransferase 2A inhibitor
    CAS:
    72882-78-1
    Catalog Number:
    10-4635
    Activity:
    Methionine adenosyltransferase 2A inhibitor
    Chemical Name:
    2-(7-Chloro-5-phenyl)-[1,2,4]triazolo[4,3-a]quinoline-1-yl)-N,N,dimethylethanamine
    Molecular Weight:
    350.85
    Molecular Formula:
    C20H19ClN4
    Solubility:
    Soluble in DMSO (up to 20 mg/ml).
    Physical Properties:
    Beige solid
    Purity:
    98% by TLC
    NMR (Conforms)
    Storage Temperature:
    -20°C
    Stability:
    Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
    Shipping Code:
    RT
  • 6-Thioguanine | Anticancer agent / Downregulates DNMT1
    CAS:
    154-42-7
    Catalog Number:
    10-1282
    Activity:
    Anticancer agent / Downregulates DNMT1
    Chemical Name:
    2-Amino-6-mercaptopurine
    Alternate Names:
    6-TG; NSC 752, NSC 76504
    Molecular Weight:
    167.19
    Molecular Formula:
    C5H5N5S
    Solubility:
    Soluble in DMF (up to 1.5 mg/ml with warming)
    Physical Properties:
    Pale yellow solid
    Purity:
    96% by HPLC
    NMR (Conforms)
    Storage Temperature:
    -20°C
    Stability:
    Stable for 1 year from date of purchase as supplied. Solutions in DMF may be stored at -20°C for up to 1 month.
    Shipping Code:
    RT
View All DNA Methylation Products

Histone Acetylation

  • WM-1119 | HAT KAT6A inhibitor
    CAS:
    2055397-28-7
    Catalog Number:
    10-4013
  • TTK21 | CBP/p300 histone acetyltransferase activator
    CAS:
    709676-56-2
    Catalog Number:
    10-5669
    Activity:
    Histone acetyltransferase CBP/p300 activator
    Chemical Names:
    N-[4-Chloro-3-(trifluoromethyl)phenyl]-2-propoxybenzamide
    Molecular Weight:
    357.76
    Molecular Formula:
    C17H15ClF3NO2
    Solubility:
    Soluble in DMSO (50 mg/ml)
    Physical Properties:
    Off-white solid
    Purity:
    >98% HPLC
    NMR (Conforms)
    Storage Temperature:
    -20°C
    Stability:
    Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
    Shipping Code:
    RT
  • Acetyl-Coenzyme A 3Li | Acetylation and fatty acid biosynthesis cofactor
    CAS:
    75520-41-1
    Catalog Number:
    10-5384
    Activity:
    Cofactor for cellular metabolism/Acetyl donor
    Chemical Name:

    Acetyl-CoA

    Molecular Weight:
    881.42
    Molecular Formula:
    C23H35Li3N7O17P3S·3H2O
    Solubility:
    Soluble in water (10 mg/ml)
    Physical Properties:
    White solid
    Purity:
    90% (enzymatic)
    Storage Temperature:
    -20°C
    Stability:
    Stable for 2 years as supplied. Solutions in water may be stored at -20°C for up to 2 weeks.
    Shipping Code:
    RT
  • Remodelin | Acetyltransferase NAT10 inhibitor
    CAS:
    949912-58-7
    Catalog Number:
    10-5085
    Activity:
    Acetyl-transferase NAT10 inhibitor
    Chemical Name:
    4-[2-(2-Cyclopentylidenehydrazinyl)-4-thiazolyl]-benzonitrile
    Molecular Weight:
    282.36
    Molecular Formula:
    C15H14N4S
    Solubility:
    Soluble in DMSO (up to 40 mg/ml).
    Physical Properties:
    Pale yellow solid
    Purity:
    98% by HPLC
    NMR (Conforms)
    Storage Temperature:
    -20°C
    Stability:
    Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
    Shipping Code:
    RT
  • Anacardic Acid | HAT inhibitor
    CAS:
    16611-84-0
    Catalog Number:
    10-4015
    Activity:
    HAT inhibitor
    Chemical Name:
    2-Hydroxy-6-pentadecylbenzoic acid
    Alternate Names:
    6-Pentadecylsalicylic acid; 6-PDSA
    Molecular Weight:
    348.52
    Molecular Formula:
    C22H36O3
    Solubility:
    Soluble in DMSO (up to at least 25 mg/ml) or in Ethanol (up to 15 mg/ml)
    Physical Properties:
    White solid
    Purity:
    98% by HPLC
    NMR (Conforms)
    Storage Temperature:
    -20°C
    Stability:
    Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
    Shipping Code:
    RT
View All Histone Acetylation Products

Histone Deacetylation

  • PCI-34051 | HDAC 8 inhibitor
    CAS:
    950762-95-5
    Catalog Number:
    10-3396
  • Phenylhexyl isothiocyanate | Chemopreventive/HDAC inhibitor/p53 reactivator
    CAS:
    133920-06-6
    Catalog Number:
    10-5258
  • BG45 | HDAC3 selective inhibitor
    CAS:
    926259-99-6
    Catalog Number:
    10-5638
  • OSS-128167 | SIRT6 Inhibitor
    CAS:
    887686-02-4
    Catalog Number:
    10-5197
    Activity:
    SIRT6 inhibitor
    Chemical Names:
    5-(3-(Furan-2-carboxamido)benzamido)-2-hydroxybenzoic acid
    Molecular Weight:
    366.33
    Molecular Formula:
    C19H14N2O6
    Solubility:
    Soluble in DMSO (25 mg/ml); Ethanol (25 mg/ml)
    Physical Properties:
    Off-white solid
    Purity:
    >98% HPLC
    NMR (Conforms)
    Storage Temperature:
    -20°C
    Stability:
    Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month.
    Shipping Code:
    RT
  • BRD73954 | Selective HDAC6/8 inhibitor
    CAS:
    1440209-96-0
    Catalog Number:
    10-4014
    Activity:
    Selective HDAC6/8 inhibitor
    Chemical Names:
    3-N-Hydroxy-1-N-(2-phenylethyl)benzene-1,3-dicarboxamide
    Molecular Weight:
    284.32
    Molecular Formula:
    C16H16N2O3
    Solubility:
    Soluble in DMSO (25 mg/ml)
    Physical Properties:
    Off-white solid
    Purity:
    >98% HPLC
    NMR (Conforms)
    Storage Temperature:
    -20°C
    Stability:
    Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
    Shipping Code:
    RT
View All Histone Deacetylation Products

Histone Demethylation

  • iPHF8 | Inhibitor of lysine demethylase PHF8
    CAS:
    1574530-99-6
    Catalog Number:
    10-4049
  • iJMJD6 | Arginine demethylase JMJD6 inhibitor
    CAS:
    899548-78-8
    Catalog Number:
    10-4039
  • Deferasirox | Iron Chelator
    CAS:
    201530-41-8
    Catalog Number:
    10-4949
    Activity:
    Iron chelator
    Chemical Names:
    4-[3,5-bis(2-Hydroxyphenyl)-1,2,4-triazol-1-yl]benzoic acid
    Alternate Name:
    ICL670
    Molecular Weight:
    373.36
    Molecular Formula:
    C21H15N3O4
    Solubility:
    Soluble in DMSO (10 mg/ml)
    Physical Properties:
    Off-white to white solid
    Purity:
    >98% HPLC
    NMR (Conforms)
    Storage Temperature:
    -20°C
    Stability:
    Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
    Shipping Code:
    RT
  • CPI-455 | Lysine demethylase KDM5 inhibitor
    CAS:
    1628208-23-0
    Catalog Number:
    10-4035
    Activity:
    Lysine demethylase KDM5 inhibitor
    Chemical Name:
    7-Oxo-5-phenyl-6-propan-2-yl-1H-pyrazolo[1,5-a]pyrimidine-3-carbonitrile
    Molecular Weight:
    278.32
    Molecular Formula:
    C16H14N4O
    Solubility:
    Soluble in DMSO (up to at least 25 mg/ml)
    Physical Properties:
    Off-white solid
    Purity:
    98% by HPLC
    NMR (Conforms)
    Storage Temperature:
    -20°C
    Stability:
    Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
    Shipping Code:
    RT
  • GSK2879552 | Potent and selective LSD1 inhibitor
    CAS:
    1401966-69-5
    Catalog Number:
    10-4020
    Activity:
    Potent and selective LSD1 inhibitor
    Chemical Name:
    4-[[4-[[[(1R,2S)-2-Phenylcyclopropyl]amino]methyl]-1-piperidinyl]methyl]benzoic acid dihydrochloride
    Molecular Weight:
    437.40
    Molecular Formula:
    C23H28N2O2 • HCl
    Solubility:
    Soluble in DMSO (up to 25 mg/ml) or in Water (up to at least 25 mg/ml)
    Physical Properties:
    White solid
    Purity:
    98% by HPLC
    NMR (Conforms)
    Storage Temperature:
    -20°C
    Stability:
    Stable for 1 year from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20°C for up to 3 months.
    Shipping Code:
    RT
View All Histone Demethylation Products

Histone Methylation

  • LD2 | PRMT9 inhibitor
    CAS:
    1134334-55-6
    Catalog Number:
    10-4872
    Activity:
    PRMT9 inhibitor
    Chemical Names:
    4-Chloro-8-methoxy-5-methyl-5H-pyrimido[5,4-b]indole
    Molecular Weight:
    247.68
    Molecular Formula:
    C12H10ClN3O
    Solubility:
    Soluble in DMSO (at least 40 mg/ml)
    Physical Properties:
    Pale yellow solid
    Purity:
    >98% HPLC
    NMR (Conforms)
    Storage Temperature:
    -20°C
    Stability:
    Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
    Shipping Code:
    RT
  • MS012 | Potent and selective GLP lysine methyltransferase inhibitor
    CAS:
    2089617-83-2
    Catalog Number:
    10-4875
    Activity:
    Potent and selective GLP lysine methyltransferase inhibitor
    Chemical Names:
    N2-Hexyl-6,7-dimethoxy-N4-(1-methylpiperidin-4-yl)quinazoline-2,4-diamine
    Molecular Weight:
    401.55
    Molecular Formula:
    C22H35N5O2
    Solubility:
    Soluble in DMSO (>25 mg/ml)
    Physical Properties:
    Off-white solid
    Purity:
    >98% HPLC
    NMR (Conforms)
    Storage Temperature:
    -20°C
    Stability:
    Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
    Shipping Code:
    RT
  • UNC0224 | G9a histone methyl transferase inhibitor
    CAS:
    1197196-48-7
    Catalog Number:
    10-5216
  • GSK126 | EZH2 methyltransferase inhibitor
    CAS:
    1346574-57-9
    Catalog Number:
    10-3394
    Activity:
    EZH2 methyltransferase inhibitor
    Chemical Names:
    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
    Molecular Weight:
    526.69
    Molecular Formula:
    C31H38N6O2
    Solubility:
    Soluble in DMSO (16 mg/ml)
    Physical Properties:
    Cream solid
    Purity:
    >98% HPLC/TLC
    NMR (Conforms)
    Storage Temperature:
    -20°C
    Stability:
    Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
    Shipping Code:
    RT
  • Intelliscreen™ Polycomb Repressive Complex Inhibitors Mini-Library Mini-Library
    Catalog Number:
    10-7315
View All Histone Methylation Products

Other Epigenetics

  • FB23-2 | FTO inhibitor
    CAS:
    2243736-45-8
    Catalog Number:
    10-4852
  • BRM014 | BRM/BRG1 ATPase inhibitor
    CAS:
    2270879-17-7
    Catalog Number:
    10-5244
  • UZH2 | METTL3 inhibitor
    CAS:
    2756566-45-5
    Catalog Number:
    10-4849
  • SGC-iMLLT | MLLT1/3 YEATS domain inhibitor
    CAS:
    2255338-25-9
    Catalog Number:
    10-4046
    Activity:
    MLLT1/3 YEATS domain inhibitor
    Chemical Names:
    (S)-1-Methyl-N-(2-((2-methylpyrrolidin-1-yl)methyl)-1H-benzo[d]imidazole-5-yl)-1H-indazole-5-carboxamide
    Molecular Weight:
    388.48
    Molecular Formula:
    C22H24N6O
    Solubility:
    Soluble in DMSO (at least 50 mg/ml)
    Physical Properties:
    Off-white to beige solid
    Purity:
    >98% HPLC
    NMR (Conforms)
    Storage Temperature:
    -20°C
    Stability:
    Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
    Shipping Code:
    RT
  • Nitazoxanide | Wnt signaling inhibitor
    CAS:
    55981-09-4
    Catalog Number:
    10-4633
    Activity:
    Wnt signaling inhibitor
    Chemical Names:
    O-[N-(5-Nitrothiazol-2-yl)carbamoyl]phenyl acetate; NTZ
    Molecular Weight:
    307.28
    Molecular Formula:
    C12H9N3O5S
    Solubility:
    Soluble in DMSO (>50 mg/ml)
    Physical Properties:
    Off-white solid
    Purity:
    99% HPLC
    NMR (Conforms)
    Storage Temperature:
    -20°C
    Stability:
    Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
    Shipping Code:
    RT
View All Other Epigenetics Products

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