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Home >> Signaling Pathways >> Chromatin/Epigenetics

Chromatin/Epigenetics

Chromatin/Epigenetics

Epigenetics

Epigenetics means above genetics. It determines how much and whether a gene is expressed without changing DNA sequences. Epigenetic regulations include, 1. DNA methylation: the addition of methyl group to DNA, converting cytosine to 5-methylcytosine, mostly at CpG sites; 2. Histone modifications: posttranslational modificationEpigeneticss of histone proteins including acetylation, methylation, ubiquitylation, phosphorylation and sumoylation; 3. miRNAs: non-coding microRNA downregulating gene expression; 4. Prions: infectious proteins viewed as epigenetic agents capable of inducing a phenotype without changing the genome.

Targets for  Chromatin/Epigenetics

Products for  Chromatin/Epigenetics

  1. Cat.No. Product Name Information
  2. GC91506 Bayer 18 Bayer 18 is a tyrosine kinase 2 (TYK2) inhibitor (IC50 = 18.7 nM). Bayer 18 Chemical Structure
  3. GC63694 BAZ1A-IN-1 BAZ1A-IN-1 is a potent inhibitor of BAZ1A (bromodomain-containing protein). BAZ1A-IN-1 shows a KD value of 0.52 μM against BAZ1A bromodomain. BAZ1A-IN-1 shows good anti-viability activity against cancer cell lines expressing a high level of BAZ1A, but weak or no activity against cancer cells with a low expression level of BAZ1A. BAZ1A-IN-1 Chemical Structure
  4. GC15175 BAZ2-ICR Selective BAZ2 bromodomain inhibitor BAZ2-ICR Chemical Structure
  5. GC35480 BB-Cl-Amidine hydrochloride BB-Cl-Amidine hydrochloride is a peptidylarginine deminase (PAD) inhibitor. BB-Cl-Amidine hydrochloride Chemical Structure
  6. GC42910 BB-F-Yne BB-F-Yne is a cell-permeable derivative of the protein arginine diminase (PAD) inhibitor BB-Cl-amidine that contains an alkyne moiety for use in click chemistry reactions. BB-F-Yne Chemical Structure
  7. GC74003 BBC0403 BBC0403 is a selective BRD2 inhibitor with Kds of 7.64 μM and 41.37 μM for BRD2 (BD2) and BRD2 (BD1), respectively. BBC0403 Chemical Structure
  8. GC18161 BCI-121

    A substrate-competitive SMYD3 inhibitor?

     BCI-121 Chemical Structure
  9. GC73279 BD-9136 BD-9136 is a highly selective BRD4 degrader. BD-9136 Chemical Structure
  10. GC15962 Belinostat (PXD101) Belinostat (PXD101) is a novel hydroxamate-type inhibitor of histone deacetylase (HDAC) activity in HeLa cell extracts with an IC50 of 27 nM. Belinostat (PXD101) Chemical Structure
  11. GC12844 Benzamide poly (ADP-ribose) synthetase inhibitor Benzamide Chemical Structure
  12. GC30763 Benzenebutyric acid (4-Phenylbutyric acid)

    4PBA

     Benzenebutyric acid (4-Phenylbutyric acid) (4-PBA) is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research. Benzenebutyric acid (4-Phenylbutyric acid) Chemical Structure
  13. GC16299 BET bromodomain inhibitor

    CPI-0610; CPI0610; CPI 0610

     Potent and selective inhibitor for BRD4 BET bromodomain inhibitor Chemical Structure
  14. GC63528 BET bromodomain inhibitor 1 BET bromodomain inhibitor 1 is an orally active, selective bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50 of 2.6 nM for BRD4. BET bromodomain inhibitor 1 binds to BRD2(2), BRD3(2), BRD4(1), BRD4(2), and BRDT(2) with high affinities (Kd values of 1.3 nM, 1.0 nM, 3.0 nM, 1.6 nM, 2.1 nM, respectively). bromodomain inhibitor 1 has anti-cancer activity. BET bromodomain inhibitor 1 Chemical Structure
  15. GC73742 BET bromodomain inhibitor 4 BET bromodomain inhibitor 4 (example 7) is an inhibitor of the BET bromodomain domain. BET bromodomain inhibitor 4 Chemical Structure
  16. GC35505 BET-BAY 002 BET-BAY 002 is a potent BET inhibitor; shows efficacy in a multiple myeloma model. BET-BAY 002 Chemical Structure
  17. GC35506 BET-BAY 002 S enantiomer BET-BAY 002 S enantiomer Chemical Structure
  18. GC31831 BET-IN-1 BET-IN-1 is a pan-inhibitor of all eight BET bromodomains, and selectivity over other representative bromodomain-containing proteins. BET-IN-1 Chemical Structure
  19. GC73423 BET-IN-14 BET-IN-14 is an orally active pan BET inhibitor (IC50: 5.35 nM). BET-IN-14 Chemical Structure
  20. GC72960 BET-IN-19 BET-IN-19 (Compound 146) is a BET inhibitor. BET-IN-19 Chemical Structure
  21. GC65506 BETd-246 BETd-246 is a second-generation and PROTAC-based BET bromodomain (BRD) inhibitor connected by ligands for Cereblon and BET, exhibiting superior selectivity, potency and antitumor activity. BETd-246 Chemical Structure
  22. GC32791 BETd-260 (ZBC 260)

    ZBC 260

     BETd-260 (ZBC 260) (ZBC 260) is a PROTAC connected by ligands for Cereblon and BET, with as low as 30 pM against BRD4 protein in RS4;11 leukemia cell line. BETd-260 (ZBC 260) potently suppresses cell viability and robustly induces apoptosis in hepatocellular carcinoma (HCC) cells. BETd-260 (ZBC 260) Chemical Structure
  23. GC12074 BG45 Novel HDAC3-selective inhibitor BG45 Chemical Structure
  24. GC14380 BGP-15 PARP inhibitor BGP-15 Chemical Structure
  25. GC12450 BI 2536

    BI-2536;BI2536

     A potent inhibitor of Plk1 BI 2536 Chemical Structure
  26. GC50540 BI 9321 Nuclear receptor-binding SET domain (NSD) 3 antagonist; selectively binds PWWP1 domain BI 9321 Chemical Structure
  27. GC16726 BI-7273 BRD9 bromodomain inhibitor BI-7273 Chemical Structure
  28. GC17828 BI-847325 dual inhibitor of MEK and Aurora kinases BI-847325 Chemical Structure
  29. GC39663 BI-9321 trihydrochloride BI-9321 trihydrochloride is a potent, selective and cellular active nuclear receptor-binding SET domain 3 (NSD3)-PWWP1 domain antagonist with a Kd value of 166 nM. BI-9321 trihydrochloride is inactive against NSD2-PWWP1 and NSD3-PWWP2. BI-9321 trihydrochloride specifically disrupts histone interactions of the NSD3-PWWP1 domain with an IC50 of 1.2 μM in U2OS cells. BI-9321 trihydrochloride Chemical Structure
  30. GC16817 BI-9564 BRD9/7 specific inhibitor BI-9564 Chemical Structure
  31. GC42933 Binucleine 2 Binucleine 2 is an isoform-specific and ATP-competitive inhibitor of Drosophila Aurora B kinase (Ki = 0.36 μM), a kinase involved in cell division. Binucleine 2 Chemical Structure
  32. GC64789 Biotinylated-JQ1

    Biotin-JQ1

     Biotinylated-JQ1 (Biotin-JQ1) is a biotinylated derivative of JQ1 with high affinity for the bromodomain of BRD4. Biotinylated-JQ1 inhibits MM1.S multiple myeloma cells proliferation with the EC50?of 0.4 μM. Biotinylated-JQ1 Chemical Structure
  33. GC25139 Biphenyl-4-sulfonyl chloride

    p-Phenylbenzenesulfonyl chloride, 4-Phenylbenzenesulfonyl chloride, p-Biphenylsulfonyl chloride

     Biphenyl-4-sulfonyl chloride (p-Phenylbenzenesulfonyl, 4-Phenylbenzenesulfonyl, p-Biphenylsulfonyl) is a HDAC inhibitor with synthetic applications in palladium-catalyzed desulfitative C-arylation. Biphenyl-4-sulfonyl chloride Chemical Structure
  34. GC48463 Bisubstrate Inhibitor 78 An inhibitor of NNMT Bisubstrate Inhibitor 78 Chemical Structure
  35. GC12171 BIX 01294 An inhibitor of G9a histone methyltransferase BIX 01294 Chemical Structure
  36. GC50659 BIX NHE1 inhibitor BIX NHE1 inhibitor is potent sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor, with IC50s of 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays, respectively. BIX NHE1 inhibitor Chemical Structure
  37. GC33301 BIX-01338 hydrate (BIX01338 hydrate) BIX-01338 hydrate (BIX01338 hydrate) is a histone lysine methyltransferase inhibitor. BIX-01338 hydrate (BIX01338 hydrate) Chemical Structure
  38. GC42944 BIX01294 (hydrochloride hydrate) The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression. BIX01294 (hydrochloride hydrate) Chemical Structure
  39. GC16114 Bizine LSD1 inhibitor Bizine Chemical Structure
  40. GC25159 BMF-219 BMF-219 is a highly selective and irreversible inhibitor of menin which has shown very promising activity in in-vitro and in-vivo preclinical tumour models. BMF-219 Chemical Structure
  41. GC12822 BML-210(CAY10433)

    NphenylN'(2Aminophenyl)hexamethylenediamide, CAY10433

     BML-210(CAY10433) is a novel HDAC inhibitor, and its mechanism of action has not been characterized. BML-210(CAY10433) Chemical Structure
  42. GC18408 BML-278 BML-278 is an activator of sirtuin 1 (SIRT1) that has an EC150 value (effective concentration able to increase the enzyme by 150%) of 1 uM. BML-278 Chemical Structure
  43. GC15932 BMN 673

    Talazoparib

     A PARP inhibitor BMN 673 Chemical Structure
  44. GC10920 BMN-673 8R,9S BMN-673 8R,9S Chemical Structure
  45. GC50633 BMS 986094 Prodrug of HCV RNA polymerase inhibitor 2'-C-methyl guanosine triphosphate; potent HCV replication inhibitor BMS 986094 Chemical Structure
  46. GC32028 BMS-066 BMS-066 is an IKKβ/Tyk2 pseudokinase inhibitor, with IC50s of 9 nM and 72 nM, respectively. BMS-066 Chemical Structure
  47. GC13926 BMS-345541(free base) BMS-345541(free base) is a selective inhibitor of the catalytic subunits of IKK (IKK-2 IC50=0.3 μM, IKK-1 IC50=4 μM). BMS-345541(free base) binds at an allosteric site of IKK. BMS-345541(free base) Chemical Structure
  48. GC12454 BMS-911543 A potent, selective JAK2 inhibitor BMS-911543 Chemical Structure
  49. GC32812 BMS-986158 A BET bromodomain inhibitor BMS-986158 Chemical Structure
  50. GC62491 BMS-986202 BMS-986202 is a potent, selective and orally active Tyk2 inhibitor that binds to Tyk2 JH2 with an IC50 of 0.19 nM and a Ki of 0.02 nM. BMS-986202 Chemical Structure
  51. GC48495 BMS-P5 BMS-P5 is a specific and orally active peptidylarginine deiminase 4 (PAD4) inhibitor. BMS-P5 blocks MM-induced NET formation and delays progression of MM in a syngeneic mouse model. BMS-P5 Chemical Structure
  52. GC70471 BNS BNS is a cell penetrant, potent and selective PHD2 (prolyl-hydroxylase 2) inhibitor. BNS Chemical Structure
  53. GC46935 Bobcat 339

    BC339

     A TET1 and TET2 inhibitor Bobcat 339 Chemical Structure
  54. GC34498 Bobcat339 hydrochloride Bobcat339 hydrochloride is a potent and selective cytosine-based inhibitor of TET enzyme, with the IC50s of 33 μM and 73 μM for TET1 and TET2, respectively. Bobcat339 hydrochloride is useful to the field of epigenetics and serves as a starting point for new therapeutics that target DNA methylation and gene transcription. Bobcat339 hydrochloride Chemical Structure
  55. GC11641 Boc-Lys(Ac)-AMC

    GPCR G2A/GPR132 agonist

     Boc-Lys(Ac)-AMC Chemical Structure
  56. GC64865 Bomedemstat

    IMG-7289

     Bomedemstat (IMG-7289) is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis. Bomedemstat Chemical Structure
  57. GC68795 Bomedemstat dihydrochloride

    IMG-7289 dihydrochloride

    Bomedemstat (IMG-7289) dihydrochloride is an orally active and irreversible inhibitor of lysine-specific demethylase 1 (LSD1). Bomedemstat dihydrochloride can increase the methylation of H3K4 and H3K9, which then alters gene expression. Bomedemstat dihydrochloride has anti-cancer activity, inhibiting cancer cell proliferation and inducing apoptosis.

     Bomedemstat dihydrochloride Chemical Structure
  58. GC67921 Bomedemstat ditosylate

    IMG-7289 ditosylate

     Bomedemstat ditosylate Chemical Structure
  59. GC65879 Bomedemstat hydrochloride

    IMG-7289 hydrochloride

     Bomedemstat (IMG-7289) hydrochloride is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat hydrochloride can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat hydrochloride shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis. Bomedemstat hydrochloride Chemical Structure
  60. GC48620 BPKDi A PKD inhibitor BPKDi Chemical Structure
  61. GC64538 BPTF-IN-BZ1 BPTF-IN-BZ1, a BPTF inhibitor, possesses a high potency (Kd = 6.3 nM). BPTF-IN-BZ1 Chemical Structure
  62. GC15974 bpV(HOpic) (potassium salt, technical grade)

    Bisperoxovanadium(HOpic)

     bpV(HOpic) (potassium salt, technical grade) is a potent and selective inhibitor of PTEN with an IC50 of 14 nM. bpV(HOpic) (potassium salt, technical grade) Chemical Structure
  63. GC35547 BR102375 BR102375 is a non-TZD peroxisome proliferator-activated receptor γ (PPAR γ) full agonist for the treatment of type 2 diabetes, reveals EC50 value of 0.28?μM and Amax ratio?of 98%. BR102375 Chemical Structure
  64. GC33223 BRCA1-IN-1 BRCA1-IN-1 is a novel small-molecule-like BRCA1 inhibitor with IC50 and Ki of 0.53 μM and 0.71 μM, respecrively. BRCA1-IN-1 Chemical Structure
  65. GC35550 BRCA1-IN-2 BRCA1-IN-2 (compound 15) is a cell-permeable protein-protein interaction (PPI) inhibitor for BRCA1 with an IC50 of 0.31 μM and a Kd of 0.3 μM, which shows antitumor activities via the disruption of BRCA1 (BRCT)2/protein interactions. BRCA1-IN-2 Chemical Structure
  66. GC33331 BRD 4354 BRD 4354 is a moderately potent inhibitor of HDAC5 and HDAC9, with IC50s of 0.85 and 1.88 μM, respectively. BRD 4354 Chemical Structure
  67. GC35551 BRD 4354 ditrifluoroacetate BRD 4354 (ditrifluoroacetate) is a moderately potent inhibitor of HDAC5 and HDAC9, with IC50s of 0.85 and 1.88 μM, respectively. BRD 4354 ditrifluoroacetate Chemical Structure
  68. GC50322 BRD 9757 Potent and selective HDAC6 inhibitor BRD 9757 Chemical Structure
  69. GC38742 BRD-6929

    JQ12

     An HDAC1 and HDAC2 inhibitor BRD-6929 Chemical Structure
  70. GC35552 BRD-IN-3 BRD-IN-3 ((R,R)-36n) is a highly potent PCAF bromodomain (BRD) inhibitor, with an IC50 of 7 nM. BRD-IN-3 also exhibits activity against GCN5 and FALZ. BRD-IN-3 Chemical Structure
  71. GC63731 BRD0639 BRD0639 is a first-in-class inhibitor of the PRMT5-substrate adaptor interaction. BRD0639 is a PRMT5 binding motif (PBM)-competitive agent that can support studies of PBM dependent PRMT5 activities. BRD0639 Chemical Structure
  72. GC72945 BRD2492 BRD2492 (compound 6d) is a potent, selective HDAC1 and HDAC2 inhibitor with IC50s of 13.2 nM and 77.2 nM, respecrtively. BRD2492 Chemical Structure
  73. GC39551 BRD3308 BRD3308 is a highly selective HDAC3 inhibitor with an IC50 of 54 nM. BRD3308 Chemical Structure
  74. GC33017 BRD4 degrader AT1 BRD4 degrader AT1 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4 as a highly selective Brd4 degrader, with a Kd of 44 nM for Brd4BD2 in cells. BRD4 degrader AT1 Chemical Structure
  75. GC64960 BRD4 Inhibitor-10 BRD4 Inhibitor-10 is a potent BRD4-BD1 inhibitor extracted from patent WO2015022332A1, Compound II-25, has an IC50 of 8 nM. BRD4 Inhibitor-10 Chemical Structure
  76. GC68803 BRD4 Inhibitor-20

    BRD4 Inhibitor-20 is an effective inhibitor of the bromodomain-containing protein 4 (BRD4) with oral activity. It has inhibitory activity against both BRD4 (BD1) and BRD4 (BD2), with IC50 values of 19 nM and 28 nM, respectively. BRD4 Inhibitor-20 also exhibits anti-proliferative activity in cancer cell lines. It can be used for research on various cancers such as colon cancer.

     BRD4 Inhibitor-20 Chemical Structure
  77. GC65569 BRD4 Inhibitor-24 BRD4 Inhibitor-24 (compound 3U) is a potent BRD4 inhibitor, BRD4 Inhibitor-24 shows antitumor activity against MCF7 and K652 cells, with IC50 values of 33.7 and 45.9 μM, respectively (extracted from patent CN107721975A). BRD4 Inhibitor-24 Chemical Structure
  78. GC73879 BRD4 Inhibitor-30 BRD4 inhibitor-30 (Compound 1) is a BRD4 inhibitor with a IC50 value of 415 nM. BRD4 Inhibitor-30 Chemical Structure
  79. GC73958 BRD4 ligand 6 TFA BRD4 ligand 6 TFA is the TFA salt form of BRD4 ligand 6. BRD4 ligand 6 TFA Chemical Structure
  80. GC66441 BRD4/CK2-IN-1 BRD4/CK2-IN-1 is the first highly effective and oral active dual-target inhibitor of BRD4/CK2 (bromodomain-containing protein 4/casein kinase 2), with IC50s of 180 nM and 230 nM for BRD4 and CK2, respectively. BRD4/CK2-IN-1 has strong anticancer activity without obvious toxicities. BRD4/CK2-IN-1 induces apoptosis and autophagy-associated cell death in triple-negative breast cancer (TNBC) BRD4/CK2-IN-1 Chemical Structure
  81. GC73953 BRD4/NAMPT-IN-1 BRD4/NAMPT-IN-1 (Compound A2) shows strong inhibitory effects on NAMPT and BRD4 (IC50=35 nM (NAMPT) and 58 nM (BRD4)). BRD4/NAMPT-IN-1 Chemical Structure
  82. GC10259 BRD4770

    HMTase Inhibitor VI

     novel G9a(EHMT2) inhibitor BRD4770 Chemical Structure
  83. GC40923 BRD4884 BRD4884 is an HDAC inhibitor with IC50 values of 29 nM, 62 nM, and 1.09 μM for HDAC1, 2, and 3, respectively. BRD4884 Chemical Structure
  84. GC13088 BRD6688 HDAC inhibitor BRD6688 Chemical Structure
  85. GC34505 BRD7-IN-1 BRD7-IN-1, a modified derivative of BI7273 (BRD7/9 inhibitor), binds to a VHL ligand via a linker to form a PROTAC VZ185 (VZ185 against BRD7/9 with DC50s of 4.5 and 1.8 nM, respectively). BRD7-IN-1 Chemical Structure
  86. GC71086 BRD7-IN-2 BRD7-IN-2 (compound 2-77) is a potent inhibitor of bromodomain-containing protein 7 (BRD7), targeting to prostate cancer cells. BRD7-IN-2 Chemical Structure
  87. GC12484 BRD73954 potent and selective HDAC inhibitor BRD73954 Chemical Structure
  88. GC32988 BRD9539 An inhibitor of EHMT2/G9a and PRC2 in enzyme assays BRD9539 Chemical Structure
  89. GC25168 Brepocitinib (PF-06700841)

    PF-841

     Brepocitinib (PF-06700841, PF-841) is a potent inhibitor of Tyk2 and Jak1 with IC50s of 23 nM, 17 nM, 77 nM for Tyk2, Jak1 and Jak2 respectively. It has appropriate in-family selectivity against JAK2 and JAK3. Brepocitinib (PF-06700841) Chemical Structure
  90. GC35554 Brevilin A

    6-O-Angeloylprenolin, Brevelin A

     A sesquiterpene lactone with anticancer activity Brevilin A Chemical Structure
  91. GC64541 BRM/BRG1 ATP Inhibitor-2 BRM/BRG1 ATP Inhibitor-2 is a BRG1/BRM ATPase inhibitor for the treatment of BAF-related disorders. BRM/BRG1 ATP Inhibitor-2 Chemical Structure
  92. GC35557 Bromodomain IN-1 Bromodomain IN-1 is a Bromodomain inhibitor extracted from patent WO2016069578A1, compound 4 . Bromodomain IN-1 Chemical Structure
  93. GC16531 Bromodomain Inhibitor, (+)-JQ1 A selective inhibitor of BET bromodomains Bromodomain Inhibitor, (+)-JQ1 Chemical Structure
  94. GC35558 Bromodomain inhibitor-8 Bromodomain inhibitor-8 (Intermediate 21) is a BET bromodomain inhibitor for treating autoimmune and inflammatory diseases. Bromodomain inhibitor-8 Chemical Structure
  95. GC10402 Bromosporine A non-specific bromodomain inhibitor Bromosporine Chemical Structure
  96. GC15410 Bufexamac COX inhibitor Bufexamac Chemical Structure
  97. GC64761 Butyric acid-13C1 Butyric acid-13C1 Chemical Structure
  98. GC46104 Butyric Acid-d7 An internal standard for the quantification of sodium butyrate Butyric Acid-d7 Chemical Structure
  99. GC10226 Butyrolactone 3

    histone acetyltransferase Gcn5 inhibitor

     Butyrolactone 3 Chemical Structure
  100. GC68819 Butyzamide

    Butyzamide is an orally effective Mpl activator, where Mpl is a receptor for thrombopoietin (TPO) involved in platelet production. Butyzamide increases the phosphorylation levels of JAK2, STAT3, STAT5 and MAPK. In mouse xenograft experiments, Butyzamide increases human platelet levels.

     Butyzamide Chemical Structure
  101. GC10690 BYK 204165

    PARP Inhibitor XIV

     A selective inhibitor of PARP1 BYK 204165 Chemical Structure

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