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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. GC16509 Adox Adox, a purine nucleoside analogue, is a potent inhibitor of S-Adenosylhomocysteine hydrolase (SAHH) (Ki=3.3 nM). Adenosine Dialdehyde exhibits potent anti-tumor activity in vivo and can be used for the cancer research. Adox  Chemical Structure
  3. GC64527 ADTL-SA1215 ADTL-SA1215 is a first-in-class specific small-molecule activator of SIRT3 that modulates autophagy in triple negative breast cancer. ADTL-SA1215  Chemical Structure
  4. GC65330 AES-135 AES-135, a hydroxamic acid-based pan-HDAC inhibitor, prolongs survival in an orthotopic mouse model of pancreatic cancer. AES-135 inhibits HDAC3, HDAC6, HDAC8, and HDAC11 with IC50s ranging from 190-1100 nM. AES-135  Chemical Structure
  5. GC48775 AES-350 An inhibitor of class I and class IIb HDACs AES-350  Chemical Structure
  6. GC66379 AFM-30a hydrochloride AFM-30a hydrochloride is a potent protein arginine deiminase 2 (PAD2) inhibitor and has excellent PAD2-selectivity. AFM-30a hydrochloride binds to PAD2 with an EC50 value of 9.5 μM. AFM-30a hydrochloride also inhibits H3 citrullination with an EC50 value of 0.4 μM. AFM-30a hydrochloride can be used for the research of certain cancers and a variety of autoimmune diseases including rheumatoid arthritis (RA), multiple sclerosis, lupus, and ulcerative colitis. AFM-30a hydrochloride  Chemical Structure
  7. GC33416 AFP464 AFP464 (NSC710464 free base), is an active HIF-1α inhibitor with an IC50 of 0.25 μM, also is a potent aryl hydrocarbon receptor (AhR) activator. AFP464  Chemical Structure
  8. GC16318 AG-14361 A PARP1 inhibitor AG-14361  Chemical Structure
  9. GC17881 AGK 2

    AGK2 is a selective SIRT2 inhibitor, with an IC50 of 3.

    AGK 2  Chemical Structure
  10. GC15931 AGK7 cell-permeable, selective inhibitor of SIRT2 AGK7  Chemical Structure
  11. GN10413 Agrimol B Agrimol B  Chemical Structure
  12. GC10676 AK-7

    selective and brain-permeable SIRT2 inhibitor

    AK-7  Chemical Structure
  13. GC62277 AKB-6899 Ro24-7429 is a potent and orally active HIV-1 transactivator protein Tat antagonist. Ro24-7429 is also a runt-related transcription factor 1 (RUNX1) inhibitor. Ro24-7429 has anti-HIV, antifibrotic and anti-inflammatory effects. AKB-6899  Chemical Structure
  14. GC62433 AKI603 AKI603 is an inhibitor of Aurora kinase A (AurA), with an IC50 of 12.3 nM. AKI603 is developed to overcome resistance mediated by BCR-ABL-T315I mutation. AKI603 exhibits strong anti-proliferative activity in leukemic cells. AKI603  Chemical Structure
  15. GC17344 Alexidine dihydrochloride An alkyl bis(biguanide) antiseptic Alexidine dihydrochloride  Chemical Structure
  16. GC49393 all-trans-13,14-Dihydroretinol A metabolite of all-trans retinoic acid all-trans-13,14-Dihydroretinol  Chemical Structure
  17. GC35297 Alobresib A BET bromodomain inhibitor Alobresib  Chemical Structure
  18. GC67984 Alteminostat Alteminostat  Chemical Structure
  19. GC13198 AMG-900 A selective pan-Aurora kinase inhibitor AMG-900  Chemical Structure
  20. GC17275 AMI-1 A cell permeable inhibitor of PRMTs AMI-1  Chemical Structure
  21. GC39840 AMI-1 free acid AMI-1 free acid is a potent, cell-permeable and reversible inhibitor of protein arginine N-methyltransferases (PRMTs), with IC50s of 8.8 μM and 3.0 μM for human PRMT1 and yeast-Hmt1p, respectively. AMI-1 free acid exerts PRMTs inhibitory effects by blocking peptide-substrate binding. AMI-1 free acid  Chemical Structure
  22. GC17546 AMI5 Eosin Y (disodium) is a soluble acid red dye molecule. AMI5  Chemical Structure
  23. GC42785 Amifostine (hydrate) Amifostine (hydrate) (WR2721 trihydrate) is a broad-spectrum cytoprotective agent and a radioprotector. Amifostine (hydrate) selectively protects normal tissues from damage caused by radiation and chemotherapy. Amifostine (hydrate) is potent hypoxia-inducible factor-α1 (HIF-α1) and p53 inducer. Amifostine (hydrate) protects cells from damage by scavenging oxygen-derived free radicals. Amifostine (hydrate) reduces renal toxicity and has antiangiogenic action. Amifostine (hydrate)  Chemical Structure
  24. GC42790 Amodiaquine Amodiaquine is an aminoquinoline antimalarial compound. Amodiaquine  Chemical Structure
  25. GC60579 Amodiaquine dihydrochloride Amodiaquine dihydrochloride (Amodiaquin dihydrochloride), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor with a Ki of 18.6 nM. Amodiaquine dihydrochloride  Chemical Structure
  26. GC10905 Amodiaquine dihydrochloride dihydrate histamine N-methyl transferase inhibitor Amodiaquine dihydrochloride dihydrate  Chemical Structure
  27. GC67912 Amredobresib Amredobresib  Chemical Structure
  28. GC17284 Anacardic acid

    A histone acetyltransferase inhibitor

    Anacardic acid  Chemical Structure
  29. GC40674 APHA Compound 8 A class I and II HDAC inhibitor APHA Compound 8  Chemical Structure
  30. GC12961 Apicidin

    A cell-permeable HDAC inhibitor

    Apicidin  Chemical Structure
  31. GC14590 AR-42 (OSU-HDAC42)

    HDAC inhibitor,novel and potent

    AR-42 (OSU-HDAC42)  Chemical Structure
  32. GC32685 ARV-771 ARV-771 is a potent BET PROTAC based on E3 ligase von Hippel-Lindau with Kds of 34 nM, 4.7 nM, 8.3 nM, 7.6 nM, 9.6 nM, and 7.6 nM for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1), and BRD4(2), respectively. ARV-771  Chemical Structure
  33. GC19038 ARV-825 ARV-825 is a BRD4 Inhibitor based on PROTAC technology. ARV-825  Chemical Structure
  34. GC65918 AS-85 AS-85 is a potent ASH1L histone methyltransferase inhibitor (IC50=0.6 μM) with anti-leukemic activity. AS-85 strongly binds to the ASH1L SET domain, with the Kd value of 0.78μM. AS-85  Chemical Structure
  35. GC62615 AS-99 AS-99 is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50=0.79μM, Kd=0.89μM) with anti-leukemic activity. AS-99 blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo. AS-99  Chemical Structure
  36. GC62849 AS-99 TFA AS-99 TFA is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50=?0.79??M, Kd=?0.89??M) with anti-leukemic activity. AS-99 TFA blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo. AS-99 TFA  Chemical Structure
  37. GC17820 AS8351 histone demethylase inhibitor AS8351  Chemical Structure
  38. GC10638 AT9283 A broad spectrum kinase inhibitor AT9283  Chemical Structure
  39. GC50066 Atiprimod dihydrochloride JAK2 inhibitor Atiprimod dihydrochloride  Chemical Structure
  40. GC46892 ATRA-BA Hybrid A prodrug form of all-trans retinoic acid and butyric acid ATRA-BA Hybrid  Chemical Structure
  41. GN10627 Atractylenolide I Atractylenolide I  Chemical Structure
  42. GC64271 AU-15330 AU-15330 is a proteolysis-targeting chimera (PROTAC) degrader of the SWI/SNF ATPase subunits, SMARCA2 and SMARCA4. AU-15330 induces potent inhibition of tumour growth in xenograft models of prostate cancer and synergizes with the AR antagonist enzalutamide. AU-15330 induces disease remission in castration-resistant prostate cancer (CRPC) models without toxicity. AU-15330  Chemical Structure
  43. GC39699 Aurintricarboxylic acid Aurintricarboxylic acid is a nanomolar-potency, allosteric antagonist with selectivity towards αβ-methylene-ATP-sensitive P2X1Rs and P2X3Rs, with IC50s of 8.6 nM and 72.9 nM for rP2X1R and rP2X3R, respectively. Aurintricarboxylic acid  Chemical Structure
  44. GC13332 Aurora A Inhibitor I A potent and selective inhibitor of Aurora A kinase Aurora A Inhibitor I  Chemical Structure
  45. GC33379 Aurora B inhibitor 1 Aurora B inhibitor 1 is an Aurora B (Aurora-1) inhibitor extracted from patent WO2007059299A1, compound 1-3, has a Ki value of <0.010 uM. Aurora B inhibitor 1  Chemical Structure
  46. GC38441 Aurora Kinase Inhibitor 3 A potent inhibitor of Aurora A kinase Aurora Kinase Inhibitor 3  Chemical Structure
  47. GC40667 Aurora Kinase Inhibitor II Aurora Kinase Inhibitor II is a selective and ATP-competitive Aurora kinase inhibitor with IC50s of 310 nM and 240 nM for Aurora A and Aurora B, respectively. Aurora Kinase Inhibitor II  Chemical Structure
  48. GC15711 Aurora Kinase Inhibitor III Aurora Kinase Inhibitor III is a strong and selective Aurora A kinase inhibitor with an IC50 of 42 nM, and weakly inhibits EGFR with an IC50 of >10 μM. Aurora Kinase Inhibitor III  Chemical Structure
  49. GC67899 Aurora kinase inhibitor-8 Aurora kinase inhibitor-8  Chemical Structure
  50. GC13433 AZ 960 A JAK2 inhibitor AZ 960  Chemical Structure
  51. GC65899 AZ3391 AZ3391 is a potent inhibitor of PARP. AZ3391 is a quinoxaline derivative. PARP family of enzymes play an important role in a number of cellular processes, such as replication, recombination, chromatin remodeling, and DNA damage repair. AZ3391 has the potential for the research of diseases and conditions occurring in tissues in the central nervous system, such as the brain and spinal cord (extracted from patent WO2021260092A1, compound 23). AZ3391  Chemical Structure
  52. GC13744 AZ505 SMYD2 inhibitor,potent and selective AZ505  Chemical Structure
  53. GC13103 AZ505 ditrifluoroacetate SMYD2 inhibitor AZ505 ditrifluoroacetate  Chemical Structure
  54. GC64124 AZ506 AZ506 is a potent SMYD2 inhibitor with an IC50 of 17 nM. AZ506 inhibits SMYD2 methyltransferase activity in cells, leading to a decrease in the SMYD2-mediated methylation signal. AZ506  Chemical Structure
  55. GC16725 AZ6102 TNKS1/2 inhibitor AZ6102  Chemical Structure
  56. GC46900 AZ9482 A PARP inhibitor AZ9482  Chemical Structure
  57. GC48971 AZD 1152 (hydrochloride) A prodrug for a potent Aurora B inhibitor AZD 1152 (hydrochloride)  Chemical Structure
  58. GC13014 AZD 5153 orally available, bivalent inhibitor of the bromodomain and extraterminal (BET) protein BRD4. AZD 5153  Chemical Structure
  59. GC14709 AZD1152 AZD1152  Chemical Structure
  60. GC12660 AZD1208 A pan-Pim kinase inhibitor AZD1208  Chemical Structure
  61. GC35447 AZD1208 hydrochloride AZD1208 hydrochloride is an orally bioavailable, highly selective PIM kinases inhibitor. AZD1208 hydrochloride  Chemical Structure
  62. GC12504 AZD1480 A potent JAK2 inhibitor AZD1480  Chemical Structure
  63. GC17965 AZD2461 A PARP inhibitor AZD2461  Chemical Structure
  64. GC35448 AZD5153 6-Hydroxy-2-naphthoic acid AZD5153 6-Hydroxy-2-naphthoic acid is the 6-Hydroxy-2-naphthoic acid of AZD5153. AZD5153 is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor; disrupts BRD4 with an IC50 of 1.7 nM. AZD5153 6-Hydroxy-2-naphthoic acid  Chemical Structure
  65. GC62310 AZD5305 AZD5305 is a potent, selective and oral active PARP inhibitor. AZD5305 is potent and efficacious in animal xenografts and PDX models. AZD5305  Chemical Structure
  66. GC14955 Barasertib (AZD1152-HQPA) A selective Aurora kinase B inhibitor Barasertib (AZD1152-HQPA)  Chemical Structure
  67. GC11572 Bardoxolone methyl A synthetic triterpenoid with potent anticancer and antidiabetic activity Bardoxolone methyl  Chemical Structure
  68. GC14844 Baricitinib (LY3009104, INCB028050) A JAK1 and JAK2 inhibitor Baricitinib (LY3009104, INCB028050)  Chemical Structure
  69. GC13830 Baricitinib phosphate A JAK1 and JAK2 inhibitor Baricitinib phosphate  Chemical Structure
  70. GC12698 BAY 87-2243 A HIF-1 inhibitor,potent and selective BAY 87-2243  Chemical Structure
  71. GC18508 BAY-299 BAY-299 is a potent and selective inhibitor of the bromodomain and PHD finger-containing (BRPF) family protein BRD1 (IC50 = 6 nM), also known as BRPF2, and the second bromodomain of transcription initiation factor TFIID subunits 1 (TAF1; IC50 = 13 nM). BAY-299  Chemical Structure
  72. GC18159 BAY-598

    A potent and selective SMYD2 inhibitor

    BAY-598  Chemical Structure
  73. GC45389 BAY-6035   BAY-6035  Chemical Structure
  74. GC33104 BAY1238097 BAY1238097 is a potent and selective inhibitor of BET binding to histones and has strong anti-proliferative activity in different AML (acute myeloid leukemia) and MM (multiple myeloma) models through down-regulation of c-Myc levels and its downstream transcriptome (IC50 <100 nM). BAY1238097  Chemical Structure
  75. 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
  76. GC15175 BAZ2-ICR Selective BAZ2 bromodomain inhibitor BAZ2-ICR  Chemical Structure
  77. GC35480 BB-Cl-Amidine hydrochloride BB-Cl-Amidine hydrochloride is a peptidylarginine deminase (PAD) inhibitor. BB-Cl-Amidine hydrochloride  Chemical Structure
  78. 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
  79. GC18161 BCI-121

    A substrate-competitive SMYD3 inhibitor?

    BCI-121  Chemical Structure
  80. GC15962 Belinostat (PXD101)

    Belinostat is an effective HDAC inhibitor with an IC50 of 27 nM in HeLa cell extracts.

    Belinostat (PXD101)  Chemical Structure
  81. GC12844 Benzamide poly (ADP-ribose) synthetase inhibitor Benzamide  Chemical Structure
  82. GC30763 Benzenebutyric acid (4-Phenylbutyric acid) 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
  83. GC16299 BET bromodomain inhibitor Potent and selective inhibitor for BRD4 BET bromodomain inhibitor  Chemical Structure
  84. 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
  85. GC35505 BET-BAY 002 BET-BAY 002 is a potent BET inhibitor; shows efficacy in a multiple myeloma model. BET-BAY 002  Chemical Structure
  86. GC35506 BET-BAY 002 S enantiomer BET-BAY 002 S enantiomer  Chemical Structure
  87. 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
  88. 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
  89. GC32791 BETd-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
  90. GC12074 BG45 Novel HDAC3-selective inhibitor BG45  Chemical Structure
  91. GC14380 BGP-15 PARP inhibitor BGP-15  Chemical Structure
  92. GC12450 BI 2536 A potent inhibitor of Plk1 BI 2536  Chemical Structure
  93. GC50540 BI 9321 Nuclear receptor-binding SET domain (NSD) 3 antagonist; selectively binds PWWP1 domain BI 9321  Chemical Structure
  94. GC16726 BI-7273 BRD9 bromodomain inhibitor BI-7273  Chemical Structure
  95. GC17828 BI-847325 dual inhibitor of MEK and Aurora kinases BI-847325  Chemical Structure
  96. 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
  97. GC16817 BI-9564 BRD9/7 specific inhibitor BI-9564  Chemical Structure
  98. 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
  99. GC64789 Biotinylated-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
  100. GC25139 Biphenyl-4-sulfonyl 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
  101. GC48463 Bisubstrate Inhibitor 78 An inhibitor of NNMT Bisubstrate Inhibitor 78  Chemical Structure

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