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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. GC35227 ACBI1 ACBI1 is a potent and cooperative SMARCA2, SMARCA4 and PBRM1 degrader with DC50s of 6, 11 and 32 nM, respectively. ACBI1 is a PROTAC degrader. ACBI1 shows anti-proliferative activity. ACBI1 induces apoptosis. ACBI1 Chemical Structure
  3. GC73359 ACBI2 ACBI2 is a highly potent and orally active VHL PROTAC SMARCA2 degrader (EC50: 7 nM), which selectively degrades SMARCA2 with a DC50 value of 1 nM in RKO cells. ACBI2 Chemical Structure
  4. GC12917 Acetaminophen

    4-Acetamidophenol, APAP, 4'-Hydroxyacetanilide, NSC 3991, NSC 109028, Paracetamol

    A COX inhibitor

     Acetaminophen Chemical Structure
  5. GC64137 Acetaminophen-d3 Acetaminophen-d3 Chemical Structure
  6. GC35230 Acetylarenobufagin Acetylarenobufagin is a steroidal hypoxia inducible factor-1 (HIF-I) modulator. Acetylarenobufagin Chemical Structure
  7. GC32083 Acriflavine Acriflavine is a fluorescent dye for labeling high molecular weight RNA. Acriflavine Chemical Structure
  8. GC62354 Acriflavine hydrochloride Acriflavine hydrochloride (Acriflavinium chloride hydrochloride) is a fluorescent acridine dye that can be used to label nucleic acid. Acriflavine hydrochloride Chemical Structure
  9. GC34458 ACY-1083

    ACY-1083 is a selective and brain-penetrating HDAC6 inhibitor with an IC50 of 3 nM and is 260-fold more selective for HDAC6 than all other classes of HDAC isoforms. ACY-1083 effectively reverses chemotherapy-induced peripheral neuropathy.

     ACY-1083 Chemical Structure
  10. GC10417 ACY-241

    Citarinostat

     ACY-241 (ACY241) is a second generation potent, orally active and high-selective HDAC6 inhibitor with an IC50 of 2.6 nM (IC50s of 35 nM, 45 nM, 46 nM and 137 nM for HDAC1, HDAC2, HDAC3 and HDAC8, respectively). ACY-241 has anticancer effects. ACY-241 Chemical Structure
  11. GC19020 ACY-738 ACY-738 is a potent, selective and orally-bioavailable HDAC6 inhibitor, with an IC50s of 1.7 nM; ACY-738 also inhibits HDAC1, HDAC2, and HDAC3, with IC50s of 94, 128, and 218 nM. ACY-738 Chemical Structure
  12. GC30782 ACY-775 An HDAC6 inhibitor ACY-775 Chemical Structure
  13. GC30526 ACY-957 ACY-957 is an orally active and selective inhibitor of HDAC1 and HDAC2, with IC50s of 7 nM, 18 nM, and 1300 nM against HDAC1/2/3, respectively, and shows no inhibition on HDAC4/5/6/7/8/9. ACY-957 Chemical Structure
  14. GC12487 Adaptaquin

    HIF prolyl hydroxylase inhibitor

     HIF-prolyl hydroxylase-2 (PHD2) inhibitor Adaptaquin Chemical Structure
  15. 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
  16. 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
  17. 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
  18. GC48775 AES-350 An inhibitor of class I and class IIb HDACs AES-350 Chemical Structure
  19. 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
  20. GC33416 AFP464

    NSC710464 free base

     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
  21. GC73864 AFP464 dihydrochloride

    NSC710464 dihydrochloride

     AFP464 (didrochloride) (NSC710464 (didrochloride)) is the drochloride form of AFP464 and is a potent HIF-1α inhibitor with an IC50 value of 0.25 μM. AFP464 dihydrochloride Chemical Structure
  22. GC50003 AG 490 EGFR-kinase inhibitor. Also JAK2, JAK3 inhibitor AG 490 Chemical Structure
  23. GC16318 AG-14361 A PARP1 inhibitor AG-14361 Chemical Structure
  24. GC17881 AGK 2 AGK2 is a selective SIRT2 inhibitor, with an IC50 of 3.5 µM. AGK2 inhibits SIRT1 and SIRT3 with IC50 of 30 and 91 µM, respectively. AGK 2 Chemical Structure
  25. GC15931 AGK7

    SIRT2 Inhibitor (Inactive Control)

     cell-permeable, selective inhibitor of SIRT2 AGK7 Chemical Structure
  26. GN10413 Agrimol B Agrimol B Chemical Structure
  27. GC10676 AK-7

    selective and brain-permeable SIRT2 inhibitor

     AK-7 Chemical Structure
  28. 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
  29. 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
  30. GC17344 Alexidine dihydrochloride An alkyl bis(biguanide) antiseptic Alexidine dihydrochloride Chemical Structure
  31. GC73642 ALK-IN-26 ALK-IN-26 is an ALK inhibitor with IC50 value of 7.0 μM for ALK tyrosine kinase. ALK-IN-26 Chemical Structure
  32. GC40094 all-trans Retinoic Acid-d5

    atRA-d5, RA-d5, Vitamin A Acid-d5

     all-trans Retinoic acid-d5 is intended for use as an internal standard for the quantification of all-trans retinoic acid by GC- or LC-MS. all-trans Retinoic Acid-d5 Chemical Structure
  33. GC49393 all-trans-13,14-Dihydroretinol A metabolite of all-trans retinoic acid all-trans-13,14-Dihydroretinol Chemical Structure
  34. GC35297 Alobresib

    GS-5829

     A BET bromodomain inhibitor Alobresib Chemical Structure
  35. GC67984 Alteminostat

    CKD-581

     Alteminostat Chemical Structure
  36. GC70420 Amelparib Amelparib is a potent, orally active, and water-soluble inhibitor of PARP-1. Amelparib Chemical Structure
  37. GC70421 Amelparib hydrochloride Amelparib (JPI-289) hydrochloride is a potent, orally active, and water-soluble inhibitor of PARP-1. Amelparib hydrochloride Chemical Structure
  38. GC13198 AMG-900 A selective pan-Aurora kinase inhibitor AMG-900 Chemical Structure
  39. GC17275 AMI-1 A cell permeable inhibitor of PRMTs AMI-1 Chemical Structure
  40. GC42784 AMI-1 (sodium salt)

    Arginine N-Methyltransferase Inhibitor-1

     Protein arginine methyltransferases (PRMTs) post-translationally modify proteins, including histones, and in this way regulate gene expression, signal transduction, and protein-protein interactions. AMI-1 (sodium salt) Chemical Structure
  41. 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
  42. GC17546 AMI5 Eosin Y (disodium) is a soluble acid red dye molecule. AMI5 Chemical Structure
  43. GC42785 Amifostine (hydrate)

    Ethyol, WR 2721

     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
  44. GC42790 Amodiaquine

    Camoquine, Flavoquine, NSC 13453, SN 10751

     Amodiaquine is an aminoquinoline antimalarial compound. Amodiaquine Chemical Structure
  45. 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
  46. GC10905 Amodiaquine dihydrochloride dihydrate histamine N-methyl transferase inhibitor Amodiaquine dihydrochloride dihydrate Chemical Structure
  47. GC67912 Amredobresib Amredobresib Chemical Structure
  48. GC17284 Anacardic acid

    Hydroginkgolic acid; Ginkgolic Acid C15

    A histone acetyltransferase inhibitor

     Anacardic acid Chemical Structure
  49. GC73278 Anticancer agent 126 Anticancer agent 126 (compound 12) is a WDR5 inhibitor with anticancer effects. Anticancer agent 126 Chemical Structure
  50. GC40674 APHA Compound 8

    MC 1353

     A class I and II HDAC inhibitor APHA Compound 8 Chemical Structure
  51. GC12961 Apicidin

    OSI 2040

    A cell-permeable HDAC inhibitor

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

    HDAC inhibitor,novel and potent

     AR-42 (OSU-HDAC42) Chemical Structure
  53. 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
  54. GC19038 ARV-825 ARV-825 is a BRD4 Inhibitor based on PROTAC technology. ARV-825 Chemical Structure
  55. 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
  56. 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
  57. 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
  58. GC17820 AS8351

    NCI 51355, NSC 51355

     histone demethylase inhibitor AS8351 Chemical Structure
  59. GC10638 AT9283 A broad spectrum kinase inhibitor AT9283 Chemical Structure
  60. GC50066 Atiprimod dihydrochloride JAK2 inhibitor Atiprimod dihydrochloride Chemical Structure
  61. GC46892 ATRA-BA Hybrid A prodrug form of all-trans retinoic acid and butyric acid ATRA-BA Hybrid Chemical Structure
  62. GN10627 Atractylenolide I Atractylenolide I Chemical Structure
  63. 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
  64. GC74035 AU-24118 AU-24118 is orally bioavailable proteolysis targeting chimera (PROTAC) degrader of mSWI/SNF ATPases (SMARCA2 and SMARCA4) and PBRM1. AU-24118 Chemical Structure
  65. 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
  66. GC72964 Aurkin A Aurkin A is an allosteric inhibitor for the interaction between Aurora A Kinase (also known also Aurka) and TPX2, through targeting the TPX2 binding sites with Kd of 3.77 μM. Aurkin A Chemical Structure
  67. GC13332 Aurora A Inhibitor I A potent and selective inhibitor of Aurora A kinase Aurora A Inhibitor I Chemical Structure
  68. 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
  69. GC38441 Aurora Kinase Inhibitor 3 A potent inhibitor of Aurora A kinase Aurora Kinase Inhibitor 3 Chemical Structure
  70. GC40667 Aurora Kinase Inhibitor II

    4-(4-Benzamidoanilino)-6,7-dimethoxyquinazoline

     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
  71. 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
  72. GC67899 Aurora kinase inhibitor-8 Aurora kinase inhibitor-8 Chemical Structure
  73. GC73375 Aurora Kinases-IN-3 Aurora Kinases-IN-3 (Compound 15a) is an orally active AURKB inhibitor that elicits an AURKB-suppressive activity by disrupting the mitotic localization of AURKB. Aurora Kinases-IN-3 Chemical Structure
  74. GC13433 AZ 960 A JAK2 inhibitor AZ 960 Chemical Structure
  75. GC68711 AZ13824374

    AZ13824374 is an efficient selective inhibitor of ATAD2, which has anti-proliferative activity against breast cancer. In ATAD2 FRET and ATAD2 NanoBRET assays, AZ13824374 showed pIC50 values of 8.2 and 6.2 for ATAD2, respectively.

     AZ13824374 Chemical Structure
  76. 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
  77. GC13744 AZ505 SMYD2 inhibitor,potent and selective AZ505 Chemical Structure
  78. GC13103 AZ505 ditrifluoroacetate SMYD2 inhibitor AZ505 ditrifluoroacetate Chemical Structure
  79. 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
  80. GC16725 AZ6102 TNKS1/2 inhibitor AZ6102 Chemical Structure
  81. GC46900 AZ9482 A PARP inhibitor AZ9482 Chemical Structure
  82. GC48971 AZD 1152 (hydrochloride)

    Barasertib

     A prodrug for a potent Aurora B inhibitor AZD 1152 (hydrochloride) Chemical Structure
  83. GC13014 AZD 5153 orally available, bivalent inhibitor of the bromodomain and extraterminal (BET) protein BRD4. AZD 5153 Chemical Structure
  84. GC73919 AZD-9574-acid AZD-9574-acid (70D), a PPAR-1 inhibitor, can be used for the synthesis of PROTAC (CAS 2923686-70-6). AZD-9574-acid Chemical Structure
  85. GC14709 AZD1152 AZD1152 Chemical Structure
  86. GC12660 AZD1208

    AZD 1208;AZD-1208

     AZD1208 is a potent, highly selective, and orally available Pim kinase inhibitor, with IC50 values of 0.4, 5, and 1.9nM for PIM1, PIM2, and PIM3, respectively. AZD1208 Chemical Structure
  87. GC35447 AZD1208 hydrochloride AZD1208 hydrochloride is an orally bioavailable, highly selective PIM kinases inhibitor. AZD1208 hydrochloride Chemical Structure
  88. GC12504 AZD1480 A potent JAK2 inhibitor AZD1480 Chemical Structure
  89. GC17965 AZD2461 A PARP inhibitor AZD2461 Chemical Structure
  90. 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
  91. GC62310 AZD5305

    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
  92. GC14955 Barasertib (AZD1152-HQPA)

    BarasertibHQPA

     A selective Aurora kinase B inhibitor Barasertib (AZD1152-HQPA) Chemical Structure
  93. GC11572 Bardoxolone methyl

    Bardoxolone methyl, NSC 713200, RTA 402, TP155

     A synthetic triterpenoid with potent anticancer and antidiabetic activity Bardoxolone methyl Chemical Structure
  94. GC14844 Baricitinib (LY3009104, INCB028050)

    INCB 028050, LY3009104

     A JAK1 and JAK2 inhibitor Baricitinib (LY3009104, INCB028050) Chemical Structure
  95. GC13830 Baricitinib phosphate A JAK1 and JAK2 inhibitor Baricitinib phosphate Chemical Structure
  96. GC73130 Basroparib

    STP1002

     Basroparib is a potent poly (ADP-ribose) polymerase (PARP) inhibitor, with antineoplastic activity. Basroparib Chemical Structure
  97. GC12698 BAY 87-2243 A HIF-1 inhibitor,potent and selective BAY 87-2243 Chemical Structure
  98. 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
  99. GC18159 BAY-598

    A potent and selective SMYD2 inhibitor

     BAY-598 Chemical Structure
  100. GC45389 BAY-6035   BAY-6035 Chemical Structure
  101. 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

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