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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. GC43889 I-CBP112 (hydrochloride) cAMP-responsive element-binding protein binding protein (CREBBP) and E1A-associated protein p300 (EP300) are transcriptional co-activators that modulate DNA replication, DNA repair, cell growth, transformation, and development. I-CBP112 (hydrochloride) Chemical Structure
  3. GC33042 IACS-9571 (ASIS-P040) IACS-9571 (ASIS-P040) is a potent and selective inhibitor of TRIM24 and BRPF1, with IC50 of 8 nM for TRIM24, and Kds of 31 nM and 14 nM for TRIM24 and BRPF1, respectively. IACS-9571 (ASIS-P040) Chemical Structure
  4. GC60925 IACS-9571 hydrochloride IACS-9571 (ASIS-P040) hydrochloride is a potent and selective inhibitor of TRIM24 and BRPF1, with an IC50 of 8 nM for TRIM24, and Kds of 31 nM and 14 nM for TRIM24 and BRPF1, respectively. IACS-9571 hydrochloride Chemical Structure
  5. GC34437 IACS-9571 Hydrochloride (ASIS-P040 Hydrochloride) IACS-9571 Hydrochloride (ASIS-P040 Hydrochloride) Chemical Structure
  6. GC48548 iBET-BD2 A BD2 bromodomain inhibitor iBET-BD2 Chemical Structure
  7. GC32948 IDF-11774 A novel HIF-1 inhibitor IDF-11774 Chemical Structure
  8. GC64108 Ifidancitinib Ifidancitinib (ATI-50002) is a potent and selective inhibitor of JAK kinases 1/3. Ifidancitinib Chemical Structure
  9. GC47450 IL-4 Inhibitor IL-4 Inhibitor (compound 52) is an IL-4 inhibitor, with an EC50 of 1.81 μM. IL-4 Inhibitor Chemical Structure
  10. GC32809 Ilginatinib (NS-018) Ilginatinib (NS-018) (NS-018) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM). Ilginatinib (NS-018) Chemical Structure
  11. GC33037 Ilginatinib hydrochloride (NS-018 hydrochloride) Ilginatinib hydrochloride (NS-018 hydrochloride) (NS-018 hydrochloride) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM). Ilginatinib hydrochloride (NS-018 hydrochloride) Chemical Structure
  12. GC33018 Ilginatinib maleate (NS-018 (maleate)) Ilginatinib maleate (NS-018 (maleate)) (NS-018 maleate) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM). Ilginatinib maleate (NS-018 (maleate)) Chemical Structure
  13. GC34159 Ilorasertib (ABT-348) Ilorasertib (ABT-348) (ABT-348) is a potent, orally active and ATP-competitive aurora inhibitor with IC50s of116, 5, 1 nM for aurora A, aurora B, aurora C, respectively. Ilorasertib (ABT-348) also is a potent VEGF, PDGF inhibitor. Ilorasertib (ABT-348) has the potential for the research of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS). Ilorasertib (ABT-348) Chemical Structure
  14. GC38519 Ilorasertib hydrochloride Ilorasertib (ABT-348) hydrochloride is a potent, orally active and ATP-competitive aurora inhibitor with IC50s of116, 5, 1 nM for aurora A, aurora B, aurora C, respectively. Ilorasertib hydrochloride also is a potent VEGF, PDGF inhibitor. Ilorasertib hydrochloride has the potential for the research of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS). Ilorasertib hydrochloride Chemical Structure
  15. GC63309 Ilunocitinib Ilunocitinib (compound 27) is a JAK inhibitor (extracted from patent WO2009114512A1). Ilunocitinib Chemical Structure
  16. GC14755 Inauhzin SIRT1 inhibitor Inauhzin Chemical Structure
  17. GC16117 INCA-6 A cell-permeant inhibitor of NFAT signaling INCA-6 Chemical Structure
  18. GC19200 INCB-057643 INCB-057643 is a novel, orally bioavailable BET inhibitor. INCB-057643 Chemical Structure
  19. GC33026 INCB054329 INCB054329 is a potent BET inhibitor. INCB054329 Chemical Structure
  20. GC30644 INCB054329 Racemate INCB054329 Racemate is a BET protein inhibitor. INCB054329 Racemate Chemical Structure
  21. GC15353 Iniparib (BSI-201) A PARP1 inhibitor Iniparib (BSI-201) Chemical Structure
  22. GC12496 INO-1001 A PARP inhibitor INO-1001 Chemical Structure
  23. GC38385 INO-1001 INO-1001 Chemical Structure
  24. GC17754 IOX 1 histone demethylase JMJD inhibitor IOX 1 Chemical Structure
  25. GC13018 IOX2(Glycine) A selective PHD2 inhibitor IOX2(Glycine) Chemical Structure
  26. GC12255 IOX4 PHD2 inhibitor IOX4 Chemical Structure
  27. GC50721 iP300w iP300w Chemical Structure
  28. GC10727 Ischemin sodium salt CBP bromodomain inhibitor Ischemin sodium salt Chemical Structure
  29. GC19204 Itacitinib Itacitinib is a potent and selective inhibitor of JAK1, with >20-fold selectivity for JAK1 over JAK2 and >100-fold over JAK3 and TYK2; Itacitinib is used in the research of myelofibrosis. Itacitinib Chemical Structure
  30. GC36351 Itacitinib adipate Itacitinib adipate is an orally bioavailable and selective JAK1 inhibitor which has been tested for efficacy and safety in a phase II trial in myelofibrosis. Itacitinib adipate Chemical Structure
  31. GC63416 Itacnosertib Itacnosertib (TP-0184) is both inhibitor to JAK2, ACVR1 (ALK2) and ALK5 as described in WO2014151871. Itacnosertib Chemical Structure
  32. GC17836 ITF2357 (Givinostat)

    HDAC inhibitor with anti-inflammatory and antineoplastic activities

     ITF2357 (Givinostat) Chemical Structure
  33. GC14597 ITSA-1 (ITSA1) ITSA-1 (ITSA1) is an activator of histone deacetylase (HDAC), and counteract trichostatin A (TSA)-induced cell cycle arrest, histone acetylation, and transcriptional activation. ITSA-1 (ITSA1) Chemical Structure
  34. GC63703 Ivaltinostat formic Ivaltinostat (CG-200745) formic is an orally active, potent pan-HDAC inhibitor which has the hydroxamic acid moiety to bind zinc at the bottom of catalytic pocket. Ivaltinostat formic Chemical Structure
  35. GC15836 IWP 12 Potent inhibitor of Porcupine (PORCN) IWP 12 Chemical Structure
  36. GC62313 Izencitinib Izencitinib (TD-1473) is an orally active, non-selective and gut-restricted JAK inhibitor. Izencitinib Chemical Structure
  37. GC63828 Izilendustat Izilendustat is a potent inhibitor of prolyl hydroxylase which can stabilize hypoxia inducible factor- 1 alpha (HIF- lα) and hypoxia inducible factor-2 (HIF-2). Izilendustat Chemical Structure
  38. GC34629 J22352 J22352 is a PROTAC (proteolysis-targeting chimeras)-like and highly selective HDAC6 inhibitor with an IC50 value of 4.7 nM. J22352 promotes HDAC6 degradation and induces anticancer effects by inhibiting autophagy and eliciting the antitumor immune response in glioblastoma cancers, and leading to the restoration of host antitumor activity by reducing the immunosuppressive activity of PD-L1. J22352 Chemical Structure
  39. GC31866 JAK inhibitor 1 JAK inhibitor 1 is an inhibitor of JAK extracted from patent US20170121327A1, compound example 283. JAK inhibitor 1 Chemical Structure
  40. GC31999 JAK-IN-1 JAK-IN-1 is a JAK1/2/3 inhibitor with IC50s of 0.26, 0.8 and 3.2 nM, respectively. JAK-IN-1 Chemical Structure
  41. GC36366 JAK-IN-10 JAK-IN-10 is a JAK inhibitor. JAK-IN-10 Chemical Structure
  42. GC63448 JAK-IN-14 JAK-IN-14 is a potent and selective JAK1 inhibitor, with an IC50 of <5 μM. JAK-IN-14 Chemical Structure
  43. GC68000 JAK-IN-23 JAK-IN-23 Chemical Structure
  44. GC65453 JAK-IN-3 JAK-IN-3 (compound 22) is a potent JAK inhibitor, with IC50 values of 3 nM, 5 nM, 34 nM and 70 nM for JAK3, JAK1, TYK2 and JAK2, respectively. JAK-IN-3 Chemical Structure
  45. GC64959 JAK/HDAC-IN-1 JAK/HDAC-IN-1 is a potent JAK2/HDAC dual inhibitor, exhibits antiproliferative and proapoptotic activities in several hematological cell lines. JAK/HDAC-IN-1 shows IC50s of 4 and 2 nM for JAK2 and HDAC, respectively. JAK/HDAC-IN-1 Chemical Structure
  46. GC33036 JAK1-IN-3 JAK1-IN-3 (AZD4205) is a selective JAK1 inhibitor, with an IC50 of 73 nM, weakly inhibits JAK2 (IC50>14.7 μM), and shows little inhibition on JAK3 (IC50>30 μM). JAK1-IN-3 Chemical Structure
  47. GC33258 JAK1-IN-4 JAK1-IN-4 is a potent and selective JAK1 inhibitor, with IC50s of 85 nM, 12.8 μM and >30 μM for JAK1, JAK2, and JAK3, respectively. JAK1-IN-4 inhibits STAT3 phosphorylation in NCI-H 1975 cells (IC50, 227 nM). JAK1-IN-4 Chemical Structure
  48. GC36363 JAK1-IN-7 JAK1-IN-7 (JAK1-IN-7) is a Janus-associated kinase 1 (JAK1) inhibitor extracted from patent WO2018134213A1, Example 63, has an anti-inflammatory effect. JAK1-IN-7 Chemical Structure
  49. GC63029 JAK1-IN-8 JAK1-IN-8, a potent JAK1 inhibitor (IC50<500 nM), compound 28, extracted from patent WO2016119700A1. JAK1-IN-8 Chemical Structure
  50. GC13826 JAK2 Inhibitor V, Z3 A selective inhibitor of the autophosphorylation of wild type and V617F mutant forms of JAK JAK2 Inhibitor V, Z3 Chemical Structure
  51. GC36364 JAK2-IN-4 JAK2-IN-4 (compound 16h) is a selective JAK2/JAK3 inhibitor, with IC50 values of 0.7 nM and 23.2 nM for JAK2 and JAK3, respectively. JAK2-IN-4 Chemical Structure
  52. GC65405 JAK2-IN-6 JAK2-IN-6, a multiple-substituted aminothiazole derivative, is a potent and selective JAK2 inhibitor with an IC50 of 22.86 μg/mL. JAK2-IN-6 shows no activity against JAK1 and JAK3. JAK2-IN-6 has anti-proliferative effect against cancer cells. JAK2-IN-6 Chemical Structure
  53. GC62500 JAK2-IN-7 JAK2-IN-7 is a selective JAK2 inhibitor with IC50s of 3, 11.7, and 41 nM for JAK2, SET-2, and Ba/F3V617F cells, respectively. JAK2-IN-7 possesses >14-fold selectivity over JAK1, JAK3, FLT3. JAK2-IN-7 stimulates cell cycle arrest in the G0/G1 phase and induces tumor cellapoptosis. Antitumor activities. JAK2-IN-7 Chemical Structure
  54. GC62665 JAK2/FLT3-IN-1 TFA JAK2/FLT3-IN-1 (TFA) is a potent and orally active dual JAK2/FLT3 inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. JAK2/FLT3-IN-1 (TFA) has anti-cancer activity. JAK2/FLT3-IN-1 TFA Chemical Structure
  55. GC36365 JAK3 covalent inhibitor-1 JAK3 covalent inhibitor-1 is a potent and selective janus kinase 3 (JAK3) covalent inhibitor with an IC50 of 11 nM and shows 246-fold selectivity vs other JAKs. JAK3 covalent inhibitor-1 Chemical Structure
  56. GC33046 JAK3-IN-1 JAK3-IN-1 is a potent, selective and orally active JAK3 inhibitor with an IC50 of 4.8 nM. JAK3-IN-1 shows over 180-fold more selective for JAK3 than JAK1 (IC50 of 896 nM) and JAK2 (IC50 of 1050 nM). JAK3-IN-1 Chemical Structure
  57. GC31902 JAK3-IN-6 JAK3-IN-6 is a potent, selective irreversible Janus Associated Kinase 3 (JAK3) inhibitor, with an IC50 of 0.15 nM. JAK3-IN-6 Chemical Structure
  58. GC33382 JAK3-IN-7 JAK3-IN-7 is a potent and selective JAK3 inhibitor extracted from patent WO2011013785A1, has an IC50 of <0.01 μM. JAK3-IN-7 Chemical Structure
  59. GC14671 JANEX-1 A selective JAK3 inhibitor JANEX-1 Chemical Structure
  60. GC14686 JFD00244 inhibitor of SIRT2 JFD00244 Chemical Structure
  61. GC13062 JGB1741 SIRT1 inhibitor JGB1741 Chemical Structure
  62. GC15603 JIB-04 Jumonji histone demethylase inihibitor JIB-04 Chemical Structure
  63. GC15476 JNJ-26481585 A pan-HDAC inhibitor JNJ-26481585 Chemical Structure
  64. GC15379 JNJ-42041935 Hypoxia-inducible factor (HIF) prolyl hydroxylase (PHD) inhibitor JNJ-42041935 Chemical Structure
  65. GC19465 JNJ-64619178 JNJ-64619178 is a PRMT5 inhibitor JNJ-64619178 Chemical Structure
  66. GC12612 JNJ-7706621 A dual inhibitor of CDKs and Aurora kinases JNJ-7706621 Chemical Structure
  67. GC19210 JQ-1 carboxylic acid JQ-1 carboxylic acid is a highly potent, selective and cell-permeable BRD4 inhibitor with IC50s of 77 nM and 33 nM for BRD4(1) and BRD4(2), respectively. JQ-1 carboxylic acid Chemical Structure
  68. GC19211 JQEZ5 JQEZ5 is a novel and potent EZH2 inhibitor. JQEZ5 Chemical Structure
  69. GC64841 JQKD82 trihydrochloride JQKD82 (JADA82) trihydrochloride is a cell-permeable and selective KDM5 inhibitor. JQKD82 trihydrochloride increases H3K4me3 and can be used for the research of multiple myeloma. JQKD82 trihydrochloride Chemical Structure
  70. GC34195 K-756 K-756 is a direct and selective tankyrase (TNKS) inhibitor, which inhibits the ADP-ribosylation activity of TNKS1 and TNKS2 with IC50s of 31 and 36 nM, respectively. K-756 Chemical Structure
  71. GC45489 K-Biotin-W-Histone H2B (108-125) (trifluoroacetate salt)   K-Biotin-W-Histone H2B (108-125) (trifluoroacetate salt) Chemical Structure
  72. GC62430 KA2507 KA2507 is a potent, orally active and selective HDAC6 inhibitor, with an IC50 of 2.5 nM. KA2507 shows antitumor activities and immune modulatory effects in preclinical models. KA2507 Chemical Structure
  73. GC62374 KA2507 monohydrochloride KA2507 hydrochloride is a potent and highly selective inhibitor of HDAC6 (IC50=2.5 nM) with no significant toxicities. KA2507 monohydrochloride Chemical Structure
  74. GC13141 KC7F2 An inhibitor of HIF-1a protein synthesis KC7F2 Chemical Structure
  75. GC13435 KD 5170 An inhibitor of class I and II HDACs KD 5170 Chemical Structure
  76. GC36388 KDM2A/7A-IN-1 KDM2A/7A-IN-1 is a first-in-class, selective and cell-permeable inhibitor of histone lysine demethylases KDM2A/7A, with an IC50 of 0.16?μM for KDM2A, exhibits 75 fold selevtivity over other JmjC lysine demethylases, and is inactive on methyl transferases, and histone acetyl transferases. KDM2A/7A-IN-1 Chemical Structure
  77. GC69327 KDM2B-IN-4

    KDM2B-IN-4 is a histone demethylase KDM2B inhibitor. It can be used for cancer research. For more information, please refer to compound 182b in patent document WO2016112284A1.

     KDM2B-IN-4 Chemical Structure
  78. GC36389 KDM4-IN-2 KDM4-IN-2 (Compound 19a) is a potent and selective KDM4/KDM5 dual inhibitor with Kis of 4 and 7?nM for KDM4A and KDM5B, respectively. KDM4-IN-2 Chemical Structure
  79. GC31887 KDM4D-IN-1 KDM4D-IN-1 is a new histone lysine demethylase 4D (KDM4D) inhibitor with an IC50 value of 0.41±0.03 μM. KDM4D-IN-1 Chemical Structure
  80. GC32790 KDM5-IN-1 KDM5-IN-1 is a potent, selective and orally bioavailable KDM5 inhibitor with an IC50 of 15.1 nM. KDM5-IN-1 Chemical Structure
  81. GC32842 KDM5A-IN-1 KDM5A-IN-1 is a potent, orally bioavailable pan-histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 45 nM, 56 nM and 55 nM for KDM5A, KDM5B and KDM5C, respectively, and with an EC50 value of 960 nM for PC9 H3K4Me3. KDM5A-IN-1 is significantly less potent against other KDM5B enzymes (1A, 2B, 3B, 4C, 6A, 7B). KDM5A-IN-1 Chemical Structure
  82. GC38709 KDOAM-25 citrate KDOAM-25 citrate is a potent and highly selective histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 71 nM, 19 nM, 69 nM, 69 nM for KDM5A, KDM5B, KDM5C, KDM5D, respectively. KDOAM-25 citrate increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells. KDOAM-25 citrate Chemical Structure
  83. GC31654 KG-501 (Naphthol AS-E phosphate) KG-501 (Naphthol AS-E phosphate) is a CREB inhibitor, with an IC50 of 6.89 μM. KG-501 (Naphthol AS-E phosphate) Chemical Structure
  84. GC65907 KSQ-4279 KSQ-4279 (USP1-IN-1, Formula I) is a USP1 and PARP inhibitor (extracted from patent WO2021163530). KSQ-4279 Chemical Structure
  85. GC25552 KT-531 KT-531 (KT531) is a potent, selective HDAC6 inhibitor with IC50 of 8.5 nM, displays 39-fold selectivity over other HDAC isoforms. KT-531 Chemical Structure
  86. GC14592 KW 2449 A multi-kinase inhibitor KW 2449 Chemical Structure
  87. GC50395 L Moses dihydrochloride High affinity and selective PCAF bromodomain inhibitor L Moses dihydrochloride Chemical Structure
  88. GC33183 L-45 (L-Moses) L-45 (L-Moses) (L-45) is the first potent, selective, and cell-active p300/CBP-associated factor (PCAF) bromodomain (Brd) inhibitor with a Kd of 126 nM. L-45 (L-Moses) Chemical Structure
  89. GC34377 L-45 dihydrochloride (L-Moses dihydrochloride) L-45 dihydrochloride (L-Moses dihydrochloride) Chemical Structure
  90. GC47579 L-Pyrohomoglutamic Acid An amino acid building block L-Pyrohomoglutamic Acid Chemical Structure
  91. GC15731 L002 p300 inhibitor L002 Chemical Structure
  92. GC65289 Lademirsen

    Lademirsen (SAR339375; RG-012) is a single stranded, chemically modified oligonucleotide that binds to and inhibits the function of miR-21.

     Lademirsen Chemical Structure
  93. GC15114 LAQ824 (NVP-LAQ824,Dacinostat) A hydroxamate-based HDAC inhibitor LAQ824 (NVP-LAQ824,Dacinostat) Chemical Structure
  94. GC12189 LB-100 protein phosphatase 2A(PP2A)inhibitor LB-100 Chemical Structure
  95. GC14857 LFM-A13 BTK-specific tyrosine kinase inhibitor LFM-A13 Chemical Structure
  96. GC14362 Lin28 1632 Lin28 1632 (compound 1632) is a potent antagonist of Lin28/pre-let-7 interaction. Lin28 1632 Chemical Structure
  97. GC36464 LIN28 inhibitor LI71 LIN28 inhibitor LI71 is a potent and cell-permeable LIN28 inhibitor, which abolishes LIN28-mediated oligouridylation with an IC50 of 7 uM. LIN28 inhibitor LI71 directly binds the cold shock domain (CSD) to suppress LIN28’s activity against let-7 in leukemia cells and embryonic stem cells. LIN28 inhibitor LI71 Chemical Structure
  98. GC30501 Lin28-let-7a antagonist 1 Lin28-let-7a antagonist 1 shows a clear antagonistic effect against the Lin28-let-7a interaction with an IC50 of 4.03 μM for Lin28A-let-7a-1 interaction. Lin28-let-7a antagonist 1 Chemical Structure
  99. GC13154 LKB1(AAK1 dual inhibitor) LKB1(AAK1 dual inhibitor) Chemical Structure
  100. GC33184 LLY-283 A PRMT5 inhibitor LLY-283 Chemical Structure
  101. GC25580 LLY-284 LLY-284 is the diastereomer of LLY-283, which is a potent and selective SAM-competitive chemical probe for PRMT5. LLY-284 is much less active than LLY-283 and can be used as a negative control for LLY-283. LLY-284 Chemical Structure

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