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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. GC12171 BIX 01294 An inhibitor of G9a histone methyltransferase BIX 01294  Chemical Structure
  3. 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
  4. GC33301 BIX-01338 hydrate (BIX01338 hydrate) BIX-01338 hydrate (BIX01338 hydrate) is a histone lysine methyltransferase inhibitor. BIX-01338 hydrate (BIX01338 hydrate)  Chemical Structure
  5. 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
  6. GC16114 Bizine LSD1 inhibitor Bizine  Chemical Structure
  7. GC12822 BML-210(CAY10433) BML-210(CAY10433) is a novel HDAC inhibitor, and its mechanism of action has not been characterized. BML-210(CAY10433)  Chemical Structure
  8. 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
  9. GC15932 BMN 673 A PARP inhibitor BMN 673  Chemical Structure
  10. GC10920 BMN-673 8R,9S BMN-673 8R,9S  Chemical Structure
  11. GC50633 BMS 986094 Prodrug of HCV RNA polymerase inhibitor 2'-C-methyl guanosine triphosphate; potent HCV replication inhibitor BMS 986094  Chemical Structure
  12. GC32028 BMS-066 BMS-066 is an IKKβ/Tyk2 pseudokinase inhibitor, with IC50s of 9 nM and 72 nM, respectively. BMS-066  Chemical Structure
  13. 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
  14. GC12454 BMS-911543 A potent, selective JAK2 inhibitor BMS-911543  Chemical Structure
  15. GC32812 BMS-986158 A BET bromodomain inhibitor BMS-986158  Chemical Structure
  16. 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
  17. 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
  18. GC46935 Bobcat 339 A TET1 and TET2 inhibitor Bobcat 339  Chemical Structure
  19. 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
  20. GC11641 Boc-Lys(Ac)-AMC

    GPCR G2A/GPR132 agonist

    Boc-Lys(Ac)-AMC  Chemical Structure
  21. GC64865 Bomedemstat 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
  22. GC67921 Bomedemstat ditosylate Bomedemstat ditosylate  Chemical Structure
  23. GC65879 Bomedemstat 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
  24. GC48620 BPKDi A PKD inhibitor BPKDi  Chemical Structure
  25. GC64538 BPTF-IN-BZ1 BPTF-IN-BZ1, a BPTF inhibitor, possesses a high potency (Kd = 6.3 nM). BPTF-IN-BZ1  Chemical Structure
  26. GC15974 bpV(HOpic) (potassium salt, technical grade) 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
  27. 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
  28. 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
  29. 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
  30. 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
  31. 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
  32. GC50322 BRD 9757 Potent and selective HDAC6 inhibitor BRD 9757  Chemical Structure
  33. GC38742 BRD-6929 An HDAC1 and HDAC2 inhibitor BRD-6929  Chemical Structure
  34. 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
  35. 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
  36. 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
  37. 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
  38. 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
  39. 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
  40. GC10259 BRD4770 novel G9a(EHMT2) inhibitor BRD4770  Chemical Structure
  41. 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
  42. GC13088 BRD6688 HDAC inhibitor BRD6688  Chemical Structure
  43. 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
  44. GC12484 BRD73954 potent and selective HDAC inhibitor BRD73954  Chemical Structure
  45. GC32988 BRD9539 An inhibitor of EHMT2/G9a and PRC2 in enzyme assays BRD9539  Chemical Structure
  46. GC25168 Brepocitinib (PF-06700841) 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
  47. GC35554 Brevilin A A sesquiterpene lactone with anticancer activity Brevilin A  Chemical Structure
  48. 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
  49. GC35557 Bromodomain IN-1 Bromodomain IN-1 is a Bromodomain inhibitor extracted from patent WO2016069578A1, compound 4 . Bromodomain IN-1  Chemical Structure
  50. GC16531 Bromodomain Inhibitor, (+)-JQ1 A selective inhibitor of BET bromodomains Bromodomain Inhibitor, (+)-JQ1  Chemical Structure
  51. 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
  52. GC10402 Bromosporine A non-specific bromodomain inhibitor Bromosporine  Chemical Structure
  53. GC15410 Bufexamac COX inhibitor Bufexamac  Chemical Structure
  54. GC64761 Butyric acid-13C1 Butyric acid-13C1  Chemical Structure
  55. GC46104 Butyric Acid-d7 An internal standard for the quantification of sodium butyrate Butyric Acid-d7  Chemical Structure
  56. GC10226 Butyrolactone 3

    histone acetyltransferase Gcn5 inhibitor

    Butyrolactone 3  Chemical Structure
  57. GC10690 BYK 204165 A selective inhibitor of PARP1 BYK 204165  Chemical Structure
  58. GC14434 BYK 49187 Potent PARP-1/PARP-2 inhibitor BYK 49187  Chemical Structure
  59. GC16130 C 21 Protein arginine methyltransferase 1 (PRMT1) inhibitor C 21  Chemical Structure
  60. GC17011 C2 Ceramide A cell-permeable analog of naturally occurring ceramides C2 Ceramide  Chemical Structure
  61. GC12733 C646 C646, a potent and selective p300/CBP histone acetyltransferase inhibitor (Ki 400 nM), has been shown to have pleiotropic activity, including neuroprotective, anti-cancer and anti-epithelial-mesenchymal transition (anti-EMT) effects.. C646  Chemical Structure
  62. GC12005 C7280948 Novel PRMT1 inhibitor C7280948  Chemical Structure
  63. GC62886 Cannabisin F Cannabisin F  Chemical Structure
  64. GC12082 Cantharidic Acid (sodium salt) PP1 and PP2A inhibitor Cantharidic Acid (sodium salt)  Chemical Structure
  65. GC34108 CARM1-IN-1 A selective inhibitor of PRMT4/CARM1 CARM1-IN-1  Chemical Structure
  66. GC34424 CARM1-IN-1 hydrochloride CARM1-IN-1 hydrochloride is a potent and specific CARM1(Coactivator-associated arginine methyltransferase 1) inhibitor with IC50 of 8.6 uM; shows very low activity against PRMT1 and SET7(IC50 > 600 uM). CARM1-IN-1 hydrochloride  Chemical Structure
  67. GC43147 CAY10398 CAY10398 is an inhibitor of histone deacetylase (HDAC1) with an IC50 value of 10 μM. CAY10398  Chemical Structure
  68. GC41601 CAY10591 CAY10591 is a potent activator of Sirt1 and suppresses TNF-α in a dose-dependent manner. CAY10591  Chemical Structure
  69. GC18228 CAY10602 Sirtuin 1 (SIRT1) is an evolutionarily conserved NAD-dependent protein deacetylase that has been implicated in cell metabolism, differentiation, stress and DNA damage response, and the control of multidrug resistance in cancer. CAY10602  Chemical Structure
  70. GC12971 CAY10603

    potent and selective inhibitor of HDAC6

    CAY10603  Chemical Structure
  71. GC40767 CAY10669 CAY10669 is an inhibitor of the histone acetyltransferase PCAF (p300/CREB-binding protein-associated factor; IC50 = 662 μM), displaying a 2-fold improvement in inhibitory potency over anacardic acid. CAY10669  Chemical Structure
  72. GC18949 CAY10677 Post-translational protein prenylation is a 3-step process that occurs at the C-terminus of a number of proteins involved in cell growth control and oncogenesis. CAY10677  Chemical Structure
  73. GC43192 CAY10685 CAY10685 is a cell-active analog of the lysine acetyltransferase inhibitor CPTH2 that contains an alkyne moiety for use in click chemistry reactions. CAY10685  Chemical Structure
  74. GC43200 CAY10721 CAY10721 is an inhibitor of sirtuin 3 (SIRT3), a class III HDAC (39% SIRT3 inhibition at 200 μM). CAY10721  Chemical Structure
  75. GC43201 CAY10722 CAY10722 is an inhibitor of sirtuin 3 (SIRT3), a class III HDAC (71% inhibition at 200 μM). CAY10722  Chemical Structure
  76. GC43202 CAY10723 CAY10723 is a potent protein arginine deiminase 2 (PAD2) inhibitor and has excellent PAD2-selectivity. CAY10723  Chemical Structure
  77. GC47050 CAY10727 A PAD3 inhibitor CAY10727  Chemical Structure
  78. GC47055 CAY10749 CAY10749 (compound 15) is a potent PARP/PI3K inhibitor with pIC50 values of 8.22, 8.44, 8.25, 6.54, 8.13, 6.08 for PARP-1, PARP-2, PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ, respectively. CAY10749 is a highly effective anticancer compound targeted against a wide range of oncologic diseases. CAY10749  Chemical Structure
  79. GC47056 CAY10753 A TNKS2 inhibitor CAY10753  Chemical Structure
  80. GC49029 CAY17c An inhibitor of BRD4 and class I and class IIb HDACs CAY17c  Chemical Structure
  81. GC35621 CBB1003 CBB1003 is a novel histone demethylase LSD1 inhibitor with IC50 of 10.54 uM. CBB1003  Chemical Structure
  82. GC35622 CBB1003 hydrochloride CBB1003 Hcl is a novel histone demethylase LSD1 inhibitor with IC50 of 10.54 uM. CBB1003 hydrochloride  Chemical Structure
  83. GC14151 CBB1007 LSD1 inhibitor,potent and selective CBB1007  Chemical Structure
  84. GC35623 CBB1007 hydrochloride CBB1007 Hcl is a cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC50 = 5.27 μM for hLSD1). CBB1007 hydrochloride  Chemical Structure
  85. GC35624 CBB1007 trihydrochloride CBB1007 trihydrochloride is a cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC50 = 5.27 μM for hLSD1). CBB1007 trihydrochloride  Chemical Structure
  86. GC14058 CBHA CBHA is a potent HDAC inhibitor, exhibiting ID50 values of 10 and 70 nM in vitro for HDAC1 and HDAC3, respectively. CBHA also induces apoptosis and suppresses tumor growth. CBHA  Chemical Structure
  87. GC34517 CBP-IN-1 CBP-IN-1 (CCS1477) is an orally active, potent, and selective inhibitor of the p300/CBP bromodomain. CBP-IN-1 binds to p300 and CBP with Kd values of 1.3 and 1.7 nM, respectively, and with 170/130-fold selectivity compared with BRD4 with a Kd of 222 nM. CCS1477 inhibits cell proliferation in prostate cancer cell lines and decreases androgen receptor (AR)- and C-MYC-regulated gene expression. CBP-IN-1  Chemical Structure
  88. GC61577 CBP/p300-IN-1 CBP/p300-IN-1 is a CBP/EP300 bromodomain inhibitor. CBP/p300-IN-1  Chemical Structure
  89. GC64696 CBP/p300-IN-12 CBP/p300-IN-12 is a potent and selective covalent histone acetyltransferases p300 (IC50 of 166 nM) and CBP inhibitor. CBP/p300-IN-12 decreases the levels of H3K27Ac of PC-3 cells (EC50 of 37 nM). CBP/p300-IN-12 forms a covalent adduct with C1450. CBP/p300-IN-12  Chemical Structure
  90. GC38469 CBP/p300-IN-3 CBP/p300-IN-3, a p300/CBP histone acetyltransferase inhibitor, Compound 6, is sourced from patent WO 2019049061 A1. CBP/p300-IN-3  Chemical Structure
  91. GC62330 CC-90010 CC-90010 (compound 1) is a reversible and orally active BET inhibitor. CC-90010 is applied in the study for advanced solid tumors. CC-90010  Chemical Structure
  92. GC12891 CCT007093 PPM1D inhibitor CCT007093  Chemical Structure
  93. GC11310 CCT129202 An Aurora kinase inhibitor CCT129202  Chemical Structure
  94. GC14566 CCT137690 An inhibitor of Aurora kinases and FLT3 CCT137690  Chemical Structure
  95. GC19092 CCT241736 CCT241736 is a potent and orally bioavailable dual FLT3 and Aurora kinase inhibitor, which inhibits Aurora kinases (Aurora-A Kd, 7.5 nM, IC50, 38 nM; Aurora-B Kd, 48 nM), FLT3 kinase (Kd, 6.2 nM), and FLT3 mutants including FLT3-ITD (Kd, 38 nM) and FLT3(D835Y) (Kd, 14 nM). CCT241736  Chemical Structure
  96. GC48982 CD532 An inhibitor of Aurora A kinase activity and the Aurora A-N-Myc protein-protein interaction CD532  Chemical Structure
  97. GC62189 CD532 hydrochloride CD532 hydrochloride is a potent Aurora A kinase inhibitor with an IC50 of 45 nM. CD532 hydrochloride has the dual effect of blocking Aurora A kinase activity and driving degradation of MYCN. CD532 hydrochloride also can directly interact with AURKA and induces a global conformational shift. CD532 hydrochloride can be used for the research of cancer. CD532 hydrochloride  Chemical Structure
  98. GC19098 CeMMEC1 CeMMEC1 is an inhibitor of BRD4, and also has high affinity for TAF1, with an IC50 of 0.9 uM for TAF1, and a Kd of 1.8 uM for TAF1 (2). CeMMEC1  Chemical Structure
  99. GC35651 Cenisertib Cenisertib (AS-703569) is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia. Cenisertib  Chemical Structure
  100. GC12083 CEP-33779 A potent, orally available inhibitor of JAK2 CEP-33779  Chemical Structure
  101. GC11209 Cerdulatinib (PRT062070) Cerdulatinib (PRT062070) (PRT062070) is a selective Tyk2 inhibitor with an IC50 of 0.5 nM. Cerdulatinib (PRT062070) (PRT062070) also is a dual JAK and SYK inhibitor with IC50s of 12, 6, 8 and 32 for JAK1, 2, 3 and SYK, respectively. Cerdulatinib (PRT062070)  Chemical Structure

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