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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. 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
  3. GC16261 LLY507 SMYD2 inhibitor LLY507 Chemical Structure
  4. GC13237 LMK 235 A selective inhibitor of HDAC4 and HDAC5 LMK 235 Chemical Structure
  5. GC11778 Lomeguatrib

    Inactivator of O6-methylguanine-DNA methyltransferase

     Lomeguatrib Chemical Structure
  6. GC64372 Lorpucitinib Lorpucitinib is a Gut-Restricted JAK Inhibitor for the research of Inflammatory Bowel Disease. Lorpucitinib Chemical Structure
  7. GC18731 LP99 LP99 is a potent inhibitor of the bromodomain containing proteins BRD7 and BRD9 that binds with Kd values of 99 and 909 nM, respectively, as determined by isothermal titration calorimetry. LP99 Chemical Structure
  8. GC36484 LSD1-IN-5 LSD1-IN-5 (Compound 4e) is a potent and reversible inhibitor of lysine-specific demethylase 1 (LSD1), with an IC50 of 121 nM. LSD1-IN-5 increases dimethylated Lys4 of histone H3, shows no effect on expression of LSD1. LSD1-IN-5 Chemical Structure
  9. GC36485 LSD1-IN-6 LSD1-IN-6 (Compound 4m) is a potent and reversible inhibitor of lysine-specific demethylase 1 (LSD1), with an IC50 of 123 nM. LSD1-IN-6 increases dimethylated Lys4 of histone H3, shows no effect on expression of LSD1. LSD1-IN-6 Chemical Structure
  10. GC62434 LSD1/HDAC6-IN-1 LSD1/HDAC6-IN-1 is an orally active dual inhibitor of lysine specific demethylase 1(LSD1)/Histone deacetylase 6 (HDAC6), with anti-tumor activity. LSD1/HDAC6-IN-1 can be used for the research of multiple myeloma (MM). LSD1/HDAC6-IN-1 Chemical Structure
  11. GC62591 LT052 LT052 is a highly selective BET BD1 inhibitor with an IC50 of 87.7 nM. LT052 Chemical Structure
  12. GC32724 LW6 (HIF-1α inhibitor) LW6 (HIF-1α inhibitor) (HIF-1α inhibitor) is a novel HIF-1 inhibitor with an IC50 of 4.4 μM. LW6 (HIF-1α inhibitor) decreases HIF-1α protein expression without affecting HIF-1β expression. LW6 (HIF-1α inhibitor) Chemical Structure
  13. GC13848 LY2784544 Potent inhibitor of JAK2 LY2784544 Chemical Structure
  14. GC33057 LY3295668 (AK-01) LY3295668 (AK-01) (AK-01) is a potent, orally active and highly specific Aurora-A kinase inhibitor, with Ki values of 0.8 nM and 1038 nM for AurA and AurB, respectively. LY3295668 (AK-01) Chemical Structure
  15. GC68405 Lys-CoA TFA Lys-CoA TFA Chemical Structure
  16. GC13534 Lysine-specific Demethylase Inhibitor (1C) lysine-specific demethylase Inhibitor Lysine-specific Demethylase Inhibitor (1C) Chemical Structure
  17. GC47586 Lysine-specific Demethylase Inhibitor (1C) (hydrochloride) An LSD1 inhibitor Lysine-specific Demethylase Inhibitor (1C) (hydrochloride) Chemical Structure
  18. GC34138 M-110 M-110 is a highly selective, ATP-competitive inhibitor of PIM kinases with a preference for PIM-3 (IC50=47 nM). M-110 inhibits PIM-1 and PIM-2 with similar IC50s of 2.5 μM. M-110 inhibits the proliferation of prostate cancer cell lines with IC50s of 0.6 to 0.9 μM. M-110 Chemical Structure
  19. GC47693 m-Methoxybenzamide m-Methoxybenzamide (3-MBA), an inhibitor of ADP-ribosyltransferase (ADPRTs) and PARP, inhibits cell division in Bacillus subtilis, leading to filamentation and eventually lysis of cells. m-Methoxybenzamide (3-MBA) enhances in vitro plant growth, microtuberization, and transformation efficiency of blue potato (Solanum tuberosum L. subsp. andigenum). m-Methoxybenzamide Chemical Structure
  20. GC64945 M1001 M1001 is a weak hypoxia-inducible factor-2α (HIF-2α) agonist. M1001 can bind to the HIF-2α PAS-B domain, with a Kd of 667 nM. M1001 can be used in chronic kidney disease research. M1001 Chemical Structure
  21. GC65046 M1002 M1002 is a hypoxia-inducible factor-2 (HIF-2) agonist, and can enhance the expression of HIF-2 target genes. M1002 shows synergy with prolyl-hydroxylase domain (PHD) inhibitors. M1002 Chemical Structure
  22. GC16456 M344 HDAC inhibitor M344 Chemical Structure
  23. GC36521 M89 M-89 is a highly potent and specific menin inhibitor, with a Kd of 1.4 nM for binding to menin. M89 Chemical Structure
  24. GC63056 MAK683-CH2CH2COOH

    MAK683-CH2CH2COOH binds to EED (embryonic ectoderm development protein). MAK683-CH2CH2COOH and a VHL ligand for the E3 ubiquitin ligase have been used to design PROTAC EED degrader-1 and PROTAC EED degrader-2.

     MAK683-CH2CH2COOH Chemical Structure
  25. GC61029 Marein A glucoside chalcone with diverse biological activities Marein Chemical Structure
  26. GC15965 MC1568 A selective class IIa HDAC inhibitor MC1568 Chemical Structure
  27. GC45906 MC1742 An inhibitor of class I and class IIb HDACs MC1742 Chemical Structure
  28. GC34431 MC3482 MC3482 is a specific sirtuin5 (SIRT5) inhibitor. MC3482 Chemical Structure
  29. GC65254 MC4355 MC4355 is a dual inhibitor of EZH2 and histone deacetylase (HDAC). MC4355 Chemical Structure
  30. GC15049 MCB-613

    stimulator of steroid receptor coactivator (SRC)

     MCB-613 Chemical Structure
  31. GC52188 MDL 800 MDL 800 Chemical Structure
  32. GC13419 ME0328 PARP inhibitor,potent and selective ME0328 Chemical Structure
  33. GC62252 Mefuparib hydrochloride Mefuparib hydrochloride (MPH) is an orally active, substrate-competitive and selective PARP1/2 inhibitor with IC50s of 3.2 nM and 1.9 nM, respectively. Mefuparib hydrochloride induces apoptosis and possesses prominent anticancer activity in vitro and in vivo. Mefuparib hydrochloride Chemical Structure
  34. GC63064 Menin-MLL inhibitor 19 Menin-MLL inhibitor 19, a potent exo-aza spiro inhibitor of menin-mll interaction, example A17, extracted from patent WO2019120209A1. Menin-MLL inhibitor 19 Chemical Structure
  35. GC63538 Menin-MLL inhibitor 20 Menin-MLL inhibitor 20 is an irreversible menin-MLL interaction inhibitor with antitumor activities (WO2020142557A1, Intermediate 6). Menin-MLL inhibitor 20 Chemical Structure
  36. GC48805 Methapyrilene (hydrochloride) An H1 receptor antagonist and non-genotoxic carcinogen Methapyrilene (hydrochloride) Chemical Structure
  37. GC44184 Methylstat (hydrate) Methylstat is a methyl ester prodrug of a Jumonji C domain-containing histone demethylase (JMJD) inhibitor that has favorable cell permeability. Methylstat (hydrate) Chemical Structure
  38. GC61058 Metoprine Metoprine (BW 197U) is a potent histamine N-methyltransferase (HMT) inhibitor. Metoprine Chemical Structure
  39. GC11439 MG 149 HAT inhibitor MG 149 Chemical Structure
  40. GC11949 MI-192 inhibitor of histone deacetylases (HDACs) MI-192 Chemical Structure
  41. GC11418 MI-2 An inhibitor of menin-MLL fusion protein interactions MI-2 Chemical Structure
  42. GC12199 MI-3 An inhibitor of menin-MLL fusion protein interactions MI-3 Chemical Structure
  43. GC19246 MI-463 MI-463 is a highly potent and orally bioavailable small molecule inhibitor of the menin-mLL interaction. MI-463 Chemical Structure
  44. GC19247 MI-503 MI-503 is a highly potent and orally bioavailable small molecule inhibitor of the menin-mLL interaction. MI-503 Chemical Structure
  45. GC32798 MI-538 MI-538 is an inhibitor of the interaction between menin and MLL fusion proteins with an IC50 of 21 nM. MI-538 Chemical Structure
  46. GC65581 MIND4-19 MIND4-19 is a potent SIRT2 inhibitor with an IC50 value of 7.0 μM. MIND4-19 Chemical Structure
  47. GC32929 MIR96-IN-1 MIR96-IN-1 targets the Drosha site in the miR-96 (miRNA-96, microRNA-96) hairpin precursor, inhibiting its biogenesis, derepressing downstream targets, and triggering apoptosis in breast cancer cells. MIR96-IN-1 binds to RNAs with Kds of 1.3, 9.4, 3.4, 1.3 and 7.4 μM for RNA1, RNA2, RNA3, RNA4 and RNA5, respectively. MIR96-IN-1 Chemical Structure
  48. GC64487 Miravirsen Miravirsen (SPC-3649), a β-d-oxy-locked nucleic acid-modified phosphorothioate antisense oligonucleotide, inhibit the biogenesis of miR-122. Miravirsen Chemical Structure
  49. GC19248 Mivebresib Mivebresib is a potent and orally available bromodomain and extraterminal domain (BET) bromodomain inhibitor. Mivebresib Chemical Structure
  50. GC17802 MK-4827 An orally bioavailable PARP1/2 inhibitor MK-4827 Chemical Structure
  51. GC12756 MK-4827 hydrochloride MK-4827 hydrochloride (MK-4827 hydrochloride) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. MK-4827 hydrochloride leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity. MK-4827 hydrochloride Chemical Structure
  52. GC17052 MK-4827 Racemate selective inhibitor of PARP1/PARP2 MK-4827 Racemate Chemical Structure
  53. GC11537 MK-4827 tosylate MK-4827 tosylate (MK-4827 tosylate) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with an IC50 of 3.8 and 2.1 nM, respectively. MK-4827 tosylate leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity. MK-4827 tosylate Chemical Structure
  54. GC17162 MK-5108 (VX-689) A potent inhibitor of Aurora kinases MK-5108 (VX-689) Chemical Structure
  55. GC19251 MK-8617 MK-8617 is an orally active pan-inhibitor of hypoxia-inducible factor prolyl hydroxylase 1-3 (HIF PHD1-3) with an IC50 of 1 nM for PHD2. MK-8617 Chemical Structure
  56. GC10442 MK-8745 Aurora A inhibitor,potent and selective MK-8745 Chemical Structure
  57. GC14319 ML 228 A HIF pathway activator ML 228 Chemical Structure
  58. GC12557 ML324 JMJD2 demethylase inhibitor, potent and cell-permeable ML324 Chemical Structure
  59. GC12208 MLN8054 An inhibitor of Aurora A kinase MLN8054 Chemical Structure
  60. GC12690 MLN8237 (Alisertib)

    An Aurora A kinase inhibitor

     MLN8237 (Alisertib) Chemical Structure
  61. GC14652 MM-102 MLL1 inhibitor,high-affinity peptidomimetic MM-102 Chemical Structure
  62. GC36632 MM-102 TFA MM-102 TFA (HMTase Inhibitor IX TFA) is a potent WDR5/MLL interaction inhibitor, achieves IC50 = 2.4 nM with an estimated Ki 200 times more potent than the ARA peptide. MM-102 TFA Chemical Structure
  63. GC67758 MM-401 TFA MM-401 TFA Chemical Structure
  64. GC33278 MM-589 MM-589 is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction. MM-589 binds to WDR5 with an IC50 of 0.90 nM and inhibits the MLL H3K4 methyltransferase activity with an IC50 of 12.7 nM. MM-589 Chemical Structure
  65. GC65037 MM-589 TFA MM-589 TFA is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction. MM-589 binds to WDR5 with an IC50 of 0.90 nM and inhibits the MLL H3K4 methyltransferase activity with an IC50 of 12.7 nM. MM-589 TFA Chemical Structure
  66. GC16914 MN 64 tankyrase inhibitor MN 64 Chemical Structure
  67. GC13055 Mocetinostat (MGCD0103, MG0103) An orally available HDAC inhibitor Mocetinostat (MGCD0103, MG0103) Chemical Structure
  68. GC34675 Molibresib besylate Molibresib besylate (GSK 525762C; I-BET 762 besylate) is a BET bromodomain inhibitor with IC50 of 32.5-42.5 nM. Molibresib besylate Chemical Structure
  69. GC10046 Molidustat (BAY85-3934) Molidustat (BAY85-3934) (BAY 85-3934) is a novel inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) with mean IC50 values of 480 nM for PHD1, 280 nM for PHD2, and 450 nM for PHD3. Molidustat (BAY85-3934) Chemical Structure
  70. GC36646 Momelotinib Mesylate Momelotinib Mesylate (CYT387 Mesylate) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, appr 10-fold selectivity versus JAK3. Momelotinib Mesylate Chemical Structure
  71. GC62406 Moracin O Moracin O is a 2-arylbenzofuran isolated from the Mori Cortex Radicis. Moracin O Chemical Structure
  72. GC33371 MOZ-IN-2 An inhibitor of KAT6A/MOZ MOZ-IN-2 Chemical Structure
  73. GC64729 MPT0B390 MPT0B390 is an arylsulfonamide-based derivative with potent HDAC inhibitory ability. MPT0B390, TIMP3 inducer, inhibits tumor growth, metastasis and angiogenesis. MPT0B390 shows antiproliferative activity against human colon cancer cell line HCT116 with the GI50 of 0.03 μM. MPT0B390 Chemical Structure
  74. GC65965 MPT0E028 MPT0E028 is an orally active and selective HDAC inhibitor with IC50s of 53.0 nM, 106.2 nM, 29.5 nM for HDAC1, HDAC2 and HDAC6, respectively. MPT0E028 reduces the viability of B-cell lymphomas by inducing apoptosis and possesses potent direct Akt targeting ability and reduces Akt phosphorylation in B-cell lymphoma. MPT0E028 has good anticancer activity. MPT0E028 Chemical Structure
  75. GC62308 MPT0G211 MPT0G211 is a potent, orally active and selective HDAC6 inhibitor (IC50=0.291?nM). MPT0G211 Chemical Structure
  76. GC61468 MR837 MR837 is an inhibitor of NSD2-PWWP1. MR837 can bind with human nuclear receptor binding SET domain protein 2 (PWWP domain). MR837 Chemical Structure
  77. GC50576 MRK 740 Potent PRDM9 inhibitor MRK 740 Chemical Structure
  78. GC63558 MRTX-1719 MRTX-1719 is a potent first-in-class selective inhibitor of the PRMT5/MTA complex, with an IC50 of less than 10 nM in PRMT5/MTA MTAPDEL SDMA cells. MRTX-1719 Chemical Structure
  79. GC69499 MRTX-1719 hydrochloride

    MRTX-1719 hydrochloride is an effective, novel, and selective inhibitor of the PRMT5/MTA complex. Its IC50 value for PRMT5/MTA MTAPDEL SDMA cell lines is <10 nM.

     MRTX-1719 hydrochloride Chemical Structure
  80. GC62715 MRTX9768 MRTX9768 is a potent, selective, orally active, first-in-class PRMT5-MTA complex inhibitor. MRTX9768 Chemical Structure
  81. GC63080 MRTX9768 hydrochloride MRTX9768 hydrochloride is a potent, selective, orally active, first-in-class PRMT5-MTA complex inhibitor. MRTX9768 hydrochloride Chemical Structure
  82. GC40791 MS-1020 MS-1020 is a cell-permeable inhibitor of janus kinase 3 (JAK3), strongly inhibiting constitutive autophosphorylation of JAK3 in L540 cells when used at 30-50 μM. MS-1020 Chemical Structure
  83. GC10099 MS023 MS023 is a potent, selective, and cell-active inhibitor of type I protein arginine methyltransferases (PRMTs). MS023 Chemical Structure
  84. GC16432 MS023 (hydrochloride) type I PRMTs inhibitor MS023 (hydrochloride) Chemical Structure
  85. GC36655 MS023 dihydrochloride MS023 dihydrochloride is a potent, selective, and cell-active inhibitor of human type I protein arginine methyltransferases (PRMTs) inhibitor, with IC50s of 30, 119, 83, 4 and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, respectively. MS023 dihydrochloride Chemical Structure
  86. GC36656 MS049 MS049 is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 is not toxic and does not affect the growth of HEK293 cells. MS049 Chemical Structure
  87. GC14240 MS049 (hydrochloride) MS049 (hydrochloride) is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 (hydrochloride) reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 (hydrochloride) is not toxic and does not affect the growth of HEK293 cells. MS049 (hydrochloride) Chemical Structure
  88. GC36657 MS31 MS31 is a potent, highly affinity and selective fragment-like methyllysine reader protein spindlin 1 (SPIN1) inhibitor. MS31 potently inhibits the interactions between SPIN1 and H3K4me3 (IC50=77 nM, AlphaLISA; 243 nM, FP). MS31 selectively binds Tudor domain II of SPIN1 (Kd=91 nM). MS31 potently inhibits binding of trimethyllysine-containing peptides to SPIN1. MS31 is not toxic to nontumorigenic cells. MS31 Chemical Structure
  89. GC39252 MS31 trihydrochloride MS31 trihydrochloride is a potent, highly affinity and selective fragment-like methyllysine reader protein spindlin 1 (SPIN1) inhibitor. MS31 trihydrochloride potently inhibits the interactions between SPIN1 and H3K4me3 (IC50=77 nM, AlphaLISA; 243 nM, FP). MS31 trihydrochloride selectively binds Tudor domain II of SPIN1 (Kd=91 nM). MS31 trihydrochloride potently inhibits binding of trimethyllysine-containing peptides to SPIN1, and is not toxic to nontumorigenic cells. MS31 trihydrochloride Chemical Structure
  90. GC44250 MS351

    MS351 is an antagonist of chromobox 7 (CBX7) that acts by binding the CBX7 chromodomain.

     MS351 Chemical Structure
  91. GC12630 MS37452 competitive inhibitor of CBX7 chromodomain binding to H3K27me3 MS37452 Chemical Structure
  92. GC64999 MS402 MS402 is a BD1-selective BET BrD inhibitor with Kis of 77 nM, 718 nM, 110 nM, 200 nM, 83 nM, and 240 nM for BRD4(BD1), BRD4(BD2), BRD3(BD1), BRD3(BD2), BRD2(BD1) and BRD2(BD2), respectively. MS402 Chemical Structure
  93. GC31881 MS417 (GTPL7512) MS417 (GTPL7512) is a selective BET-specific BRD4 inhibitor, binds to BRD4-BD1 and BRD4-BD2 with IC50s of 30, 46 nM and Kds of 36.1, 25.4 nM, respectively, with weak selectivity at CBP BRD (IC50, 32.7 μM). MS417 (GTPL7512) Chemical Structure
  94. GC13148 MS436 BRD4 inhibitor MS436 Chemical Structure
  95. GC38474 MS645 MS645 is a bivalent BET bromodomains (BrD) inhibitor with a Ki of 18.4 nM for BRD4-BD1/BD2. MS645 spatially constrains bivalent inhibition of BRD4 BrDs resulting in a sustained repression of BRD4 transcriptional activity in solid-tumor cells. MS645 Chemical Structure
  96. GC64295 MS67 MS67 is a potent and selective WD40 repeat domain protein 5 (WDR5) degrader with a Kd of 63 nM. MS67 is inactive against other protein methyltransferases, kinases, GPCRs, ion channels, and transporters. MS67 shows potent acticancer effects. MS67 Chemical Structure
  97. GC69504 MS8815

    MS8815 is a selective PROTAC degrader of zeste homolog 2 (EZH2). It has inhibitory activity against EZH2 with an IC50 value of 8.6 nM. MS8815 can be used for research on triple-negative breast cancer (TNBC).

     MS8815 Chemical Structure
  98. GC18729 MZ1 MZ1 is a hybrid compound that drives the selective proteasomal degradation of bromodomain-containing protein 4 (BRD4). MZ1 Chemical Structure
  99. GC33102 MZP-54 MZP-54 is a PROTAC connected by ligands for von Hippel-Lindau and BRD3/4, with a Kd of 4 nM for Brd4BD2. MZP-54 Chemical Structure
  100. GC33363 MZP-55 MZP-55 is a PROTAC connected by ligands for von Hippel-Lindau and BRD3/4, with a Kd of 8 nM for Brd4BD2. MZP-55 Chemical Structure
  101. GC62154 N-Descyclopropanecarbaldehyde Olaparib N-Descyclopropanecarbaldehyde Olaparib is an analogue of Olaparib containing DOTA moiety. N-Descyclopropanecarbaldehyde Olaparib is a CRBN-based ligand for synthesizing novel dual EGFR and PARP PROTAC, DP-C-4. N-Descyclopropanecarbaldehyde Olaparib can be radiolabeled F-18 or fluorophore for positron emission tomography (PET) or optical imaging in several types of tumor. N-Descyclopropanecarbaldehyde Olaparib Chemical Structure

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