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
- Bromodomain(52)
- Aurora Kinase(89)
- DNA Methyltransferase(40)
- HDAC(218)
- Histone Acetyltransferases(67)
- Histone Demethylases(98)
- Histone Methyltransferase(212)
- HIF(101)
- JAK(178)
- MBT Domains(1)
- PARP(128)
- Pim(35)
- Protein Ser/Thr Phosphatases(41)
- RNA Polymerase(8)
- Sirtuin(84)
- Sphingosine Kinase-2(1)
- Polycomb repressive complex(2)
- SUMOylation(3)
- PAD(18)
- Epigenetic Reader Domain(207)
- MicroRNA(13)
- Protein Arginine Deiminase(12)
- Chromodomain(1)
- Citrullination(15)
- DNA/RNA Demethylation(1)
- DNA/RNA Methylation(6)
- Histone Deacetylation(38)
- Histones/Histone Peptides(7)
- PHD Domains(0)
- Tandem Tudor & Tudor-like Domains(1)
- PRMT(2)
Products for Chromatin/Epigenetics
- Cat.No. Product Name Information
- GC30530 Dot1L-IN-2 Dot1L-IN-2 is a potent, selective and orally bioavailable inhibitor of Dot1L (a histone methyltransferase), with an IC50 and Ki of 0.4 nM and 0.08 nM, respectively.
- GC62613 Dot1L-IN-4 Dot1L-IN-4 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 SPA DOT1L of 0.11 nM.
- GC65962 Dot1L-IN-5 Dot1L-IN-5 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 SPA DOT1L of 0.17 nM.
- GC12680 DR 2313 A PARP inhibitor
- GC13706 Droxinostat An inhibitor of HDAC3, HDAC6, and HDAC8
- GC45927 DS-437 A dual inhibitor of PRMT5 and PRMT7
- GC35904 dTRIM24 dTRIM24 is a selective bifunctional degrader of TRIM24 based on PROTAC, consists of ligands for von Hippel-Lindau and TRIM24.
- GC35914 DW14800 DW14800 is a protein arginine methyltransferase 5 (PRMT5) inhibitor, with an IC50 of 17 nM. DW14800 reduces H4R3me2s levels and enhances the transcription of HNF4α, but does not alter PRMT5 expression. Anti-cancer activity.
- GC33403 E-7386 E-7386 is an orally active CBP/beta-catenin modulator.
- GC64209 E7016 E7016 (GPI 21016) is an orally available PARP inhibitor. E7016 can enhance tumor cell radiosensitivity in vitro and in vivo through the inhibition of DNA repair. E7016 acts as a potential anticancer agent.
- GC18172 E7449 E7449 is an inhibitor of poly(ADP-ribose) polymerase 1 (PARP1) and PARP2 (IC50s = 1 and 1.2 nM, respectively) as well as tankyrase (TNKS) 1/2 (IC50s = 50-100 nM).
- GC12991 EB 47 A PARP1 and TNKS2 inhibitor
- GC33220 EBI-2511 EBI-2511 is a highly potent and orally active EZH2 inhibitor, with an IC50 of 6 nM in Pfeffiera cell lines, respectively.
- GC18236 Echinomycin An inhibitor of HIF1mediated gene transcription
- GC19129 EDO-S101 EDO-S101 is a pan HDAC inhibitor; inhibits HDAC1, HDAC2 and HDAC3 with IC50 values of 9, 9 and 25 nM, respectively.
- GC19130 EED226 EED226 is a potent, selective, and orally bioavailable embryonic ectoderm development (EED) inhibitor with an IC50 of 22 nM.
- GC67934 EEDi-5285
- GC34567 EHMT2-IN-1 EHMT2-IN-1 is a potent EHMT inhibitor, with IC50s of all <100 nM for EHMT1 peptide, EHMT2 peptide and cellular EHMT2. Used in the research of blood disorder or cancer.
- GC34568 EHMT2-IN-2 EHMT2-IN-2 is a potent EHMT inhibitor, with IC50s of all <100 nM for EHMT1 peptide, EHMT2 peptide and cellular EHMT2. Used in the research of blood disease or cancer.
- GC14756 EI1 EZH2 inhibitor
- GC33043 EL-102 EL-102 is a hypoxia-induced factor 1 (Hif1α) inhibitor. EL-102 induces apoptosis, inhibits tubulin polymerisation and shows activities against prostate cancer. EL-102 can be used for the research of cancer.
- GC64191 Elevenostat Elevenostat (JB3-22) is a selective HDAC11 inhibitor (IC50=0.235??M). Anti-multiple myeloma (MM) activity.
- GC31245 EML 425 An inhibitor of p300 and CBP
- GC49124 EN219 EN219 is a moderately selective synthetic covalent ligand against an N-terminal cysteine (C8) of RNF114 with an IC50 of 470 nM. EN219 inhibits RNF114-mediated autoubiquitination and p21 ubiquitination.
- GC33634 Enarodustat (JTZ-951) Enarodustat (JTZ-951) is a potent and orally active hypoxia-inducible factor prolyl hydroxylase inhibitor, with an EC50 of 0.22 μM.
- GC33170 ENMD-119 (ENMD 1198) ENMD-119 (ENMD 1198) (IRC-110160), an orally active microtubule destabilizing agent, is a 2-methoxyestradiol analogue with antiproliferative and antiangiogenic activity. ENMD-119 (ENMD 1198) is suitable for inhibiting HIF-1alpha and STAT3 in human HCC cells and leads to reduced tumor growth and vascularization.
- GC16519 ENMD-2076 A multi-kinase inhibitor
- GC12145 ENMD-2076 L-(+)-Tartaric acid
- GC50182 ent-LP 99 ent-LP 99 is a potent and selective BRD7 and BRD9 inhibitor with an KD of 99 nM for BRD9.
- GC17334 Entacapone A reversible COMT inhibitor
- GC47294 Entacapone-d10 An internal standard for the quantification of entacapone
- GC11625 Entinostat (MS-275,SNDX-275) A histone deacetylase inhibitor
-
GC14062
EPZ-6438
A EZH2 inhibitor,potent and selective
- GC64343 EPZ-719 EPZ-719 is a novel and potent SETD2 inhibitor ( IC50 = 0.005 μM) with a high selectivity over other histone methyltransferases.
- GC13383 EPZ004777 A potent inhibitor of DOT1L
- GC48980 EPZ004777 (formate) A potent inhibitor of DOT1L
- GC15259 EPZ004777 HCl EPZ004777 HCl is a potent, selective DOT1L inhibitor with an IC50 of 0.4 nM.
- GC13878 EPZ005687 A potent, selective inhibitor of EZH2
- GC19141 EPZ011989 EPZ011989 is a potent, selective orally bioavailable EZH2 inhibitor with Ki 3000-fold selectivity over other HMTase.
- GC34136 EPZ011989 trifluoroacetate (EPZ-011989 trifluoroacetate) EPZ-011989 trifluoroacetate is a potent and orally active Zeste Homolog 2 (EZH2) inhibitor with metabolic stability. EPZ-011989 trifluoroacetate has inhibitory inhibition for EZH2 with a Ki value of <3 nM. EPZ-011989 trifluoroacetate shows robust methyl mark inhibition and anti-tumor activity. EPZ-011989 trifluoroacetate can be used for the research of various cancers.
- GC15302 EPZ015666 PRMT5 inhibitor
- GC15102 EPZ020411 PRMT6 inhibitor
- GC36000 EPZ020411 hydrochloride EPZ020411 hydrochloride is a selective inhibitor of PRMT6 with an IC50 of 10 nM, it has >10 folds selectivity for PRMT6 over PRMT1 and PRMT8. EPZ020411 hydrochloride can be used for the research of cancer.
- GC16224 EPZ031686 A SMYD3 inhibitor
- GC12932 EPZ5676 A highly potent DOT1L inhibitor
- GC64575 Et-29 Et-29 is a potent and selective SIRT5 inhibitor (Ki=40 nM).
- GC61669 Ethyl 3,4-dihydroxybenzoate Ethyl 3,4-dihydroxybenzoate (Ethyl protocatechuate), an antioxidant, is a prolyl-hydroxylase inhibitor found in the testa of peanut seeds.
- GC10635 EX 527 (SEN0014196) A SIRT1 inhibitor
- GC17126 EX-527 R-enantiomer EX-527 R-enantiomer ((R)-EX-527) is a R-enantiomer of Selisistat. Selisistat (EX-527) is a potent and selective SIRT1 inhibitor with IC50 of 98 nM.
- GC13417 EX-527 S-enantiomer EX-527 S-enantiomer ((S)-EX-527) is a potent and selective SIRT1 inhibitor, with an IC50 of 98 nM.
- GC65980 EZH2-IN-13 EZH2-IN-13 is a potent EZH2 inhibitor, for details please refer to compound 73 in patent WO2017139404. EZH2-IN-13 can be used to study cancers or precancerous lesions associated with EZH2 activity.
- GC19149 EZM 2302 EZM 2302 is an inhibitor of coactivator-associated arginine methyltransferase 1 (CARM1) with an IC50 of 6 nM.
- GC64900 EZM0414 EZM0414 is a potent, selective, orally bioavailable inhibitor of SETD2 (IC50=18 nM in SETD2 biochemical assay; IC50=34 nM in cellular assay). EZM0414 can be used for the research of relapsed or refractory multiple myeloma and diffuse large B-cell lymphoma.
- GC43651 F-Amidine (trifluoroacetate salt) F-amidine is an inhibitor of protein arginine deiminases (PADs) that is selective for PAD1 and PAD4 (IC50s = 29.5, 350, and 21.6 μM for PAD1, PAD3, and PAD4 in vitro, respectively).
- GC13139 FG-4592 (ASP1517) An inhibitor of HIF-PH enzymes
- GC16638 FG2216 HIF-prolyl hydroxylase inhibitor
- GC64821 FHD-286 FHD-286 is a BRG1/BRM ATPase inhibitor for the treatment of BAF-related disorders such as acute myeloid leukemia.
- GC65160 FHT-1015 FHT-1205 is a potent SMARCA4/SMARCA2 ATPase (BRG1 and BRM) inhibitor with IC50s of ≤10 nM (WO2020160180A1; compound 67).
- GC64777 FHT-1204 FHT-1204 is a potent SMARCA4/SMARCA2 ATPase (BRG1 and BRM) inhibitor with IC50s of ≤10 nM (WO2020160180A1; compound 70).
- GC46148 Filgotinib-d4 An internal standard for the quantification of filgotinib
- GN10030 Fisetin
- GC33015 FL-411 (BRD4-IN-1) FL-411 (BRD4-IN-1) is a potent and selective BRD4 inhibitor with an IC50 of 0.43±0.09 μM for BRD4(1).
- GC16875 FLLL32 STAT3 inhibitor
- GC50506 Fluorescein-NAD+ Fluorescent NAD+; substrate for ADP-ribosylation for use in PARP assays
- GC62121 Fluzoparib Fluzoparib (SHR3162) is a potent and orally active PARP1 inhibitor (IC50=1.46±0.72 nM, a cell‐free enzymatic assay) with superior antitumor activity. Fluzoparib selectively inhibits the proliferation of homologous recombination repair (HR)‐deficient cells, and sensitizes both HR‐deficient and HR‐proficient cells to cytotoxic agents. Fluzoparib exhibits good pharmacokinetic properties in vivo and can be used for BRCA1/2-mutant relapsed ovarian cancer research.
- GC50537 FM19G11 A HIF α-subunit inhibitor
-
GC19408
FM381
FM-381 is a highly potent and JAK3-selective janus kinase (JAK) inhibitor
- GC62461 FNDR-20123 FNDR-20123 is a safe, first-in-class, and orally active anti-malarial HDAC inhibitor with IC50s of 31 nM and 3 nM for Plasmodium and human HDAC, respectively.
- GC14395 Fostriecin sodium salt A potent inhibitor of protein phosphatases 2A and 4
- GC38044 Fraxinellone
- GC65206 FT895 FT895 is a potent and selective HDAC11 inhibitor with an IC50 of 3 nM.
- GC63545 FTX-6058 FTX-6058 ((S)-FTX-6058) is a potent and orally active inhibitor of Embryonic Ectoderm Development (EED).
- GC63546 FTX-6058 hydrochloride (S)-Pociredir ((S)-FTX-6058) hydrochloride is a potent and orally active inhibitor of Embryonic Ectoderm Development (EED).
-
GC10456
Fucosterol
Fucosterol is a plant sterol found in algae
- GC43715 Furamidine (hydrochloride) Furamidine (hydrochloride) (DB75 dihydrochloride) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM.
- GC13541 G007-LK tankyrase 1/2 inhibitor
- GC62246 G5-7 G5-7, an orally active and allosteric JAK2 inhibitor, selectively inhibits JAK2 mediated phosphorylation and activation of EGFR (Tyr1068) and STAT3 by binding to JAK2. G5-7 induces cell cycle arrest, apoptosis and possesses antiangiogenic effect. G5-7 has the potential for glioma study.
- GC38062 Gambogenic acid Gambogenic acid is an active ingredient in gamboge, with anticancer activity. Gambogenic acid acts as an effective inhibitor of EZH2, specifically and covalently binds to Cys668 within the EZH2-SET domain, and induces EZH2 ubiquitination.
- GC40900 Ganoderic Acid D Ganoderic acid D is an oxygenated triterpenoid that has been found in G.
-
GC13474
Garcinol
Inhibitor of PCAF and p300 histone acetyltransferase (HAT) activity
- GC60172 Gardenia yellow Gardenia yellow is an active member of crocin, increases mRNA expression of SIRT3, and acts as an orally active antidepressant agent.
- GC32958 GDC-0339 GDC-0339 is a potent, orally bioavailable and well tolerated pan-Pim kinase inhibitor, with Kis of 0.03 nM, 0.1 nM and 0.02 nM for Pim1, Pim2 and Pim3, respectively. GDC-0339 is discovered as a potential treatment of multiple myeloma.
- GC68378 GDC-4379
-
GC19542
GeA-69
GeA-69 is a selective, highly cell permeable allosteric inhibitor
- GN10473 Ginkgolide C
- GN10584 Ginsenoside Rk1
- GC48994 Girard’s Reagent P-d5 An internal standard for the quantification of Girard’s reagent P
- GC33050 Givinostat (ITF-2357) Givinostat (ITF-2357) (ITF-2357) is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively.
- GC33159 Givinostat hydrochloride (ITF-2357 hydrochloride) Givinostat (ITF-2357) hydrochloride is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively.
- GC12579 GLPG0634 GLPG0634 (GLPG0634) is a selective and orally active JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively.
- GC17222 GLPG0634 analogue GLPG0634 analogue (Compoun 176) is a broad spectrum JAK inhibitor with IC50 values of <100 nM against JAK1, JAK2 and JAK3.
- GC30263 Glucosamine (D-Glucosamine) Glucosamine (D-Glucosamine) (D-Glucosamine (D-Glucosamine)) is an amino sugar and a prominent precursor in the biochemical synthesis of glycosylated proteins and lipids, is used as a dietary supplement.
- GN10669 Glucosamine sulfate
- GC36153 Glucose-conjugated MGMT inhibitor Glucose-conjugated MGMT inhibitor is a potent O6-methylguanine-DNAmethyl-transferase (MGMT) inhibitor, with IC50s of 32 nM in vitro (cell extracts) and 10 nM in HeLa S3 cells.
- GC34595 GN44028 A HIF-1 inhibitor
- GC36168 GNA002 GNA002 is a highly potent, specific and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor with an IC50 of 1.1 μM. GNA002 can specifically and covalently bind to Cys668 within the EZH2-SET domain, triggering EZH2 degradation through COOH terminus of Hsp70-interacting protein (CHIP)-mediated ubiquitination. GNA002 efficiently reduces EZH2-mediated H3K27 trimethylation, reactivates polycomb repressor complex 2 (PRC2)-silenced tumor suppressor genes.
- GC32960 GNE-049 GNE-049 is a highly potent and selective CBP inhibitor with an IC50 of 1.1 nM in TR-FRET assay. GNE-049 also inhibits BRET and BRD4(1) with IC50s of 12 nM and 4200 nM, respectively.
- GC68439 GNE-064
- GC33212 GNE-207 GNE-207 is a potent, selective and orally bioavailable inhibitor of the bromodomain of CBP, with an IC50 of 1 nM, exhibits a selectively index of?>2500-fold against BRD4 (1). GNE-207 shows excellent CBP potency, with an EC50 of 18 nM for MYC expression in MV-4-11 cells.
- GC32747 GNE-272 GNE-272 is a potent and selective CBP/EP300 inhibitor with IC50 values of 0.02, 0.03 and 13 μM for CBP, EP300 and BRD4, respectively. GNE-272 is also a selective in vivo probe for CBP/EP300.