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
- GC12171 BIX 01294 An inhibitor of G9a histone methyltransferase
- 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.
- GC33301 BIX-01338 hydrate (BIX01338 hydrate) BIX-01338 hydrate (BIX01338 hydrate) is a histone lysine methyltransferase inhibitor.
- GC42944 BIX01294 (hydrochloride hydrate) The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression.
- GC16114 Bizine LSD1 inhibitor
- GC12822 BML-210(CAY10433) BML-210(CAY10433) is a novel HDAC inhibitor, and its mechanism of action has not been characterized.
- 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.
- GC15932 BMN 673 A PARP inhibitor
- GC10920 BMN-673 8R,9S
- GC50633 BMS 986094 Prodrug of HCV RNA polymerase inhibitor 2'-C-methyl guanosine triphosphate; potent HCV replication inhibitor
- GC32028 BMS-066 BMS-066 is an IKKβ/Tyk2 pseudokinase inhibitor, with IC50s of 9 nM and 72 nM, respectively.
- 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.
- GC12454 BMS-911543 A potent, selective JAK2 inhibitor
- GC32812 BMS-986158 A BET bromodomain inhibitor
- 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.
- 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.
- GC46935 Bobcat 339 A TET1 and TET2 inhibitor
- 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.
-
GC11641
Boc-Lys(Ac)-AMC
GPCR G2A/GPR132 agonist
- 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.
- GC67921 Bomedemstat ditosylate
- 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.
- GC48620 BPKDi A PKD inhibitor
- GC64538 BPTF-IN-BZ1 BPTF-IN-BZ1, a BPTF inhibitor, possesses a high potency (Kd = 6.3 nM).
- 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.
- 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%.
- 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.
- 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.
- GC33331 BRD 4354 BRD 4354 is a moderately potent inhibitor of HDAC5 and HDAC9, with IC50s of 0.85 and 1.88 μM, respectively.
- 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.
- GC50322 BRD 9757 Potent and selective HDAC6 inhibitor
- GC38742 BRD-6929 An HDAC1 and HDAC2 inhibitor
- 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.
- 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.
- 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.
- 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.
- 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).
- 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)
- GC10259 BRD4770 novel G9a(EHMT2) inhibitor
- 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.
- GC13088 BRD6688 HDAC inhibitor
- 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).
- GC12484 BRD73954 potent and selective HDAC inhibitor
- GC32988 BRD9539 An inhibitor of EHMT2/G9a and PRC2 in enzyme assays
- 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.
- GC35554 Brevilin A A sesquiterpene lactone with anticancer activity
- GC64541 BRM/BRG1 ATP Inhibitor-2 BRM/BRG1 ATP Inhibitor-2 is a BRG1/BRM ATPase inhibitor for the treatment of BAF-related disorders.
- GC35557 Bromodomain IN-1 Bromodomain IN-1 is a Bromodomain inhibitor extracted from patent WO2016069578A1, compound 4 .
- GC16531 Bromodomain Inhibitor, (+)-JQ1 A selective inhibitor of BET bromodomains
- GC35558 Bromodomain inhibitor-8 Bromodomain inhibitor-8 (Intermediate 21) is a BET bromodomain inhibitor for treating autoimmune and inflammatory diseases.
- GC10402 Bromosporine A non-specific bromodomain inhibitor
- GC15410 Bufexamac COX inhibitor
- GC64761 Butyric acid-13C1
- GC46104 Butyric Acid-d7 An internal standard for the quantification of sodium butyrate
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GC10226
Butyrolactone 3
histone acetyltransferase Gcn5 inhibitor
- GC10690 BYK 204165 A selective inhibitor of PARP1
- GC14434 BYK 49187 Potent PARP-1/PARP-2 inhibitor
- GC16130 C 21 Protein arginine methyltransferase 1 (PRMT1) inhibitor
- GC17011 C2 Ceramide A cell-permeable analog of naturally occurring ceramides
- 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..
- GC12005 C7280948 Novel PRMT1 inhibitor
- GC62886 Cannabisin F
- GC12082 Cantharidic Acid (sodium salt) PP1 and PP2A inhibitor
- GC34108 CARM1-IN-1 A selective inhibitor of PRMT4/CARM1
- 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).
- GC43147 CAY10398 CAY10398 is an inhibitor of histone deacetylase (HDAC1) with an IC50 value of 10 μM.
- GC41601 CAY10591 CAY10591 is a potent activator of Sirt1 and suppresses TNF-α in a dose-dependent manner.
- 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.
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GC12971
CAY10603
potent and selective inhibitor of HDAC6
- 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.
- 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.
- 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.
- GC43200 CAY10721 CAY10721 is an inhibitor of sirtuin 3 (SIRT3), a class III HDAC (39% SIRT3 inhibition at 200 μM).
- GC43201 CAY10722 CAY10722 is an inhibitor of sirtuin 3 (SIRT3), a class III HDAC (71% inhibition at 200 μM).
- GC43202 CAY10723 CAY10723 is a potent protein arginine deiminase 2 (PAD2) inhibitor and has excellent PAD2-selectivity.
- GC47050 CAY10727 A PAD3 inhibitor
- 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.
- GC47056 CAY10753 A TNKS2 inhibitor
- GC49029 CAY17c An inhibitor of BRD4 and class I and class IIb HDACs
- GC35621 CBB1003 CBB1003 is a novel histone demethylase LSD1 inhibitor with IC50 of 10.54 uM.
- GC35622 CBB1003 hydrochloride CBB1003 Hcl is a novel histone demethylase LSD1 inhibitor with IC50 of 10.54 uM.
- GC14151 CBB1007 LSD1 inhibitor,potent and selective
- 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).
- 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).
- 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.
- 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.
- GC61577 CBP/p300-IN-1 CBP/p300-IN-1 is a CBP/EP300 bromodomain inhibitor.
- 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.
- GC38469 CBP/p300-IN-3 CBP/p300-IN-3, a p300/CBP histone acetyltransferase inhibitor, Compound 6, is sourced from patent WO 2019049061 A1.
- 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.
- GC12891 CCT007093 PPM1D inhibitor
- GC11310 CCT129202 An Aurora kinase inhibitor
- GC14566 CCT137690 An inhibitor of Aurora kinases and FLT3
- 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).
- GC48982 CD532 An inhibitor of Aurora A kinase activity and the Aurora A-N-Myc protein-protein interaction
- 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.
- 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).
- 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.
- GC12083 CEP-33779 A potent, orally available inhibitor of JAK2
- 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.