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
- GC16509 Adox Adox, a purine nucleoside analogue, is a potent inhibitor of S-Adenosylhomocysteine hydrolase (SAHH) (Ki=3.3 nM). Adenosine Dialdehyde exhibits potent anti-tumor activity in vivo and can be used for the cancer research.
- GC64527 ADTL-SA1215 ADTL-SA1215 is a first-in-class specific small-molecule activator of SIRT3 that modulates autophagy in triple negative breast cancer.
- GC65330 AES-135 AES-135, a hydroxamic acid-based pan-HDAC inhibitor, prolongs survival in an orthotopic mouse model of pancreatic cancer. AES-135 inhibits HDAC3, HDAC6, HDAC8, and HDAC11 with IC50s ranging from 190-1100 nM.
- GC48775 AES-350 An inhibitor of class I and class IIb HDACs
- GC66379 AFM-30a hydrochloride AFM-30a hydrochloride is a potent protein arginine deiminase 2 (PAD2) inhibitor and has excellent PAD2-selectivity. AFM-30a hydrochloride binds to PAD2 with an EC50 value of 9.5 μM. AFM-30a hydrochloride also inhibits H3 citrullination with an EC50 value of 0.4 μM. AFM-30a hydrochloride can be used for the research of certain cancers and a variety of autoimmune diseases including rheumatoid arthritis (RA), multiple sclerosis, lupus, and ulcerative colitis.
- GC33416 AFP464 AFP464 (NSC710464 free base), is an active HIF-1α inhibitor with an IC50 of 0.25 μM, also is a potent aryl hydrocarbon receptor (AhR) activator.
- GC16318 AG-14361 A PARP1 inhibitor
-
GC17881
AGK 2
AGK2 is a selective SIRT2 inhibitor, with an IC50 of 3.
- GC15931 AGK7 cell-permeable, selective inhibitor of SIRT2
- GN10413 Agrimol B
-
GC10676
AK-7
selective and brain-permeable SIRT2 inhibitor
- GC62277 AKB-6899 Ro24-7429 is a potent and orally active HIV-1 transactivator protein Tat antagonist. Ro24-7429 is also a runt-related transcription factor 1 (RUNX1) inhibitor. Ro24-7429 has anti-HIV, antifibrotic and anti-inflammatory effects.
- GC62433 AKI603 AKI603 is an inhibitor of Aurora kinase A (AurA), with an IC50 of 12.3 nM. AKI603 is developed to overcome resistance mediated by BCR-ABL-T315I mutation. AKI603 exhibits strong anti-proliferative activity in leukemic cells.
- GC17344 Alexidine dihydrochloride An alkyl bis(biguanide) antiseptic
- GC49393 all-trans-13,14-Dihydroretinol A metabolite of all-trans retinoic acid
- GC35297 Alobresib A BET bromodomain inhibitor
- GC67984 Alteminostat
- GC13198 AMG-900 A selective pan-Aurora kinase inhibitor
- GC17275 AMI-1 A cell permeable inhibitor of PRMTs
- GC39840 AMI-1 free acid AMI-1 free acid is a potent, cell-permeable and reversible inhibitor of protein arginine N-methyltransferases (PRMTs), with IC50s of 8.8 μM and 3.0 μM for human PRMT1 and yeast-Hmt1p, respectively. AMI-1 free acid exerts PRMTs inhibitory effects by blocking peptide-substrate binding.
- GC17546 AMI5 Eosin Y (disodium) is a soluble acid red dye molecule.
- GC42785 Amifostine (hydrate) Amifostine (hydrate) (WR2721 trihydrate) is a broad-spectrum cytoprotective agent and a radioprotector. Amifostine (hydrate) selectively protects normal tissues from damage caused by radiation and chemotherapy. Amifostine (hydrate) is potent hypoxia-inducible factor-α1 (HIF-α1) and p53 inducer. Amifostine (hydrate) protects cells from damage by scavenging oxygen-derived free radicals. Amifostine (hydrate) reduces renal toxicity and has antiangiogenic action.
- GC42790 Amodiaquine Amodiaquine is an aminoquinoline antimalarial compound.
- GC60579 Amodiaquine dihydrochloride Amodiaquine dihydrochloride (Amodiaquin dihydrochloride), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor with a Ki of 18.6 nM.
- GC10905 Amodiaquine dihydrochloride dihydrate histamine N-methyl transferase inhibitor
- GC67912 Amredobresib
-
GC17284
Anacardic acid
A histone acetyltransferase inhibitor
- GC40674 APHA Compound 8 A class I and II HDAC inhibitor
-
GC12961
Apicidin
A cell-permeable HDAC inhibitor
-
GC14590
AR-42 (OSU-HDAC42)
HDAC inhibitor,novel and potent
- GC32685 ARV-771 ARV-771 is a potent BET PROTAC based on E3 ligase von Hippel-Lindau with Kds of 34 nM, 4.7 nM, 8.3 nM, 7.6 nM, 9.6 nM, and 7.6 nM for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1), and BRD4(2), respectively.
- GC19038 ARV-825 ARV-825 is a BRD4 Inhibitor based on PROTAC technology.
- GC65918 AS-85 AS-85 is a potent ASH1L histone methyltransferase inhibitor (IC50=0.6 μM) with anti-leukemic activity. AS-85 strongly binds to the ASH1L SET domain, with the Kd value of 0.78μM.
- GC62615 AS-99 AS-99 is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50=0.79μM, Kd=0.89μM) with anti-leukemic activity. AS-99 blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo.
- GC62849 AS-99 TFA AS-99 TFA is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50=?0.79??M, Kd=?0.89??M) with anti-leukemic activity. AS-99 TFA blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo.
- GC17820 AS8351 histone demethylase inhibitor
- GC10638 AT9283 A broad spectrum kinase inhibitor
- GC50066 Atiprimod dihydrochloride JAK2 inhibitor
- GC46892 ATRA-BA Hybrid A prodrug form of all-trans retinoic acid and butyric acid
- GN10627 Atractylenolide I
- GC64271 AU-15330 AU-15330 is a proteolysis-targeting chimera (PROTAC) degrader of the SWI/SNF ATPase subunits, SMARCA2 and SMARCA4. AU-15330 induces potent inhibition of tumour growth in xenograft models of prostate cancer and synergizes with the AR antagonist enzalutamide. AU-15330 induces disease remission in castration-resistant prostate cancer (CRPC) models without toxicity.
- GC39699 Aurintricarboxylic acid Aurintricarboxylic acid is a nanomolar-potency, allosteric antagonist with selectivity towards αβ-methylene-ATP-sensitive P2X1Rs and P2X3Rs, with IC50s of 8.6 nM and 72.9 nM for rP2X1R and rP2X3R, respectively.
- GC13332 Aurora A Inhibitor I A potent and selective inhibitor of Aurora A kinase
- GC33379 Aurora B inhibitor 1 Aurora B inhibitor 1 is an Aurora B (Aurora-1) inhibitor extracted from patent WO2007059299A1, compound 1-3, has a Ki value of <0.010 uM.
- GC38441 Aurora Kinase Inhibitor 3 A potent inhibitor of Aurora A kinase
- GC40667 Aurora Kinase Inhibitor II Aurora Kinase Inhibitor II is a selective and ATP-competitive Aurora kinase inhibitor with IC50s of 310 nM and 240 nM for Aurora A and Aurora B, respectively.
- GC15711 Aurora Kinase Inhibitor III Aurora Kinase Inhibitor III is a strong and selective Aurora A kinase inhibitor with an IC50 of 42 nM, and weakly inhibits EGFR with an IC50 of >10 μM.
- GC67899 Aurora kinase inhibitor-8
- GC13433 AZ 960 A JAK2 inhibitor
- GC65899 AZ3391 AZ3391 is a potent inhibitor of PARP. AZ3391 is a quinoxaline derivative. PARP family of enzymes play an important role in a number of cellular processes, such as replication, recombination, chromatin remodeling, and DNA damage repair. AZ3391 has the potential for the research of diseases and conditions occurring in tissues in the central nervous system, such as the brain and spinal cord (extracted from patent WO2021260092A1, compound 23).
- GC13744 AZ505 SMYD2 inhibitor,potent and selective
- GC13103 AZ505 ditrifluoroacetate SMYD2 inhibitor
- GC64124 AZ506 AZ506 is a potent SMYD2 inhibitor with an IC50 of 17 nM. AZ506 inhibits SMYD2 methyltransferase activity in cells, leading to a decrease in the SMYD2-mediated methylation signal.
- GC16725 AZ6102 TNKS1/2 inhibitor
- GC46900 AZ9482 A PARP inhibitor
- GC48971 AZD 1152 (hydrochloride) A prodrug for a potent Aurora B inhibitor
- GC13014 AZD 5153 orally available, bivalent inhibitor of the bromodomain and extraterminal (BET) protein BRD4.
- GC14709 AZD1152
- GC12660 AZD1208 A pan-Pim kinase inhibitor
- GC35447 AZD1208 hydrochloride AZD1208 hydrochloride is an orally bioavailable, highly selective PIM kinases inhibitor.
- GC12504 AZD1480 A potent JAK2 inhibitor
- GC17965 AZD2461 A PARP inhibitor
- GC35448 AZD5153 6-Hydroxy-2-naphthoic acid AZD5153 6-Hydroxy-2-naphthoic acid is the 6-Hydroxy-2-naphthoic acid of AZD5153. AZD5153 is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor; disrupts BRD4 with an IC50 of 1.7 nM.
- GC62310 AZD5305 AZD5305 is a potent, selective and oral active PARP inhibitor. AZD5305 is potent and efficacious in animal xenografts and PDX models.
- GC14955 Barasertib (AZD1152-HQPA) A selective Aurora kinase B inhibitor
- GC11572 Bardoxolone methyl A synthetic triterpenoid with potent anticancer and antidiabetic activity
- GC14844 Baricitinib (LY3009104, INCB028050) A JAK1 and JAK2 inhibitor
- GC13830 Baricitinib phosphate A JAK1 and JAK2 inhibitor
- GC12698 BAY 87-2243 A HIF-1 inhibitor,potent and selective
- GC18508 BAY-299 BAY-299 is a potent and selective inhibitor of the bromodomain and PHD finger-containing (BRPF) family protein BRD1 (IC50 = 6 nM), also known as BRPF2, and the second bromodomain of transcription initiation factor TFIID subunits 1 (TAF1; IC50 = 13 nM).
-
GC18159
BAY-598
A potent and selective SMYD2 inhibitor
- GC45389 BAY-6035
- GC33104 BAY1238097 BAY1238097 is a potent and selective inhibitor of BET binding to histones and has strong anti-proliferative activity in different AML (acute myeloid leukemia) and MM (multiple myeloma) models through down-regulation of c-Myc levels and its downstream transcriptome (IC50 <100 nM).
- GC63694 BAZ1A-IN-1 BAZ1A-IN-1 is a potent inhibitor of BAZ1A (bromodomain-containing protein). BAZ1A-IN-1 shows a KD value of 0.52 μM against BAZ1A bromodomain. BAZ1A-IN-1 shows good anti-viability activity against cancer cell lines expressing a high level of BAZ1A, but weak or no activity against cancer cells with a low expression level of BAZ1A.
- GC15175 BAZ2-ICR Selective BAZ2 bromodomain inhibitor
- GC35480 BB-Cl-Amidine hydrochloride BB-Cl-Amidine hydrochloride is a peptidylarginine deminase (PAD) inhibitor.
- GC42910 BB-F-Yne BB-F-Yne is a cell-permeable derivative of the protein arginine diminase (PAD) inhibitor BB-Cl-amidine that contains an alkyne moiety for use in click chemistry reactions.
-
GC18161
BCI-121
A substrate-competitive SMYD3 inhibitor?
-
GC15962
Belinostat (PXD101)
Belinostat is an effective HDAC inhibitor with an IC50 of 27 nM in HeLa cell extracts.
- GC12844 Benzamide poly (ADP-ribose) synthetase inhibitor
- GC30763 Benzenebutyric acid (4-Phenylbutyric acid) Benzenebutyric acid (4-Phenylbutyric acid) (4-PBA) is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research.
- GC16299 BET bromodomain inhibitor Potent and selective inhibitor for BRD4
- GC63528 BET bromodomain inhibitor 1 BET bromodomain inhibitor 1 is an orally active, selective bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50 of 2.6 nM for BRD4. BET bromodomain inhibitor 1 binds to BRD2(2), BRD3(2), BRD4(1), BRD4(2), and BRDT(2) with high affinities (Kd values of 1.3 nM, 1.0 nM, 3.0 nM, 1.6 nM, 2.1 nM, respectively). bromodomain inhibitor 1 has anti-cancer activity.
- GC35505 BET-BAY 002 BET-BAY 002 is a potent BET inhibitor; shows efficacy in a multiple myeloma model.
- GC35506 BET-BAY 002 S enantiomer
- GC31831 BET-IN-1 BET-IN-1 is a pan-inhibitor of all eight BET bromodomains, and selectivity over other representative bromodomain-containing proteins.
- GC65506 BETd-246 BETd-246 is a second-generation and PROTAC-based BET bromodomain (BRD) inhibitor connected by ligands for Cereblon and BET, exhibiting superior selectivity, potency and antitumor activity.
- GC32791 BETd-260 (ZBC 260) BETd-260 (ZBC 260) (ZBC 260) is a PROTAC connected by ligands for Cereblon and BET, with as low as 30 pM against BRD4 protein in RS4;11 leukemia cell line. BETd-260 (ZBC 260) potently suppresses cell viability and robustly induces apoptosis in hepatocellular carcinoma (HCC) cells.
- GC12074 BG45 Novel HDAC3-selective inhibitor
- GC14380 BGP-15 PARP inhibitor
- GC12450 BI 2536 A potent inhibitor of Plk1
- GC50540 BI 9321 Nuclear receptor-binding SET domain (NSD) 3 antagonist; selectively binds PWWP1 domain
- GC16726 BI-7273 BRD9 bromodomain inhibitor
- GC17828 BI-847325 dual inhibitor of MEK and Aurora kinases
- GC39663 BI-9321 trihydrochloride BI-9321 trihydrochloride is a potent, selective and cellular active nuclear receptor-binding SET domain 3 (NSD3)-PWWP1 domain antagonist with a Kd value of 166 nM. BI-9321 trihydrochloride is inactive against NSD2-PWWP1 and NSD3-PWWP2. BI-9321 trihydrochloride specifically disrupts histone interactions of the NSD3-PWWP1 domain with an IC50 of 1.2 μM in U2OS cells.
- GC16817 BI-9564 BRD9/7 specific inhibitor
- GC42933 Binucleine 2 Binucleine 2 is an isoform-specific and ATP-competitive inhibitor of Drosophila Aurora B kinase (Ki = 0.36 μM), a kinase involved in cell division.
- GC64789 Biotinylated-JQ1 Biotinylated-JQ1 (Biotin-JQ1) is a biotinylated derivative of JQ1 with high affinity for the bromodomain of BRD4. Biotinylated-JQ1 inhibits MM1.S multiple myeloma cells proliferation with the EC50?of 0.4 μM.
- GC25139 Biphenyl-4-sulfonyl chloride Biphenyl-4-sulfonyl chloride (p-Phenylbenzenesulfonyl, 4-Phenylbenzenesulfonyl, p-Biphenylsulfonyl) is a HDAC inhibitor with synthetic applications in palladium-catalyzed desulfitative C-arylation.
- GC48463 Bisubstrate Inhibitor 78 An inhibitor of NNMT