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(49)
- Aurora Kinase(64)
- DNA Methyltransferase(35)
- HDAC(212)
- Histone Acetyltransferases(76)
- Histone Demethylases(110)
- Histone Methyltransferase(239)
- HIF(104)
- JAK(166)
- MBT Domains(0)
- PARP(122)
- Pim(30)
- Protein Ser/Thr Phosphatases(26)
- RNA Polymerase(5)
- Sirtuin(82)
- Sphingosine Kinase-2(1)
- Polycomb repressive complex(2)
- SUMOylation(3)
- PAD(22)
- Epigenetic Reader Domain(246)
- MicroRNA(24)
- Protein Arginine Deiminase(14)
- Chromodomain(1)
- Citrullination(20)
- DNA/RNA Demethylation(2)
- DNA/RNA Methylation(8)
- Histone Deacetylation(44)
- Histones/Histone Peptides(62)
- PHD Domains(1)
- Tandem Tudor & Tudor-like Domains(1)
- PRMT(2)
- Readers(1)
- Small Interfering RNA (siRNA)(1)
- METTL3(2)
- WDR5(1)
- TET Protein(2)
- HuR(1)
- SF3B1(1)
Products for Chromatin/Epigenetics
- Cat.No. Product Name Information
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GC14434
BYK 49187
Potent PARP-1/PARP-2 inhibitor
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GC16130
C 21
Protein arginine methyltransferase 1 (PRMT1) inhibitor
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GC17011
C2 Ceramide
C2 Ceramide (d18:1/2:0), C2 Ceramide ,Ceramide (d18:1/2:0), Cer(18:1/2:0),N-acetoyl-D-erythro-sphingosine
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
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GC62886
Cannabisin F
-
GC12082
Cantharidic Acid (sodium salt)
PP1 and PP2A inhibitor
-
GC73615
CARM1 degrader-1 hydrochloride
CARM1 degrader-1 drochloride is the drochloride salt form of CARM1 degrader-1.
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GC34108
CARM1-IN-1
Protein Arginine Methyltransferase 4/CoactivatorAssociated Arginine Methyltransferase 1 Inhibitor
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).
-
GC73386
CARM1-IN-3
CARM1-IN-3 (compound 17b) is a potent and selective co-activator associated arginine metltransferase (CARM1) inhibitor with IC50 values of 0.07, >25 µM for CARM1 and CARM3, respectively.
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GC73387
CARM1-IN-3 dihydrochloride
CARM1-IN-3 didrochloride (compound 17b) is a potent and selective co-activator associated arginine metltransferase (CARM1) inhibitor with IC50 values of 0.07, >25 µM for CARM1 and CARM3, respectively.
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GC43147
CAY10398
MD 85, PX 089274
CAY10398 is an inhibitor of histone deacetylase (HDAC1) with an IC50 value of 10 μM. -
GC41601
CAY10591
SIRT1 Activator 3, Sirtuin 1 Activator 3
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
HDAC 6 inhibitor, Histone Deacetylase Inhibitor VIII
potent and selective inhibitor of HDAC6
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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.
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GC18949
CAY10677
Icmt Inhibitor 15
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.
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GC43200
CAY10721
CAY10721 is an inhibitor of sirtuin 3 (SIRT3), a class III HDAC (39% SIRT3 inhibition at 200 μM).
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GC43201
CAY10722
CAY10722 is an inhibitor of sirtuin 3 (SIRT3), a class III HDAC (71% inhibition at 200 μM).
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GC43202
CAY10723
AFM30a, AMF30a
CAY10723 is a potent protein arginine deiminase 2 (PAD2) inhibitor and has excellent PAD2-selectivity. -
GC90710
CAY10723 (hydrochloride)
A PAD2 inhibitor
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GC47050
CAY10727
A PAD3 inhibitor
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GC45402
CAY10729 (trifluoroacetate salt) (technical grade)
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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.
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GC47056
CAY10753
A TNKS2 inhibitor
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GC49029
CAY17c
An inhibitor of BRD4 and class I and class IIb HDACs
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GC35621
CBB1003
CBB1003 is a novel histone demethylase LSD1 inhibitor with IC50 of 10.54 uM.
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GC35622
CBB1003 hydrochloride
CBB1003 Hcl is a novel histone demethylase LSD1 inhibitor with IC50 of 10.54 uM.
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GC14151
CBB1007
LSD1 inhibitor,potent and selective
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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).
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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).
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GC14058
CBHA
Histone Deacetylase Inhibitor II,m-Carboxycinnamic Acid bis-Hydroxamide
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
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.
-
GC68841
CBP/p300-IN-10
CBP/p300-IN-10 is an efficient inhibitor of histone acetyltransferases EP300 and CREBBP, with IC50 values of 26 nM and 39 nM, respectively.
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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.
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GC73365
CBP/p300-IN-20
CBP/p300-IN-20 is a potent and selective p300/CBP inhibitor, with a pIC50 of 10.1 for p300.
-
GC38469
CBP/p300-IN-3
CBP/p300-IN-3, a p300/CBP histone acetyltransferase inhibitor, Compound 6, is sourced from patent WO 2019049061 A1.
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GC62330
CC-90010
BMS-986378, 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
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GC11310
CCT129202
An Aurora kinase inhibitor
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GC14566
CCT137690
An inhibitor of Aurora kinases and FLT3
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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).
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GC48982
CD532
An inhibitor of Aurora A kinase activity and the Aurora A-N-Myc protein-protein interaction
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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.
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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
AS-703569; R-763
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)
PRT062070, PRT2070
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. -
GC33028
CF53
CF53 is a highly potent, selective and orally active inhibitor of BET protein, with a Ki of <1 nM, Kd of 2.2 nM and an IC50 of 2 nM for BRD4 BD1. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, very selective over non-BET bromodomain-containing proteins. CF53 shows potent anti-tumor activity both in vitro and in vivo.
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GC65602
CFT8634
CFT8634 is a degrader targeting BRD9 extracted from patent WO2021178920A1 compound 174. CFT8634 can be used for the research of synovial sarcoma and SMARCB1-deleted solid tumors.
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GC35668
CG-200745
CG-200745
CG-200745 (CG-200745) is an orally active, potent pan-HDAC inhibitor which has the hydroxamic acid moiety to bind zinc at the bottom of catalytic pocket. CG-200745 inhibits deacetylation of histone H3 and tubulin. CG-200745 induces the accumulation of p53, promotes p53-dependent transactivation, and enhances the expression of MDM2 and p21 (Waf1/Cip1) proteins. CG-200745 enhances the sensitivity of Gemcitabine-resistant cells to Gemcitabine and 5-Fluorouracil (5-FU; ). CG-200745 induces apoptosis and has anti-tumour effects. -
GC39679
CG347B
CG347B is a selective HDAC6 inhibitor, also involves in synthesis of other metalloenzyme inhibitors.
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GC14936
Chaetocin
Chaetocin was reported to be a nonspecific inhibitor of histone methyl transferase (HMT) such as SUV39H1, thereby affecting gene expression.
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GC11975
CHAPS
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GC64942
CHDI-390576
CHDI-390576, a potent, cell permeable and CNS penetrant class IIa histone deacetylase (HDAC) inhibitor with IC50s of 54 nM, 60 nM, 31 nM, 50 nM for class IIa HDAC4, HDAC5, HDAC7, HDAC9, respectively, shows >500-fold selectivity over class I HDACs (1, 2, 3) and ~150-fold selectivity over HDAC8 and the class IIb HDAC6 isoform.
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GC17405
Chetomin
NSC 289491
An inhibitor of HIF signaling -
GC62145
Chiauranib
CS2164
Chiauranib (CS2164) is an orally active multi-target inhibitor against tumor angiogenesis. Chiauranib potently inhibits the angiogenesis-related kinases (VEGFR1, VEGFR2, VEGFR3, PDGFRα and c-Kit), mitosis-related kinase Aurora B, and chronic inflammation-related kinase CSF-1R, with IC50 values ranging from 1-9 nM. Chiauranib has strongly anticancer effects. -
GC64255
CHIC35
CHIC35, an analog of EX-527, is a potent and selective inhibitor of SIRT1 (IC50=0.124 ?M).
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GC16042
Chidamide
CS 055, HBI 8000, Tucidinostat
Chidamide (Chidamide impurity) is an impurity of Chidamide. Chidamide is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor. -
GN10518
Chitosamine hydrochloride
D-(+)-Glucosamine, GlcN, NSC 234443, NSC 758
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GC45717
Chlamydocin
An HDAC inhibitor
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GN10308
Chlorogenic acid
3OCaffeoylquinic acid, Heriguard, NSC 407296
Chlorogenic acid is a potent neuroprotective agent and also has antiviral,antifungal antioxidant and antitumor properties. CGA is also involved in regulating glucose and lipid metabolism and improving insulin sensitivity. -
GC11652
CHZ868
Type II JAK2 inhibitor
-
GC11539
CI 976
PD 128042
CI 976 (CI 976) is a potent, orally active, and selective inhibitor of ACAT (acyl coenzyme A:cholesterol acyltransferase) with an IC50s of 73 nM. -
GC13408
CI994 (Tacedinaline)
N-Acetyldinaline, Goe 5549, PD 123654, Tacedinaline
An inhibitor of HDAC1, -2, and -3 -
GC15718
CID 2011756
An inhibitor of protein kinase D
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GC18577
CID-2818500
α-Nitrostilbene, NSC 385
An inhibitor of PRMT1 -
GC70438
cis-BG47
cis-BG47 is an cis-isomer of BG47, BG47 is a prototypical histone deacetylases HDAC1 and HDAC2 selective, optoepigenetic probe.
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GC72800
cis-MZ 1 hydrate
cis-MZ 1 drate is a negative control for BRD4-targeted PROTAC MZ 1.
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GC52351
Citrullinated α-Enolase (R8 + R14) (1-19)-biotin Peptide
Citrullinated Enolase-1-biotin, α-Enolase Peptide (Citrulline Residues 8 + 14)
A biotinylated and citrullinated α-enolase peptide -
GC52363
Citrullinated Histone H3 (R2 + R8 + R17) (2-22)-biotin Peptide
Biotin-A-Cit-TKQTA-Cit-KSTGGKAP-Cit-KQLA, Biotin-AXTKQTAXKSTGGKAPXKQLA (X=Citrulline), Citrullinated Histone H3.1-biotin
A biotinylated and citrullinated histone H3 peptide
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GC52367
Citrullinated Vimentin (G146R) (R144 + R146) (139-159)-biotin Peptide
Biotin-GQGKS(Cit)L(Cit)DLYEEEMRELRRQ, Biotin-GQGKSXLXDLYEEEMRELRRQ (X=Citrulline), Citrullinated VIM (G146R) (R144 + R146)-biotin
A biotinylated and citrullinated mutant vimentin peptide -
GC52370
Citrullinated Vimentin (R144) (139-159)-biotin Peptide
Biotin-GQGKS(Cit)LGDLYEEEMRELRRQ, Biotin-GQGKSXLGDLYEEEMRELRRQ (X=Citrulline), Citrullinated VIM (R144)-biotin
A biotinylated and citrullinated vimentin peptide -
GC40255
Citrulline-specific Probe-biotin
Citrulline-specific probe-biotin is an affinity probe that allows for detection or immobilization of citrullinated proteins through interaction with the biotin ligand.
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GC43275
Citrulline-specific Probe-Rhodamine
Rhodamine Phenylglyoxal, RhPG
Protein arginine deiminases (PADs) catalyze the posttranslational modification of arginine residues on proteins to form citrulline, which plays a large role in regulating gene expression. -
GC39485
CK2/ERK8-IN-1
A dual inhibitor of CK2 and ERK8
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GC35706
Cl-amidine
Cl-amidine (N-α-benzoyl-N5-(2-chloro-1-iminoethyl)-l-ornithine amide), is a PAD4 inactivator with enhanced potency.
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GC18925
Cl-Amidine (hydrochloride)
Cl-amidine is an inhibitor of protein arginine deiminases (PAD; IC50s = 0.8, 6.2, and 5.9 uM for PAD1, PAD3, and PAD4 in vitro, respectively).
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GC11032
Cl-Amidine (trifluoroacetate salt)
Cl-Amidine (trifluoroacetate salt) is a multi-targeting peptidylarginine deminase (PAD) inhibitor with the functional group RC(NR)NR2 that inhibits PAD1 (IC50=0.8μM), PAD3 (IC50=6.2μM), and PAD4 (IC50=5.9μM) with 15min half-time.
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GC73933
CM-1758
CM-1758 is a histone deacetylase (HDAC) inhibitor.
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GC12367
CM-272
CM-272 is a first-in-class reversible dual inhibitor against G9a and DNMTs with IC50 values of 8 nM and 382 nM, respectively [1].
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GC33320
CM-579
CM-579 is a first-in-class reversible, dual inhibitor of G9a and DNMT, with IC50 values of 16 nM, 32 nM for G9a and DNMT, respectively. Has potent in vitro cellular activity in a wide range of cancer cells.
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GC35714
CM-579 trihydrochloride
CM-579 trihydrochloride is a first-in-class reversible, dual inhibitor of G9a and DNMT, with IC50 values of 16 nM, 32 nM for G9a and DNMT, respectively. Has potent in vitro cellular activity in a wide range of cancer cells.
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GC65426
CM-675
CM-675 is a dual phosphodiesterase 5 (PDE5) and class I histone deacetylases-selective inhibitor, with IC50 values of 114 nM and 673 nM for PDE5 and HDAC1, respectively.
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GC39665
CMP-5
CMP-5 is a potent, specific, and selective PRMT5 inhibitor, while displays no activity against PRMT1, PRMT4, and PRMT7 enzymes. CMP-5 selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. CMP-5 prevents Epstein-Barr virus (EBV)-driven B-lymphocyte transformation but leaving normal B cells unaffected.
-
GC73027
Cobomarsen sodium
MRG-106 sodium
Cobomarsen sodium is an oligonucleotide inhibitor of miR-155. -
GC34165
Corin
Corin is a dual inhibitor of histone lysine specific demethylase (LSD1) and histone deacetylase (HDAC), with a Ki(inact) of 110 nM for LSD1 and an IC50 of 147 nM for HDAC1.
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GC43318
coumarin-SAHA
coumarin-Suberoylanilide Hydroxamic Acid
Suberoylanilide hydroxamic acid (SAHA) is a class I and class II histone deacetylase (HDAC) inhibitor that binds directly to the catalytic site of the enzyme thereby blocking substrate access.
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GC62908
Coumermycin A1
Coumermycin A1 is a JAK2 signal activator.
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GC25304
CP2
CP2 is a cyclic peptide that inhibits the JmjC histone demethylases KDM4 with IC50 values of 42 nM and 29 nM for KDM4A and KDM4C, respectively.
-
GC16298
CPI-1205
EZH2 inhibitor
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GC62669
CPI-1612
CPI-1612 is a highly potent, orally active EP300/CBP histone acetyltransferase (HAT) inhibitor with an IC50 of 8.1 nM for EP300 HAT. CPI-1612 has an anticancer activity.
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GC16599
CPI-169
EZH2 inhibitor
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GC14699
CPI-203
BET bromodomain inhibitor
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GC43320
CPI-268456
CPI-268456 (compound 141) is a potent BRD4 inhibitor with an IC50 of <0.5 μM.
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GC10021
CPI-360
EZH2 inhibitor
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GC10774
CPI-455
KDM5 inhibitor