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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.
Epigenetics Target Files
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UNC 1215
UNC 1215 is a potent inhibitor of L3MBTL3 methyllysine (Kme) reader domain (IC50 = 40 nM; Kd = 120 nM), which displays >100-fold selectivity over a panel of histone methyltransferases, kinases, ion channels and 7-TM receptors. Learn MoreStarting at: $149.00
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Galloflavin
Galloflavin is an inhibitor of human lactate dehydrogenase (LDH) (Ki values are 5.46 and 15.1 μM for LDH-A and LDH-B, respectively, in competition with pyruvate), which inhibits lactate production and decreases ATP synthesis in PLD/PRF/5 cells. Learn MoreStarting at: $109.00
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GPP 78 hydrochloride
GPP 78 hydrochloride is an inhibitor of nicotinamide phosphoribosyltransferase (NMPRTase); potently depletes NAD levels and exhibits cytotoxicity in vitro (IC50 values are 3.0 and 3.8 nM respectively). Learn MoreStarting at: $169.00
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I-CBP 112
I-CBP 112 is a CREBBP/EP300 bromodomain inhibitor (IC50 values are 0.142-0.17 and 0.625 μM for CREBBP and EP300 respectively). Learn MoreStarting at: $199.00
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TCS HDAC6 20b
TCS HDAC6 20b is a selective inhibitor of histone deacetylase 6 (HDAC6) that inhibits HCT116 growth in combination with taxol. Learn MoreStarting at: $149.00
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KD 5170
KD 5170 is a histone deacetylase (HDAC) inhibitor that exhibits broad spectrum inhibition of HDAC classes I and II in assays using purified recombinant human isoforms. Learn MoreStarting at: $139.00
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TC-H 106
TC-H 106 is a class I histone deacetylase (HDAC) inhibitor with IC50 values of 150, 370, 760 and 5000 nM for HDAC1, HDAC3, HDAC2 and HDAC8 respectively. Learn MoreStarting at: $125.00
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NCH 51
NCH 51 is a histone deacetylase (HDAC) inhibitor that inhibits growth of various cancer cells in vitro. Learn MoreStarting at: $115.00
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NSC 3852
NSC 3852 is a histone deacetylase inhibitor. Causes cell differentiation and antiproliferative activity in MCF-7 human breast cancer cells in vitro and displays antitumor activity in vivo. Learn MoreStarting at: $45.00
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M 344
Histone deacetylase inhibitor (IC50 = 100 nM) which induces terminal cell differentiation and causes an increase in hyperacetylated histone H4. Learn MoreStarting at: $55.00
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Sodium 4-Phenylbutyrate
Sodium 4-Phenylbutyrate is a histone deacetylase inhibitor that displays anticancer activity. Learn MoreStarting at: $65.00
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Tubacin
Tubacin is a selective inhibitor of HDAC6 which inhibits the second deacetylase domain (DD2). Learn MoreStarting at: $160.00
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UNC 0224
UNC 0224 is a potent inhibitor of G9a histone lysine methyltransferase (IC50 = 15 nM). Learn MoreStarting at: $135.00
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PSB 0777 ammonium salt
PSB 0777 ammonium salt is a potent adenosine A2A receptor full agonist (Ki = 44.4 nM for rat brain striatal A2A receptors), which exhibits subtype selectivity for A2A receptors over A1, A2B and A3 receptors (Ki ≥ 10 000 nM for rat A1, human A2B and human A3 receptors). Learn MoreStarting at: $169.00
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NSC 33994
NSC 33994 is a selective inhibitor of JAK2 with an IC50 value of 60 nM. Learn MoreStarting at: $139.00
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ZM 39923 hydrochloride
ZM 39923 hydrochloride is a potent, selective inhibitor of Janus tyrosine kinase 3 (JAK3) with pIC50 values of 7.1, 5.6, 4.4, and < 5.0 for JAK3, EGFR, JAK1 and CDK4 respectively. Learn MoreStarting at: $119.00
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1,2,3,4,5,6-Hexabromocyclohexane
1,2,3,4,5,6-Hexabromocyclohexane potently and directly inhibits JAK2 tyrosine kinase autophosphorylation, specifically inhibiting ligand-dependent JAK2 activation. Learn MoreStarting at: $75.00
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TCS 21311
TCS 21311 is a potent JAK3 inhibitor (IC50 = 8 nM), which inhibits GSK-3β, PKCα and PKCθ (IC50 values are 3, 13 and 68 nM respectively). Learn MoreStarting at: $155.00
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ZM 449829
Potent is a selective inhibitor of Janus tyrosine kinase 3 (JAK3), which binds competitively to the JAK3 ATP site. And inhibits STAT-5 phosphorylation and T-cell proliferation. Learn MoreStarting at: $89.00
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Cucurbitacin I
Cucurbitacin I is a selective inhibitor of STAT3/JAK2 signaling, which inhibits the activation of STAT3 and JAK2 and displays no activity on Src, Akt, ERK and JNK. Learn MoreStarting at: $169.00
