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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  • NSC 87877

    NSC 87877 is a potent inhibitor of shp2 and shp1 protein tyrosine phosphatases (PTP). NSC 87877 blocks epidermal growth factor receptor-induced activation of Ras and ERK1/2 in HEK293 cells, stimulates store-operated calcium entry in response to thrombin in platelets, and increased acetylcholine receptor clustering in myotubes. Learn More

    Starting at: $95.00

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  • BVT 948

    BVT 948 is a non-competitive, cell-permeable inhibitor of protein tyrosine phosphatases (PTPs) (IC50 = 0.09 - 1.7 μM); displays irreversible inhibition through catalysis of the hydrogen peroxide-dependent oxidation of PTP. Learn More

    Starting at: $95.00

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  • TCS 401

    TCS 401 is a selective inhibitor of protein-tyrosine phosphatase 1B (PTP1B) (Ki values are 0.29, 59, 560, 1100, > 2000, > 2000 and > 2000 μM for PTP1B, CD45 D1D2, PTPβ, PTPε D1, SHP-1, PTPα D1 and LAR D1D2 respectively). Learn More

    Starting at: $139.00

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  • Alexidine dihydrochloride

    Alexidine dihydrochloride is a selective inhibitor of protein tyrosine phosphatases localized to mitochondrion 1 (PTPMT1) (IC50 = 1.08 μM in vitro). Learn More

    Starting at: $70.00

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  • Okadaic acid

    Okadaic acid is a potent inhibitor of protein phosphatase 1 with an IC50 value of 3 nM) and protein phosphatase 2A with an IC50 value of 0.2-1 nM. Learn More

    Starting at: $89.00

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  • Sanguinarine chloride

    Sanguinarine chloride is an inhibitor of protein phosphatase 2C (PP2C), selective over PP1, PP2A and PP2B in vitro. Learn More

    Starting at: $99.00

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  • INCA-6

    INCA-6 is an inhibitor of interaction between calcineurin and its substrate nuclear factor of activated T cells (NFAT); blocks at the substrate recognition site but not at the catalytic site (Kd = 0.8 mM). Learn More

    Starting at: $95.00

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  • Ceramide

    Ceramide is a potent modulator of cell proliferation and differentiation, which activates protein phosphatase-1 (PP1) and -2A (PP2A), as well as ceramide-activated protein phosphatase (CAPP) in vitro. Learn More

    Starting at: $95.00

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  • PIM-1 Inhibitor 2

    PIM-1 Inhibitor 2 is a potent Pim-1 kinase inhibitor (Ki = 91 nM). Learn More

    Starting at: $125.00

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  • TCS PIM-1 1

    TCS PIM-1 1 is an ATP-competitive Pim-1 kinase inhibitor that displays selectivity over Pim-2 and MEK1/2 (IC50 values are 50, > 20000 and > 20000 nM for Pim-1, Pim-2 and MEK1/2 respectively). Learn More

    Starting at: $109.00

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  • SGC 0946

    SGC 0946 is a potent DOT1L methyltransferase inhibitor (KD = 0.06 nM, IC50 = 0.3 nM in a radioactive assay) which blocks H3K79 methylation in A431 cells and MCF10A cells (IC50 values are 2.65 and 8.8 nM respectively). Learn More

    Starting at: $199.00

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  • UNC 926 hydrochloride

    UNC 926 hydrochloride is a methyl-lysine (Kme) reader domain inhibitor; binds to the MBT domain of the L3MBTL1 protein (Kd = 3.9 μM), which selectively inhibits the L3MBTL13XMBT-H4K20me1 interaction in a peptide pull down assay. Learn More

    Starting at: $110.00

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  • NSC 33994

    NSC 33994 is a selective inhibitor of JAK2 with an IC50 value of 60 nM. Learn More

    Starting 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 More

    Starting 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 More

    Starting 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 More

    Starting 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 More

    Starting 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 More

    Starting at: $169.00

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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 More

    Starting at: $169.00

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  • UNC 0224

    UNC 0224 is a potent inhibitor of G9a histone lysine methyltransferase (IC50 = 15 nM). Learn More

    Starting at: $135.00

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