96 Well Format Sample Storage Tube With Screw Cap and Optional 2D Barcode

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Product Use Citation

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HTS Facility Partners

Customer Product Validation

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Product Description

Description & Advantages

    • A unique collection of 151 small molecule modulators (inhibitors and activators) with biological activity used for epigenetics research and associated assays. A variety of structurally and mechanistically different compounds are included
    • A valuable tool for chemical genomics, epigenetic target identification in pharmacogenomics, and other biological applications
    • This library contains inhibitors of epigenetic enzymes including Histone Deacetylase (HDACs), SIRTs, Lysine demethylases, Histone Acetyltransferases (HATs), DNA Methyltransferase (Dnmts), and SIRTs activators
    • Structurally diverse, medicinally active, and cell permeable
    • Rich documentation with structure, IC50, and customer reviews
    • NMR and HPLC validated to ensure the highest purity

Product Details

Formulation: A collection of 151 small molecule modulators (inhibitors and activators) supplied as pre-dissolved DMSO solutions
Container: 96 Well Format Sample Storage Tube With Screw Cap and Optional 2D Barcode
Stability:
12 months -20°C in DMSO
24 months -80°C in DMSO
Shipping: Blue ice
Packaging: Inert gas

Epigenetics Compound Library Contents

Download the Epigenetics Compound Library - XLSX Download the Epigenetics Compound Library - SDF

Contents are for reference only and are subject to change without notice.

Epigenetics Compound Library Composition

Customer Product Validation (10)

AS-605240 Review
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Rating
Source Nat Biotechnol ,2011, 29, 255-265. Vorinostat (SAHA, MK0683) purchased from Selleck
Method Immunofluorescence analysis
Cell Lines K562 cells
Concentrations 5 µM
Incubation Time 6 h
Results SAHA and other nonselective HDAC inhibitors increased steady-state acetylation of tubulin and histones manifested by the staining of acetylated microtubules and punctuate nuclear staining of acetylated histone.

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Rating
Source Nature, 2014, 508(7494), 118-22. Barasertib (AZD1152-HQPA) purchased from Selleck
Method Long-term cell proliferation assays
Cell Lines A375-SOX10KD cells
Concentrations 0.5 uM
Incubation Time 4 weeks
Results Compared with controls, treatment of A375-SOX10KD cells with a combination of both vemurafenib and GDC0941 lead to proliferation arrest.

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Rating
Source Nature, 2011, 471, 235-9. Vorinostat (SAHA, MK0683) purchased from Selleck
Method MTT cell viability assay
Cell Lines T-ALL cell lines
Concentrations 0.01-100 uM
Incubation Time 72 h
Results It examined responsiveness to dexamethasone and the class I/II HDAC inhibitor vorinostat in a panel of T-ALL cell lines with wild type or mutant CREBBP alleles. This demonstrated sensitivity to vorinostat at clinically useful concentrations (IC50 below 1礛) in the majority of cell lines tested.

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Source Cell , 2010, 142, 444–455. VX-680 (Tozasertib, MK-0457) purchased from Selleck
Method Immunofluorescence Microscopy
Cell Lines HeLa cells
Concentrations
Incubation Time
Results Inhibition of Aurora kinases with VX-680 sharply reduced kinetochore-localized pT422 signal (Figure G). When normalized to the total level of CENP-E at the kinetochore (which is also reduced in VX-680 treated cells (Ditchfield et al. 2003)), a > 90% reduction in T422 phosphorylation was seen following VX-680 treatment ( Figure H).

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Rating
Source Nat Methods, 2013, 10(10), 981-4. Iniparib (BSI-201) purchased from Selleck
Method Immunoblot analysis
Cell Lines HCT116
Concentrations 50 uM
Incubation Time 40 min
Results Immunoblot analysis of PARylation after treatment with AIniparib.The asterisk indicates a nonspecific band.

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Rating
Source Cell Stem Cell, 2012, 11, 179-94. Alisertib (MLN8237) purchased from Selleck
Method qPCR
Cell Lines CCE cells
Concentrations 1 uM
Incubation Time 48 h
Results Treatment with the Aurka-specific chemical inhibitor MLN8237 suppressed pluripotency TF expression and decreased fluorescence in the NG4 Nanog-GFP reporter line.

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Rating
Source Cancer Discov, 2012, 2(7), 591-7. Tofacitinib (CP-690550,Tasocitinib) purchased from Selleck
Method Western blot
Cell Lines NK-S1, KHYG-1 cells
Concentrations 0-2 uM
Incubation Time 48 h
Results To further confirm the involvement of JAK/STAT signaling in the survival of NKTCLs, we next evaluated the effect of a pan-JAK inhibitor, CP-690550, in NK-S1, KHYG-1, and K562 cells. As expected, both the NK-S1 and KHYG-1 cells showed a reduction of phosphorylated STAT5.

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Rating
Source J Clin Invest, 2014, 10.1172/JCI69094. Momelotinib (CYT387) purchased from Selleck
Method Western blot
Cell Lines IL-6- supported INA-6 cells
Concentrations 50 nM
Incubation Time 1 h
Results To further establish that constitutive GP130 activation represents a model of IL-6–activated MM, it infected the human IL-6–dependent MM line INA-6. Treatment with JAK inhibitors (CYT387 and ruxolitinib) blocked STAT3 phosphorylation and caused cell cycle arrest.

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Rating
Source J Exp Med, 2014, 10.1084/jem.20141123. Barasertib (AZD1152-HQPA) purchased from Selleck
Method Giemsa staining
Cell Lines Primary MKPs
Concentrations
Incubation Time
Results Notably, Aurora B inhibitor (AZD-1152) treatment caused primary MKPs maturation and normal DNA ploidy.

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Rating
Source Nat Commun, 2014, 5, 3479. Tubastatin A HCl purchased from Selleck
Method Immunoblotting
Cell Lines RAW264.7
Concentrations 10 uM
Incubation Time 12 h
Results Most importantly, the augmented p38 phosphorylation caused by TBSA was abrogated by MEC17 knockdown (Lanes 19-24).

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Tags: phosphatase inhibitor library
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