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SCREEN-WELL® Epigenetics library

 
BML-2836-0500 1 Library 500 µl/well Inquire for pricing
 
BML-2836-0100 1 Library 100 µl/well Inquire for pricing
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The SCREEN-WELL® Epigenetics library contains 43 compounds with defined activity against enzymes which carry out epigenetic modification of lysine. It also includes DNA methylation inhibitors. Compounds are dissolved in DMSO at 10mM and aliquoted into deep-well plates at 100 or 500µl per well. The library is a useful tool for chemical genomics, assay development and other pharmacological applications. The library contains inhibitors of these important enzymes: HDACs, SIRTs, Lysine demethylases, HATs, Histone methyl transferases, DNA methyltransferases as well as SIRT activators. A variety of structurally and mechanistically different compound classes are included.
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Product Details

Applications:HTS
 
Application Notes:Useful tool for chemical genomics, assay development, or other pharmacological applications in the study of epigenetic modifications of lysine and DNA methylation.
 
Contents:43 compounds supplied in DMSO at a concentration of 10mM.
 
Use/Stability:Stable for at least one year from the date of receipt when stored at -80°C.
 
Shipping:Shipped on Dry Ice
 
Long Term Storage:-80°C
 
Technical Info/Product Notes:

Application Note: High Throughput Screening Applications.
Application Note: Automated, High Throughput, HTRF®-Based Detection of Histone Methyltransferase and Demethylase Enzyme Activity.
Application Note: An Automated Profi ling Application using a Direct, Cell-Based, Target-Compound Interaction Assay for G9a Histone Methyltransferase and Bromodomain Proteins.
 
Regulatory Status:RUO - Research Use Only
 

Product Literature References

High-Throughput Drug Library Screening in Primary KMT2A-Rearranged Infant ALL Cells Favors the Identification of Drug Candidates That Activate P53 Signaling: P. Wander, et al.; Biomedicines 10, 638 (2022), Abstract;
RNA sequencing-based screen for reactivation of silenced alleles of autosomal genes: S. Gupta, et al.; G3 (Bethesda) 12, jkab428 (2022), Abstract;
High-throughput drug screening reveals Pyrvinium pamoate as effective candidate against pediatric MLL-rearranged acute myeloid leukemia: P. Wander, et al.; Transl. Oncol. 14, 101048 (2021), Abstract;
High-throughput screening identifies idasanutlin as a resensitizing drug for venetoclax-resistant neuroblastoma cells: L. Vernooij, et al.; Mol. Cancer Ther. 20, 1161 (2021), Abstract; Full Text
Integration of epigenetic mechanisms into non-genotoxic carcinogenicity hazard assessment: focus on DNA methylation and histone modifications: D. Desaulniers, et al.; Int. J. Mol. Sci. 22, 10969 (2021), Abstract; Full Text
Selective inhibition of HDAC6 regulates expression of the oncogenic driver EWSR1-FLI1 through the EWSR1 promoter in Ewing sarcoma: D.J. Garcia-Dominguez, et al.; Oncogene 40, 5843 (2021), Abstract; Full Text
Decitabine mildly attenuates MLL‐rearranged acute lymphoblastic leukemia in vivo, and represents a poor chemo‐sensitizer: P. Schneider, et al.; EJHaem. 1, 527 (2020), Abstract; Full Text
Functional precision medicine identifies new therapeutic candidates for medulloblastoma: J.M. Rusert, et al.; Cancer Res. 80, 5393 (2020), Abstract; Full Text
Nullscript inhibits Cryptosporidium and Toxoplasma growth: F. Murakoshi, et al.; Int. J. Parasitol. Drugs Drug Resist. 14, 159 (2020), Abstract; Full Text
Myc and loss of p53 cooperate to drive formation of choroid plexus carcinoma: J. Wang, et al.; Cancer Res. 79, 2208 (2019), Abstract; Full Text
Pan-HDAC inhibitors promote tau aggregation by increasing the level of acetylated tau: H. Jeong, et al.; Int. J. Mol. Sci. 20, 4283 (2019), Abstract; Full Text
Bortezomib prevents cytarabine resistance in MCL, which is characterized by down-regulation of dCK and up-regulation of SPIB resulting in high NF-κB activity: C. Freiburghaus, et al.; BMC Cancer. 18, 466 (2018), Abstract; Full Text
Epigenetic crosstalk: Pharmacological inhibition of HDACs can rescue defective synaptic morphology and neurotransmission phenotypes associated with loss of the chromatin reader Kismet: N.K. Latcheva, et al.; Mol. Cell. Neurosci. 87, 77 (2018), Abstract;
Neutralizing negative epigenetic regulation by HDAC5 enhances human haematopoietic stem cell homing and engraftment: X. Huang, et al.; Nat. Commun. 9, 2741 (2018), Abstract; Full Text
Highly efficient biallelic genome editing of human ES/iPS cells using a CRISPR/Cas9 or TALEN system: K. Takayama, et al.; Nucleic Acids Res. 45, 5198 (2017), Abstract;
Macrolides selectively inhibit mutant KCNJ5 potassium channels that cause aldosterone-producing adenoma: U.I. Scholl, et al.; J. Clin. Invest. 127, 2739 (2017), Abstract; Full Text
Sorafenib tosylate inhibits directly necrosome complex formation and protects in mouse models of inflammation and tissue injury: S. Martens, et al.; Cell Death Dis. 8, e2904 (2017), Abstract; Full Text
Altered neuronal network and rescue in a human MECP2 duplication model: S. Nageshappa, et al.; Mol. Psychiatry 21, 178 (2016), Application(s): Drug Screening, Abstract;
Human pluripotent stem cell-derived cortical neurons for high throughput medication screening in autism: A proof of concept study in SHANK3 haploinsufficiency syndrome: H. Darville, et al.; EBioMedicine 9, 293 (2016), Application(s): Drug screening, Abstract;
Identification of novel pathways and molecules able to down-regulate PHOX2B gene expression by in vitro drug screening approaches in neuroblastoma cells: E. Di Zanni, et al.; Exp. Cell Res. 336, 43 (2015), Application(s): Drug Screening, Abstract;
A high-content imaging assay for the quantification of the Burkholderia pseudomallei induced multinucleated giant cell (MNGC) phenotype in murine macrophages: G. Pegoraro, et al.; BMC Microbiol. 14, 98 (2014), Abstract; Full Text
Apicidin sensitizes pancreatic cancer cells to gemcitabine by epigenetically regulating MUC4 expression: D. Ansari, et al.; Anticancer Res. 34, 5269 (2014), Abstract;
TR-FRET cellular assays for interrogating posttranslational modifications of histone H3: T. Machleidt, et al.; J. Biomol. Screen. 16, 1236 (2011), Abstract; Full Text

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