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Santacruzamate A New
Highly potent and selective histone deactylase 2 (HDAC2) inhibitor (IC50 = 112 - 119 pM). Also inhibits HDAC6 in nanomolar range (IC50 = 433 nM). Displays >3500 fold selectivity for HDAC2 over HDAC6, and >8500-fold selectivity over HDAC4 (IC50 >1 μM for HDAC4). Inhibits growth of HuT-78 cutaneous T-cell lymphoma cell line. Identified as targeting human host proteins that interact with SARS-CoV-2.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 278.35. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||3.59 mL||17.96 mL||35.93 mL|
|5 mM||0.72 mL||3.59 mL||7.19 mL|
|10 mM||0.36 mL||1.8 mL||3.59 mL|
|50 mM||0.07 mL||0.36 mL||0.72 mL|
References are publications that support the biological activity of the product.
Pavlik et al (2013) Santacruzamate A, a potent and selective histone deacetylase inhibitor from the Panamanian marine cyanobacterium cf. Symploca sp. J.Nat.Prod. 76 2026 PMID: 24164245
Gordon et al (2020) A SARS-CoV-2 protein interaction map reveals targets for drug repurposing. Nature. 583 459 PMID: 32353859
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Epigenetics Scientific Review
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.
Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.
Epigenetics in Cancer Poster
Adapted from the 2015 Cancer Product Guide Edition 3, this poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.
Rheumatoid Arthritis Poster
Rheumatoid arthritis (RA) is a chronic destructive inflammatory autoimmune disease that results from a breakdown in immune tolerance, for reasons that are as yet unknown. This poster summarizes the pathology of RA and the inflammatory processes involved, as well as describing some of the epigenetic modifications associated with the disease and the potential for targeting these changes in the discovery of new treatments.