Givinostat hydrochloride

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Cat.No. 6249 - Givinostat hydrochloride | C24H27N3O4.HCl | CAS No. 199657-29-9
Description: Histone deacetylase inhibitor
Chemical Name: [6-[(Diethylamino)methyl]-2-naphthalenyl]methyl-N-[4-[(hydroxyamino)carbonyl]phenyl]carbamate hydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

Histone deacetylase (HDAC) inhibitor (IC50 = 7.5 to 16 nM). At low concentrations reduces release of pro-inflammatory cytokines, including TNFα, INFγ, IL-1α and IL-1β, from LPS stimulated PBMCs in vitro. Exhibits anti-inflammatory effects in vivo. Improves functional recovery and attenuates tissue damage in a mouse model of traumatic brain injury.

Technical Data

M. Wt 457.95
Formula C24H27N3O4.HCl
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 199657-29-9
PubChem ID 10095659
InChI Key QKSGNWJOQMSBEP-UHFFFAOYSA-N
Smiles CCN(CC1=CC2=C(C=C(C=C2)COC(NC3=CC=C(C(NO)=O)C=C3)=O)C=C1)CC.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 45.8 100

Preparing Stock Solutions

The following data is based on the product molecular weight 457.95. Batch specific molecular weights may vary from batch to batch due to solvent 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 2.18 mL 10.92 mL 21.84 mL
5 mM 0.44 mL 2.18 mL 4.37 mL
10 mM 0.22 mL 1.09 mL 2.18 mL
50 mM 0.04 mL 0.22 mL 0.44 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the biological activity of the product.

Leoni et al (2005) The histone deacetylase inhibitor ITF2357 reduces production of pro-inflammatory cytokines in vitro and systemic inflammation in vivo. Mol.Med. 11 1 PMID: 16557334

Shein et al (2009) Histone deacetylase inhibitor ITF2357 is neuroprotective, improves functional recovery, and induces glial apoptosis following experimental traumatic brain injury. FASEB.J. 23 4266 PMID: 19723705


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Citations for Givinostat hydrochloride

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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* or download your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Epigenetics

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.

Epigenetics

Epigenetics Research Bulletin

Produced by Tocris and updated in 2014, the epigenetics research bulletin gives an introduction into mechanisms of epigenetic regulation, and highlights key Tocris products for epigenetics targets including:

  • Bromodomains
  • DNA Methyltransferases
  • Histone Deacetylases
  • Histone Demethylases
  • Histone Methyltransferases
Rheumatoid Arthritis

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.