Biochem/physiol Actions

Primary Targethuman HDAC1 and HDAC3 activities

Reversible: no

Product does not compete with ATP.

Target IC₅₀: 11.57 µM and 5.39 µM in suppressing the growth of proliferating keratinocytes and squamous cell carcinoma cells, respectively

Cell permeable: yes

General description

A cell-permeable bishydroxamic acid histone deacetylase (HDAC) inhibitor with anti-tumor properties. Reported to cause an increase in acetylated histone H4 in MEL cells. Also reported to inhibit human HDAC1 and HDAC3 activities with a similar potency (ID₅₀ ~ 250-300 nM). Belongs to the hybrid polar class of compounds that induce both differentiation of transformed cells and apoptosis. Shown to suppress the growth of proliferating keratinocytes and squamous cell carcinoma cells (IC₅₀ = 11.57 µM and 5.39 µM, respectively).

A cell-permeable bishydroxamic acid histone deacetylase (HDAC) inhibitor with anti-tumor properties. Causes an increase in acetylated histone H4 in MEL cells and inhibits the human HDAC1 and HDAC3 activities with a similar potency (ID₅₀ ~ 250-300 nM). Belongs to the hybrid polar class of compounds that acts both as inducers of differentiation of transformed cells and apoptosis. Suppresses the growth of proliferating keratinocytes and squamous cell carcinoma cells (IC₅₀ = 11.57 µM and 5.39 µM, respectively).

Legal Information

Not available for sale in the United States.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Brinkmann, H., et al. 2001. J. Biol. Chem.276, 22491.Richon, V.M., et al. 1998. Proc. Natl. Acad. Sci. USA 95, 3003.Richon, V.M., et al. 1996. Proc. Natl. Acad. Sci. USA93, 5705.Marks, P.A., 1994. Proc. Natl. Acad. Sci. USA91, 10251.

Packaging

Packaged under inert gas

100 mg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.r>r>r>From Catalog:r>Desc. Field- added "cell-permeable"

Warning

Toxicity: Standard Handling (A)