MS-275 (Entinostat)

Catalog #
27011
$170 *
Size: 25 mg
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Description

MS-275, also known as Entinostat, is an inhibitor of histone deacetylases (HDACs) and preferentially inhibits HDAC1 over HDAC3. It does not inhibit HDAC8 (IC50 > 100 µM). It induces cyclin-dependent kinase inhibitor 1A (p21/CIP1/WAF1), slowing cell growth, differentiation, and tumor development in vivo. Recent studies suggest that MS-275 may be particularly useful as an antineoplastic agent when combined with other drugs like adriamycin, inhibitors of PARPs, or inhibitors of Hsp90.

This product has been cited 2 times.

Synonyms
MS-275, Entinostat
Product Info
Storage and Usage
Citations2
Purity

≥99% by HPLC.

Format
White to off-white crystalline solid.
Formula
C21H20N4O3
MW
376.4 Da
Solubility
Soluble in DMSO at 25 mg/ml with slight warming. MS-275 is poorly soluble in ethanol and water.
Biological Activity
MS-275 inhibits HDAC1 with an IC50 of 300 nM and HDAC3 with an IC50 value of 8 µM.
CAS Registry #
209783-80-2.
References

1. Hu., E. et al., J. Pharmacol. Exp. Ther. 2003; 307: 720-728.
2. Saito, A., et al., Proc. Natl. Acad. Sci. USA 1999; 96: 4592-4597.
3. Jaboin, J., et al., Cancer Res. 2002; 62: 6108-6115.
4. Xu, J. et al., Cancer Res. 2008; (68)16: 6718 – 6726.
5. Gaymes, T.J., et al., Haematologica 2009; 94: 638-646.

Application Reference:
Immune evasion by oncogenic proteins of acute myeloid leukemia (2014)