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Biological Activity: MS-275 inhibits HDAC1 with an IC50 of 300 nM and HDAC3 with an IC50 value of 8 µM.
CAS Number: 209783-80-2.
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.
Format: White to off-white crystalline solid.
Purity: ≥99% by HPLC.
Solubility: Soluble in DMSO at 25 mg/ml with slight warming. MS-275 is poorly soluble in ethanol and water.
Storage Stability: Store at or below -20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.
Biosafety Level: Not applicable (BSL-1)
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: Elias, S., et al. Blood. 2014 Mar 6;123(10):1535-43. doi: 10.1182/blood-2013-09-526590. Immune evasion by oncogenic proteins of acute myeloid leukemia (2014)
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