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Product Details

MS-275 (Entinostat) | HDAC inhibitor

MS-275 (Entinostat - 209783-80-2) is a potent HDAC inhibitor. Selective for HDAC1 (IC50 = 300 nM) over HDAC3 (IC50 = 8 μM) and HDAC8 (IC50 100 μM).1 In vivo, MS-275, has been shown to inhibit tumor growth via induction of the tumor supressors p21WAF1/CIP1 and gelsolin2 and to block cell proliferation in a variety of cancer cell lines. MS-275 has also shown significant anti-rheumatic activity in rat and mouse arthritis models.5

References/Citations
1) Hu et al. (2003), Identification of novel isoform-selective inhibitors within class 1 histone deacetylases; J. Pharmacol. Exp. Ther., 307 720
2) Saito et al. (1999), A synthetic inhibitor of histone deacetylase, MS-275, with marked in vivo antitumor activity against human tumors; Proc. Natl. Acad. Sci. USA, 96 4592
3) Eyupoglu et al. (2006), Experimental therapy of malignant gliomas using the inhibitor of histone deacetylase MS-275; Mol. Cancer Ther., 5 1248
4) Lee et al. (2001), MS-275, a histone deacetylase inhibitor, selectively induces transforming growth factor beta type II receptor expression in human breast cancer cells; J. Pharmacol. Exp. Ther., 307 720
5) Lin et al. (2007), Anti-rheumatic activities of histone deacetylase (HDAC) inhibitors in vivo in collagen-induced arthritis in rodents; Br. J. Pharmacol., 150 862
6) Fukuchi et al. (2015), Class I histone deacetylase-mediated repression of the proximal promoterof the Activity-regulated Cytoskeleton-associated Protein Gene regulates its response to brain-derived neurotrophic factor; J. Biol. Chem. 290 6825 [Focus Biomolecules Citation]

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Catalog#  10-2131

$50.00
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Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee.
 
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CAS:
209783-80-2
Catalog Number:
10-2131
Activity:
HDAC inhibitor
Alternate Names:
Entinostat
Molecular Weight:
376.42
Molecular Formula:
C21H20N4O3
Solubility:
Soluble in DMSO (up to 25 mg/ml).
Physical Properties:
Pale yellow solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20° for up to 1 week.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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