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Submit ReviewMS 275 is a class I HDAC inhibitor (IC50 values are 0.18, 0.74, 44.9 and >100 μM for HDAC1, 3, 8 and 6, respectively). Exhibits antiproliferative effects and induces apoptosis in a range of tumor cell lines in vitro and in vivo. Increases estrogen receptor α- and aromatase expression in breast cancer cells. Inhibits PCB-induced neuronal cell death by preventing HDAC3 binding and histone deacetylation within the synapsin-1 promoter.
MS 275 is also offered as part of the Tocriscreen Antiviral Library and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.
M. Wt | 376.41 |
Formula | C21H20N4O3 |
Storage | Store at -20°C |
Purity | ≥99% (HPLC) |
CAS Number | 209783-80-2 |
PubChem ID | 4261 |
InChI Key | INVTYAOGFAGBOE-UHFFFAOYSA-N |
Smiles | O=C(C1=CC=C(C=C1)CNC(OCC2=CN=CC=C2)=O)NC3=CC=CC=C3N |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 37.64 | 100 |
The following data is based on the product molecular weight 376.41. Batch specific molecular weights may vary from batch to batch due to the degree 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 | 2.66 mL | 13.28 mL | 26.57 mL |
5 mM | 0.53 mL | 2.66 mL | 5.31 mL |
10 mM | 0.27 mL | 1.33 mL | 2.66 mL |
50 mM | 0.05 mL | 0.27 mL | 0.53 mL |
References are publications that support the biological activity of the product.
Saito et al (1999) A synthetic inhibitor of histone deacetylase, MS-27-275, with marked in vivo antitumor activity against human tumors. Proc.Natl.Acad.Sci. 96 4592 PMID: 10200307
Beckers et al (2007) Distinct pharmacological properties of second generation HDAC inhibitors with the benzamide or hydroxamate head group. Int.J.Cancer 121 1138 PMID: 17455259
Formisano et al (2015) MS-275 inhibits aroclor 1254-induced SH-SY5Y neuronal cell toxicity by preventing the formation of the HDAC3/REST complex on the synapsin-1 promoter. J.Pharmacol.Exp.Ther. 352 236 PMID: 25467131
Sabnis et al (2011) Functional activation of the estrogen receptor-α and aromatase by the HDAC inhibitor entinostat sensitizes ER-negative tumors to letr. Cancer Res. 71 1893 PMID: 21245100
If you know of a relevant reference for MS 275, please let us know.
Keywords: MS 275, MS 275 supplier, MS275, HDAC1, HDAC3, inhibits, inhibitors, class, I, histone, deacetylases, SNDX275, entinostat, SNDX, 275, Class, HDACs, 6208, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for MS 275 include:
Verónica et al (2020) Differential effects of HDAC inhibitors on PPN oscillatory activity in vivo. Neuropharmacology 165 107922 PMID: 31923766
Kim (2018) Suppression of TGFβ-mediated conversion of endothelial cells and fibroblasts into cancer associated (myo)fibroblasts via HDAC inhibition. Br J Cancer 118 1359 PMID: 29695769
Do you know of a great paper that uses MS 275 from Tocris? Please let us know.
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TGF beta high responder treated with 1.5 μM MS 275 (HDAC 3 inhibitor) for 48 h. Cell lysates were analysed by western blot.
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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