Entinostat

TargetMol
Product Code: TAR-T6233
Supplier: TargetMol
CodeSizePrice
TAR-T6233-1mL1 mL * 10 mM (in DMSO)£111.00
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TAR-T6233-10mg10mg£111.00
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TAR-T6233-25mg25mg£128.00
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TAR-T6233-50mg50mg£143.00
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TAR-T6233-100mg100mg£172.00
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TAR-T6233-200mg200mg£226.00
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Prices exclude any Taxes / VAT

Overview

Regulatory Status: RUO
Shipping:
cool pack
Storage:
-20℃

Images

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Further Information

Bioactivity:
Entinostat (MS-275) is an inhibitor of HDACs that inhibits HDAC1 and HDAC3 (IC50s: 0.18/0.74 μM).
CAS:
209783-80-2
Formula:
C21H20N4O3
Molecular Weight:
376.416
Pathway:
Apoptosis; Autophagy; DNA Damage/DNA Repair; Chromatin/Epigenetic
Purity:
0.9952
SMILES:
Nc1ccccc1NC(=O)c1ccc(CNC(=O)OCc2cccnc2)cc1
Target:
Apoptosis; HDAC; Autophagy

References

Wang C, Huang M, Lin Y, et al.ENO2-derived phosphoenolpyruvate functions as an endogenous inhibitor of HDAC1 and confers resistance to antiangiogenic therapy.Nature Metabolism.2023: 1-22. Moreno-Yruela C, Zhang D, Wei W, et al. Class I Histone Deacetylases (HDAC1?3) are Histone Lysine Delactylases. Science advances. 2022, 8(3): eabi6696. Saito A, et al. A synthetic inhibitor of histone deacetylase, MS-27-275, with marked in vivo antitumor activity against human tumors. Proc Natl Acad Sci U S A, 1999, 96(8), 4592-4597. Wellinger L C, Hogg S J, Newman D M, et al. Bet inhibition enhances TNF-mediated antitumor immunity. Cancer Immunology Research. 2022, 10(1): 87-107 Lagosz K B, Bysiek A, Macina J M, et al. HDAC3 Regulates Gingival Fibroblast Inflammatory Responses in Periodontitis[J]. Journal of dental research. 2019: 0022034519885088. Jiang X C, Tu F H, Wei L Y, et al. Discovery of a Novel G-Quadruplex and Histone Deacetylase (HDAC) Dual-Targeting Agent for the Treatment of Triple-Negative Breast Cancer. Journal of Medicinal Chemistry. 2022 Wellinger L C, Hogg S J, Newman D M, et al. BET Inhibition Enhances TNF Mediated Anti-Tumor Immunity. Cancer Immunology Research. 2022, 10(1): 87-107. Zierfuss B, Weinhofer I, Buda A, et al. Targeting foam cell formation in inflammatory brain diseases by the histone modifier MS?275. Annals of Clinical and Translational Neurology. 2020, 7(11): 2161-2177 Lagosz K B, Bysiek A, Macina J M, et al. HDAC3 Regulates Gingival Fibroblast Inflammatory Responses in Periodontitis. Journal of Dental Research. 2019: 0022034519885088 Moreno-Yruela C, Zhang D, Wei W, et al. Class I Histone Deacetylases (HDAC1?3) are Histone Lysine Delactylases[J]. bioRxiv. 2021 Zhang L, Shi J, Du D, et al. Ketogenesis acts as an endogenous protective programme to restrain inflammatory macrophage activation during acute pancreatitis. eBioMedicine. 2022, 78: 103959. Wellinger L C, Hogg S J, Newman D M, et al. BET Inhibition Enhances TNF Mediated Anti-Tumor Immunity[J]. bioRxiv. 2021 Zhang ZY, et al. MS-275, an histone deacetylase inhibitor, reduces the inflammatory reaction in rat experimental autoimmune neuritis. Neuroscience. 2010 Aug 11;169(1):370-7. Beckers T, et al. Distinct pharmacological properties of second generation HDAC inhibitors with the benzamide or hydroxamate head group. Int J Cancer. 2007 Sep 1;121(5):1138-48. Rosato RR, et al. The histone deacetylase inhibitor MS-275 promotes differentiation or apoptosis in human leukemia cells through a process regulated by generation of reactive oxygen species and induction of p21CIP1/WAF1 1. Cancer Res. 2003 Jul 1;63(13):3637-45.