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Romidepsin

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    Romidepsin
  • Romidepsin
Cat No: 17130
Biochemicals - Small Molecule Inhibitors
Cayman

Romidepsin, also known as FK228, is a natural bicyclic depsipeptide that, following reduction, selectively inhibits class I histone deacetylases (HDACs).{10790} Reduction of a disulfide bond on romidepsin within the cell generates a zinc-binding thiol...

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Territorial Availability: Available through Bertin Technologies only in France
Synonyms:
  • cyclic (3?5)-disulfide-cyclo[(2Z)-2-amino-2-butenoyl-L-valyl-3S-hydroxy-7-mercapto-4E-heptenoyl-D-valyl-D-cysteinyl]
Correlated keywords:
  • biochemical natural product cancer inhibitor HDAC histone research epigenetic chromadax antibiotic FR901228 FK 228 FR-901228 NSC630176 NSC-630176 bicyclic depsipeptide inhibit inhibition deacetylase HDAC T cell 1 2 3 4 6 7 8 9 anti-cancer anti anticancer lymphoma Istodax®
Product Overview:
Romidepsin, also known as FK228, is a natural bicyclic depsipeptide that, following reduction, selectively inhibits class I histone deacetylases (HDACs).{10790} Reduction of a disulfide bond on romidepsin within the cell generates a zinc-binding thiol, allowing potent and selective inhibition of HDAC1, 2, 3, and 8 (IC50s = 53, 39, 53, and 26 nM, respectively) over HDAC4, 6, 7, and 9 (IC50s = 470, 330, 3,200, and 12,000 nM, respectively).{28023,15938} Through its effects on HDACs, romidepsin has anti-cancer activities, particularly against certain T cell lymphomas.{28022,28021,28020} Romidepsin also increases mRNA expression and nuclear protein levels of HDAC2, H3 acetylation and transcription of Grin2a, the gene for the NMDA receptor NR2A subunit, and protein levels of the NR2A subunit in the brain of Shank3-deficient mice, a model of autism.{40872} It also increases excitatory postsynaptic currents (EPSCs) in prefrontal cortex pyramidal neurons from Shank3-deficient mice. In addition, romidepsin rescues autism-like social deficits in Shank3-deficient mice for at least three weeks following administration of a 0.25 mg/kg per day dose for three days.
Size 500 µg
Shipping dry ice
CAS Number 128517-07-7
Molecular Formula C24H36N4O6S2
SMILES C/C=C(NC([C@@H](CSSCC/C=C/1)NC([C@@H](C(C)C)N2)=O)=O)/C(N[C@H](C(O[C@H]1CC2=O)=O)C(C)C)=O
Molecular Weight 540,7
Formulation A crystalline solid
Purity ≥98%
Custom Code 2922.19
UNSPSC code 12352100

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

Accreditations
ISO/IEC 17025:2005
ISO Guide 34:2009

Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.

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