A natural bicyclic depsipeptide that selectively inhibits class I HDACs (IC50s = 53

Romidepsin – 1 mg

Brand:
Cayman
CAS:
128517-07-7
Storage:
-20
UN-No:
Non-Hazardous - /

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.  

 

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Description

A natural bicyclic depsipeptide that selectively inhibits class I HDACs (IC50s = 53, 39, 53, and 26 nM, for HDAC1, 2, 3, and 8, respectively) over HDAC4, 6, 7, and 9 (IC50s = 470, 330, 3,200, and 12,000 nM, respectively); has anti-cancer activities, particularly against certain T cell lymphomas; increases mRNA expression, histone acetylation, and the levels of proteins involved in NMDA receptor function in the brain of Shank3-deficient mice; rescues autism-like deficits in Shank3-deficient mice for at least three weeks following a dose of 0.25 mg/kg per day for three days

Formal name: cyclic (3→5)-disulfide-cyclo[(2Z)-2-amino-2-butenoyl-L-valyl-3S-hydroxy-7-mercapto-4E-heptenoyl-D-valyl-D-cysteinyl]

Synonyms:  FK228|FR901228|NSC 630176

Molecular weight: 540.7

CAS: 128517-07-7

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Natural Products||Product Type|Biochemicals|Small Molecule Inhibitors|Deacetylases||Research Area|Epigenetics, Transcription, & Translation|Erasers|Histone Deacetylation||Research Area|Neuroscience|Behavioral Neuroscience

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