+ Enzyme (nM) HDAC1 1,140–5,200 HDAC2 3,000 HDAC3 400–560 HDAC4 >180,000 HDAC5 >180,000 HDAC6 >180,000 HDAC7 >180,000 HDAC8 13,200 HDAC9 HDAC10 HDAC11 Refs:
RGFP136, or RGFP-136, is a histone deacetylase (HDAC) inhibitor which is used in scientific research. It is a modestly selective or preferential HDAC3 inhibitor, with an value of 400–560nM, whereas the drug showed 2- to 13-fold lower inhibitory potency at HDAC1 and HDAC2 ( = 1,140–5,200nM and 3,000nM, respectively). It shows weak inhibition of HDAC8 and no inhibition of several other HDACs, including HDAC4, HDAC5, HDAC6, and HDAC7. RGFP136 has been found to enhance long-term memory in rodents, which led to conclusions that HDAC3 is a critical regulator of long-term memory formation. It has also been found to improve symptoms in an animal model of Friedreich ataxia. The drug's pharmacokinetics have been studied and it is brain-penetrant in rodents. RGFP136 was first described in the scientific literature by 2011.
See also Histone deacetylase inhibitor RGFP963 RGFP966
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