RGFP 966

  Cat. No.:  DC7263   Featured
Chemical Structure
1357389-11-7
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More than 5000 active chemicals with high quality for research!
Field of application
RGFP966 is specific inhibitor of HDAC3, with an IC50 of 0.08 μM and no effective inhibition of any other HDAC at concentrations up to 15 μM.
Cas No.: 1357389-11-7
Chemical Name: 2-Propenamide,N-(2-amino-4-fluorophenyl)-3-[1-[(2E)-3-phenyl-2-propen-1-yl]-1H-pyrazol-4-yl]-,(2E)-
Synonyms: RGFP966; RGFP-966
SMILES: C1=CC=C(C=C1)/C=C/CN2C=C(C=N2)/C=C/C(=O)NC3=C(C=C(C=C3)F)N
Formula: C21H19FN4O
M.Wt: 362.4
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: RGFP966 is a highly selective HDAC3 inhibitor with an IC50 of 80 nM and shows no inhibition to other HDACs at concentrations up to 15 μM.
In Vivo: RGFP966 (10 and 25 mg/kg) treatment significantly improves body weight, rotarod performance and several measures of motor function in the open field locomoter test[3]. RGFP966 at a 10 mg/kg dose penetrates the blood-brain barrier into rat auditory cortex with typical pharmacokinetics, which together establish feasibility for the modulation of A1 plasticity due to action in the auditory cortex[4].
In Vitro: RGFP966 potently and selectively inhibits HDAC 3 with IC50 of 0.21 μM in RAW 264.7 macrophages, while HDACs 1 (IC50=5.6 μM), 2 (9.7 μM) and 8 (>100 μM), indicating a good level of selectivity for HDAC 3. The mRNA levels of HDACs 1, 2 and 3 are not significantly affected by RGFP966 in RAW 264.7 macrophages, whereas the HDAC 1 and HDAC 2 protein levels are slightly, though significantly, reduced upon RGFP966 treatment. Moreover, RGFP966 significantly reduced the transcriptional activity of NF-κB p65, whereas NF-κB p65 acetylation and localization remain unaltered[2].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
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DC6303 Tubastatin A HCl Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold).
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DC5178 Tubacin (BML-GR362) Tubacin is a selective inhibitor of HDAC6 via inhibition of the second deacetylase domain (DD2).
DC8134 Trichostatin A (TSA) Trichostatin A (TSA) is a selective and potent HDAC inhibitor with IC50 of ~1.8 nM; HDAC8 is the only known member of the HDAC-family that is not affected by TSA.
DC7716 TMP269 TMP269 is a novel and selective class IIa histone deacetylase inhibitor with IC50s of 126/80/36/9 nM for HDAC 4/5/7/9, respectively; 20-400 fold selectivity over class1 HDACs.
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