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Discovery and optimization of small-molecule ligands for the CBP/p300 bromodomains
PNU 282987 has negligible activity against α1β1γδ and α3β4 nAChRs as well as a panel of monoamine
Smiles: CN(C)CCCNC(=O)C1C=CC(=CC=1)C1=CC(O)=C2N=CC=CC2=C1
CUDC-907 induces apoptosis and G2–M cell-cycle arrest in cancer cells and effectively inhibits more than 50 different cancer cells’ growth
160 nM and 100 nM for KDM5A
AK-7 - SIRT2 Inhibitor. CAS# 420831-40-9 size:2 mg solid Discovery and optimization of small-moleculeAK 7, CAS No. 420831 40 9, is a cell and brain permeable, selective sirtuin SIRT2 inhibitor (IC50 ~15. 5 M). AK 7 displays no effect on SIRT1 or SIRT3. It diminishes neuronal cell death induced by mutant huntingtin fragment. It also down regulates cholesterol biosynthetic gene expression and reduces total cholesterol levels in neurons in vivo. In two genetic mouse models of Huntingtons disease, AK 7 treatment resulted in improved motor function,
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