Shelf life (days): 1460.0
Formulation: A solid
Formal Name: 7-chloro-8-ethyl-10-[2-(2-methylpropoxy)ethyl]-benzo[g]pteridine-2,4(3H,10H)-dione
Purity: ≥98%
Formula Markup: C18H21ClN4O3
Formula Weight: 376.8
CAS Number: 2887480-87-5
Notes: JG-2016 is an inhibitor of histone acetyltransferase 1 (HAT1; IC50 = 14.8 µM).{72496} It is selective for HAT1 over lysine acetyltransferase 2A (KAT2A/GCN5) and p300/CBP-associated factor (PCAF), for which it has no activity, KAT5, KAT6B, and KAT7 (IC50s = >100, >100, and 84.82 µM, respectively), CREB-binding protein (CBP), and p300 (IC50s = 90.41 and 74.25 µM, respectively). JG-2016 (20 µM) reduces acetylation of histone H4 lysine 5 (H4K5) and H4K12 in hTert-HME1 mammary epithelial cells. It reduces the growth of HCC1806 triple-negative breast cancer and A549 lung cancer cells (EC50s = 10.4 and 1.9 µM, respectively). JG-2016 reduces intratumoral H4K12 acetylation in an A549 mouse xenograft model in a dose-dependent manner. It also reduces tumor growth in an A549 mouse xenograft model when administered at doses of 50 and 100 mg/kg once every three days.
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