7dg

7DG is a selective inhibitor of protein kinase R (PKR).

Estradiol 17-(β-D-glucuronide) (E217G) is an estrogen metabolite formed in the liver and subsequently excreted in bile.1It acts as a substrate of the multidrug resistance protein 2 (MRP2; Km= 75 μM), and through MRP2-mediated transport, functions as a cholestatic agent, decreasing bile flow.1,2In addition to binding to the MRP2 transport site, E217G has been shown to bind to an allosteric site that through positive cooperativity activates its own transportviaMRP2 and the transport of other MRP2 substrates, including the non-cholestatic estrogen metabolite, estradiol 3-(β-D-glucuronide) .2,3E217G has also been reported to be transported by MDR1, MRP1, MRP3, MRP4, MRP7, ABCG2 (a breast cancer resistance protein transporter), and the rat organic anion-transporting polypeptides 1-4.2 1.Loe, D.W., Almquist, K.C., Cole, S.P., et al.ATP-dependent 17β-estradiol 17-(β-D-glucuronide) transport by multidrug resistance protein (MRP). Inhibition by cholestatic steroidsThe Journal of Biological Chemisty271(16)9683-9689(1996) 2.Gerk, P.M., Li, W., and Vore, M.Estradiol 3-glucuronide is transported by the multidrug resistance-associated protein 2 but does not activate the allosteric site bound by estradiol 17-glucuronideDrug Metabolism and Disposition32(10)1139-1145(2004) 3.Gerk, P.M., Li, W., Megaraj, W., et al.Human multidrug resistance protein 2 transports the therapeutic bile salt tauroursodeoxycholateJournal of Pharmacology and Experimental Therapeutics320(2)893-899(2007)

FT385 is a novel USP30 inhibitor, recapitulating genetic loss of USP30 and setting the trigger for PINK1-PARKIN amplification of mitochondrial ubiquitylation.

7-Oxogedunin (Compound 7DG; Compound 16) 是一种小分子，可以保护巨噬细胞免受炭疽致死毒素 (LT) 引起的细胞焦亡 (pyroptosis)。它的作用靶点是蛋白激酶 R (PKR)，通过抑制 PKR 的非依赖性激酶功能，广泛抑制多种炎症小体 (NLRP1和NLRP3) 的组装和 caspase-1 的活化。7-Oxogedunin 还对欧洲玉米螟幼虫具有生长抑制活性，并可用于 LT 毒性抑制和杀虫研究。