BK-1361(cyclo(RLsKDK))

BK-1361(BK1361, cyclo-RLsKDK) is a cyclic peptide with RLsKDK (s=D-serine) that functions as a potent, selective inhibitor of ADAM8 with IC50 of 120 nM; displays no significant activity against ADAM 9, 10, 12, 17 , as well as MMP-2, -9, and -14 at 10 uM; inhibit shedding of CD23 with IC50 of 182 nM in cell-based shedding assays, reduces migration/invasion of pancreatic cancer cells and less ERK1/2 and MMP activation, causes change in cell morphology; decreases tumour burden and metastasis of implanted pancreatic tumour cells and provides improved metrics of clinical symptoms and survival in Kras(G12D)-driven mouse model of PDAC.

References 1. Schlomann U, et al. Nat Commun. 2015 Jan 28;6:6175. 2. Chen J, et al. Sci Rep. 2016 Jul 26;6:30451. 3. Yim V, et al. Bioorg Med Chem. 2016 Sep 15;24(18):4032-4037. View Related Products by Target Matrix Metalloproteinase (MMP)