Catalog No.: PC-60981Not For Human Use, Lab Use Only.
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.
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.
BK-1361 displays no significant activity against ADAM 9, 10, 12, 17 , as well as MMP-2, -9, and -14 at 10 uM.
BK-1361 inhibits 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.
BK-1361 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.
Physicochemical Properties
M.Wt
727.865
Formula
C31H57N11O9
Appearance
Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility
10 mM in DMSO
Chemical Name/SMILES
cyclo-RLsKDK; s=D-serine
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.
