DEC-RVRK-CMK TFA  (Synonyms: Decanoyl-Arg-Val-Arg-Lys-chloromethylketone TFA)

DEC-RVRK-CMK (Decanoyl-Arg-Val-Arg-Lys-chloromethylketone) TFA is a peptide-based CMK (chloromethylketone) inhibitor that targets and inactivates the secreted soluble kexin (Kex2) (K_i=8.45 μM). The yeast enzyme Kex2 (kexin, EC 3.4.21.61) is a calcium-dependent transmembrane protease and belongs to the mammalian protease family of the serine protease subtilisin family. The binding mechanism of Kex2 with different CMK inhibitors depends on substrate selectivity, particularly the selective differences between lysine and arginine at the P1 position^[1].

Ki: 8.45 μM (ssKex2)^[1]

744.41 (free base)

C₃₄H₆₆ClN₁₁O₅._xC₂HF₃O₂

Solid

White to off-white

{DEC}-Arg-Val-Arg-Lys-{CMK}

{DEC}-RVRK-{CMK}

NCCCC[C@@H](C(CCl)=O)NC([C@H](CCCNC(N)=N)NC([C@H](C(C)C)NC([C@H](CCCNC(N)=N)NC(CCCCCCCCC)=O)=O)=O)=O.O=C(O)C(F)(F)F.[x]

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [1]. Wheatley JL, et al. Differential P1 arginine and lysine recognition in the prototypical proprotein convertase Kex2. Proc Natl Acad Sci U S A. 2007 Apr 17;104(16):6626-31.  [Content Brief]