. Author manuscript; available in PMC: 2017 Sep 23.

Published in final edited form as: Chem Rev. 2015 Nov 9;115(22):12546–12629. doi: 10.1021/acs.chemrev.5b00434

Table 37.

Kinetic data of novel peptide based caspase inhibitors containing unnatural amino acids. CV8/9-AOMK and CV8/9-KE are caspases 8/9 specific inhibitors.³²²

INHIBITOR	IC₅₀ (μM)
INHIBITOR	Casp-3	Casp-6	Casp-7	Casp-8	Casp-9	C-3/C-8 ratio
Ac-LETD-AOMK 383	0.020	0.068	0.46	0.028	0.089	0.71
NH₂-βA-L-Q-Hyp-D-AOMK(CV8/9-AOMK) 384	43	220	250	0.30	0.32	143
NH₂-βA-L-Q-Hyp-D-KE(CV8/9-KE) 385	150	320	400	0.30	0.64	433

	k_inact/K_i (mM⁻¹s⁻¹)
Ac-LETD-AOMK 383	490	n.d.	n.d.	880	1300	0.56
NH₂-βA-L-Q-Hyp-D-AOMK(CV8/9-AOMK) 384	0.14	n.d.	n.d.	150	190	0.0009