Molecular Formula | C20H30N4O11 |
Molar Mass | 502.4724 |
Density | 1.374±0.06 g/cm3(Predicted) |
Boling Point | 1021.1±65.0 °C(Predicted) |
Solubility | DMSO |
Appearance | Morphological powder |
Color | white |
pKa | 4.19±0.10(Predicted) |
Storage Condition | -20°C |
Sensitive | Moisture Sensitive |
Physical and Chemical Properties | Bioactive Ac-DEVD-CHO (Caspase-3 Inhibitor I, N-Ac-Asp-Glu-Val-Asp-CHO) is a potent inhibitor of Group II caspases, with Ki values for caspase-3 and caspase-7 of 0.2 nM and 1.6 nM, respectively. The effect on caspase-2 preparations is weak, with Ki value of 1.7 μM. |
WGK Germany | 3 |
RTECS | EK7643000 |
Reference Show more | 1. [IF=5.192] Anhui Yang et al."Lysionotin induces apoptosis of hepatocellular carcinoma cells via caspase-3 mediated mitochondrial pathway."Chem-Biol Interact. 2021 Aug;344:109500 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.99 ml | 9.951 ml | 19.902 ml |
5 mM | 0.398 ml | 1.99 ml | 3.98 ml |
10 mM | 0.199 ml | 0.995 ml | 1.99 ml |
5 mM | 0.04 ml | 0.199 ml | 0.398 ml |
Target
Target Value
Caspase-3
(Cell-free assay) 230 pM(Ki)
caspase-8
(Cell-free assay) 0.92 nM(Ki)
caspase-7
(Cell-free assay) 1.6 nM(Ki)
caspase-10
(Cell-free assay) 12 nM(Ki)
Caspase-1
(Cell-free assay) 18 nM(Ki)
in vitro studies
Ac-DEVD-CHO is a potent inhibitor of caspase-3, Ki = 230 pM. On the contrary, the ability of caspase-2 to shear the tetrapeptide substrate is poor, Ac-DEVD-CHO has little inhibitory effect on it (Ki = 1.7 μM). Ac-DEVD-CHO widely inhibited Group III caspases, the Ki value was between 1-300 nM. In isolated rat hearts, Ac-DEVD-CHO inhibitory caspase-3 can significantly improve the recovery of myocardial contraction after ischemia, even after the onset of ischemia. The protective mechanism of Ac-DEVD-CHO may not be related to apoptosis, which does not inhibit the shearing of Troponin I.
In vivo studies
during myocardial ischemia, Ac-DEVD-CHO administration can reduce the expression of activated caspase-3 in myocardial cells of juvenile animals by 61% and the rate of myocardial apoptosis by 84%. However, in aged mice, the inhibition of caspase has no effect on the expression of activated caspase-3 or myocardial apoptosis. Ac-DEVD-CHO can inhibit or delay the progression of photoreceptor cell damage in rats. In mice carrying rd gene, the deterioration of the disease is delayed (normally, retinal degeneration occurs early in their life).