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How to Cite 1. For In-Text Citation (Materials & Methods): 2. For Key Resources Table: |
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| Formula | C20H30N4O11 |
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| Molecular Weight | 502.47 | CAS No. | 169332-60-9 | |
| Solubility (25°C)* | In vitro | Water | 100 mg/mL (199.01 mM) | |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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| Description | Ac-DEVD-CHO (Caspase-3 Inhibitor I, N-Ac-Asp-Glu-Val-Asp-CHO) is a potent aldehyde inhibitor of Group II caspases with Ki values of 0.2 nM and 0.3 nM for for caspase-3 and caspase-7, respectively. Weak inhibition for caspase-2. | |||||||||||
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| In vitro | Ac-DEVD-CHO is a potent inhibitor of caspase-3 (Ki = 230 pM). In contrast, caspase-2 cleaves the tetrapeptide substrate poorly and is only weakly inhibited by this compound (Ki = 1.7 μM). Group III caspases are broadly inhibited by this chemical with Ki values ranging from 1 to 300 nM. Inhibition of caspase-3 by this inhibitor in isolated working-heart rat model significantly improves post-ischemic contractile recovery of stunned myocardium, even when given after the onset of ischemia. The mechanism(s) of protection by this compound appear to be independent of apoptosis. Troponin I cleavage was not inhibited by this chemical. | |||||||||||
| In vivo | Ac-DEVD-CHO administered at the time of MI results in a 61% reduction in activated caspase-3 expression in cardiomyocytes (p<0.05), and an 84% reduction in cardiomyocyte apoptosis in the young animals. However, in the aging mice, caspase inhibition had no effect on activated caspase-3 expression or cardiomyocyte apoptosis. This compound suppressed and/or delayed the progression of photoreceptor cell damage in rats and delays disease progression in rd gene-carring mice, which normally develop retinal degeneration early in life. |
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Data from [ , , Int J Oncol, 2018, 53(2):539-550 ]
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