详情描述
Ac-DEVD-CHO is a specific Caspase-3 inhibitor with a Ki value of 230 pM.
Product information
CAS Number: 169332-60-9
Molecular Weight: 502.47
Formula: C20H30N4O11
Chemical Name: (4S)-4-[(2S)-3-carboxy-2-acetamidopropanamido]-4-{[(1S)-1-{[(2S)-1-carboxy-3-oxopropan-2-yl]carbamoyl}-2-methylpropyl]carbamoyl}butanoic acid
Smiles: CC(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(O)=O)C=O
InChiKey: UMBVAPCONCILTL-MRHIQRDNSA-N
InChi: InChI=1S/C20H30N4O11/c1-9(2)17(20(35)22-11(8-25)6-15(29)30)24-18(33)12(4-5-14(27)28)23-19(34)13(7-16(31)32)21-10(3)26/h8-9,11-13,17H,4-7H2,1-3H3,(H,21,26)(H,22,35)(H,23,34)(H,24,33)(H,27,28)(H,29,30)(H,31,32)/t11-,12-,13-,17-/m0/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: H2O : ≥ 50 mg/mL (99.51 mM)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
To ascertain the role of caspase-3 in SLNT-induced apoptosis, a caspase-3 inhibitor (Ac-DEVD-CHO) is used. The addition of Ac-DEVD-CHO significantly prevents SLNT-induced apoptosis (from 32.91±1.21% decreases to 15.88±1.58% while NC and Ac-DEVD-CHO groups are 6.45±0.96%, 7.77±0.79%, respectively). The apoptosis rates of cells pretreated with zVAD-fmk (5.32%) or Ac-DEVD-CHO (7.43%) decrease obviously after hypericin-mediated PDT treatment. Remarkably, 10 μmol/L Ac-DEVD-CHO partially blocks the effect of SIN-induced apoptosis and reduces the number of apoptotic nuclei. These effects of SIN are blocked by the caspase-3 inhibitor Ac-DEVD-CHO. Camptothecin (4 μM), a positive control, increases caspase-3 activity, which is also blocked by Ac-DEVD-CHO.
In Vivo:
Compare with model group, in CI group, the concentrations of serum BUN are decreased significantly at all time points after operation and those of Cr are decreased significantly at 6 hours, then restored to those of the sham group at 12 hours and 24 hours; the concentrations of serum TNF-α, IL-6 are decreased and those of IL-10 are elevated significantly at all time points. [TNF-α (μg/L) 6 hours: 436.2±64.2 vs. 653.6±8.9, 12 hours: 233.4±85.4 vs. 579.7±137.1, 24 hours: 151.0±90.3 vs. 551.0±119.8, IL-6 (μg/L) 6 hours: 1033.2±345.8 vs. 1 595.3±159.4, 12 hours: 366.3±68.3 vs. 1 330.7±249.8, 24 hours: 241.2±208.4 vs. 815.3±572.7, IL-10 (μg/L) 6 hours: 33.6±10.4 vs. 26.6±4.5, 12 hours: 37.2±5.0 vs. 24.5±4.3, 24 hours: 38.3±5.5 vs. 18.2±1.6, all P<0.05]; the renal cell apoptosis rates are decreased significantly at all time points: apoptosis rates 6 hours: (13.9±3.2)% vs. (18.3±1.4)%, 12 hours: (10.5±3.6)% vs. (15.9±3.5)%, 24 hours: (8.4±1.8)% vs.(12.5±2.1)%.
References:
- Garcia-Calvo M, et al.nhibition of human caspases by peptide-based and macromolecular inhibitors. J Biol Chem. 1998 Dec 4;273(49):32608-13.
- Jinglin Wang, et al. A polysaccharide from Lentinus edodes inhibits human colon cancer cell proliferation and suppresses tumor growth in athymic nude mice. Oncotarget. 2017 Jan 3; 8(1): 610-623.
- Junping Zhang, et al. Hypericin-mediated photodynamic therapy induces apoptosis of myoloma SP2/0 cells depended on caspase activity in vitro. Cancer Cell Int. 2015; 15: 58
Products are for research use only. Not for human use.