Ac-DEVD-CHO - Caspase 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAc-DEVD-CHOCat. No.: HY-P1001CAS No.: 169332-60-9分式: CHNO分量: 502.47Sequence: N-Acetyl-Asp-Glu-Val-Asp-alSequence Shortening: Ac-DEVD-al作靶點(diǎn): Caspase作通路: Apoptosis儲(chǔ)存式: Powder -80C 2 years-20C 1 yearIn solvent -80C 6 months-20C 1 m

2、onth溶解性數(shù)據(jù)體外實(shí)驗(yàn) H2O : 50 mg/mL (99.51 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 1.9902 mL 9.9508 mL 19.9017 mL5 mM 0.3980 mL 1.9902 mL 3.9803 mL10 mM 0.1990 mL 0.9951 mL 1.9902 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Ac-D

3、EVD-CHO種特異性 Caspase-3 抑制劑，Ki 值為 230 pM。IC50 & Target Caspase-1 Caspase-2 Caspase 3 Caspase-41/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE18 nM (Ki) 1710 nM (Ki) 0.23 nM (Ki) 132 nM (Ki)Caspase-5 Caspase-6 Caspase-7 Caspase-8205 nM (Ki) 31 nM (Ki) 1.6 nM (Ki) 0.92 nM (Ki)Caspase-9 Caspase-1060 nM

4、 (Ki) 12 nM (Ki)體外研究 To ascertain the role of caspase-3 in SLNT-induced apoptosis, a caspase-3 inhibitor (Ac-DEVD-CHO) isused. The addition of Ac-DEVD-CHO significantly prevents SLNT-induced apoptosis (from 32.911.21%decreases to 15.881.58% while NC and Ac-DEVD-CHO groups are 6.450.96%, 7.770.79%, r

5、espectively)2. The apoptosis rates of cells pretreated with zVAD-fmk (5.32%) or Ac-DEVD-CHO (7.43%) decreaseobviously after hypericin-mediated PDT treatment 3. Remarkably, 10 mol/L Ac-DEVD-CHO partially blocksthe effect of SIN-induced apoptosis and reduces the number of apoptotic nuclei. These effec

6、ts of SIN areblocked by the caspase-3 inhibitor Ac-DEVD-CHO. Camptothecin (4 M), a positive control, increasescaspase-3 activity, which is also blocked by Ac-DEVD-CHO 4.體內(nèi)研究 Compare with model group, in CI group, the concentrations of serum BUN are decreased significantly at alltime points after ope

7、ration and those of Cr are decreased significantly at 6 hours, then restored to those ofthe sham group at 12 hours and 24 hours; the concentrations of serum TNF-, IL-6 are decreased and thoseof IL-10 are elevated significantly at all time points. TNF- (g/L) 6 hours: 436.264.2 vs. 653.68.9, 12hours:

8、233.485.4 vs. 579.7137.1, 24 hours: 151.090.3 vs. 551.0119.8, IL-6 (g/L) 6 hours: 1033.2345.8vs. 1 595.3159.4, 12 hours: 366.368.3 vs. 1 330.7249.8, 24 hours: 241.2208.4 vs. 815.3572.7, IL-10 (g/L) 6 hours: 33.610.4 vs. 26.64.5, 12 hours: 37.25.0 vs. 24.54.3, 24 hours: 38.35.5 vs. 18.21.6, all P5.PR

9、OTOCOLCell Assay 4 OCLs are incubated with RANKL and treated with 0.5 mM SIN with or without the specific caspase-3 inhibitorAc-DEVD-CHO (10 M) for 24 h. At the end of the treatment, the cells are washed with PBS and are stainedfor 15 min with 10 M Hoechst 33258 dye. Images of the staineing cells ar

10、e captured with a fluorescentmicroscope. The differences are evaluated by counting the number of cells with apoptotic nuclearcondensation in each well 4.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal One hundred and two male mice are subjected t

11、o cecal ligation and puncture or sham operation. TheAdministration 5 animals are assigned into three equal groups (n=34) according to random number table: sham group, modelgroup, and caspase-3 inhibitor (CI) group. Thirty minutes before CLP, Ac-DEVD-CHO (4 g/g) is injectedsubcutaneously in CI group.

12、 The levels of blood urea nitrogen (BUN) and creatinine (Cr) are determined, andthe concentrations of tumor necrosis factor- (TNF-), interleukins (IL-6 and IL-10) are measured by enzymelinked immunosorbent assay (ELISA), the renal cell apoptosis rate is determined by flow cytometry. The 4-day and 7-

13、day survival rates of three groups of mice are observed 5.MCE has not independently confirmed the accuracy of these methods. They are for reference only.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Cell Prolif. 2019 Jul 26:e12663. Apoptosis. 2019 Jun 7. Apoptosis. 2019 Apr;24(3-4):31

14、2-325.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Garcia-Calvo M, et al.nhibition of human caspases by peptide-based and macromolecular inhibitors. J Biol Chem. 1998 Dec4;273(49):32608-13.2. Jinglin Wang, et al. A polysaccharide from Lentinus edodes inhibits human colon can

15、cer cell proliferation and suppresses tumor growthin athymic nude mice. Oncotarget. 2017 Jan 3; 8(1): 610-623.3. Junping Zhang, et al. Hypericin-mediated photodynamic therapy induces apoptosis of myoloma SP2/0 cells depended on caspaseactivity in vitro. Cancer Cell Int. 2015; 15: 584. Long-gang He,

16、et al. Sinomenine induces apoptosis in RAW 264.7 cell-derived osteoclasts in vitro via caspase-3 activation. ActaPharmacol Sin. 2014 Feb; 35(2): 203-210.5. Liu LX, et al. The effect of caspase-3 inhibitor on the concentrations of serum inflammatory cytokines in sepsis related acute kidneyinjury induced by peritoneal cavity infection in mice. Zhongguo Wei Zhong