S81390 |
Ac-DEVD-CHO |
源葉(MedMol) | 95% |
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- 產(chǎn)品描述: Ac-DEVD-CHO is a specific Caspase-3 inhibitor with a Ki value of 230 pM.
- 靶點: Caspase 3:0.23 nM (Ki);Caspase-8:0.92 nM (Ki);Caspase-7:1.6 nM (Ki);Caspase-10:12 nM (Ki);Caspase-1:18 nM (Ki);Caspase-6:31 nM (Ki);Caspase-9:60 nM (Ki);Caspase-4:132 nM (Ki);Caspase-5:205 nM (Ki);Caspase-2:1710 nM (Ki);Apoptosis;?Caspase
- 體外研究:
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
- 體內(nèi)研究:
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)%
- 參考文獻:
1. 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. 2. 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. 3. 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 4. Long-gang He, et al. Sinomenine induces apoptosis in RAW 264.7 cell-derived osteoclasts in vitro via caspase-3 activation. Acta Pharmacol 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 kidney injury induced by peritoneal cavity infection in mice. Zhongguo Wei Zhong Bing Ji Jiu Yi Xue. 2010 Dec;22(12):736-9.
- 溶解性: Soluble in H2O
- 保存條件: -20℃
- 配置溶液濃度參考:
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 50 mM 0.04 ml 0.199 ml 0.398 ml
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本計算器可幫助您計算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系,公式為:
質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)