Ac-IETD-CHO (trifluoroacetate salt)是一种caspase 8抑制剂，可阻止focal adhesion kinase (Fak)被caspase裂解，IC50值为200nM。
Sample solution is provided at 25 µL, 10mM.
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Ac-IETD-CHO (trifluoroacetate salt) is a caspase 8 inhibitor that can prevent the focal adhesion kinase (Fak) from being cleaved by caspase, with an IC50 value of 200nM [1]. Ac-IETD-CHO can prevent caspase-8 from cleaving Bid protein, prevent the loss of mitochondrial membrane potential, and inhibit cell apoptosis[2]. Ac-IETD-CHO has been widely used to inhibit DNA fragmentation and prevent various types of cell apoptosis caused by non-steroidal anti-inflammatory drugs[3].
In vitro, Ac-IETD-CHO treatment (300µM) for 24 hours significantly inhibited the death of MOLT-4N1 cells after 1.8Gy X-ray radiation, and promoted cell survival[4]. Treatment with 100µM Ac-IETD-CHO for 9 hours significantly prevented the reduction in the expression of CD31 and CD47 on the surface of Jurkat cells induced by etoposide[5].
References:
[1] Gervais F G, Thornberry N A, Ruffolo S C, et al. Caspases cleave focal adhesion kinase during apoptosis to generate a FRNK-like polypeptide[J]. Journal of Biological Chemistry, 1998, 273(27): 17102-17108.
[2] Yamada H, Tada-Oikawa S, Uchida A, et al. TRAIL causes cleavage of bid by caspase-8 and loss of mitochondrial membrane potential resulting in apoptosis in BJAB cells[J]. Biochemical and biophysical research communications, 1999, 265(1): 130-133.
[3] Inoue A, Muranaka S, Fujita H, et al. Molecular mechanism of diclofenac-induced apoptosis of promyelocytic leukemia: dependency on reactive oxygen species, Akt, Bid, cytochrome and caspase pathway[J]. Free Radical Biology and Medicine, 2004, 37(8): 1290-1299.
[4] Nakano H, Shinohara K. Time sequence analysis of caspase-3-independent programmed cell death and apoptosis in X-irradiated human leukemic MOLT-4 cells[J]. Cell and tissue research, 2002, 310(3): 305-311.
[5] Azuma Y, Nakagawa H, Dote K, et al. Decreases in CD31 and CD47 levels on the cell surface during etoposide-induced Jurkat cell apoptosis[J]. Biological and Pharmaceutical Bulletin, 2011, 34(12): 1828-1834.
Ac-IETD-CHO (trifluoroacetate salt)是一种caspase 8抑制剂，可阻止focal adhesion kinase (Fak)被caspase裂解，IC50值为200nM[1]。Ac-IETD-CHO能阻止caspase-8裂解Bid蛋白，防止线粒体膜电位丧失，并抑制细胞凋亡[2]。Ac-IETD-CHO已被广泛用于抑制DNA片段化，并预防非甾体抗炎药引起的多种类型细胞凋亡[3]。
在体外，300µM的Ac-IETD-CHO处理经1.8Gy X射线照射的MOLT-4N1细胞24小时，显著抑制了细胞死亡，并促进了细胞存活[4]。100µM的Ac-IETD-CHO处理9小时，显著阻止了依托泊苷诱导的Jurkat 细胞表面CD31和CD47表达的下调[5]。
| Cell experiment [1]: | |
Cell lines | HL-60 cells |
Preparation Method | HL-60 cells were cultured in RPMI 1640 medium supplemented with 100U/ml penicillin and 100mg/ml streptomycin in 5% CO2 at 37°C. Cells were placed in a 96 well-plate at a concentration of 1×105 cells per well and were treated with Ac-IETD-CHO (10µM) for 1h, and subsequently with or without 100μM diclofenac for 24h, then the DNA fragmentation was analyzed. |
Reaction Conditions | 10µM; 1h |
Applications | Ac-IETD-CHO treatment significantly suppressed Diclofenac-induced DNA fragmentation in HL-60 cells. |
References: | |
| Cas No. | SDF | ||
| 别名 | Caspase-8 Inhibitor | ||
| 化学名 | N-acetyl-L-isoleucyl-L-α-glutamyl-N-[(1S)-2-carboxy-1-formylethyl]-L-threoninamide, trifluoroacetate salt | ||
| Canonical SMILES | C[C@@H](O)[C@@H](C(N[C@@H](CC(O)=O)C=O)=O)NC([C@@H](NC([C@H]([C@@H](C)CC)NC(C)=O)=O)CCC(O)=O)=O.FC(F)(C(O)=O)F | ||
| 分子式 | C21H34N4O10 • XCF3COOH | 分子量 | 502.5 |
| 溶解度 | 1mg/mL in water | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.99 mL | 9.9502 mL | 19.9005 mL |
| 5 mM | 398 μL | 1.99 mL | 3.9801 mL |
| 10 mM | 199 μL | 995 μL | 1.99 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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