Z-LEHD-FMK TFA是一种不可逆的caspase-9抑制剂。
Cas No.:524746-03-0
Sample solution is provided at 25 µL, 10mM.
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Z-LEHD-FMK TFA is an irreversible caspase-9 inhibitor. Z-LEHD-FMK TFA prevents apoptosis by inhibiting caspase-9 activity and reduces neural damage by protecting neurons[1-2]. Z-LEHD-FMK TFA can be used in research related to apoptosis and neuroprotection[3-4].
In vitro, pretreatment of HTLV-1-transformed C81 cells with Z-LEHD-FMK TFA (100μM) for 1 hour, followed by stimulation with LY294002 (40μM) for 24-72 hours, significantly prevented LY294002-induced apoptosis[5]. Pretreatment of SGC7901 cells with Z-LEHD-FMK TFA (20μM) for 30 minutes, followed by co-incubation with G503 (20μM) for 24 hours, reduced the rate of G503-induced apoptotic cells[6].
In vivo, a single intraperitoneal injection of Z-LEHD-FMK TFA (3mg/kg) 2 hours before CCl₄ injection was administered to C57BL/b6N mice. Z-LEHD-FMK TFA significantly exacerbated CCl₄-induced acute liver injury and down-regulated the expression of hepatoprotective autophagy markers[7]. A single intravenous injection of Z-LEHD-FMK TFA (0.8μmol/kg) administered 1 minute after trauma, or continuous injection for 7 days, was used in rats that suffered thoracic spinal cord contusion. Z-LEHD-FMK TFA effectively blocked post-traumatic apoptosis and was associated with better neurological functional recovery outcomes[8].
References:
[1] Mullani N, Singh MK, Sharma A, et al. Caspase-9 inhibitor Z-LEHD-FMK TFA enhances the yield of in vitro produced buffalo (Bubalus bubalis) pre-implantation embryos and alters cellular stress response. Res Vet Sci. 2016 Feb;104:4-9.
[2] Ozoren N, Kim K, Burns TF, et al. The caspase 9 inhibitor Z-LEHD-FMK TFA protects human liver cells while permitting death of cancer cells exposed to tumor necrosis factor-related apoptosis-inducing ligand. Cancer Res. 2000 Nov 15;60(22):6259-65.
[3] Zhang J, Chen Z, Wang S, et al. Prodelphinidin from purple sweet potato induces apoptosis in human triple-negative breast cancer cells via ROS-mediated ER stress activation. Med Oncol. 2025 Mar 6;42(4):92.
[4] Kim TI, Pak JH, Tchah H, et al. Ceramide-induced apoptosis in rabbit corneal fibroblasts. Cornea. 2005 Jan;24(1):72-9.
[5] Jeong SJ, Dasgupta A, Jung KJ, et al. PI3K/AKT inhibition induces caspase-dependent apoptosis in HTLV-1-transformed cells. Virology. 2008 Jan 20;370(2):264-72.
[6] Huang L, Zhang T, Li S, et al. Anthraquinone G503 induces apoptosis in gastric cancer cells through the mitochondrial pathway. PLoS One. 2014 Sep 30;9(9):e108286.
[7] Guo R, Lin B, Pan JF, et al. Inhibition of caspase-9 aggravates acute liver injury through suppression of cytoprotective autophagy. Sci Rep. 2016 Sep 1;6:32447.
[8] Colak A, Karaoğlan A, Barut S, et al. Neuroprotection and functional recovery after application of the caspase-9 inhibitor Z-LEHD-FMK TFA in a rat model of traumatic spinal cord injury. J Neurosurg Spine. 2005 Mar;2(3):327-34.
Z-LEHD-FMK TFA是一种不可逆的caspase-9抑制剂。Z-LEHD-FMK TFA可抑制caspase-9活性来防止细胞凋亡，同时通过保护神经元以减少神经损伤[1-2]。Z-LEHD-FMK TFA可用于细胞凋亡研究和神经保护研究的相关研究[3-4]。
在体外，Z-LEHD-FMK TFA（100μM）预处理HTLV-1转化的C81细胞1小时，随后以LY294002（40μM）刺激24-72小时，可显著防止LY294002诱导的细胞凋亡[5]。Z-LEHD-FMK TFA（20μM）预处理SGC7901细胞30分钟，随后与G503（20μM）共同孵育24小时，可降低G503诱导的凋亡细胞率[6]。
在体内，Z-LEHD-FMK TFA（3mg/kg）在CCl4注射前2小时单次腹腔注射，用于处理C57BL/b6N小鼠。Z-LEHD-FMK TFA显著加剧了CCl4诱导的急性肝损伤，并下调了肝保护性自噬标志物的表达[7]。Z-LEHD-FMK TFA（0.8μmol/kg）在创伤后1分钟单次静脉注射，或连续注射7天，用于处理遭受胸段脊髓挫伤的大鼠。Z-LEHD-FMK TFA有效阻断了创伤后的细胞凋亡，并与更好的神经功能恢复结果相关[8]。
| Cell experiment [1]: | |
Cell lines | HTLV-1-transformed C81 cells (human T-cell leukemia virus type 1-transformed cell line) |
Preparation Method | HTLV-1-transformed C81 cells were pretreated with the caspase-9 specific inhibitor Z-LEHD-FMK TFA (100μM) for one hour prior to the addition of the PI3K/AKT inhibitor LY294002. |
Reaction Conditions | 100μM; 1h pretreatment. |
Applications | Pretreatment of the cells with the caspase-9 specific inhibitor Z-LEHD-FMK TFA significantly reduced LY294002-induced apoptosis. |
| Animal experiment [2]: | |
Animal models | C57BL/b6N mice |
Preparation Method | Mice were pretreated with a single intraperitoneal injection of the caspase-9 inhibitor Z-LEHD-FMK TFA (3mg/kg) 2 hours before the administration of carbon tetrachloride (CCl4) to induce acute liver injury. |
Dosage form | 3mg/kg; i.p.; single injection. |
Applications | Pretreatment with Z-LEHD-FMK TFA significantly exacerbated CCl4-induced acute hepatocellular injury, as evidenced by increased hepatic necrosis and inflammation, and a marked up-regulation in serum ALT levels. Z-LEHD-FMK TFA also down-regulated the expression of autophagy markers (Beclin1, LC3II, LAMP1), indicating the suppression of cytoprotective autophagy. Z-LEHD-FMK TFA up-regulated the levels of pro-inflammatory mediators (TNF-α, IL-1β) and aggravated hepatic necroptosis via the NF-κB pathway. |
References: | |
| Cas No. | 524746-03-0 | SDF | Download SDF |
| 别名 | Caspase-9 Inhibitor | ||
| 分子式 | C34H44F4N6O12 | 分子量 | 804.74 |
| 溶解度 | Water: 100 mg/mL (124.26 mM); | 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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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.2426 mL | 6.2132 mL | 12.4264 mL |
| 5 mM | 248.5 μL | 1.2426 mL | 2.4853 mL |
| 10 mM | 124.3 μL | 621.3 μL | 1.2426 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 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 | ||||||||||
| 计算重置 | ||||||||||
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，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
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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