- E-64-c
- Cathepsin G Inhibitor I
- CA 074
- L 006235
- E 64d
- E-64
| CA-074 MeCathepsin B inhibitor |
Sample solution is provided at 25 µL, 10mM.
- 1. Chen CH, Bhasin S, et al. "Study of Cathepsin B inhibition in VEGFR TKI treated human renal cell carcinomaxenografts." Oncogenesis. 2019 Feb 22;8(3):15.PMID:30796200
- 2. Xu Z, Zhang Y, et al. "Novelhalf-sandwich iridium OˆC (carbene)-Complexes: In vitro and in vivo tumor growth suppression and pro-apoptosis via ROS-mediated cross-talk between mitochondria and lysosomes." Cancer Lett. 2019 Apr 10;447:75-85.PMID:30673591
- 3. Yan X, Li F, et al. "Interleukin-1beta released by microglia initiates the enhanced glutamatergic activity in the spinal dorsal horn during paclitaxel-associated acute pain syndrome." Glia. 2018 Dec 21.PMID:30578561
- 4. Gonzalez EA, Martins GR, et al. "Cathepsin B inhibition attenuates cardiovascular pathology inmucopolysaccharidosis I mice." Life Sci. 2018 Mar 1;196:102-109.PMID:29366749
- 5. Shao G, Wang R, et al. "The E3 ubiquitin ligase NEDD4 mediates cell migration signaling of EGFR in lung cancer cells." Mol Cancer. 2018 Feb 19;17(1):24.PMID:29455656
- 6. Clerc P, Jeanjean P, et al. "Targeted Magnetic Intra-Lysosomal Hyperthermia produces lysosomal reactive oxygen species and causes Caspase-1 dependent cell death." J Control Release. 2017 Dec 1;270:120-134.PMID:29203413
Quality Control & MSDS
- View current batch:
- Purity = 98.06%
- COA (Certificate Of Analysis)
- HPLC
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
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| Description | CA-074 Me is a selective and cell-permeable inhibitor of cathepsin B. | |||||
| Targets | cathepsin B | |||||
| IC50 | 2.2 nM | |||||
| Cell experiment: [1] | |
Cell lines | McNtcp.24 cells |
Preparation method | The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
Reaction Conditions | 0.1 µM, 2 hours |
Applications | Cells were incubated in medium alone or with 50 µM GCDC in the absence or presence of 0.1 µM CA-074 Me. Apoptosis was quantitated after 2 h of incubation. The cathepsin B inhibitor CA-074 Me reduced the GCDC-mediated increase in cathepsin B activity and apoptosis in McNtcp.24 cells. The result confirms that cathepsin B activity increases and contributes to bile salt–mediated apoptosis in primary rat hepatocytes. |
| Animal experiment: [2] | |
Animal models | CatB+/+ mice |
Dosage form | Intraperitoneal injection, 4 mg/100g |
Applications | Serum ALT levels after TNF-α-treatment were significantly reduced in catB+/+ mice pretreated with CA-074 Me compared to saline-injected controls. In contrast, liver architecture was preserved and only moderate damage was observed in catB+/+ mice pretreated with CA-074 Me. These results suggest that pharmacological inhibition of cat B may partially attenuate TNF-α-induced liver damage. |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1] Faubion W A, Guicciardi M E, Miyoshi H, et al. Toxic bile salts induce rodent hepatocyte apoptosis via direct activation of Fas. The Journal of clinical investigation, 1999, 103(1): 137-145. [2] Guicciardi M E, Miyoshi H, Bronk S F, et al. Cathepsin B knockout mice are resistant to tumor necrosis factor-α-mediated hepatocyte apoptosis and liver injury: implications for therapeutic applications. The American journal of pathology, 2001, 159(6): 2045-2054. | |
CA-074 Me Dilution Calculator
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| Cas No. | 147859-80-1 | SDF | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | methyl (2S)-1-[(2S)-3-methyl-2-[[(2S,3S)-3-(propylcarbamoyl)oxirane-2-carbonyl]amino]pentanoyl]pyrrolidine-2-carboxylate | ||
| Canonical SMILES | CCCNC(=O)C1C(O1)C(=O)NC(C(C)CC)C(=O)N2CCCC2C(=O)OC | ||
| Formula | C19H31N3O6 | M.Wt | 397.5 |
| Solubility | ≥19.875mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A yellow oil | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
CA-074 Me is a membrane-permeable and selective inhibitor of cathepsin B with IC50 value of 36.3 nM [1, 2].
CA-074 Me is a methyl ester derivative of CA-074. In cultured human gingival fibroblasts, CA-074 Me exerted a 95% inhibition of cathepsin B and partial inhibition (54%) of the combined activities of cathepsins B and L. CA-074 Me was also found to inhibit cathespin L under reducing conditions. It inhibited the activity of purified human cathepsin L by more than 90% when the enzyme had been pre-incubated with 1.4 mM DTT or 4.2 mM GSH for 2 hours. Besides that, CA-074 Me completely inhibited cathepsin B in the presence of 1.4 mM DTT [2, 3].
References:[1] Wu X, Zhang L, Gurley E, et al. Prevention of free fatty acid–induced hepatic lipotoxicity by 18β-glycyrrhetinic acid through lysosomal and mitochondrial pathways. Hepatology, 2008, 47(6): 1905-1915.[2] Steverding D. The cathepsin B-selective inhibitors CA-074 and CA-074Me inactivate cathepsin L under reducing conditions. Open Enzyme Inhibition Journal, 2011, 4: 11-16.[3] Buttle D J, Murata M, Knight C G, et al. CA074 methyl ester: a proinhibitor for intracellular cathepsin B. Archives of biochemistry and biophysics, 1992, 299(2): 377-380.
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制冰机原理：
制冰机是一种将水通过蒸发器由制冷系统制冷剂冷却后生成冰的制冷机械设备。根据蒸发器和生成过程方式原理不同，生成的冰的形状也不同，人们一般根据冰形状将制冰机分为颗粒冰机、片冰机、板冰机、管冰机、壳冰机等等。
制冰机的分类：
按冰的形状可分：鳞形片冰机，雪花制冰机，条冰机，板冰机，块冰机（可分食用小块冰机和工业用大块冰机），冰粒机，颗粒机，管冰机，子弹头制冰机。
实验室制冰机种类选择：
我们平时在外面就餐时，经常看到商家在饮料中加入冰块，有时候是方块的，有时候是中空的，还有在菜市场买海鲜的时候也会看到下面铺着一层冰，究竟有什么区别吗？我们在开展实验室工作的时候，应如何选择制冰机呢？
实验室制冰机主要是用于在开展生命科学相关实验时，给样品提供冰浴环境，防止样品（如核酸、蛋白）因为温度的变化导致降解或变质，从而保障实验结果的准确性和有效性。绝大部分的时候，我们的样品是放在EP管、离心管、pcr管等容器里面，然后把样品管插在冰浴中，靠接触来实现温度的保持。由于样品和冰无法直接接触，而是要通过管壁来传输，所以管壁和冰浴的接触面积是冰浴效果的保障，为了更好的保障样品，应尽量的扩大管壁和冰浴的接触面积。
针对以上考虑，实验室制冰机一般选择雪花制冰机，该种类型的制冰机生产出来的冰呈雪花状碎冰，由于颗粒很小，可以和管壁进行密切的接触，保障冰浴效果。
对于出冰的具体要求中，还有一点是非常重要的，出来的雪花冰要求有15-25%的含水量，这样可极大的提高冰浴和管壁的接触效果。
文章来源：厦门国仪科学仪器有限公司
2：冰满探头调整太靠近冰格，顺时针调整180度就好了，也有可能冰满探头坏了。需要更换。
3：水位浮球开关坏，更换。
