Home>>Signaling Pathways>> Proteases>> Cathepsin>>CA 074

CA 074 Sale

(Synonyms: CA-074,CA074) 目录号 : GC16317

A selective cathepsin B inhibitor

CA 074 Chemical Structure

Cas No.:134448-10-5

规格 价格 库存 购买数量
1mg
¥651.00
现货
5mg
¥1,100.00
现货
10mg
¥1,800.00
现货
25mg
¥2,800.00
现货

电话:400-920-5774 Email: sales@glpbio.cn

Customer Reviews

Based on customer reviews.

Sample solution is provided at 25 µL, 10mM.

客户使用产品发表文献 1

产品文档

Quality Control & SDS

View current batch:

实验参考方法

Cell experiment [1]:

Cell lines

Human umbilical vein endothelial cells (HUVECs)

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

24 h; 10 mM

Applications

The effects on the viability of HUVECs of cathepsin B specific inhibitors 10 mM CA-074 (96.9±1.2% viability ) and its membrane-permeable analog CA-074-Me (101.7±0.4% viability) was negligible, as was that of Minocycline (102.3±2.6% ) at 10mM.

Animal experiment [2]:

Animal models

Female Balb/c mice

Dosage form

50 mg/kg; intraperitoneal injection

Applications

To test the therapeutic efficacy of cysteine protease inhibitors in vivo, we treated 4T1.2 tumor –bearing mice with the selective CA-074 inhibitor. Treatment of 4T1.2 tumor–bearing mice with the inhibitor had no impact on primary tumor growth. However, analysis of metastasis revealed a significant difference between in the compounds. CA-074 treatment significantly decreased metastasis to lung (P < 0.05) and bone (P < 0.05).

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] Premzl A, Turk V, Kos J. Intracellular proteolytic activity of cathepsin B is associated with capillary‐like tube formation by endothelial cells in vitro[J]. Journal of cellular biochemistry, 2006, 97(6): 1230-1240.

[2] Withana N P, Blum G, Sameni M, et al. Cathepsin B inhibition limits bone metastasis in breast cancer[J]. Cancer research, 2012, 72(5): 1199-1209.

产品描述

CA-074, a specific cathepsin B inhibitor, also abolished the neurotoxic effects caused by Abeta42-activated BV2 cell [1]. Co-treatment of cultures with the cathepsin B inhibitors CA-074 or Z-FA-FMK suppressed the cytostatic effects of TPA and activation of pro-uPA [2]. Administration of CA-074 suppresses the response to exogenous antigens, such as hepatitis B virus antigen, ovalbumin and Leishmania major antigen, and induces switching of the helper T cell responses from Th-2 to Th-1 of CD4+ T cell, thereby down regulating the production of IgE and IgG1 [3]. Pharmacological inhibition of cat B in catB(+/+) mice with L-3-trans-(propylcarbamoyl)oxirane-2-carbonyl-Lisoleucyl-L-proline (CA-074 Me) also reduced TNF-alpha-induced liver damage. [4] Administration of cathepsin B inhibitors, E-64, CA-074 and vitamin B6, caused the strong suppression of the Th-2 type immune responses .

 Inhibitor of cathepsin B (Ki = 2-5 nM). Displays selectivity over cathepsins H and L (Ki = 40-200 μM). Shown to reduce bone metastasis in a 4T1.2 breast cancer model.

References:
1. Identification of cathepsin B as a mediator of neuronal death induced by Abeta-activated microglial cells using a functional genomics approach. Gan, L., Ye, S., Chu, A., Anton, K., Yi, S., Vincent, V.A., von Schack, D., Chin, D., Murray, J., Lohr, S., Patthy, L., Gonzalez-Zulueta, M., Nikolich, K., Urfer, R. J. Biol. Chem. (2004)
2. Phorbol ester activation of a proteolytic cascade capable of activating latent transforming growth factor-betaL a process initiated by the exocytosis of cathepsin B. Guo, M., Mathieu, P.A., Linebaugh, B., Sloane, B.F., Reiners, J.J. J. Biol. Chem. (2002)
3. Insights into the roles of cathepsins in antigen processing and presentation revealed by specific inhibitors. Katunuma, N., Matsunaga, Y., Himeno, K., Hayashi, Y. Biol. Chem. (2003)
4. Cathepsin B knockout mice are resistant to tumor necrosis factor-alpha-mediated hepatocyte apoptosis and liver injury: implications for therapeutic applications. Guicciardi, M.E., Miyoshi, H., Bronk, S.F., Gores, G.J. Am. J. Pathol. (2001)

Chemical Properties

Cas No. 134448-10-5 SDF
别名 CA-074,CA074
化学名 (2S)-1-[(2S,3S)-3-methyl-2-[[(3S)-3-(propylcarbamoyl)oxirane-2-carbonyl]amino]pentanoyl]pyrrolidine-2-carboxylic acid
Canonical SMILES CCCNC(=O)C1C(O1)C(=O)NC(C(C)CC)C(=O)N2CCCC2C(=O)O
分子式 C18H29N3O6 分子量 383.44
溶解度 ≥ 19.17mg/mL in DMSO 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。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

制备储备液
1 mg 5 mg 10 mg
1 mM 2.608 mL 13.0398 mL 26.0797 mL
5 mM 0.5216 mL 2.608 mL 5.2159 mL
10 mM 0.2608 mL 1.304 mL 2.608 mL
  • 摩尔浓度计算器

  • 稀释计算器

  • 分子量计算器

质量
=
浓度
x
体积
x
分子量
 
 
 
*在配置溶液时,请务必参考产品标签上、MSDS / COA(可在Glpbio的产品页面获得)批次特异的分子量使用本工具。

计算

动物体内配方计算器 (澄清溶液)

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
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % saline
计算重置

Research Update

1. CA-074, but not its methyl ester CA-074Me, is a selective inhibitor of cathepsin B within living cells. Biol Chem. 2002 Jul-Aug;383(7-8):1305-8.
Abstract
CA-074 is better-suited for cathepsin B specific inactivation in living cells, since it selectively inhibited cathepsin B leaving cathepsin L unaffected.
2. Inhibition of ischaemic hippocampal neuronal death in primates with cathepsin B inhibitor CA-074: a novel strategy for neuroprotection based on 'calpain-cathepsin hypothesis'. Eur J Neurosci. 1998 May;10(5):1723-33.
Abstract
Intravenous administration of CA-074 exhibited excellent inhibition against cathepsin B and saved CA1 neurons from delayed neuronal death in monkeys undergoing a complete 20 min whole brain ischaemia.