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KEA1-97

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Chemical Structure| 2138882-71-8 同义名 : -
CAS号 : 2138882-71-8
货号 : A1465541
分子式 : C15H9Cl2FN4
纯度 : 99%+
分子量 : 335.163
MDL号 : MFCD31697744
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(313.28 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Thioredoxin is an endogenous protein with antioxidant and antiapoptotic activity in a variety of tissues Zhuming Yin,et al. Thioredoxin Protects Skin Flaps from Ischemia-Reperfusion Injury: A Novel Prognostic and Therapeutic Target.. Caspase-3 (Casp-3) is an enzyme that efficiently induces apoptosis, a form of programmed cell death[1]. The EC(50) for caspase-3 activation by reduced thioredoxin-1 was 2.5 mM, by reduced glutathione 1.0 mM and by dithiothreitol 3.5 mM. A catalytic site redox-inactive mutant thioredoxin-1 was almost as active as thioredoxin-1 in activating caspase-3. Caspase activation was shown to correlate with the number of reduced cysteine residues in the thioredoxins. Reduced insulin and serum albumin were as effective on a molar basis as thioredoxin-1 in activating caspase-3[2]. Compared with the model group, the mRNA expression of caspase-3 and the protein levels of caspase-3 and cleaved-caspase-3 were notably elevated in the Weimaining group. After in vivo bioluminescent imaging, the total photon number of the Weimaining group was found to be lower than that of the LWMH group on day 14 after administration. Additionally, the AI and expression levels of caspase-3 mRNA, caspase-3, and cleaved-caspase-3 protein of the WMN group were higher than those of the LWMH group. Kea1-97 is a selective disruptor of interaction between thioredoxin and caspase-3 (IC50 = 10 μM)[3]. KEA1-97 disrupts the interaction of thioredoxin with caspase 3, activates caspases, and induces apoptosis without affecting thioredoxin activity. Moreover, KEA1-97 impairs in vivo breast tumor xenograft growth. KEA1-97 impairs 231MFP TNBC survival and proliferation without significantly affecting nontransformed MCF10A cell viability and that KEA1–97daily treatment at 5 mg/kg ip is well-tolerated in mice[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.98mL

0.60mL

0.30mL

14.92mL

2.98mL

1.49mL

29.84mL

5.97mL

2.98mL
参考文献

[1] Nina B Hentzen,et al. Intracellular Photoactivation of Caspase-3 by Molecular Glues for Spatiotemporal Apoptosis Induction. J Am Chem Soc. 2020 May 6;142(18):8080-8084.

[2] A Baker,et al. Redox control of caspase-3 activity by thioredoxin and other reduced proteins. Biochem Biophys Res Commun.2000 Feb 5;268(1):78-81.

[3]Haoliang Ke,et al. Effect of weimaining on apoptosis and Caspase-3 expression in a breast cancer mouse model. J Ethnopharmacol. 2021 Jan 10;264:113363.

[4]Kimberly E Anderson,et al. Chemoproteomics-Enabled Covalent Ligand Screening Reveals a Thioredoxin-Caspase 3 Interaction Disruptor That Impairs Breast Cancer Pathogenicity. ACS Chem Biol. 2017 Oct 20;12(10):2522-2528.