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MCU-i4

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Chemical Structure| 371924-24-2 同义名 : -
CAS号 : 371924-24-2
货号 : A1445645
分子式 : C23H27N3O2
纯度 : 99%+
分子量 : 377.479
MDL号 : MFCD02730422
存储条件:

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 12 mg/mL(31.79 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 The mitochondrial calcium uniporter is a multi-subunit Ca2+-activated Ca2+ channel, made up of the pore-forming the mitochondrial calcium uniporter (MCU) protein, a metazoan-specific EMRE subunit, and MICU1/MICU2, which mediate Ca2+ activation[2]. Ca2+ uptake by mitochondria regulates bioenergetics, apoptosis, and Ca2+ signaling. The primary pathway for mitochondrial Ca2+ uptake is the MCU, a Ca2+ selective ion channel in the inner mitochondrial membrane[3]. MCU dysfunction has been shown to alter mitochondrial Ca2+ dynamics, in turn eliciting cell apoptosis. Changes in mitochondrial Ca2+ uptake have been implicated in pathological conditions affecting multiple organs, including the heart, skeletal muscle, and brain[4]. MCU, Nrf2, and MICU1 were strongly expressed in OSCC as compared to normal tissues, while MICU2 was relatively weakly expressed in OSCC tissues. Knockdown of MCU distinctly weakened proliferation and migration and lowered MMP level in CAL 27 cells[5]. MCU had a higher expression in gastric cancer tissues than normal tissues. Compared to gastric cancer tissues, its expression was significantly higher after omental metastasis. MCU expression was significantly correlated with depth of invasion (p=0.048), lymph metastasis (p=0.027), TNM stage (p=0.036) and distant metastasis (p=0.029)[6]. MCU-i4 is a novel negative modulator of the MCU, binding MICU1 and impairing muscle cell growth[7].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.65mL

0.53mL

0.26mL

13.25mL

2.65mL

1.32mL

26.49mL

5.30mL

2.65mL

参考文献

[1]Di Marco G, Vallese F, Jourde B, Bergsdorf C, Sturlese M, De Mario A, Techer-Etienne V, Haasen D, Oberhauser B, Schleeger S, Minetti G, Moro S, Rizzuto R, De Stefani D, Fornaro M, Mammucari C. A High-Throughput Screening Identifies MICU1 Targeting Compounds. Cell Rep. 2020 Feb 18;30(7):2321-2331.e6. doi: 10.1016/j.celrep.2020.01.081. PMID: 32075766; PMCID: PMC7034061.

[2]Anna M Van Keuren,et al. Mechanisms of EMRE-Dependent MCU Opening in the Mitochondrial Calcium Uniporter Complex.Cell Rep.2020 Dec 8;33(10):108486.

[3]Horia Vais,et al. Coupled transmembrane mechanisms control MCU-mediated mitochondrial Ca 2+ uptake. Proc Natl Acad Sci U S A. 2020 Sep 1;117(35):21731-21739.

[4]B Rita Alevriadou,et al. Molecular nature and physiological role of the mitochondrial calcium uniporter channel. Am J Physiol Cell Physiol. 2021 Apr 1;320(4):C465-C482.

[5]Ran Wu. MCU That Is Transcriptionally Regulated by Nrf2 Augments Malignant Biological Behaviors in Oral Squamous Cell Carcinoma Cells. Biomed Res Int. 2021 Jun 3;2021:6650791.

[6]Xiaofei Wang,et al. The Regulatory Mechanism and Biological Significance of Mitochondrial Calcium Uniporter in the Migration, Invasion, Angiogenesis and Growth of Gastric Cancer. Onco Targets Ther. 2020 Nov 17;13:11781-11794.

[7]Marco G D , Vallese F , Jourde B , et al. A High-Throughput Screening Identifies MICU1 Targeting Compounds[J]. Cell Reports, 2020, 30(7):2321-2331.e6.