MitoBloCK-10

产品说明书

Print
Chemical Structure| 394694-98-5 同义名 : -
CAS号 : 394694-98-5
货号 : A1365283
分子式 : C12H8FN3O3S
纯度 : 99%+
分子量 : 293.274
MDL号 : MFCD00813373
存储条件：

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

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(409.17 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 A complex containing the integral membrane proteins Tim17 and Tim23 constitutes the import channel for preproteins containing amino-terminal hydrophilic presequences. This complex is associated with Tim44 which serves as an adaptor protein for the binding of mtHsp70 to the membrane. mtHsp70, a 70 kDa heat shock protein of the mitochondrial matrix, drives the ATP-dependent import reaction of the processed preprotein after cleavage of the presequence[2]. Tim44 is tightly associated with the inner mitochondrial membrane on the matrix side. The Tim44 C-Terminal Domain (CTD) functions as an Inner Mitochondrial Membrane (IMM) anchor that recruits the Presequence protein Associated Motor (PAM) to the TIM23 channel[3]. Tim44 plays multiple roles in mitochondrial protein import by recruiting Ssc1 and its J protein cochaperone to the translocon and coordinating their interactions to promote efficient protein translocation in vivo[4].Hsp70 chaperones interact with substrate proteins in a coordinated fashion that is regulated by nucleotides and enhanced by assisting cochaperones[5]. MitoBloCK-10 inhibits inner membrane(Tim)44 binding to the precursor and to Hsp70.MitoBloCK-10 is the first small molecule modulator to attenuate protein-associated motor (PAM) complex activity. MB-10 (100 μM) is a potential attenuator of protein import into mitochondria.MB-10 inhibits the import of substrates that use the TIM23 import pathway.MB-10 (0-100 μM) inhibits protein import into mammalian mitochondria[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.41mL

0.68mL

0.34mL

17.05mL

3.41mL

1.70mL

34.10mL

6.82mL

3.41mL
参考文献

[1]Miyata N, Tang Z, Conti MA, Johnson ME, Douglas CJ, Hasson SA, Damoiseaux R, Chang CA, Koehler CM. Adaptation of a Genetic Screen Reveals an Inhibitor for Mitochondrial Protein Import Component Tim44. J Biol Chem. 2017 Mar 31;292(13):5429-5442. doi: 10.1074/jbc.M116.770131. Epub 2017 Feb 6. PMID: 28167535; PMCID: PMC5392686.

[2]J Rassow,et al. The preprotein translocase of the mitochondrial inner membrane: function and evolution. J Mol Biol. 1999 Feb 12;286(1):105-20.

[3] Wenjun Cui,et al. Membrane binding mechanism of yeast mitochondrial peripheral membrane protein TIM44. Protein Pept Lett. 2011 Jul;18(7):718-25.

[4]Dirk Schiller,et al. Mol Cell Biol. 2008 Jul;28(13):4424-33.

[5]Natacha Larburu,et al. Open Biol.2020 Aug;10(8):200089.

[6] Non Miyata, et al. Adaptation of a Genetic Screen Reveals an Inhibitor for Mitochondrial Protein Import Component Tim44. J Biol Chem. 2017 Mar 31;292(13):5429-5442.