MitoBloCK-6, 2-(((4-Anilinophenyl)imino)methyl)-4,6-dichlorophenol, 2,4-Dichloro-6-(((((phenylamino)phenyl)imino)methyl)phenol), Mitochondrial Protein Import Blocker from the Carla Koehler laboratory, MB6, MB-6
A cell-permeable, stable dichlorosalicylaldehyde Schiff′s base that acts as a potent, selective inhibitor of Mia40/Erv1 redox-mediated import pathway (IC50 = 700 nM, 900 nM, and 1.4 µM for ALR, Erv1, and Erv2, respectively). Significantly reduces the import of CX9 proteins, Erv1, Tim23, and ADP/ATP carrier (AAC). However, it does not affect mitochondrial membrane integrity as evidenced by the lack of aconitase, AAC, Tim54, Mia40, and cytochrome c release. Has no effect on protein disulfide isomerase, flavin adenine dinucleotide, and succinate dehydrogenase activities and does not disrupt mitochondrial net work or reduce viability of cells even at high concentrations (~100 µM in HeLa and HEK293 cells). Reported to specifically cause cytochrome c release, activate caspase-3, and induce apoptosis in human embryonic stem cells (~20 µM), but not in differentiated cells. Reversibly impairs cardiac development and reduces heart rate in zebra fish that is attributed to mitochondrial dysfunction.
Biochem/physiol Actions
Cell permeable: yes
Primary Target Erv1
Reversible: no
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Use only fresh DMSO for reconstitution.
Other Notes
Dabir, D.V., et al. 2013. Dev. Cell25, 81.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
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The mitochondrial disulfide relay system of Mia40 and Erv1/ALR facilitates import of the small translocase of the inner membrane (Tim) proteins and cysteine-rich proteins. A chemical screen identified small molecules that inhibit Erv1 oxidase activity, thereby facilitating dissection of the
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