A PINK1 activator
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MTK 458

Item No. 41391

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[(1R)-1,2,3,4-tetrahydro-1-naphthalenyl]-6-(trifluoromethyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine
CAS Number
2499962-58-0
Synonyms
  • EP-0035985
Molecular Formula
C17H15F3N4
Formula Weight
332.3
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/ml
SMILES
FC(F)(C1=CC2=C(N[C@@H]3CCCC4=CC=CC=C43)N=CN=C2N1)F
InChi Code
InChI=1S/C17H15F3N4/c18-17(19,20)14-8-12-15(21-9-22-16(12)24-14)23-13-7-3-5-10-4-1-2-6-11(10)13/h1-2,4,6,8-9,13H,3,5,7H2,(H2,21,22,23,24)/t13-/m1/s1
InChi Key
JOIONRWKOGDQOG-CYBMUJFWSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $28

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    5 mg

    $97

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    10 mg

    $152

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    25 mg

    $310

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    Cayman Chemical
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    Product Description

    MTK 458 is a PTEN-inducible putative kinase 1 (PINK1) activator.1 It, in combination with the mitochondria uncoupler FCCP (Item No. 15218), increases levels of PINK1 and phosphorylated ubiquitin (pUb) in HeLa cervical cancer cells when used at a concentration of 6.6 µM. MTK 458, in combination with FCCP, induces mitophagy in HeLa cells (EC50 = 0.44 µM). It inhibits doxycycline-induced increases in the mitochondrial levels of insoluble ornithine transcarbamylase (OTC) in HeLa cells when used at concentrations of 25 or 50 µM. In vivo, MTK 458 (50 mg/kg per day) decreases the midbrain levels of total α-synuclein and insoluble α-synuclein aggregates in a mouse model of Parkinson's disease induced by α-synuclein injection in the ipsilateral striatum.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. De Roulet, D., Bartholomeus, J., Johnstone, S., et al. Compositions and methods of using the same for treatment of neurodegenerative and mitochondrial disease. (2020).