MTK 458

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Description: PINK1 activator
Chemical Name: N-[(1R)-1,2,3,4-Tetrahydro-1-naphthalenyl]-6-(trifluoromethyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine
Purity: ≥98% (HPLC)
Datasheet
Citations
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Biological Activity for MTK 458

MTK 458 is a brain penetrant PTEN-induced kinase 1 (PINK1) activator. It binds to and stabilizes the active form of PINK1, increasing its activity and activating mitophagy downstream. It mediates clearance of pathogenic α-synuclein and normalizes pS65-Ubiquitin (pUb) in in vivo Parkinson's models. MTK458 is orally bioavailable.

Licensing Information

Sold with kind permission of Mitokinin

Technical Data for MTK 458

M. Wt 332.33
Formula C17H15F3N4
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2499962-58-0
PubChem ID 155187445
InChI Key JOIONRWKOGDQOG-CYBMUJFWSA-N
Smiles FC(F)(F)C1=CC(C(N1)=NC=N2)=C2N[C@H]3C4=CC=CC=C4CCC3

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for MTK 458

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 16.62 50
ethanol 6.65 20

Preparing Stock Solutions for MTK 458

The following data is based on the product molecular weight 332.33. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.5 mM 6.02 mL 30.09 mL 60.18 mL
2.5 mM 1.2 mL 6.02 mL 12.04 mL
5 mM 0.6 mL 3.01 mL 6.02 mL
25 mM 0.12 mL 0.6 mL 1.2 mL

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References for MTK 458

References are publications that support the biological activity of the product.

Chin et al (2023) Pharmacological PINK1 activation ameliorates pathology in Parkinson's disease models. bioRxiv PMID: 36824886


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Citations for MTK 458

Citations are publications that use Tocris products.

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