2. Cell Cycle/DNA Damage Autophagy
  3. Deubiquitinase Mitophagy
  4. MTX115325

MTX115325 (Example 1) is an orally active, brain-penetrating USP30 inhibitor (IC50=12 nM) with neuroprotective activity. MTX115325 increases ubiquitination (EC50=32 nM) of the mitochondrial outer membrane protein TOM20 (a USP30 substrate), increasing mitophagy. MTX115325 prevents dopaminergic neuron loss and preserves striatal dopamine.

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MTX115325 Chemical Structure

MTX115325 Chemical Structure

CAS No. : 2750895-97-5

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5 mg USD 2200 In-stock
10 mg USD 3600 In-stock
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Based on 1 publication(s) in Google Scholar

MTX115325 Related Antibodies

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USP1 USP2 USP7 USP8 USP30 UCHL1

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Description

MTX115325 (Example 1) is an orally active, brain-penetrating USP30 inhibitor (IC50=12 nM) with neuroprotective activity. MTX115325 increases ubiquitination (EC50=32 nM) of the mitochondrial outer membrane protein TOM20 (a USP30 substrate), increasing mitophagy. MTX115325 prevents dopaminergic neuron loss and preserves striatal dopamine[1].

IC50 & Target

IC50: 12 nM (USP30)
EC50: 32 nM (TOM20, the outer mitochondrial membrane protein)[1]
In Vitro

MTX115325 (37 nM-1 μM; 72 h) shows promotion of mitochondrial autophagy in SH-SY5Y cells[1].
MTX115325 (10 nM-1 μM; 90 min) promotes ubiquitination of TOM20 and inhibits USP30 activity in both HeLa cells and YFP-Parkin overexpressing HeLa cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

MTX115325 Related Antibodies
In Vivo

MTX115325 (i.g.; 15 mg/kg and 50 mg/kg; twice daily for 10 weeks) reduces phosphorylated S129-αSyn levels and decreases the total area of GFAP staining in AAV-A53T-SNCA Mouse Model, indicating lower astrocyte activation[1].
MTX115325 (i.g.; 10 mg/kg; single dose) demonstrates excellent oral bioavailability (98%) and good CNS penetration with a brain partition coefficient (Kpu,u) of approximately 0.4[1].
MTX115325 (i.g.; single dose) has a Cmax of 7546.9 ng/mL at 15 mg/kg and a Cmax of 16374.3 ng/mL at 50 mg/kg. At a 50 mg/kg dosage, the drug concentration consistently remained above the EC50 for TOM20 ubiquitination[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: AAV-A53T-SNCA Mouse Model [1]
Dosage: 15 mg/kg and 50 mg/kg
Administration: i.g.; twice daily for 10 weeks
Result: Reduced the loss of dopaminergic neurons in the substantia nigra (SN) and preserved dopamine levels in the striatum.
Increased the percentage of tyrosine hydroxylase (TH)+ neurons.
Molecular Weight

348.36

Formula

C18H16N6O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=NC=C(C2=CC=NC(C#N)=C2)O1)N3[C@]4([H])[C@@](CC3)([H])[C@H](N(C4)C#N)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (717.65 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8706 mL 14.3530 mL 28.7059 mL
5 mM 0.5741 mL 2.8706 mL 5.7412 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.08%

SDS (251 KB)

COA (249 KB) HNMR (261 KB) LCMS (96 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8706 mL 14.3530 mL 28.7059 mL 71.7648 mL
5 mM 0.5741 mL 2.8706 mL 5.7412 mL 14.3530 mL
10 mM 0.2871 mL 1.4353 mL 2.8706 mL 7.1765 mL
15 mM 0.1914 mL 0.9569 mL 1.9137 mL 4.7843 mL
20 mM 0.1435 mL 0.7176 mL 1.4353 mL 3.5882 mL
25 mM 0.1148 mL 0.5741 mL 1.1482 mL 2.8706 mL
30 mM 0.0957 mL 0.4784 mL 0.9569 mL 2.3922 mL
40 mM 0.0718 mL 0.3588 mL 0.7176 mL 1.7941 mL
50 mM 0.0574 mL 0.2871 mL 0.5741 mL 1.4353 mL
60 mM 0.0478 mL 0.2392 mL 0.4784 mL 1.1961 mL
80 mM 0.0359 mL 0.1794 mL 0.3588 mL 0.8971 mL
100 mM 0.0287 mL 0.1435 mL 0.2871 mL 0.7176 mL
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MTX115325 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MTX1153252750895-97-5MTX 115325MTX-115325DeubiquitinaseMitophagyDUBsMitochondrial AutophagyOral effectivebrain permeabilityneuroprotective activityInhibitorinhibitorinhibit

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