2. Cytoskeleton Metabolic Enzyme/Protease
  3. Calpain
  4. CAST-calpain-2 stabilizer-1

CAST-calpain-2 stabilizer-1 is a blood-brain barrier permeable stabilizer of CAST-calpain-2 interaction. CAST-calpain-2 stabilizer-1 shows no activity against GSK3. CAST-calpain-2 stabilizer-1 can be used in the research of Huntington's disease and tauopathies.

For research use only. We do not sell to patients.

CAST-calpain-2 stabilizer-1

CAST-calpain-2 stabilizer-1 Chemical Structure

CAS No. : 3110929-05-7

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CAST-calpain-2 stabilizer-1 Related Antibodies

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Description

CAST-calpain-2 stabilizer-1 is a blood-brain barrier permeable stabilizer of CAST-calpain-2 interaction. CAST-calpain-2 stabilizer-1 shows no activity against GSK3. CAST-calpain-2 stabilizer-1 can be used in the research of Huntington's disease and tauopathies[1].

In Vitro

CAST-calpain-2 stabilizer-1 (dose-response range) potently restores mitochondrial membrane potential in HdhQ111 mouse striatal neuron-like cells with an EC50 of ~2.77 μM[1].
CAST-calpain-2 stabilizer-1 (0-20 μM) upregulates CAST protein expression in HdhQ111 mouse striatal neuron-like cells with an EC50 of ~3.55 μM[1].
CAST-calpain-2 stabilizer-1 (0.625-10 μM) reduces mitochondrial ROS production in HdhQ111 mouse striatal neuron-like cells with an IC50 of ~1.43 μM[1].
CAST-calpain-2 stabilizer-1 enhances the endogenous interaction between CAST and calpain-2 in HdhQ111 mouse striatal neuron-like cells[1].
CAST-calpain-2 stabilizer-1 (0-500 μM; 40 min (with lysates); 5 min (Pronase digestion)) directly binds and stabilizes CAST protein in HdhQ111 mouse striatal neuron-like cell lysates in a dose-dependent manner[1].
CAST-calpain-2 stabilizer-1 (10 μM (TMRM assay); 5-10 μM (MTT assay); 48 h (TMRM assay)) requires endogenous CAST and calpain-2 to exert its mitochondrial protective and viability-enhancing effects in HdhQ111 mouse striatal neuron-like cells[1].
CAST-calpain-2 stabilizer-1 (1 μM; 5 consecutive days) restores neuronal marker expression, suppresses calpain-2 activity, and rescues neurite outgrowth in human patient iPSC-derived HD medium spiny neurons[1].

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

CAST-calpain-2 stabilizer-1 Related Antibodies

Cell Viability Assay[1]

Cell Line: HdhQ111 mouse striatal neuron-like cells
Concentration: 5-10 μM
Incubation Time: 5-10 μM (MTT assay); 48 h (TMRM assay)
Result: Exerted mitochondrial protective and viability-enhancing effects in HdhQ111 mouse striatal neuron-like cell with endogenous CAST and calpain-2.
In Vivo

CAST-calpain-2 stabilizer-1 (10 mg/kg; i.p.; 5 days per week; 6 weeks) restores CAST-calpain-2 signaling, reduces Huntington's disease-associated neuropathology, improves motor function, and increases survival by 30% at 12 weeks in R6/2 mice[1].
CAST-calpain-2 stabilizer-1 (10 mg/kg; i.p.; 5 days per week; 5 months) restores CAST-calpain-2 signaling, reduces tauopathy-associated neuropathology and neuroinflammation, and improves both short-term and long-term memory in PS19 mice[1].

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

Animal Model: B6;C3Tg (Prnp-MAPT*P301S) PS19 (male, tauopathy model expressing mutant P301S human tau protein)[1]
Dosage: 10 mg/kg
Administration: i.p.; once daily, 5 days per week; 5 months
Result: Improved short-term memory, as shown by enhanced spontaneous alternation performance in the Y maze test.
Improved long-term memory, as shown by reduced escape latency in the Barnes maze test.
Reduced hippocampal phosphorylated tau (AT8-positive) levels.
Reduced neuroinflammation, as shown by decreased IBA1 (microglia) and GFAP (astrocyte) immunodensity in the hippocampus.
Restored hippocampal CAST protein expression and reduced cleavage of calpain-2 substrates (α-spectrin, p35 to p25).
Reduced hippocampal Drp1 phosphorylation at Ser616.
Restored the interaction between endogenous CAST and calpain-2 in hippocampal tissue.
Molecular Weight

471.34

Formula

C22H20Cl2N6O2
CAS No.
SMILES

N#CC1=CN=C(C=C1)OCCNC2=NC=C(N3CCOCC3)C(C4=C(Cl)C=C(Cl)C=C4)=N2
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Room temperature in continental US; may vary elsewhere.
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Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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CAST-calpain-2 stabilizer-1 Related Classifications

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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:

CAST-calpain-2 stabilizer-13110929-05-7Calpaincalcium-activated neutral cysteine proteaseCAST proteinhuntington’s diseaseGSK3CAST-calpain-2 complextauopathyp-Drp1 S616human patient iPSC-derived HD medium spiny neuronsHdhQ111 mouse striatal neuron-like cellsR6/2 micecalpain-2Inhibitorinhibitorinhibit

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