CAST-calpain-2 stabilizer-1

Name: CAST-calpain-2 stabilizer-1
Brand: MedChemExpress
SKU: HY-186130
Rating: 4.5 (0 reviews)

Cat. No.: HY-186130: Data Sheet Handling Instructions
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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.

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CAST-calpain-2 stabilizer-1 화학구조

CAS No. : 3110929-05-7

사이즈	재고	수량
1 mg	견적 받기 6 - 8 Weeks 5 - 7 Weeks 7 - 9 Weeks 6 - 8 weeks	Estimated Time of Arrival: December 31
5 mg	견적 받기 6 - 8 Weeks 5 - 7 Weeks 7 - 9 Weeks 6 - 8 weeks	Estimated Time of Arrival: December 31
10 mg	견적 받기 6 - 8 Weeks 5 - 7 Weeks 7 - 9 Weeks 6 - 8 weeks	Estimated Time of Arrival: December 31
25 mg	견적 받기 6 - 8 Weeks 5 - 7 Weeks 7 - 9 Weeks 6 - 8 weeks	Estimated Time of Arrival: December 31
50 mg	견적 받기 6 - 8 Weeks 5 - 7 Weeks 7 - 9 Weeks 6 - 8 weeks	Estimated Time of Arrival: December 31
100 mg	견적 받기
200 mg	견적 받기

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고객리뷰

Based on 1 Customer Validation

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Biological Activity
순도&문서
References
고객리뷰

제품 설명

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.

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.

분자량

471.34

화학식

C₂₂H₂₀Cl₂N₆O₂

CAS No.

3110929-05-7

SMILES

N#CC1=CN=C(C=C1)OCCNC2=NC=C(N3CCOCC3)C(C4=C(Cl)C=C(Cl)C=C4)=N2

선적

Room temperature in continental US; may vary elsewhere.

보관

Please store the product under the recommended conditions in the Certificate of Analysis.

순도&문서

Handling Instructions (2659 KB)

References

[1]. Hu D, et al. A small-molecule stabilizer of the calpastatin-calpain-2 complex restores mitochondrial function and mitigates neurodegeneration. Sci Adv. 2026;12(13):eaeb1174. [Content Brief]