PDIA1/A3-IN-1
PDIA1/A3-IN-1 is a PDIA1 and PDIA3 inhibitor, with an IC50 value of 5.30 μM against PDIA1 and an IC50 value of 9.33 μM against PDIA3. PDIA1/A3-IN-1 can be used in research related to prostate cancer, breast cancer, glioblastoma, and cervical cancer.
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- 화학식: C20H19ClN2O3
- 분자량:370.83
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
[1]|
PDIA1 5.30 μM (IC50) |
PDIA3 9.33 μM (IC50) |
In Vitro
PDIA1/A3-IN-1 (Compound 2e) potently inhibits purified recombinant PDIA1 (IC50 = 5.30 μM) and PDIA3 (IC50 = 9.33 μM), while its individual enantiomers (−)-2e and (+)-2e show slightly reduced potency against these two subtypes compared with the racemate[1].
PDIA1/A3-IN-1 (5 μM; 48 h) induces the formation of PDIA3-positive intracellular aggregates in glioblastoma T98G cells[1].
PDIA1/A3-IN-1 covalently modifies the cysteine at the catalytic active site of purified recombinant human PDIA1, and mainly targets non-catalytic cysteines (Cys85, Cys92, Cys244) in purified recombinant human PDIA3[1].
PDIA1/A3-IN-1 (24-48 h) reduces the viability of DU-145, PC-3, MDA-MB-231, T98G and HeLa cell lines, with EC50 values ranging from 3.25 μM to 13.90 μM depending on the cell line and incubation time[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:DU-145, PC-3, MDA-MB-231, T98G, HeLa
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Concentration:20 μM (initial screening); dose-response ranges (EC50 determination)
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Incubation Time:24 h, 48 h
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Result:Achieved EC50 values of 7.64 μM (DU-145), 13.90 μM (PC-3), 6.39 μM (MDA-MB-231), 12.44 μM (T98G), and 7.44 μM (HeLa) after 24 h incubation.
Achieved EC50 values of 3.25 μM (DU-145), 4.73 μM (PC-3), 5.26 μM (MDA-MB-231), 13.07 μM (T98G), and 5.28 μM (HeLa) after 48 h incubation.
Exhibited cytotoxicity comparable to reference compound 16F16 across all cell lines at 20 μM.
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Cell Line:T98G
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Concentration:5 μM
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Incubation Time:48 h
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Result:Induced the formation of PDIA3-positive intracellular aggregates.
Chemical Information
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분자량 370.83
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화학식 C20H19ClN2O3
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SMILES
COC1=CC(C2N(C(CCl)=O)CCC3=C2NC4=C3C=CC=C4)=CC=C1O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocol
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PDIA1/A3-IN-1 Related Classifications
HY-187198 Related Classifications
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