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.
For research use only. We do not sell to patients.
- Formula: C20H19ClN2O3
- Molecular Weight:370.83
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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PDIA1 5.30 μM (IC50) |
PDIA3 9.33 μM (IC50) |
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.
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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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Molecular Weight 370.83
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Formula C20H19ClN2O3
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SMILES
COC1=CC(C2N(C(CCl)=O)CCC3=C2NC4=C3C=CC=C4)=CC=C1O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PDIA1/A3-IN-1 Related Classifications
HY-187198 Related Classifications
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