2. Disease Areas
  3. Cancer Blood or Cardio-cerebrovascular Disease
  4. Blood Disease Leukemia/Lymphoma/Myeloma
  5. Multiple Myeloma Leukemia/Lymphoma/Myeloma Platelet Disease
  6. PDI-IN-2

PDI-IN-2 is a highly selective PDI inhibitor. PDI-IN-2 has an IC50 of 0.63-4.01 μM against human PDI, and exhibits higher targeting specificity compared with ERp57 and ERp72. PDI-IN-2 inhibits platelet aggregation induced by U46619, collagen and tumor cells, and also blocks platelet-promoted tumor cell proliferation as well as the growth of multiple myeloma cells. PDI-IN-2 serves as an important tool reagent for research on multiple myeloma and associated thrombosis.

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

PDI-IN-2

PDI-IN-2 Chemical Structure

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PDI-IN-2 Related Antibodies

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Description

PDI-IN-2 is a highly selective PDI inhibitor. PDI-IN-2 has an IC50 of 0.63-4.01 μM against human PDI, and exhibits higher targeting specificity compared with ERp57 and ERp72. PDI-IN-2 inhibits platelet aggregation induced by U46619, collagen and tumor cells, and also blocks platelet-promoted tumor cell proliferation as well as the growth of multiple myeloma cells. PDI-IN-2 serves as an important tool reagent for research on multiple myeloma and associated thrombosis[1].

Cellular Effect
Cell Line Type Value Description References
A549 IC50
8.95 μM
Compound: 22
Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 24 hrs by resazurin assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 24 hrs by resazurin assay
[PMID: 38381886]
EA.hy 926 IC50
5.42 μM
Compound: 22
Cytotoxicity against human EA.hy 926 cells assessed as reduction in cell viability incubated for 24 hrs by resazurin assay
Cytotoxicity against human EA.hy 926 cells assessed as reduction in cell viability incubated for 24 hrs by resazurin assay
[PMID: 38381886]
MDA-MB-231 IC50
4.42 μM
Compound: 22
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 24 hrs by resazurin assay
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 24 hrs by resazurin assay
[PMID: 38381886]
Platelet IC50
0.5 μM
Compound: 22
Antiplatelet activity in human platelets assessed as inhibition of collagen-induced platelet aggregation by turbidimetric analysis
Antiplatelet activity in human platelets assessed as inhibition of collagen-induced platelet aggregation by turbidimetric analysis
[PMID: 38381886]
Platelet IC50
1.54 μM
Compound: 22
Antiplatelet activity in human platelets assessed as inhibition of U46619-induced platelet aggregation by turbidimetric analysis
Antiplatelet activity in human platelets assessed as inhibition of U46619-induced platelet aggregation by turbidimetric analysis
[PMID: 38381886]
RPMI-8226 IC50
0.66 μM
Compound: 22
Cytotoxicity against human RPMI-8226 cells assessed as reduction in cell viability incubated for 24 hrs by resazurin assay
Cytotoxicity against human RPMI-8226 cells assessed as reduction in cell viability incubated for 24 hrs by resazurin assay
[PMID: 38381886]
RPMI-8226 IC50
48 nM
Compound: 22
Cytotoxicity against human RPMI-8226 cells assessed as reduction in cell viability incubated for 72 hrs by resazurin assay
Cytotoxicity against human RPMI-8226 cells assessed as reduction in cell viability incubated for 72 hrs by resazurin assay
[PMID: 38381886]
U-87MG ATCC IC50
3.22 μM
Compound: 22
Cytotoxicity against human U87 cells assessed as reduction in cell viability incubated for 24 hrs by resazurin assay
Cytotoxicity against human U87 cells assessed as reduction in cell viability incubated for 24 hrs by resazurin assay
[PMID: 38381886]
In Vitro

PDI-IN-2 (compound 22) inhibits platelet surface PDI reductase activity with an IC50 of 0.62 μM, matching the potency of Juglone (HY-N6949)[1].
PDI-IN-2 inhibits recombinant human PDI reductase activity with an IC50 of 0.63 μM, outperforming the parent compound juglone[1].
PDI-IN-2 inhibits U46619-induced human platelet aggregation with an IC50 of 1.54 μM, showing greater potency than juglone[1].
PDI-IN-2 inhibits collagen-induced human platelet aggregation with an IC50 of 0.50 μM, outperforming juglone[1].
PDI-IN-2 (1-2 μM; up to 25 min) significantly inhibits tumor cell-induced platelet aggregation by A549, MDA-MB-231, and RPMI 8226 cells at concentrations of 1 μM and 2 μM[1].
PDI-IN-2 shows selective inhibition of recombinant human PDI over ERp57 and ERp72, with IC50 values of 3.24 μM for ERp57 and 4.01 μM for ERp72, which are 5.1-fold and 6.4-fold higher than its PDI IC50[1].
PDI-IN-2 (10 μM) exhibits reduced PDI inhibitory activity in the presence of 1 mM GSH, indicating it acts as a covalent PDI inhibitor susceptible to thiol competition[1].

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

PDI-IN-2 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: A549 cancer cells, washed human platelets
Concentration: 0.5-2 μM
Incubation Time: 48 h
Result: Blunted platelet-enhanced A549 cell growth at concentrations of 0.5 μM and 2 μM, with more significant inhibition at 2 μM.
Showed no significant reduction in A549 cell growth in the absence of platelets at these concentrations.
Molecular Weight

520.44

Formula

C24H24O13
SMILES

OC1=C2C(C(C=C(C2=O)O[C@H]3O[C@@H]([C@H]([C@@H]([C@H]3OC(C)=O)OC(C)=O)OC(C)=O)COC(C)=O)=O)=CC=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PDI-IN-2 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:

PDI-IN-2RPMI 8226ERp57Protein Disulfide Isomeraseplatelet aggregationERp72MDA-MB-231A549multiple myelomahuman PDIEA.hy926 endothelial cellsInhibitorinhibitorinhibit

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