BAP2
BAP2 is an allosteric protein disulfide isomerase (PDI) inhibitor with a IC50 of 0.85 μM. BAP2 binds to His256 in the b′ domain of PDI and exerts inhibitory effects through allosteric binding to the b′ domain. BAP2 upregulates GRP78. BAP2 inhibits the growth of glioblastoma cells. BAP2 can be used in studies related to glioblastoma.
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- CAS No.: 2284589-16-6
- Formule: C16H11NO2
- Masse moléculaire:249.26
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Activité biologique
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Cell Line
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Type | Value | Description | References |
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| A 172 | IC50 |
16.8 μM
Compound: 6; BAP2
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Cytotoxicity against human A172 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Cytotoxicity against human A172 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
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[PMID: 30759340] |
BAP2 (1 h) potently inhibits the reductase activity of recombinant wild-type PDI, with an IC50 of 0.85 μM[1].
BAP2 binds to recombinant wild-type PDI, with a Kd value of 9.1 μM as determined by isothermal titration calorimetry[1].
BAP2 moderately inhibits the viability of U87MG, A172 and NU04 glioblastoma cells, with IC50 values ranging from 10.3 μM to 16.8 μM; it is 5.8 times more potent against NU04 cells compared with normal HFF-1 fibroblasts[1].
BAP2 (20 μM; 2-24 h) induces endoplasmic reticulum stress in U87MG and A172 glioblastoma cells via the expression level of GRP78, without altering the level of PDI[1].
BAP2 (10-30 μM; 24 h) inhibits the migration of A172 glioblastoma cells in wound healing assays[1].
BAP2 (1 μM; 10-12 days) acts synergistically with ionizing radiation to reduce the clonogenic survival rate of D54 glioblastoma cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U87MG and A172 human glioblastoma cells
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Concentration:20 μM
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Incubation Time:2 h (EIF2α phosphorylation analysis); 24 h (GRP78 expression analysis)
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Result:Upregulated expression of GRP78, a marker of ER stress.
Left PDI expression unchanged.
Chemical Information
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CAS No. 2284589-16-6
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Masse moléculaire 249.26
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Formule C16H11NO2
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SMILES
N#CC1=CC=CC(/C=C/C(C2=CC=C(C=C2)O)=O)=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BAP2 Related Classifications
HY-W851050A Related Classifications
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