Orpinolide
Orpinolide is an OSBP and ORP4L inhibitor. Orpinolide disrupts Golgi homeostasis by inhibiting sterol and phosphatidylinositol phosphate countertransport at ER-Golgi membrane contact sites, while also inhibiting cholesterol biosynthesis, attenuating AKT signaling, and delaying anterograde protein transport, thereby inducing antiproliferative and cytotoxic activity in leukemia cells. Orpinolide can be used for research on leukemia.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Formule: C30H45NO4
- Masse moléculaire:483.68
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Stockage:
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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Activité biologique
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Activité biologique
Description
In Vitro
Orpinolide (485 nM; 6 h) downregulates cholesterol biosynthesis genes in KBM7 cells[1].
Orpinolide (1 μM; 8 h) alters 175 proteins in KBM7 cells, decreasing 116 including Golgi-localized and glycoprotein biosynthesis proteins[1].
Orpinolide (243 nM; 20 days) enriches sgRNAs targeting ARMH3, PITPNB, TMED2 and TMED10 in KBM7-Cas9 cells[1].
Orpinolide efficacy in KBM7 cells requires PITPNB and ARMH3 and is reversed by PI4KB inhibitors MI14 and BF738735[1].
Orpinolide (5 μM; 2 h) shifts 113 melting profiles in KBM7 cells and identifies OSBP as a putative target[1].
Orpinolide stabilizes OSBP and ORP4L in KBM7 CETSA but not ORP1, ORP2, ORP9 or ORP11[1].
Orpinolide (100 nM; 4 h) relocalizes OSBP to the TGN in HeLa cells and causes Golgi fragmentation at higher concentrations or longer times[1].
Orpinolide (1 μM) delays PC2 anterograde trafficking in RCS cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:leukemia cell panel including K562, KBM7, MV4-11, OCIAML3, NALM6, Jurkat, LOUCY, MOLT4 and P12-Ichikawa
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Concentration:10, 3, 1, 0.3, 0.1, 0.03, 0.01, 0.003 μM
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Incubation Time:72 h
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Result:A cluster of cytotoxic analogs showed pronounced cytotoxicity across all tested cell lines except K562.
Was particularly toxic in KBM7 cells and T cell leukemia-derived cells, with EC50 values in the lower nanomolar range.
In over 20 additional cell lines, leukemia cells were hypersensitive.
Selected nonleukemic cancer cell lines (HeLa, SK-ES-1 and A673) were also affected.
Did not substantially affect viability of nonmalignant PBMCs, 293T cells or RPE-1 cells.
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Cell Line:HeLa cells
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Concentration:100 nM or 1 μM
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Incubation Time:4 h or 8 h
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Result:Short incubation (4 h) at 100 nM disrupted cytoplasmic distribution of OSBP in HeLa cells, with OSBP predominantly localized within the TGN.
Partial Golgi fragmentation became evident at higher concentrations and later time points.
Chemical Information
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Masse moléculaire 483.68
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Formule C30H45NO4
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SMILES
O[C@H](C1)CC[C@@]2(C)C1=CC[C@]3([H])[C@]2([H])CC[C@@]4(C)[C@@]3([H])CC[C@]4([H])[C@H](C)[C@H]5CC(N6CCOCC6)=CC(O5)=O
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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)
Orpinolide Related Classifications
HY-161798 Related Classifications
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