Calphostin C
Based on 2 publication(s) in Google Scholar
Calphostin C is a highly selective PKC inhibitor (IC50=0.05 μM) and tumor apoptosis inducer. Calphostin C competitively binds to PKC and inhibits PKC-mediated phosphorylation signal transduction. Calphostin C restores Na+/K+ ATPase activity in the sciatic nerve of diabetic mice and improves neuropathy. Calphostin C can be used in the study of anti-tumor and diabetic complications.
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- Pureza: 99.9%
- No. CAS: 121263-19-2
- Fòrmula: C44H38O14
- Peso molecular:790.76
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Calphostin C
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Actividad biológica
protein kinase C[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
3.2 μM
Compound: cal C
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Inhibition of Wnt2/beta-casein signaling in human A549 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay
Inhibition of Wnt2/beta-casein signaling in human A549 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay
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[PMID: 20729080] |
| A549 | IC50 |
3.2 μM
Compound: Cal C
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Cytotoxicity against human A549 cells expressing Wnt2 after 24 to 72 hrs by MTS assay
Cytotoxicity against human A549 cells expressing Wnt2 after 24 to 72 hrs by MTS assay
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[PMID: 21855350] |
| HCT-116 | IC50 |
2.86 μM
Compound: 83; PKF115-584
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Antiproliferative activity against human HCT-116 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTS assay
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTS assay
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[PMID: 33445154] |
Calphostin C blocks the binding of [3H]PDBu to PKC and inhibits its activation process with IC50=0.03 μM[1].
Calphostin C (5 μM; 10 min-6 h) induces apoptosis in NALM-6 leukemia cells[2].
Calphostin C (2 μM; 24 h) is metabolized to inactive Calphostin B by esterases, and Calphostin B is not toxic to NALM-6 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NALM-6 (human B-cell leukemia)
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Concentration:5 μM
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Incubation Time:6 h
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Result:Rapidly accumulated in NALM-6 cells, reaching a peak intracellular concentration of 212 pmol/10^6 cells (tmax=84.4 min) and inducing apoptosis via calcium mobilization.
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Cell Line:NALM-6 (human B-cell leukemia)
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Concentration:2 μM
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Incubation Time:24 h
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Result:Induced 100% cell death in NALM-6 cells, as confirmed by calcein/ethidium homodimer staining. Showed 90% of cells undergoing apoptosis, characterized by phosphatidylserine externalization (MC540-positive) and membrane permeability (PI-positive) in flow cytometry assay.
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Cell Line:NALM-6 (human B-cell leukemia)
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Concentration:2-4 μM
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Incubation Time:24 h
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Result:Showed no cytotoxicity in NALM-6 cells, with <5% cell death observed at 4 μM. Confirmed no induction of phosphatidylserine externalization or membrane permeability.
Calphostin C (1 μg/kg and 10 μg/kg; i.p.; single dose) restores the sciatic nerve Na+/K+ ATPase activity to normal levels in a streptozotocin (STZ)-induced diabetic mouse model[3].
Calphostin C (50 μg/mL; continuous administration by mini-osmotic pump; 0.5 μL per day; 2 weeks) restores the sciatic nerve Na+/K+ ATPase activity to normal levels in diabetic mice without affecting blood glucose levels[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 121263-19-2
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Appearance Solid
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Peso molecular 790.76
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Fòrmula C44H38O14
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Color Brown to reddish brown
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SMILES
O=C(O[C@@H](CC1=C(C(C2=C(C=C(C(C3=C4C5=C(O)C=C3OC)=C2C1=C4C(C[C@@H](C)OC(C6=CC=CC=C6)=O)=C(OC)C5=O)OC)O)=O)OC)C)OC7=CC=C(C=C7)O
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Synonyms
UCN-1028C
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Insect Mol Biol
Juvenile hormone controls trehalose metabolism by regulating trehalase 2 activity in ovarian development of Helicoverpa armigera. [Abstract]2025 Apr;34(2):249-262. PMID: 39503533 -
Solvente y solubilidad
DMSO : 1 mg/mL (1.26 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (284 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Kobayashi E, et al. Calphostin C (UCN-1028C), a novel microbial compound, is a highly potent and specific inhibitor of protein kinase C. Biochem Biophys Res Commun. 1989;159(2):548-553. [Content Brief]
[2]. Chen CL, et al. Pharmacokinetic features and metabolism of calphostin C, a naturally occurring perylenequinone with antileukemic activity. Pharm Res. 1999 Jul;16(7):1003-9. [Content Brief]
[3]. Hermenegildo C, et al. Sustained recovery of Na(+)-K(+)-ATPase activity in sciatic nerve of diabetic mice by administration of H7 or calphostin C, inhibitors of PKC. Diabetes. 1993 Feb;42(2):257-62. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.2646 mL | 6.3230 mL | 12.6461 mL | 31.6152 mL |
Calphostin C Related Classifications
HY-105416 Related Classifications
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