Calphostin C  (Synonyms: UCN-1028C)

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^[1][2][3].

protein kinase C^[1]

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.

Calphostin C (40 mg/kg; i.p.; single dose) has a maximum plasma concentration of 2.9 μM and an elimination half-life of 91.3 minutes in CD-1 mice, and showed no toxicity^[2].
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.

790.76

C₄₄H₃₈O₁₄

121263-19-2

Solid

Light yellow to brown

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

Room temperature in continental US; may vary elsewhere.

* 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.

• [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]