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 阻断 [³H]PDBu 与 PKC 的结合，抑制其激活过程，IC₅₀=0.03 μM^[1]。
Calphostin C (5 μM；10 min-6 h) 诱导 NALM-6 白血病细胞细胞凋亡^[2]。
Calphostin C (2 μM；24 h) 通过酯酶代谢为无活性的 Calphostin B，Calphostin B 对 NALM-6 细胞无毒性^[2]。

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

Calphostin C (40 mg/kg；腹腔注射；单次给药) 在 CD-1 小鼠中的最大血浆浓度为 2.9 μM，消除半衰期为 91.3 分钟，且未表现出毒性^[2]。
Calphostin C (1 μg/kg 和 10 μg/kg；腹腔注射；单次给药) 在链脲佐菌素 (STZ) 诱导的糖尿病小鼠模型中，分别使坐骨神经 Na+/K+ ATPase 酶活性恢复至正常水平^[3]。
Calphostin C (50 μg/mL；微型渗透泵持续给药；每日 0.5 μL；2 周) 在糖尿病小鼠中，让坐骨神经 Na+/K+ ATPase 酶活性持续恢复至正常水平，且不影响血糖水平^[3]。

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

790.76

C₄₄H₃₈O₁₄

121263-19-2

固体

Brown to reddish brown

Room temperature in continental US; may vary elsewhere.

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储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

• [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]