(-)-Indolactam V-d8(Synonyms: Indolactam V-d8)

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(-)-Indolactam V-d8 (Synonyms: Indolactam V-d8)

(-)-Indolactam V-d8 (Indolactam V-d8) 是 (-)-Indolactam V 的氘代物。(-)-Indolactam V 是 PKC 的激活剂，对 η-CRD2 (PKCη 代替肽)，γ-CRD2 (PKCγ 代替肽) 的 Ki 值分别为 3.36 nM 和 1.03 μM，对 PKC C1A 和 C1B 结构域的 Kd 值分别为 5.5 nM (η-C1B)，7.7 nM (ε-C1

(-)-Indolactam V-d8(Synonyms: Indolactam V-d8)

(-)-Indolactam V-d8 Chemical Structure

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生物活性

(-)-Indolactam V-d8 (Indolactam V-d8) is the deuterium labeled (-)-Indolactam V. (-)-Indolactam V is a PKC activator, with Kis of 3.36 nM, 1.03 μM for η-CRD2 (PKCη surrogate peptide), γ-CRD2 (PKCγ surrogate peptide), and Kds of 5.5 nM (η-C1B), 7.7 nM (ε-C1B), 8.3 nM (δ-C1B), 18.9 nM (β-C1A-long), 20.8 nM (α-C1A-long), 137 nM (β-C1B), 138 nM (γ-C1A), 213 nM (γ-C1B), and has antitumor activity.

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

309.43

Formula

C17H15D8N3O2
中文名称

吲哚内酰胺 V d8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Nakagawa Y, et al. Synthesis and biological activities of indolactone-V, the lactone analogue of the tumor promoter (-)-indolactam-V. Biosci Biotechnol Biochem. 1997 Aug;61(8):1415-7.

    [3]. Masuda A, et al. Binding selectivity of conformationally restricted analogues of (-)-indolactam-V to the C1 domains of protein kinase C isozymes. Biosci Biotechnol Biochem. 2002 Jul;66(7):1615-7.

    [4]. Chen S, et al. A small molecule that directs differentiation of human ESCs into the pancreatic lineage. Nat Chem Biol. 2009 Apr;5(4):258-65.

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