(-)-Indolactam V
Cat. No.:YN310163
产品名称: | (-)-Indolactam V |
CAS No.: | 90365-57-4 |
Chemical Name: | (2S,5S)-1,2,4,5,6,8-hexahydro-5-(hydroxymethyl)-1-methyl-2-(1-methylethyl)-3H-pyrrolo[4,3,2-gh]-1,4-benzodiazonin-3-one |
Synonyms: | Indolactam V |
分子量: | 301.38 |
分子式: | C₁₇H₂₃N₃O₂ |
SMILES: | CC(C)[C@@H](C1=O)N(C)C2=C3C(NC=C3C[C@H](N1)CO)=CC=C2 |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | (-)-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-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) 和 213 nM (γ-C1B),具有抗肿 |
IC50和靶点: | [{name:"PKCη-CRD2:3.36 nM (Ki)"},{name: "PKCη-C1B:5.5 nM (Kd)"},{name: "PKCε-C1B:7.7 nM (Kd)"},{name: "PKCδ-C1B:8.3 nM (Kd)"},{name: "PKCθ-C1B:8.7 nM (Kd)"},{name: "PKCβ-C1A-long:18.9 nM (Kd)"},{name: "PKCα-C1A-long:20.8 nM (Kd)"},{name: "PKCβ-C1B:137 nM (Kd)"},{name: "PKCγ-C1A:138 nM (Kd)"},{name: "PKCγ-C1B:213 nM (Kd)"},{name: "PKCγ-CRD2:1030 nM (Ki)"},{name: "PKCδ-C1A:1900 nM (Kd)"},{name: "PKCη-C1A:3770 nM (Kd)"},{name: "PKCα-C1B-long:4000 nM (Kd)"},{name: "PKCε-C1A:4110 nM (Kd)"}] |
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Nakagawa, Y., Irie, K., Nakamura, Y., et al.Synthesis and biological activities of indolactone-V, the lactone analogue of the tumor promoter (-)-indolactam-VBiosci. Biotechnol. Biochem.61(8),1415-1417(1997)
Masuda, A., Irie, K., Nakagawa, Y., et al.Binding selectivity of conformationally restricted analogues of (-)-indolactam-V to the C1 domains of protein kinase C isozymesBiosci. Biotechnol. Biochem.66(7),1615-1617(2002)
Chen, S., Borowiak, M., Fox, J.L., et al.A small molecule that directs differentiation of human ESCs into the pancreatic lineageNat. Chem. Biol.5(4),258-265(2009)