K-252c

• 常用名: K-252c
• 英文名: K252C
• CAS号: 85753-43-1
• 分子量: 311.33700
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₀H₁₃N₃O
• 熔点: N/A
• 闪点: N/A

K-252c用途

K-252c,一种十字孢碱的类似物,可从Nocardiopsis sp.中分离得到,是一种能透过细胞的、PKC 的抑制剂,IC50 值为2.45 µM。K-252c可诱导人慢性粒细胞白血病癌细胞凋亡。K-252c还能抑制β内酰胺酶、胰凝乳蛋白酶和苹果酸脱氢酶。

K-252c名称

• 英文名: K-252c,6,7,12,13-Tetrahydro-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazol-5-one

K-252c生物活性

• 描述: K-252c,一种十字孢碱的类似物,可从Nocardiopsis sp.中分离得到,是一种能透过细胞的、PKC 的抑制剂,IC50 值为2.45 µM。K-252c可诱导人慢性粒细胞白血病癌细胞凋亡。K-252c还能抑制β内酰胺酶、胰凝乳蛋白酶和苹果酸脱氢酶。
• 相关类别:
  信号通路 >> 表观遗传学 >> PKC
  研究领域 >> 癌症
  研究领域 >> 感染
  信号通路 >> TGF-beta/Smad 信号通路 >> PKC
  信号通路 >> 抗感染 >> 细菌
• 靶点实验:

  IC50: 2.45 µM (PKC)[1].

• 参考文献:

  [1]. Pereira, E.R., et al. Structure-activity relationships in a series of substituted indolocarbazoles: Topoisomerase I and protein kinase C inhibition and antitumoral and antimicrobial properties J. Med. Chem. 39(22), 4471-4477 (1996).

  [2]. Liu, R., et al. Two indolocarbazole alkaloids with apoptosis activity from a marine-derived actinomycete Z2039-2 Arch. Pharm. Res. 30(3), 270-274 (2007).

  [3]. Zimmermann, A., et al. Indolocarbazoles exhibit strong antiviral activity against human cytomegalovirus and are potent inhibitors of the pUL97 protein kinase Antiviral Res. 48(1), 49-60 (2000).

  [4]. McGovern, S.L., et al. Kinase inhibitors: Not just for kinases anymore Journal of Medicinal Chemistry 46, 1478-1483 (2003).

K-252c物理化学性质

• 分子式: C₂₀H₁₃N₃O
• 分子量: 311.33700
• 精确质量: 311.10600
• PSA: 60.68000
• LogP: 4.52780
• InChIKey: MEXUTNIFSHFQRG-UHFFFAOYSA-N
• SMILES: O=C1NCc2c1c1c3ccccc3[nH]c1c1[nH]c3ccccc3c21
• 储存条件: -20°C，密闭，干燥

K-252c安全信息

• 安全声明 (欧洲): 22-24/25
• WGK德国: 3
• 海关编码: 2933990090

K-252c海关

• 海关编码: 2933990090
• 中文概述: 2933990090. 其他仅含氮杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%
• 申报要素: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期
• Summary: 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

K-252c靶点实验

查看更多实验

实验名称：Inhibition of His-tagged human PKCalpha expressed in Escherichia coli at 10 uM 来源：ChEMBL 靶标：Protein kinase C alpha type External Id：CHEMBL1247618

实验名称：qHTS to identify inhibitors of the New Delhi Metallo-beta-lactamase (NDM): assay vali... 来源：NCGC External Id：adst_MBL_Abs_LOPAC_o1

实验名称：Inhibition of bovine heart PKA at 10 uM 来源：ChEMBL 靶标：N/A External Id：CHEMBL1247617

实验名称：In vitro for inhibitory activity against protein kinase C from rat brain 来源：ChEMBL 靶标：Protein kinase C theta type External Id：CHEMBL767476

实验名称：Inhibition of His-tagged human PRAK expressed in Sf9 cells at 10 uM 来源：ChEMBL 靶标：MAP kinase-activated protein kinase 5 External Id：CHEMBL1247616

实验名称：Compound was tested in vitro for choline acetyltransferase (ChAT) activity (maximal C... 来源：ChEMBL 靶标：Choline O-acetyltransferase External Id：CHEMBL660256

实验名称：Inhibition of His-tagged human MSK1 expressed in Sf9 cells at 10 uM 来源：ChEMBL 靶标：Ribosomal protein S6 kinase alpha-5 External Id：CHEMBL1247615

实验名称：USP8 deubiquitinase inhibition: Primary qHTS 来源：24642 靶标：ubiquitin specific peptidase 8 External Id：USP8 FAST DUB HTS Primary

实验名称：Inhibition of Gst-tagged human MAPKAPK2 expressed in Escherichia coli at 10 uM 来源：ChEMBL 靶标：MAP kinase-activated protein kinase 2 External Id：CHEMBL1247614

实验名称：Inhibition of MAPKAPK1b from rabbit skeletal muscle at 10 uM 来源：ChEMBL 靶标：N/A External Id：CHEMBL1247613

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K-252c英文别名

• staurosporine aglycon
• Staurosporinone,K-252c
• Staurosporinone
• K-252C
• STAUROSPORINE AGLYCONE