K252d
目录号 : GC47522A PKC inhibitor
Cas No.:105114-22-5
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >70.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
K252d is an indolocarbazole alkaloid found in Nocardiopsis.1 It is a PKC inhibitor that inhibits PKC isolated from rat brain (IC50 = 350 nM). It also inhibits calcium- and calmodulin-dependent phosphodiesterase isolated from bovine heart (IC50 = 46.2 µM).
1.Nakanishi, S., Matsuda, Y., Iwahashi, K., et al.K-252b, c and d, potent inhibitors of protein kinase C from microbial originJ. Antibiot. (Tokyo) 39(8)1066-1071(1986)
Cas No. | 105114-22-5 | SDF | |
Canonical SMILES | O=C1NCC2=C1C(C(C=CC=C3)=C3N4[C@@]5([H])[C@H](O)[C@H](O)[C@@H](O)[C@H](C)O5)=C4C6=C2C7=C(C=CC=C7)N6 | ||
分子式 | C26H23N3O5 | 分子量 | 457.5 |
溶解度 | DMSO: soluble,Ethanol: soluble | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-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。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.1858 mL | 10.929 mL | 21.8579 mL |
5 mM | 0.4372 mL | 2.1858 mL | 4.3716 mL |
10 mM | 0.2186 mL | 1.0929 mL | 2.1858 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
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工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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Biosynthesis of indocarbazostatin B, incorporation of D-[U-13C] glucose and L-[2-13C] tryptophan
J Antibiot (Tokyo) 2005 Dec;58(12):759-65.PMID:16506693DOI:10.1038/ja.2005.103.
High incorporation of D-[U-13C] glucose and L-[indole-2-13C] tryptophan into indocarbazostatin B (2) was observed in a biosynthetic study using a mutant strain, Streptomyces sp. MUV-7-8. The original strain, Streptomyces sp. TA-0403 produced a small amount of indocarbazostatin (1) and indocarbazostatin B (2), which displayed potent biological activities. To facilitate biosynthetic studies, we selected high indocarbazostatin producing mutant strains. The first mutants, Streptomyces sp. MUV-6-83 and MUV-6-17, produced indocarbazostatins C (3) and D (4) as well as 1 and 2. When the production medium was supplemented with D-tryptophan, the MUV-6-17 mutant produced K252c (5), whereas when L-tryptophan was added, it produced K252d (6). On further UV treatment of the mutant strain MUV-6-83, we finally obtained a new mutant producer, Streptomyces sp. MUV-7-8, that produced 2 as a major metabolite with higher productivity. This mutant producer enabled us to do a feeding experiment of the envisioned precursors, glucose and tryptophan.