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K252d Sale

目录号 : GC47522

A PKC inhibitor

K252d Chemical Structure

Cas No.:105114-22-5

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1 mg
¥4,437.00
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产品描述

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)

Chemical Properties

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
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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
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Research Update

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.