互变霉素

互变霉素用途

Tautomycin 是可从 Streptomyces verticillatus 中分离得到的一种真菌类抗生素,是蛋白磷酸酶 1 和 2A 的有效特异性抑制剂,在没有Ca2+ 的情况下诱导平滑肌收缩,Kiapp 值分别为 0.16 nM 和 0.4 nM。

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互变霉素名称

[ CAS 号 ]:
109946-35-2

[ 中文名 ]:
互变霉素

[ 英文名 ]:
Tautomycin

[英文别名 ]:

MFCD00236438
tautomycin

互变霉素生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> 磷酸酶

研究领域 >> 炎症/免疫

[ 靶点 ]

Kiapp: 0.16 nM (PP1), 0.4 nM (PP2A)[1].

[体外研究]

Tautomycin(0-1000 nM,48小时)以剂量依赖性方式抑制MTC细胞生长[2]。 Tautomycin(0-1000 nM,48小时)以剂量依赖性方式降低人MTC细胞中的NE标记ASCL1和CgA [2]。细胞增殖测定[2]细胞系：人MTC细胞浓度：0-1000nM孵育时间：48小时结果：以剂量依赖性方式抑制MTC细胞生长。蛋白质印迹分析[2]细胞系：人MTC细胞浓度：0-1000nM孵育时间：48小时结果：导致NE标记ASCL1和CgA的剂量依赖性降低。

[参考文献]

[1]. MacKintosh C, et al. Tautomycin from the bacterium Streptomyces verticillatus. Another potent and specific inhibitor of protein phosphatases 1 and 2A. FEBS Lett. 1990 Dec 17;277(1-2):137-40.

[2]. Adler JT, et al. Tautomycetin and tautomycin suppress the growth of medullary thyroid cancer cells via inhibition of glycogen synthase kinase-3beta. Mol Cancer Ther. 2009 Apr;8(4):914-20.

互变霉素物理化学性质

[ 密度 ]:
1.18g/cm3

[ 沸点 ]:
854.3ºC at 760mmHg

[ 分子式 ]:
C₄₁H₆₆O₁₃

[ 分子量 ]:
766.95500

[ 闪点 ]:
247.5ºC

[ 精确质量 ]:
766.45000

[ PSA ]:
192.19000

[ LogP ]:
4.78530

[ 外观性状 ]:
固体

[ 蒸汽压 ]:
5.62E-34mmHg at 25°C

[ 折射率 ]:
1.527

[ 储存条件 ]:
2-8°C，密封，干燥

互变霉素MSDS

详细MSDS(安全技术说明书)

互变霉素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: WX1000000

CHEMICAL NAME :: Tautomycin

CAS REGISTRY NUMBER :: 109946-35-2

LAST UPDATED :: 199410

DATA ITEMS CITED :: 3

MOLECULAR FORMULA :: C42-H70-O12.3/2H2-O

MOLECULAR WEIGHT :: 793.00

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 7500 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 5 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

MUTATION DATA

TYPE OF TEST :: Morphological transformation

TEST SYSTEM :: Human Leukocyte

DOSE/DURATION :: 1 mg/L

REFERENCE :: JANTAJ Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo, 141, Japan) V.2-5, 1948-52; V.21- 1968- Volume(issue)/page/year: 41,932,1988

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互变霉素安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H300

[ 警示性声明 ]:
P264-P301 + P310

[ 个人防护装备 ]:
Eyeshields;Faceshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T+: Very toxic;

[ 风险声明 (欧洲) ]:
R28

[ 安全声明 (欧洲) ]:
S22

[ 危险品运输编码 ]:
UN 3462 6.1/PG 2

[ RTECS号 ]:
WX1000000

互变霉素合成路线

详细合成路线

互变霉素上下游产品

互变霉素上游产品

互变霉素下游产品

互变霉素文献

Characterization of the tautomycetin biosynthetic gene cluster from Streptomyces griseochromogenes provides new insight into dialkylmaleic anhydride biosynthesis.

J. Nat. Prod. 72(3) , 450-9, (2009)

Tautomycetin (TTN) is a highly potent and specific protein phosphatase inhibitor isolated from Streptomyces griseochromogenes. The biological activity of TTN makes it an important lead for drug discov...

The bifunctional glyceryl transferase/phosphatase OzmB belonging to the HAD superfamily that diverts 1,3-bisphosphoglycerate into polyketide biosynthesis.

J. Am. Chem. Soc. 128(32) , 10386-7, (2006)

The HAD superfamily protein OzmB from the oxazolomycin biosynthetic pathway is shown to divert the primary metabolite 1,3-diphosphoglycerate into the polyketide biosynthetic pathway as glycerate via l...

PR55 alpha, a regulatory subunit of PP2A, specifically regulates PP2A-mediated beta-catenin dephosphorylation.

J. Biol. Chem. 284 , 22649 - 22656, (2009)

A central question in Wnt signaling is the regulation of beta-catenin phosphorylation and degradation. Multiple kinases, including CKI alpha and GSK3, are involved in beta-catenin phosphorylation. Pro...

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