根赤壳菌素

根赤壳菌素用途

Radicicol 是 ATPase/kinase 的抑制剂,对于 Hsp90, Topo VI 和 PDK3的 IC50 值分别为 1 μM,100 μM 和 400 μM。Radicicol 靶向 Hsp90 抑制多种肿瘤细胞系,与 Hsp90 的 ATP 酶结构域结合并阻止 Hsp90 蛋白成熟,导致蛋白酶体降解。Radicicol 是一种具有抗疟疾活性的抗真菌抗生素,通过靶向恶性疟原虫拓扑异构酶 VIB 来削弱线粒体复制。 Radicicol 是脂肪和肥胖相关蛋白(FTO) 的抑制剂,表现出剂量依赖性的 FTO 去甲基化活性抑制,其 IC50 值为 16.04 μM。

根赤壳菌素名称

[ CAS 号 ]:
12772-57-5

[ 中文名 ]:
根赤壳菌素

[ 英文名 ]:
Radicicol

[中文别名 ]:

根赤壳霉素

[英文别名 ]:

monorden
monorderne
[Biotinyl]-Radicicol
Monorden/Radicicol
humicola fuscoatra
Radicicol from Diheterospora chlamydosporia
MFCD01709459
KF9-A
RADISICOL
Radicicol

根赤壳菌素生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 细胞凋亡 >> 细胞凋亡

研究领域 >> 感染

信号通路 >> 跨膜转运 >> ATP合成酶

[ 靶点 ]

IC50: of 1 μM (Hsp90), 100 μM (Topo VI) and 400 μM (PDK3)[1]

[参考文献]

[1]. Kato M, et al. Distinct structural mechanisms for inhibition of pyruvate dehydrogenase kinase isoforms by AZD7545, dichloroacetate, and radicicol. Structure. 2007 Aug;15(8):992-1004. Epub 2007 Aug 2.

[2]. Chalapareddy S, et al. Radicicol confers mid-schizont arrest by inhibiting mitochondrial replication in Plasmodium falciparum. Antimicrob Agents Chemother. 2014 Aug;58(8):4341-52.

[3]. Wang R, et al. Identification of Natural Compound Radicicol as a Potent FTO Inhibitor. Mol Pharm. 2018 Sep 4;15(9):4092-4098.

根赤壳菌素物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
656.2±55.0 °C at 760 mmHg

[ 熔点 ]:
190-194ºC

[ 分子式 ]:
C₁₈H₁₇ClO₆

[ 分子量 ]:
364.777

[ 闪点 ]:
350.7±31.5 °C

[ 精确质量 ]:
364.071381

[ PSA ]:
96.36000

[ LogP ]:
1.53

[ 外观性状 ]:
白色/黄色粉末

[ 蒸汽压 ]:
0.0±2.0 mmHg at 25°C

[ 折射率 ]:
1.583

[ 储存条件 ]:
-20°C

根赤壳菌素MSDS

详细MSDS(安全技术说明书)

根赤壳菌素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: RR1105000

CHEMICAL NAME :: 6H-Oxireno(e)(2)benzoxacyclotetradecin-6,12(7H)-dione , 8-chloro-1a,14,15,15a-tetrahydro-9, 11-dihydroxy-14-methyl-

CAS REGISTRY NUMBER :: 12772-57-5

LAST UPDATED :: 199609

DATA ITEMS CITED :: 2

MOLECULAR FORMULA :: C18-H17-Cl-O6

MOLECULAR WEIGHT :: 364.80

WISWESSER LINE NOTATION :: T F3-14-6 BVO GO MV IU KUTT&J D1 PG QQ SQ

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 :: 300 mg/kg

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

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: 48,824,1995

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 175 mg/kg

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

REFERENCE :: 85GDA2 "CRC Handbook of Antibiotic Compounds," Vols.1- , Berdy, J., Boca Raton, FL, CRC Press, 1980- Volume(issue)/page/year: 2,448,1980

根赤壳菌素安全信息

[ 符号 ]:

GHS06, GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301-H340-H350

[ 警示性声明 ]:
Missing Phrase - N15.00950417-P201-P280-P308 + P313

[ 危害码 (欧洲) ]:
Xn: Harmful;

[ 风险声明 (欧洲) ]:
R22

[ 安全声明 (欧洲) ]:
26

[ 危险品运输编码 ]:
UN 2811 6.1/PG 3

[ WGK德国 ]:
1

[ RTECS号 ]:
RR1105000

[ 危险类别 ]:
6.1

[ 海关编码 ]:
29322090

根赤壳菌素合成路线

详细合成路线

根赤壳菌素上下游产品

根赤壳菌素上游产品

根赤壳菌素下游产品

根赤壳菌素文献

Screening for negative effects of candidate ascidian antifoulant compounds on a target aquaculture species, Perna canaliculus Gmelin.

Biofouling 29(1) , 29-37, (2013)

The natural chemical compounds radicicol, polygodial and ubiquinone-10 (Q10) have previously been identified as inhibitors of metamorphosis in ascidian larvae. Accordingly, they have potential as a sp...

[Thermosensitization of tumor cells with inhibitors of chaperone activity and expression].

Biomed. Khim. 58(6) , 662-72, (2012)

Effects of inhibitors of the heat shock protein 90 (HSP90) chaperone activity and inhibitors of the heat shock protein (HSP) expression on sensitivity of HeLa tumor cells to hyperthermia were studied....

Geldanamycin and its derivatives as Hsp90 inhibitors.

Front. Biosci. (Landmark Ed.) 17 , 2269-77, (2012)

The Hsp90 molecule, one of the most abundant heat shock proteins in mammalian cells, maintains homeostasis and prevents stress-induced cellular damage. Hsp90 is expressed under normal conditions at a ...

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