蛋白磷酸酯酶抑制剂

中文名称:

蛋白磷酸酯酶抑制剂

中文同义词:

蛋白磷酸酯酶抑制剂;PP2A催化亚基抑制剂(CALYCULIN A);花萼海绵诱癌素

英文名称:

CALYCULIN A

英文同义词:

C05370;N-[(3S)-[4-(1E)-3-[(2R,3R,4R,7S,8S,9R)-2-[(1S,3S,4S,5R,7E,9E,11E,13Z)-14-Cyano-3,5-dihydroxy-1-methoxy-4,6,8,9,13-pentamethyl-7,9,11,13-tetradecatetraenyl]-9-hydroxy-4,4,8-trimethyl-3-(phosphonooxy)-1,6-dioxaspiro[4.5]dec-7-yl]-1-propenyl]-2-oxazoly]butyl]-4-deoxy-4-(dimethylamino)-5-O-methyl-L-ribonamide;CALYCULIN A;CALYCULIN A, DISCODERMIA CALYX;calyculin A from discodermia calyx;CALYCULIN A FROM DISCODERMIA CALYX, 10 U G;N-[(3S)-[4-(1E)-3-[(2R,3R,4R,7S,8S,9R)-2-[(1S,3S,4S,5R,7E,9E,11E,13Z)-14-Cyano-3,5-dihydroxy-1-methoxy-4,6,8,9,13-pentam;N-[(3S)-[4-(1E)-3-[(2R,3R,4R,7S,8S,9R)-2-[(1S,3S,4S,5R,7E,9E,11E,13Z)-14-Cyano-3,5-dihydroxy-1-Methoxy-4,6,8,9,13-pentaMethyl-7,9,11,13-tetradecatetraenyl]-9-hydroxy-4,4,8-triMethyl-3-(phosphonooxy)-1,6-dioxaspiro[4.5]dec-7-yl]-1-propenyl]-2-o

CAS号:

101932-71-2

分子式:

C50H81N4O15P

分子量:

1009.17

EINECS号:

相关类别:

细胞生物学试剂;Kinase/Phosphatase Biology;Serine/Threonine Kinase Biology;Protein phosphatase-1, Catalytic SubunitCancer Research;Tumor Promotors;Cell Signaling and Neuroscience;P to;Serine/Threonine Phosphatase Substrates;Phosphatase InhibitorsSerine/Threonine Kinase Biology;Protein Phosphatase 1 (PP1)Enzyme Inhibitors by Enzyme;Serine/Threonine Phosphatase Inhibitors;Tumor Growth Regulation;Inhibitor

Mol文件:

101932-71-2.mol

熔点 

247-249°

比旋光度 

D -60° (c = 0.1 in ethanol)

密度 

1.25±0.1 g/cm3(Predicted)

储存条件 

-20°C

溶解度 

DMSO: soluble

形态

solid

酸度系数(pKa)

1.81±0.10(Predicted)

颜色

white

水溶解性 

Soluble in DMSO (50 mM), ethanol (1 mg/ml), methanol, acetone, acetonitrile, chloroform, methylene chloride, and benzene. Insoluble in water.

Merck 

13,1731

BRN 

4903216

生物活性

Calyculin A ((-)-Calyculin A) 是有效，可渗透细胞的蛋白磷酸酶 1 (PP1) 和蛋白磷酸酶 2A (PP2A) 抑制剂，其 IC50 值分别为 2 nM 和 0.5-1 nM。

靶点

IC50: 2 nM (PP1); 0.5-1 nM (PP2A)

体外研究

Calyculin A (1-10 nM; 24 hours) induces cytotoxicity in MG63 cells in a dose-dependent manner up to 10 nM in MG63 cells. Cell Cytotoxicity Assay Cell Line: Human osteosarcoma MG63 cells Concentration: 0, 1, 2, 5, 10 nM Incubation Time: 24 hours Result: Treatment with 0.1 nM for 24 h had a minimal effect on MG63 cell survival. Cell rounding and shrinking were obvious in the cultures treated for 24 h with 5 nM. The level of the cell viability treated with 10 nM was 27% that of the control cultures.

Cell Line:

Human osteosarcoma MG63 cells

Concentration:

0, 1, 2, 5, 10 nM

Incubation Time:

24 hours

Result:

Treatment with 0.1 nM for 24 h had a minimal effect on MG63 cell survival. Cell rounding and shrinking were obvious in the cultures treated for 24 h with 5 nM. The level of the cell viability treated with 10 nM was 27% that of the control cultures.

危险品标志 

T

危险类别码 

23/24/25-38

安全说明 

36/37/39-45

危险品运输编号 

UN 3462 6.1/PG 3

WGK Germany 

3

F 

8-10

HazardClass 

6.1(a)

PackingGroup 

II