101932-71-2
中文名稱
蛋白磷酸酯酶抑制劑
英文名稱
CALYCULIN A
CAS
101932-71-2
分子式
C50H81N4O15P
分子量
1009.17
MOL 文件
101932-71-2.mol
更新日期
2026/01/14 15:11:18
101932-71-2 結構式
基本信息
中文別名
花萼海綿誘癌素蛋白磷酸酯酶抑制劑
PP2A催化亞基抑制劑(CALYCULIN A)
英文別名
C05370CALYCULIN A
(-)-CALYCULIN A
Calyculin A ((-)-Calyculin A)
CALYCULIN A, DISCODERMIA CALYX
calyculin A from discodermia calyx
CALYCULIN A FROM DISCODERMIA CALYX, 10 U G
Calyculin A, Discodermia calyx - CAS 101932-71-2 - Calbiochem
InSolution Calyculin A, Discodermia calyx - CAS 101932-71-2 - Calbiochem
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
物理化學性質
熔點247-249°
比旋光度D -60° (c = 0.1 in ethanol)
密度1.25±0.1 g/cm3(Predicted)
儲存條件-20°C
溶解度DMSO: soluble
溶解度可溶于DMSO
酸度系數(shù)(pKa)1.81±0.10(Predicted)
形態(tài)solid
顏色white
生物來源sea sponge (Discodermia calyx)
旋光度 (Optical Rotation)+59.815 (Ethanol)
水溶解性Soluble in DMSO (50 mM), ethanol (1 mg/ml), methanol, acetone, acetonitrile, chloroform, methylene chloride, and benzene. Insoluble in water.
Merck13,1731
BRN4903216
InChIKeyFKAWLXNLHHIHLA-YCBIHMBMSA-N
安全數(shù)據(jù)
警示詞危險
危險性描述H301+H311+H331-H315
危險品標志T
危險類別碼23/24/25-38
安全說明36/37/39-45
危險品運輸編號UN 3462 6.1/PG 3
危險品運輸編號UN 3462 6.1/PG 3
WGK Germany3
WGK Germany3
F8-10
危險等級6.1(a)
包裝類別II
海關編碼2934999090
存儲類別6.1C - Combustible acute toxic Cat.3
toxic compounds or compounds which causing chronic effects
toxic compounds or compounds which causing chronic effects
危險性類別Acute Tox. 3 Dermal
Acute Tox. 3 Inhalation
Acute Tox. 3 Oral
Skin Irrit. 2
Acute Tox. 3 Inhalation
Acute Tox. 3 Oral
Skin Irrit. 2
常見問題列表
生物活性
蛋白磷酸酯酶抑制劑是一種存在于杯海鞘中的海洋毒素，作為蛋白磷酸酶1（PP1）和蛋白磷酸酶2A（PP2A-C）的結構獨特抑制劑，已被證實能抑制平滑肌肌球蛋白B的內源性磷酸酶活性，并誘導肌纖維收縮。它能誘導的收縮伴隨著細胞質游離Ca2+濃度的升高。此外，有報道稱該化合物能夠與小鼠皮膚中的蛋白磷酸酶結合，這些蛋白磷酸酶是奧卡達酸的受體。因此，它會在小鼠皮膚中誘導鳥氨酸脫羧酶的產(chǎn)生，并被認為能夠促進腫瘤生長。
生物活性
Calyculin A ((-)-Calyculin A) 是有效，可滲透細胞的蛋白磷酸酶 1 (PP1) 和蛋白磷酸酶 2A (PP2A) 抑制劑，其 IC50 值分別為 2 nM 和 0.5-1 nM。靶點
IC50: 2 nM (PP1); 0.5-1 nM (PP2A)
體外研究
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. |