(+)-抗生素 K 252A

(+)-抗生素 K 252A用途

K-252a 可从土壤真菌Nocardiopsis sp.中分离得到的一种十字孢碱的类似物,是蛋白激酶的抑制剂,对 PKC、PKA、II型钙调素依赖性激酶和磷酸化酶激酶的 IC50 值分别为470 nM、140 nM、270 nM和1.7 nM。

(+)-抗生素 K 252A名称

[ CAS 号 ]:
99533-80-9

[ 中文名 ]:
(+)-抗生素 K 252A

[ 英文名 ]:
K-252a

[英文别名 ]:

antibiotick252a
PROTEIN KINASE INHIBITOR FROM NORCARDIOP SIS SP.
PROTEIN KINASE INHIBITOR K-252A
PROTEIN KINASE INHIBITOR
K252a
K-252A,NOCARDIOPSIS SP
K-252a
antibioticsf2370
sf2370

(+)-抗生素 K 252A生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 表观遗传学 >> PKC

信号通路 >> 神经信号通路 >> 蛋白激酶

研究领域 >> 感染

信号通路 >> 蛋白酪氨酸激酶 >> PKA

信号通路 >> 干细胞及 Wnt 通路 >> PKA

信号通路 >> TGF-beta/Smad 信号通路 >> PKC

[ 靶点 ]

IC50: 470 nM (PKC), 140 nM (PKA), 270 nM (Ca2+/calmodulin-dependent kinase type II), 1.7 nM (phosphorylase kinase)[1][2].

[参考文献]

[1]. Yasuzawa, T., et al. The structures of the novel protein kinase C inhibitors K-252a, b, c AND d Journal of Antibiotics 39(8), 1072-1078 (1986).

[2]. Davis, P.D., et al. Inhibitors of protein kinase C. 1.1 2,3-bisarylmaleimides Journal of Medicinal Chemistry 35, 177-184 (1992).

(+)-抗生素 K 252A物理化学性质

[ 密度 ]:
1.7±0.1 g/cm3

[ 沸点 ]:
685.3±55.0 °C at 760 mmHg

[ 分子式 ]:
C₂₇H₂₁N₃O₅

[ 分子量 ]:
467.473

[ 闪点 ]:
368.2±31.5 °C

[ 精确质量 ]:
467.148132

[ PSA ]:
94.72000

[ LogP ]:
4.23

[ 蒸汽压 ]:
0.0±2.2 mmHg at 25°C

[ 折射率 ]:
1.841

[ 储存条件 ]:
-20°C，密闭，干燥

(+)-抗生素 K 252AMSDS

(+)-抗生素 K 252A毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: KC6500000

CAS REGISTRY NUMBER :: 99533-80-9

LAST UPDATED :: 199212

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C27-H21-N3-O5

MOLECULAR WEIGHT :: 467.51

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Intraperitoneal

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: 38,1437,1985

(+)-抗生素 K 252A安全信息

[ 符号 ]:

GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H360D-H371

[ 警示性声明 ]:
P201-P260-P308 + P311

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
Xi: Irritant;

[ 安全声明 (欧洲) ]:
22-24/25

[ 危险品运输编码 ]:
NONH for all modes of transport

[ RTECS号 ]:
NZ0550000

(+)-抗生素 K 252A合成路线

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