细胞松弛素 B

中文名称:

细胞松弛素 B

中文同义词:

细胞松弛素 B 来源于长蠕孢菌;细胞松弛素 B 来源于DRECHSLERA DEMATIOIDEA;CYTOCHALASIN B 细胞松弛素B;松胞素B;细胞分裂抑素B;细胞松驰素B;细胞松弛素 B;细胞松弛素B

英文名称:

CYTOCHALASIN B

英文同义词:

CytochalasinB from Drechslera dematioidea,Phomin;Cytochalasin B, froM Drechslera deMatoidea;Cytochalasin B (7S),(20R)-Dihydroxy-16(R)-methyl-10-phenyl-24-oxa[14]cytochalasa-6(12),13(E),21(E)-triene-1,23-dione;Cytochalasin B from Helminthosporium dematioideum;cytochalasin;ec[2,3-d]isoindole-2,18(5h)-dione;(E,E)-16-BENZYL-6,7,8,9,10,12A,13,14,15,15A,16,17-DODECAHYDRO-5,13-DIHYDROXY-9,15-DIMETHYL-14-METHYLENE-2H-OXACYCLOTETRADE[2,3-D]ISOINDOLE-2,18(5H)-DIONE;CYTOCHALASIN B, HELMINTHOSPORIUM DEMATIOIDEUM

CAS号:

14930-96-2

分子式:

C29H37NO5

分子量:

479.61

EINECS号:

239-000-2

相关类别:

抗生素;其他生化试剂;微生物代谢物;生化试剂;酶类;抗生素及抗病毒;医药原料药-科研原料;生物碱;医药原料;antibiotic

Mol文件:

14930-96-2.mol

熔点 

218-223 °C

沸点 

577.96°C (rough estimate)

密度 

1.1490 (rough estimate)

折射率 

1.6290 (estimate)

闪点 

85℃

储存条件 

-20°C

溶解度 

ethanol: 20 mg/mL

酸度系数(pKa)

13.60±0.70(Predicted)

形态

powder

颜色

white

Merck 

13,2819

BRN 

1096207

InChIKey

UXVDBQLLXVKPRS-UZBFCAAUSA-N

EPA化学物质信息

Cytochalasin B (14930-96-2)

生物活性

Cytochalasin B 是一种能透过细胞的真菌毒素，能够与肌动蛋白丝的有刺端结合，扰乱肌动蛋白聚合物的形成，对 F-actin 的 Kd 值为 1.4-2.2 nM。

靶点

Kd: 2.2 nM (F-actin, with Mg 2+ ), 1.4 nM (F-actin, with Mg 2+ /K + )

体外研究

Cytochalasin B is a cell-permeable mycotoxin binding to the barbed end of actin filaments, inhibits the enlongation and shortening of actin filaments, with K d s of 2.2 nM and 1.4 nM for F-actin in the presence of MgCl 2 (2 mM) or MgCl 2 (2 mM) plus KCl, respectively. Cytochalasin B (0.1-10 μM) shows inhibitory effect on multiple murine cancer cell lines, with IC 50 s of 2.56 μM (M109c), 10.46 μM (B16BL6), 105.5 μM (P388/ADR), 51.9 μM (P388/S) and IC 80 s of 12.23 μM (M109c), 44.86 μM (B16BL6), 188.4 μM (P388/ADR), 84.1 μM (P388/S) after treatment for 3 h, with IC 50 s of 0.25 μM (M109c), 0.37 μM (B16F10), 0.87 μM (B16BL6), and IC 80 s of 0.75 μM (M109c), 1.21 μM (B16F10), 10.41 μM (B16BL6) after treatment for 4 days. Cytochalasin B (6 μM) increases the myofibrillar fragmentation index (MFI), which is attributed to the intensely breaking of myofibrillar proteins into short segments. Cytochalasin B also accelerates the disruption of actin filaments. In addition, Cytochalasin B accelerates the transformation from F-actin to G-actin, lowering the content of F-actin and significantly increasing G-actin bands during postmortem conditioning.

体内研究

Cytochalasin B (10, 25, 50 mg/kg, i.p.) dose-dependently increases the life expectancy of Balb/c mice bearing with P388/ADR leukemias. Cytochalasin B at 50 mg/kg produces 10 % long-term survival in the multidrug resistant P388/ADR cohort, and 40 % long-term survival in the drug sensitive P388/S cohort.

用途 

第一个用于研究细胞骨架的药物，它是真菌分泌的生物碱。细胞松弛素(细胞松弛素B及其衍生物)在细胞内同微丝的正端结合, 并引起F-肌动蛋白解聚，阻断亚基的进一步聚合。当将细胞松弛素加入到活细胞后，肌动蛋白纤维骨架消失，使动物细胞的各种活动瘫痪, 包括细胞的移动、吞噬作用、胞质分裂等。它对微管没有作用, 也不抑制肌收缩, 因肌纤维中肌动蛋白丝是稳定的结构, 不发生组装及解聚的动态平衡

危险品标志 

T+,T

危险类别码 

26/27/28-63-23/24/25

安全说明 

28-36/37-45

危险品运输编号 

UN 1544 6.1/PG 2

WGK Germany 

3

RTECS号

RO0205000

F 

10

HazardClass 

6.1(a)

PackingGroup 

I

海关编码 

29349990

毒害物质数据

14930-96-2(Hazardous Substances Data)

毒性

LD50 intraperitoneal in mouse: 30mg/kg