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埃博霉素A

埃博霉素A用途

Epothilone A 是紫杉醇和管蛋白 (tubulin) 聚合物结合的竞争性抑制剂,其 Ki 值为 0.6-1.4 μM。

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埃博霉素A名称

[ CAS 号 ]:
152044-53-6

[ 中文名 ]:
埃博霉素 A

[ 英文名 ]:
Epothilone A

[中文别名 ]:

[英文别名 ]:

UNII-51E07YBX96
Epothilone A
(-)-Epothilone A
Epo A
Epothilon A
epithilone A
Epothilones

埃博霉素A生物活性

[ 描述 ]:

Epothilone A 是紫杉醇和管蛋白 (tubulin) 聚合物结合的竞争性抑制剂,其 Ki 值为 0.6-1.4 μM。

[ 相关类别 ]:

信号通路 >> 细胞周期/DNA损伤 >> 微管/微管蛋白

信号通路 >> 细胞骨架 >> 微管/微管蛋白

研究领域 >> 癌症

天然产物 >> 其他

[体外研究]

埃坡霉素A是[3H]紫杉醇与微管蛋白聚合物结合的竞争性抑制剂。通过Hanes分析,Epothilone A的表观Ki值为1.4μM,Dixon分析的表观Ki值为0.6μM[1]。当应用于人T-24膀胱癌细胞系时,埃坡霉素A在体外具有高度细胞毒性(IC 50 =0.05μM)。基于竞争测定,埃坡霉素A与微管蛋白的结合亲和力与紫杉醇对微管蛋白的结合亲和力具有相同的数量级。从微管蛋白结合位点取出100nM(3H)紫杉醇的IC50对于紫杉醇为3.6μM,对于埃坡霉素A为2.3μM,对于patupilone为3.3μM[2]。

[参考文献]

[1]. Kowalski RJ, et al. Activities of the microtubule-stabilizing agents epothilones A and B with purified tubulin and in cells resistant to paclitaxel (Taxol(R)). J Biol Chem. 1997 Jan 24;272(4):2534-41.

[2]. Cheng KL, et al. Novel microtubule-targeting agents - the epothilones. Biologics. 2008 Dec;2(4):789-811.

[相关活性小分子]

埃博霉素A物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
683.3±55.0 °C at 760 mmHg

[ 熔点 ]:
95ºC

[ 分子式 ]:
C₂₆H₃₉NO₆S

[ 分子量 ]:
493.656

[ 闪点 ]:
367.1±31.5 °C

[ 精确质量 ]:
493.249817

[ PSA ]:
137.49000

[ LogP ]:
2.54

[ 蒸汽压 ]:
0.0±2.2 mmHg at 25°C

[ 折射率 ]:
1.532

[ 储存条件 ]:
-20°C

埃博霉素A安全信息

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

埃博霉素A合成路线

详细合成路线

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埃博霉素A文献

Identifying off-target effects and hidden phenotypes of drugs in human cells.

Nat. Chem. Biol. 2 , 329-37, (2006)

We present a strategy for identifying off-target effects and hidden phenotypes of drugs by directly probing biochemical pathways that underlie therapeutic or toxic mechanisms in intact, living cells. ...

Neuronal transcriptional repressor REST suppresses an Atoh7-independent program for initiating retinal ganglion cell development.

Dev. Biol. 349 , 90-9, (2011)

As neuronal progenitors differentiate into neurons, they acquire a unique set of transcription factors. The transcriptional repressor REST prevents progenitors from undergoing differentiation. Notably...

Conformational preferences of natural and C3-modified epothilones in aqueous solution.

J. Med. Chem. 51 , 1469-73, (2008)

The conformational properties of the microtubule-stabilizing agent epothilone A ( 1a) and its 3-deoxy and 3-deoxy-2,3-didehydro derivatives 2 and 3 have been investigated in aqueous solution by a comb...

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