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  1. Cytoskeleton
  2. Arp2/3 Complex
  3. Latrunculin A

Latrunculin A (LAT-A) 是一種 G-肌動(dòng)蛋白聚合 (G-actin polymerization) 抑制劑,在紅海海綿 Latrunculia magnifica 中發(fā)現(xiàn)的。Latrunculin A 能夠與肌動(dòng)蛋白 (actin) 單體結(jié)合,抑制其聚集,對(duì) ATP-actin,ADP-Pi-actin,ADP-actin 和 G-actin 的 Kd 值分別為 0.1,0.4,4.7 μM 和 0.19 μM。Latrunculin A 具有有效的抗轉(zhuǎn)移特性,可用于癌癥的研究。Latrunculin A 抑制細(xì)胞遷移。

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Latrunculin A Chemical Structure

Latrunculin A Chemical Structure

CAS No. : 76343-93-6

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100 μg (237.2 μM * 1 mL in Ethanol) ¥4300
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  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Latrunculin A (LAT-A), found in the red sea sponge Latrunculia magnifica, is a G-actin polymerization inhibitor. Latrunculin A binds to actin monomers and inhibits polymerization of actin with Kds of 0.1, 0.4, 4.7 μM and 0.19 μM for ATP-actin, ADP-Pi-actin, ADP-actin and G-actin, respectively. Latrunculin A has effective anti-metastatic properties for cancer research. Latrunculin A blocks cell migration[1][2][3][4][5][6].

IC50 & Target

Kd: 0.1 μM (ATP-actin), 0.4 μM (ADP-Pi-actin), 4.7 μM (ADP-actin), 0.19 μM (G-actin)[2]

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
0.06 μg/mL
Compound: 1
Cytotoxicity against human A549 cells after 48 hrs by MTT assay
Cytotoxicity against human A549 cells after 48 hrs by MTT assay
[PMID: 8350092]
HCT-116 IC50
1.1 μM
Compound: 1, NSC-613011
Cytotoxicity against human HCT116 cells after 3 days by trypan blue assay
Cytotoxicity against human HCT116 cells after 3 days by trypan blue assay
[PMID: 18942825]
HT-29 IC50
0.06 μg/mL
Compound: 1
Cytotoxicity against human HT-29 cells after 48 hrs by MTT assay
Cytotoxicity against human HT-29 cells after 48 hrs by MTT assay
[PMID: 8350092]
HT-29 IC50
0.08 μg/mL
Compound: 10
Antiproliferative activity against human HT-29 cells assessed as cell viability after 96 hrs by CellTiter-Glo luminescence assay
Antiproliferative activity against human HT-29 cells assessed as cell viability after 96 hrs by CellTiter-Glo luminescence assay
[PMID: 22129061]
MCF7 IC50
0.48 μM
Compound: 99a
Anticancer activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Anticancer activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 33940466]
MDA-MB-231 IC50
4.19 μM
Compound: 99a
Anticancer activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Anticancer activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 33940466]
MDA-MB-435 IC50
0.04 μg/mL
Compound: 10
Antiproliferative activity against human MDA-MB-435 cells assessed as cell viability after 96 hrs by CellTiter-Glo luminescence assay
Antiproliferative activity against human MDA-MB-435 cells assessed as cell viability after 96 hrs by CellTiter-Glo luminescence assay
[PMID: 22129061]
MDA-MB-435 IC50
2.8 μM
Compound: 1, NSC-613011
Cytotoxicity against human MDA-MB-435 cells 48 hrs by SRB assay
Cytotoxicity against human MDA-MB-435 cells 48 hrs by SRB assay
[PMID: 18942825]
P388 IC50
4.1 μg/mL
Compound: 1
Cytotoxicity against mouse P388 cells after 48 hrs by MTT assay
Cytotoxicity against mouse P388 cells after 48 hrs by MTT assay
[PMID: 8350092]
T47D IC50
25 μM
Compound: 1,Latrunculin A
Inhibition of 1,10-phenanthroline-induced HIF1 activation in human T47D cells by cell based reporter gene assay
Inhibition of 1,10-phenanthroline-induced HIF1 activation in human T47D cells by cell based reporter gene assay
[PMID: 18298079]
T47D IC50
6.7 μM
Compound: 1,Latrunculin A
Inhibition of hypoxia-induced HIF1 activation in human T47D cells by cell based reporter gene assay
Inhibition of hypoxia-induced HIF1 activation in human T47D cells by cell based reporter gene assay
[PMID: 18298079]
U-937 IC50
0.07 μg/mL
Compound: 10
Antiproliferative activity against human U937 cells assessed as cell viability after 96 hrs by CellTiter-Glo luminescence assay
Antiproliferative activity against human U937 cells assessed as cell viability after 96 hrs by CellTiter-Glo luminescence assay
[PMID: 22129061]
體外研究
(In Vitro)

LatruncuLin A (50-1000 nM) 對(duì)人前列腺癌 PC-3M 細(xì)胞具有強(qiáng)效抗侵襲活性,可抑制 PC-3M-CT+ 球體解聚和細(xì)胞遷移[3]
LatruncuLin A (3-30 μM) 抑制缺氧誘導(dǎo)的 HIF-1 激活,在人乳腺癌 T47D 細(xì)胞中的 IC50 值為 6.7 μM[3]
LatruncuLin A (0-0.2 μM,4 小時(shí)) 在高濃度 (例如 0.2 μM) 下對(duì)人肝癌 HepG2 細(xì)胞中的 HuR 水平具有顯著抑制作用,而在 0.02 μM 時(shí)僅抑制 HuR,但在高濃度下對(duì)人肝癌 Huh7 沒(méi)有抑制作用cells[4]。
LatruncuLin A (0.1 μM,24 hours) 可導(dǎo)致細(xì)胞遷移顯著減少,并對(duì)人肝癌細(xì)胞系 HepG2 的細(xì)胞增殖具有抑制作用[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

體內(nèi)研究
(In Vivo)

LatruncuLin A (腹腔注射,0.05 mg/kg,前20天分3次給藥,120天) 對(duì)感染腺癌 (MKN45) 或癌 (NugC-4) 的雄性BALB/c裸鼠模型具有較強(qiáng)的抗腫瘤作用[5]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male BALB/c nude mice models infected with adenocarcinoma (MKN45) or carcinoma (NUGC-4)[5]
Dosage: 0.05 mg/kg
Administration: Intraperitoneal injection; three doses in the first 20 days; 120 days
Result: Extended the mean life expectancy to 23.5 days comparing to control of 16 days in adenocarcinoma (MKN45) mice and the mean survival time was 42 days comparing to untreated of 31 days in carcinoma (NUGC-4) mice.
Clinical Trial
分子量

421.55

Formula

C22H31NO5S

CAS 號(hào)
性狀

液體

顏色

Colorless to light yellow

結(jié)構(gòu)分類
初始來(lái)源

red sea sponge Latrunculia magnifica

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式

Solution, -20°C, 2 years

純度 & 產(chǎn)品資料

純度: ≥98.0%

參考文獻(xiàn)
  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Latrunculin A
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