Cytochalasin B (Synonyms: 細(xì)胞松弛素B; Phomin)
生物活性
Cytochalasin B is a cell-permeable mycotoxin binding to the barbed end of actin filaments, disrupting the formation of actin polymers, with Kd value of 1.4-2.2 nM for F-actin.
IC50 & Target
Kd: 2.2 nM (F-actin, with Mg2+), 1.4 nM (F-actin, with Mg2+/K+)
體外研究(In Vitro)
Cytochalasin B is a cell-permeable mycotoxin binding to the barbed end of actin filaments, inhibits the enlongation and shortening of actin filaments, with Kds of 2.2 nM and 1.4 nM for F-actin in the presence of MgCl2 (2 mM) or MgCl2 (2 mM) plus KCl, respectively[1]. Cytochalasin B (0.1-10 μM) shows inhibitory effect on multiple murine cancer cell lines, with IC50s of 2.56 μM (M109c), 10.46 μM (B16BL6), 105.5 μM (P388/ADR), 51.9 μM (P388/S) and IC80s 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 IC50s of 0.25 μM (M109c), 0.37 μM (B16F10), 0.87 μM (B16BL6), and IC80s of 0.75 μM (M109c), 1.21 μM (B16F10), 10.41 μM (B16BL6) after treatment for 4 days[2]. 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
體內(nèi)研究(In Vivo)
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
分子量：479.61
Formula：C29H37NO5
CAS 號：14930-96-2
中文名稱：細(xì)胞松弛素B；松胞菌素B
運輸條件：Room temperature in continental US; may vary elsewhere.
儲存方式：
| Powder | -20°C | 3 years |
|---|---|---|
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
溶解性數(shù)據(jù)
DMSO : 83.33 mg/mL (173.75 mM; ultrasonic and warming and heat to 60°C)
Ethanol : 25 mg/mL (52.13 mM; Need ultrasonic)
| 濃度溶劑體積質(zhì)量 | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.0850 mL | 10.4251 mL | 20.8503 mL |
| 5 mM | 0.4170 mL | 2.0850 mL | 4.1701 mL |
| 10 mM | 0.2085 mL | 1.0425 mL | 2.0850 mL |
請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 儲存時，請在 6 個月內(nèi)使用，-20°C 儲存時，請在 1 個月內(nèi)使用。
以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用； 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶
- 1.
請依序添加每種溶劑： 0.5% CMC-Na 0.5% Tween-80
Solubility: 5 mg/mL (10.43 mM); Suspened solution; Need ultrasonic
- 2.
請依序添加每種溶劑： 10% EtOH 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (5.21 mM); Clear solution
- 3.
請依序添加每種溶劑： 10% EtOH 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (5.21 mM); Clear solution
- 4.
請依序添加每種溶劑： 10% EtOH 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.21 mM); Clear solution
- 5.
請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (4.34 mM); Clear solution
- 6.
請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (4.34 mM); Clear solution
- 7.
請依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.34 mM); Clear solution
參考文獻(xiàn)
[1]. Theodoropoulos PA, et al. Cytochalasin B may shorten actin filaments by a mechanism independent of barbed end capping. Biochem Pharmacol. 1994 May 18;47(10):1875-81.
[2]. Trendowski M, et al. Chemotherapy with cytochalasin congeners in vitro and in vivo against murine models. Invest New Drugs. 2015 Apr;33(2):290-9.
[3]. Zhou C, et al. The effect of Cytochalasin B and Jasplakinolide on depolymerization of actin filaments in goose muscles during postmortem conditioning. Food Res Int. 2016 Dec;90:1-7.
注：產(chǎn)品僅用于科研
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