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  1. Cell Cycle/DNA Damage Cytoskeleton Apoptosis
  2. Kinesin Apoptosis
  3. S-Trityl-L-cysteine

S-Trityl-L-cysteine  (Synonyms: NSC 83265; S-Tritylcysteine; 3-Tritylthio-L-alanine)

目錄號(hào): HY-W011102 純度: 99.10%
COA 產(chǎn)品使用指南 技術(shù)支持

S-Trityl-L-cysteine (NSC 83265) 是一種選擇性的別構(gòu)驅(qū)動(dòng)蛋白 Eg5 抑制劑,抑制基礎(chǔ) ATPase 活性的 IC50 為 1 μM,抑制微管激活的 ATPase 活性的 IC50 為 140 nM。S-Trityl-L-cysteine 具有抗腫瘤活性。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào),我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

S-Trityl-L-cysteine Chemical Structure

S-Trityl-L-cysteine Chemical Structure

CAS No. : 2799-07-7

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10 mM * 1 mL in DMSO ¥550
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50 mg ¥500
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  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

S-Trityl-L-cysteine (NSC 83265) is a selective and allosteric kinesin Eg5 inhibitor with an IC50 of 1 μM for the inhibition of basal ATPase activity and 140 nM for the microtubule-activated ATPase activity. S-Trityl-L-cysteine has antitumor activities[1][2].

IC50 & Target[1]

Eg5

 

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
BXPC-3 GI50
1563 nM
Compound: 4
Growth inhibition of human BxPC3 cells after 72 hrs by Alamar blue assay
Growth inhibition of human BxPC3 cells after 72 hrs by Alamar blue assay
[PMID: 23394180]
BXPC-3 GI50
1563 nM
Compound: 4, STLC
Cytotoxicity against human BxPC3 cells after 72 hrs by Alamar blue assay
Cytotoxicity against human BxPC3 cells after 72 hrs by Alamar blue assay
[PMID: 22749640]
BXPC-3 GI50
1563 nM
Compound: 1, STLC
Antiproliferative activity against human BxPC3 cells after 72 hrs by Alamar blue assay
Antiproliferative activity against human BxPC3 cells after 72 hrs by Alamar blue assay
[PMID: 22248262]
HCT-116 GI50
553 nM
Compound: 4
Growth inhibition of human HCT116 cells after 72 hrs by Alamar blue assay
Growth inhibition of human HCT116 cells after 72 hrs by Alamar blue assay
[PMID: 23394180]
HCT-116 GI50
553 nM
Compound: 4, STLC
Cytotoxicity against human HCT116 cells after 72 hrs by Alamar blue assay
Cytotoxicity against human HCT116 cells after 72 hrs by Alamar blue assay
[PMID: 22749640]
HCT-116 GI50
553 nM
Compound: 1, STLC
Antiproliferative activity against human HCT116 cells after 72 hrs by Alamar blue assay
Antiproliferative activity against human HCT116 cells after 72 hrs by Alamar blue assay
[PMID: 22248262]
HCT-116 IC50
910 nM
Compound: 3; STLC
Growth inhibition of human HCT116 cells after 72 hrs by MTS assay
Growth inhibition of human HCT116 cells after 72 hrs by MTS assay
[PMID: 26396688]
HeLa EC50
0.7 μM
Compound: 1, STLC
Induction of mitotic arrest in human HeLa cells assessed as monoastral spindle formation after 24 hrs
Induction of mitotic arrest in human HeLa cells assessed as monoastral spindle formation after 24 hrs
[PMID: 18266314]
HeLa EC50
1.7 μM
Compound: 1, STLC
Induction of mitotic arrest in human HeLa cells after 24 hrs
Induction of mitotic arrest in human HeLa cells after 24 hrs
[PMID: 18266314]
K562 GI50
1452 nM
Compound: 4, STLC
Cytotoxicity against human K562 cells after 72 hrs by Alamar blue assay
Cytotoxicity against human K562 cells after 72 hrs by Alamar blue assay
[PMID: 22749640]
K562 GI50
1452 nM
Compound: 1, STLC
Antiproliferative activity against human K562 cells after 72 hrs by Alamar blue assay
Antiproliferative activity against human K562 cells after 72 hrs by Alamar blue assay
[PMID: 22248262]
K562 GI50
1791 nM
Compound: 4
Growth inhibition of human K562 cells after 72 hrs by Alamar blue assay
Growth inhibition of human K562 cells after 72 hrs by Alamar blue assay
[PMID: 23394180]
LNCaP GI50
811 nM
Compound: 4
Growth inhibition of human LNCAP cells after 72 hrs by Alamar blue assay
Growth inhibition of human LNCAP cells after 72 hrs by Alamar blue assay
[PMID: 23394180]
NCI-H1299 GI50
1549 nM
Compound: 4
Growth inhibition of human NCI-H1299 cells after 72 hrs by Alamar blue assay
Growth inhibition of human NCI-H1299 cells after 72 hrs by Alamar blue assay
[PMID: 23394180]
NCI-H1299 GI50
1549 nM
Compound: 4, STLC
Cytotoxicity against human NCI-H1299 cells after 72 hrs by Alamar blue assay
Cytotoxicity against human NCI-H1299 cells after 72 hrs by Alamar blue assay
[PMID: 22749640]
NCI-H1299 GI50
1549 nM
Compound: 1, STLC
Antiproliferative activity against human NCI-H1299 cells after 72 hrs by Alamar blue assay
Antiproliferative activity against human NCI-H1299 cells after 72 hrs by Alamar blue assay
[PMID: 22248262]
PC-3 GI50
1371 nM
Compound: 4
Growth inhibition of human PC3 cells after 72 hrs by Alamar blue assay
Growth inhibition of human PC3 cells after 72 hrs by Alamar blue assay
[PMID: 23394180]
體外研究
(In Vitro)

S-Trityl-L-cysteine 與由二級(jí)結(jié)構(gòu)元件 (螺旋 a2/環(huán) L5/螺旋 a3) 形成的 Eg5 運(yùn)動(dòng)域中的獨(dú)特口袋結(jié)合[1]。
S-Trityl-L-cysteine (1 -20 μM;持續(xù) 72 小時(shí)) 可以劑量依賴性方式介導(dǎo)細(xì)胞凋亡和細(xì)胞周期停滯。S-Trityl-L-cysteine 介導(dǎo)的細(xì)胞凋亡和細(xì)胞周期阻滯是通過(guò)激活絲裂原激活的蛋白激酶和核因子 kB 信號(hào)通路觸發(fā)的[1]
S-Trityl-L-cysteine 在具有特征性單星形紡錘體的 HeLa 細(xì)胞中誘導(dǎo)有絲分裂停滯 (IC50 為 700 nM)[2]。

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

分子量

363.47

Formula

C22H21NO2S

CAS 號(hào)
性狀

固體

顏色

White to off-white

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

DMSO 中的溶解度 : 25 mg/mL (68.78 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響,請(qǐng)使用新開封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.7513 mL 13.7563 mL 27.5126 mL
5 mM 0.5503 mL 2.7513 mL 5.5025 mL
查看完整儲(chǔ)備液配制表

* 請(qǐng)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(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物實(shí)驗(yàn):

請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液,再依次添加助溶劑:
——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過(guò)加熱和/或超聲的方式助溶

  • 方案 一

    請(qǐng)依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1 mg/mL (2.75 mM); 澄清溶液

    此方案可獲得 ≥ 1 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 10.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中,混合均勻;再向上述體系中加入 50 μL Tween-80,混合均勻;然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制:將 0.9 g 氯化鈉,溶解于 ddH?O 并定容至 100 mL,可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請(qǐng)依序添加每種溶劑: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 1 mg/mL (2.75 mM); 澄清溶液

    此方案可獲得 ≥ 1 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 10.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中,混合均勻。

    2 g SBE-β-CD(磺丁基醚 β-環(huán)糊精)粉末定容于 10 mL 的生理鹽水中,完全溶解至澄清透明。
動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息:

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

由于實(shí)驗(yàn)過(guò)程有損耗,建議您多配一只動(dòng)物的量
請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠,建議 DMSO 中的在最后工作液體系中的占比盡量不超過(guò) 2%。
方案所需 助溶劑 包括:DMSO, ,均可在 MCE 網(wǎng)站選購(gòu)。 Tween 80,均可在 MCE 網(wǎng)站選購(gòu)。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO(母液濃度為 mg/mL)。
您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度,以下方案僅供參考,如有需要,請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液,加入 μL 。 μL ,混合均勻至澄清,再加 μL Tween 80,混合均勻至澄清,再加 μL 生理鹽水
連續(xù)給藥周期超過(guò)半月以上,請(qǐng)謹(jǐn)慎選擇該方案。
請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài),從左到右依次添加助溶劑。您可采用超聲加熱 (超聲清洗儀,建議頻次 20-40 kHz),渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 99.10%

參考文獻(xiàn)

S-Trityl-L-cysteine 相關(guān)分類

完整儲(chǔ)備液配制表

* 請(qǐng)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(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7513 mL 13.7563 mL 27.5126 mL 68.7815 mL
5 mM 0.5503 mL 2.7513 mL 5.5025 mL 13.7563 mL
10 mM 0.2751 mL 1.3756 mL 2.7513 mL 6.8781 mL
15 mM 0.1834 mL 0.9171 mL 1.8342 mL 4.5854 mL
20 mM 0.1376 mL 0.6878 mL 1.3756 mL 3.4391 mL
25 mM 0.1101 mL 0.5503 mL 1.1005 mL 2.7513 mL
30 mM 0.0917 mL 0.4585 mL 0.9171 mL 2.2927 mL
40 mM 0.0688 mL 0.3439 mL 0.6878 mL 1.7195 mL
50 mM 0.0550 mL 0.2751 mL 0.5503 mL 1.3756 mL
60 mM 0.0459 mL 0.2293 mL 0.4585 mL 1.1464 mL
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產(chǎn)品名稱:
S-Trityl-L-cysteine
目錄號(hào):
HY-W011102
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