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  2. NF-κB Immunology/Inflammation
  3. NF-κB PD-1/PD-L1
  4. Sulindac

Sulindac  (Synonyms: 舒林酸; MK-231)

目錄號(hào): HY-B0008 純度: 99.81%
COA 產(chǎn)品使用指南

Sulindac (MK-231) 是一種口服活性非甾體類(lèi)抗炎藥。Sulindac 也是一種免疫調(diào)節(jié)劑。Sulindac 可用于脊柱關(guān)節(jié)炎、痛風(fēng)性關(guān)節(jié)炎及多種癌癥如結(jié)直腸癌、肺癌的研究。

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)

Sulindac Chemical Structure

Sulindac Chemical Structure

CAS No. : 38194-50-2

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥605
In-stock
100 mg ￥550
In-stock
500 mg ￥950
In-stock
1 g   詢(xún)價(jià)  
5 g   詢(xún)價(jià)  

* Please select Quantity before adding items.

Customer Review

Other Forms of Sulindac:

查看 NF-κB 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Sulindac (MK-231) is an orally active nonsteroidal anti-inflammatory agent. Sulindac also is an immunomodulatory agent. Sulindac can be used for the research of arthritis of the spine, gouty arthritis and kinds of cancer including colorectal cancer (CRC) and lung cancer[1][2].

IC50 & Target[1]

COX-2

 

Autophagy

 

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
> 50 μM
Compound: Sulindac
Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
[PMID: 32987314]
A549 IC50
> 50 μM
Compound: Sulindac
Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
[PMID: 32987314]
A549 IC50
> 50 μM
Compound: Sulindac
Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
[PMID: 32987314]
BXPC-3 IC50
980 μM
Compound: SUL
Cytotoxicity against human BxPC3 cells assessed as growth inhibition after 24 hrs by MTT assay
Cytotoxicity against human BxPC3 cells assessed as growth inhibition after 24 hrs by MTT assay
[PMID: 24273639]
COLO 320 IC50
> 200 μM
Compound: a
Cytotoxicity against human COLO320 cells after 72 hrs by WST-1 assay
Cytotoxicity against human COLO320 cells after 72 hrs by WST-1 assay
[PMID: 20801552]
HeLa IC50
> 50 μM
Compound: Sulindac
Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
[PMID: 32987314]
HeLa IC50
> 50 μM
Compound: Sulindac
Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
[PMID: 32987314]
HeLa IC50
> 50 μM
Compound: Sulindac
Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
[PMID: 32987314]
HT-29 IC50
1729 μM
Compound: Sulindac
Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay
Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay
[PMID: 22940705]
HT-29 IC50
800 μM
Compound: SUL
Cytotoxicity against human HT-29 cells assessed as growth inhibition after 24 hrs by MTT assay
Cytotoxicity against human HT-29 cells assessed as growth inhibition after 24 hrs by MTT assay
[PMID: 24273639]
Jurkat IC50
699 μM
Compound: SUL
Cytotoxicity against human Jurkat cells assessed as growth inhibition after 24 hrs by MTT assay
Cytotoxicity against human Jurkat cells assessed as growth inhibition after 24 hrs by MTT assay
[PMID: 24273639]
MCF7 IC50
> 50 μM
Compound: Sulindac
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
[PMID: 32987314]
MCF7 IC50
> 50 μM
Compound: Sulindac
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
[PMID: 32987314]
MCF7 IC50
> 50 μM
Compound: Sulindac
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
[PMID: 32987314]
MCF7 IC50
965 μM
Compound: SUL
Cytotoxicity against human MCF7 cells assessed as growth inhibition after 24 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as growth inhibition after 24 hrs by MTT assay
[PMID: 24273639]
MDCK IC50
300 μM
Compound: Sulindac
Anti-proliferative activity was evaluated by its ability to inhibit proliferation of MDCK cells
Anti-proliferative activity was evaluated by its ability to inhibit proliferation of MDCK cells
[PMID: 11844707]
MDCK IC50
320 μM
Compound: Sulindac
Anti-proliferative activity was evaluated by its ability to inhibit proliferation of MDCK-f3 (Madin-Darby canine kidney f3) cell line
Anti-proliferative activity was evaluated by its ability to inhibit proliferation of MDCK-f3 (Madin-Darby canine kidney f3) cell line
[PMID: 11844707]
MIA PaCa-2 IC50
> 200 μM
Compound: a
Cytotoxicity against human MIAPaCa2 cells after 72 hrs by WST-1 assay
Cytotoxicity against human MIAPaCa2 cells after 72 hrs by WST-1 assay
[PMID: 20801552]
MIA PaCa-2 IC50
300 μM
Compound: Sulindac
Cytotoxicity against human MIA PaCa-2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Cytotoxicity against human MIA PaCa-2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 35439009]
NIH3T3 IC50
200 μM
Compound: Sulindac
Anti-proliferative activity was evaluated by its ability to inhibit proliferation of murine NIH3T3 fibroblasts
Anti-proliferative activity was evaluated by its ability to inhibit proliferation of murine NIH3T3 fibroblasts
[PMID: 11844707]
REF IC50
100 μM
Compound: Sulindac
Anti-proliferative activity was evaluated by its ability to inhibit proliferation of rat embryonic fibroblasts (REF)
Anti-proliferative activity was evaluated by its ability to inhibit proliferation of rat embryonic fibroblasts (REF)
[PMID: 11844707]
SW480 IC50
> 50 μM
Compound: Sulindac
Cytotoxicity against human SW480 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
Cytotoxicity against human SW480 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
[PMID: 32987314]
SW480 IC50
> 50 μM
Compound: Sulindac
Cytotoxicity against human SW480 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
Cytotoxicity against human SW480 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
[PMID: 32987314]
SW480 IC50
> 50 μM
Compound: Sulindac
Cytotoxicity against human SW480 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
Cytotoxicity against human SW480 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
[PMID: 32987314]
SW480 IC50
800 μM
Compound: Sulindac
Anti-proliferative activity was evaluated by its ability to inhibit proliferation of SW480 cells
Anti-proliferative activity was evaluated by its ability to inhibit proliferation of SW480 cells
[PMID: 11844707]
體外研究
(In Vitro)

Sulindac (MK-231) (500 μM，48 小時(shí)) 可有效預(yù)防 TGF-β1 誘導(dǎo)的 EMT，表現(xiàn)為上皮標(biāo)記物 E-鈣粘蛋白的上調(diào)以及間充質(zhì)標(biāo)記物和轉(zhuǎn)錄因子的下調(diào)[1]。
Sulindac (500 μM，48 h) 抑制 TGF-β1 增強(qiáng)的 A549 細(xì)胞遷移和侵襲[1]。
Sulindac (500 μM，48 h) 增強(qiáng) Sulindac 對(duì) TGF-β1 誘導(dǎo)的 EMT 的逆轉(zhuǎn)作用，SIRT1 上調(diào)促進(jìn) TGF-β1 誘導(dǎo)的 EMT[1]。

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

Western Blot Analysis[1]

Cell Line: A549 cells
Concentration: 500 μM
Incubation Time: 48 h
Result: Inhibit transforming growth factor (TGF)-β1-induced epithelial-mesenchymal transition in A549 cells.

Immunofluorescence[1]

Cell Line: A549 cells
Concentration: 500 μM
Incubation Time: 48 h
Result: Reversed SIRT-1 expression by TGF-β1 and inhibited the TGF-β1-induced cadherin switch.

Cell Migration Assay [1]

Cell Line: A549 cells
Concentration: 500 μM
Incubation Time: 48 h
Result: Inhibited migration, decreased resistance co-treatment with TGF-β1.

Cell Invasion Assay[1]

Cell Line: A549 cells
Concentration: 500 μM
Incubation Time: 40 h; 48 h
Result: Could effectively inhibit the TGF- β1-induced increase in invasion by lung cancer cells.
體內(nèi)研究
(In Vivo)

Sulindac (MK-231) (15 mg/kg，po，bid (單獨(dú) Sulindac)；7.5 mg/kg po，bid (Sulindac 與 PD-L1 組合)) 顯示腫瘤體積顯著減少并增加 CD8+ T 淋巴細(xì)胞的浸潤(rùn)當(dāng)用聯(lián)合療法處理時(shí)在腫瘤組織中[2]。
Sulindac (15 mg/kg，口服，每天兩次 (Sulindac 單獨(dú)使用)；7.5 mg/kg 口服，每天兩次 (Sulindac 與PD-L1)) 可通過(guò)阻斷 NF-κB 信號(hào)通路下調(diào) PD-L1，進(jìn)而導(dǎo)致外泌體 P[2]減少。
Sulindac (15 mg/kg，po，bid (單獨(dú) Sulindac)；7.5 mg/kg po，bid (Sulindac 與 PD-L1 聯(lián)合)) 通過(guò)在聯(lián)合處理中下調(diào) PD-L1 導(dǎo)致 PD-L1 Ab 的可用性增加[2]。
Sulindac (15 mg/kg，po，bid (單獨(dú) Sulindac)；7.5 mg/kg po，bid (Sulindac 與 PD-L1 組合)) 在低劑量下對(duì)前列腺素 E2 (PGE2) 沒(méi)有系統(tǒng)性抑制作用[2]。

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

Animal Model: CT26 syngeneic mouse tumor model[2]
Dosage: 15 mg/kg; 7.5 mg/kg
Administration: 15 mg/kg, p.o., bid (sulindac alone); 7.5 mg/kg p.o., bid (sulindac combination with PD-L1)
Result: Downregulated PD-L1 through the blockade of NF-κB signaling and modulate the response of pMMR CRC to anti-PD-L1 immunotherapy.
Cound effectively inhibit PD-L1 with no significant systematic toxicity.
Clinical Trial
分子量

356.41

Formula

C20H17FO3S
CAS 號(hào)
性狀

固體

顏色

White to yellow

中文名稱(chēng)

舒林酸
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 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 50 mg/mL (140.29 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(kāi)封的 DMSO)

H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.8058 mL 14.0288 mL 28.0576 mL
5 mM 0.5612 mL 2.8058 mL 5.6115 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, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(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: ≥ 2.5 mg/mL (7.01 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (7.01 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 25.0 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

只
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: 99.81%

參考文獻(xiàn)

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, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(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 2.8058 mL 14.0288 mL 28.0576 mL 70.1439 mL
5 mM 0.5612 mL 2.8058 mL 5.6115 mL 14.0288 mL
10 mM 0.2806 mL 1.4029 mL 2.8058 mL 7.0144 mL
15 mM 0.1871 mL 0.9353 mL 1.8705 mL 4.6763 mL
20 mM 0.1403 mL 0.7014 mL 1.4029 mL 3.5072 mL
25 mM 0.1122 mL 0.5612 mL 1.1223 mL 2.8058 mL
30 mM 0.0935 mL 0.4676 mL 0.9353 mL 2.3381 mL
40 mM 0.0701 mL 0.3507 mL 0.7014 mL 1.7536 mL
50 mM 0.0561 mL 0.2806 mL 0.5612 mL 1.4029 mL
60 mM 0.0468 mL 0.2338 mL 0.4676 mL 1.1691 mL
80 mM 0.0351 mL 0.1754 mL 0.3507 mL 0.8768 mL
100 mM 0.0281 mL 0.1403 mL 0.2806 mL 0.7014 mL
Help & FAQs
  • 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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產(chǎn)品名稱(chēng)：
Sulindac
目錄號(hào)：
HY-B0008
需求量：