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  2. Stem Cell/Wnt TGF-beta/Smad Apoptosis
  3. Organoid TGF-β Receptor Apoptosis
  4. SB-431542

SB-431542 是 TGF-β 受體激酶抑制劑 (TRKI)。SB-431542 對(duì) ALK4、ALK5 和 ALK7 活性有抑制作用， IC50 值分別為 1 μM、0.75 μM 和 2 μM。SB-431542 還能抑制 TGF-β 誘導(dǎo)的轉(zhuǎn)錄、基因表達(dá)、細(xì)胞凋亡和生長(zhǎng)抑制。SB-431542 可用于癌癥及其信號(hào)轉(zhuǎn)導(dǎo)途徑的研究。

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)

SB-431542 Chemical Structure

SB-431542 Chemical Structure

CAS No. : 301836-41-9

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥880
In-stock
5 mg ￥500
In-stock
10 mg ￥800
In-stock
50 mg ￥3380
In-stock
100 mg 現(xiàn)貨 詢(xún)價(jià)
200 mg   詢(xún)價(jià)  
500 mg   詢(xún)價(jià)  

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Customer Review

Other Forms of SB-431542:

MCE 顧客使用本產(chǎn)品發(fā)表的 194 篇科研文獻(xiàn)

WB
RT-PCR

    SB-431542 purchased from MCE. Usage Cited in: Biomed Pharmacother. 2023 Mar 16;161:114537.  [Abstract]

    SB431542 (4.2?mg/kg; i.p.; single daily for 3 days) reduces the expression of α-SMA, collagen-I and p-Smad3 in SiO2-induced fibrosis lungs of mice.

    SB-431542 purchased from MCE. Usage Cited in: Stem Cells. 2019 Feb;37(2):190-201.  [Abstract]

    Western blot analyses show the repression of SMC specific markers in the sh-GPM6B TGF-β1 group are abolished by Alantolactone in the sh-GPM6B and the enrichment of SMC specific markers in the GPM6B-sgRNA cells is cancelled by treatment with SB431542.

    SB-431542 purchased from MCE. Usage Cited in: Stem Cells. 2019 Feb;37(2):190-201.  [Abstract]

    Western blot images show Smad2/3 phosphorylation is lower than baseline in the sh-GPM6B cells and higher than baseline in the GPM6B-sgRNA cells. The phosphorylation of Smad2/3 in the sh-GPM6B TGF-β1 group is elevated by Alantolactone and the phosphorylation is reduced by treatment with SB431542.

    SB-431542 purchased from MCE. Usage Cited in: Mol Med Rep. 2019 Mar;19(3):2107-2114.  [Abstract]

    Effects of the TGF?β1 inhibitor SB (20 μM) on mechanical force?induced COL?1 and MMP?1 mRNA expression.

    SB-431542 purchased from MCE. Usage Cited in: Phytother Res. 2019 Jan;33(1):214-223.  [Abstract]

    Western analysis of FN and α-SMA in cardiac fibroblasts or NIH3T3 with treatments of (+)‐isobicyclogermacrenal, spathulenol, oxymatrine (OMT), and SB431542 at indicated concentrations.

    SB-431542 purchased from MCE. Usage Cited in: Mol Oncol. 2018 Mar;12(3):305-321.  [Abstract]

    Western blot analysis of EGFR, total and phosphorylated Smad3, total and phosphorylated ERK protein expression in cell lysates from two breast cancer cells pretreated with SB431542 and then stimulated with TGF-β for the indicated times.

    SB-431542 purchased from MCE. Usage Cited in: Int J Mol Sci. 2018 May 23;19(6). pii: E1556.  [Abstract]

    E-cadherin, N-cadherin, Snail, and MMP-2 expression in HCC cells is examined by Western blot analysis. GAPDH is used as a loading control.

    SB-431542 purchased from MCE. Usage Cited in: J Cell Mol Med. 2018 Sep;22(9):4354-4365.  [Abstract]

    p-FOXO3a (Thr32), p-FOXO3a (Ser253), FOXO3a, p-Akt and Akt expression via western blot following treatment with PBS, ASV, TGF-b1, TGF-b1+ASV, TGF-b1+SB431542 or TGF-b1+LY294002.

    SB-431542 purchased from MCE. Usage Cited in: Immunol Lett. 2019 Feb;206:33-40.  [Abstract]

    Monocytes were cultured with 20 ng/mL M-CSF with or without 10 ng/mL TGF-β1 for 2 days, with SB431542 (1 or 50 μM) or SIS3 (2.5 μM) having been added 30 min beforehand. Whole-cell lysates were subjected to SDS-PAGE and immunoblotted.

    SB-431542 purchased from MCE. Usage Cited in: Mol Cell Biochem. 2018 Feb;439(1-2):117-129.  [Abstract]

    Protein expression levels of E-cadherin N-cadherin, p-ERK, ERK, TGF-β1, p-Smad2, and p-Smad3 in each group are analyzed by western blotting.

    SB-431542 purchased from MCE. Usage Cited in: Brain Res Bull. 2018 May;139:38-47.  [Abstract]

    pSmad2/3 protein levels are down-regulated by the ALK5 inhibitor SB431542 (rGDF11 group vs. rGDF11+SB group, p=0.000).

    SB-431542 purchased from MCE. Usage Cited in: Oncol Lett. 2018 Mar;15(3):2801-2806.  [Abstract]

    A549 cells are co cultured with 10.0 mM SB431542 for 48 h, the expression of TGF β1, Smad2 and caspase 3 are tested by western blot analysis and then analyzed.

    SB-431542 purchased from MCE. Usage Cited in: Oncol Lett. 2018 Jun;15(6):9681-9686.  [Abstract]

    A549 cells are treated with 1.0% CSE with or without 10.0 mM SB431542 for 48 h, the levels of TGF β1, p Smad2, and MMP3 is assayed by western blot analysis.

    SB-431542 purchased from MCE. Usage Cited in: Int J Mol Sci. 2017 Apr 18;18(4). pii: E853.  [Abstract]

    The protein level of Six2 and Ki67 after the treatment of phosphorylation Smad3 ( p-Smad3) inhibitor SB431542 (10 μM) for 48 h.

    SB-431542 purchased from MCE. Usage Cited in: Oncol Lett. 2017 Jul;14(1):541-546.  [Abstract]

    To investigate the effect of SB431542 on the accumulation of TGFβ1 and MMP3 in MM cells, RPMI 8226 cells are treated with 10, 100 and 1,000 nmol/mL SB431542 for 48 h. Western blotting is performed. The results demonstrate that SB431542 significantly decreases the accumulation of TGFβ1 and MMP3 at 100 and 1,000 nmol/mL when compared with the control. Smad2, as a signaling molecule, can be initially activated by TGFβ1. Therefore, the effect of SB431542 on the expression of Smad2 and p-Smad2 in RPM

    SB-431542 purchased from MCE. Usage Cited in: Chin J Immun. 2016 (5): 615-619.

    10-1000 nM of SB431542 are co-cultured with RLE-6TN cells for 48 h. Expressions of p-Smad2 and Smad are detected by Western blot.

    SB-431542 purchased from MCE. Usage Cited in: Int Immunopharmacol. 2015 Sep;28(1):707-14.  [Abstract]

    SB431542 is used to block the TGF-β1/Smad2 pathway and the expression of PLTP, p-Smad2 and cleaved caspase-3 is analyzed. (A) RLE-6TN cells are treated with 5–500 nM SB431542 for 72 h. Expression of PLTP and p-Smad2 is analyzed by Western blot. (B) CSE-treated rat lung epithelial cells are treated with 500 nM SB431542 to block the TGF-β1/Smad2 pathway.

    查看 TGF-β Receptor 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

    SB-431542 is a TGF-β receptor kinase inhibitor (TRKI). SB-431542 has inhibitory activity for ALK4, ALK5 and ALK7 with IC50 values of 1 μM, 0.75 μM and 2 μM, respectively. SB-431542 also inhibits TGF-β-induced transcription, gene expression, apoptosis, and growth suppression. SB-431542 can be used for the research of cancer and signal transduction pathways[1][2][3].

    IC50 & Target[1]

    ALK4

    1 μM (IC50)

    ALK5

    0.75 μM (IC50)

    ALK7

    2 μM (IC50)

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    HaCaT EC50
    172 nM
    Compound: 1a, SB-431542
    Inhibition of TGFbeta receptor in human HaCaT cells assessed as Smad phosphorylation by ELISA
    Inhibition of TGFbeta receptor in human HaCaT cells assessed as Smad phosphorylation by ELISA
    		[PMID: 20919678]
    HEK-293T IC50
    0.066 μM
    Compound: SB-431542, SB
    Inhibition of TGBR2 signaling in human HEK293T cells assessed as inhibition of SMAD activation after 2 to 22 hrs by dual Luciferase Assay
    Inhibition of TGBR2 signaling in human HEK293T cells assessed as inhibition of SMAD activation after 2 to 22 hrs by dual Luciferase Assay
    		[PMID: 23130626]
    HepG2 IC50
    250 nM
    Compound: SB-431542
    Inhibition of TGFR-1 in human HepG2 cells expressing PAI-luciferase by luciferase reporter gene assay
    Inhibition of TGFR-1 in human HepG2 cells expressing PAI-luciferase by luciferase reporter gene assay
    		[PMID: 19914068]
    NCI-H1299 IC50
    0.5 μM
    Compound: 3, SB-431542
    Antimigratory activity against human H1299 cells assessed as inhibition of cell migration after 12 to 24 hrs by transwell migration assay
    Antimigratory activity against human H1299 cells assessed as inhibition of cell migration after 12 to 24 hrs by transwell migration assay
    		[PMID: 24417479]
    Sf9 IC50
    67.1 nM
    Compound: SB-431542
    Inhibition of recombinant human N-terminal GST-tagged TGFbeta1 receptor (80 to end residues) expressed in baculovirus infected Sf9 insect cells using casein as substrate measured after 2 hrs by ADP-Glo assay
    Inhibition of recombinant human N-terminal GST-tagged TGFbeta1 receptor (80 to end residues) expressed in baculovirus infected Sf9 insect cells using casein as substrate measured after 2 hrs by ADP-Glo assay
    		[PMID: 31408333]
    體外研究
    (In Vitro)

    SB-431542 可抑制 ALK4、ALK5 和 ALK7 的活性，IC50 值分別為 1 μM、0.75 μM 和 2 μM[1]。
    SB-431542 (0- 10 μM；24 小時(shí)) 抑制 ALK5 以及激活素 I 型受體 ALK4 和淋巴結(jié) I 型受體 ALK7，它們?cè)诩っ附Y(jié)構(gòu)域中與 ALK5 高度相關(guān)[1]。
    SB-431542 (0.1、0.5、1、5 或 10 μM；30 分鐘) 有效抑制由 TGF-β 和激活素而非 BMP4 誘導(dǎo)的 Smad 磷酸化[1]。
    SB-431542 (0-10 μM) 抑制 TGF-β 誘導(dǎo)的轉(zhuǎn)錄、基因表達(dá)、細(xì)胞凋亡和生長(zhǎng)抑制[2]。

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

    Western Blot Analysis[1]

    Cell Line: NIH 3T3 cells; HaCaT, NIH 3T3, C2C12 cells and T47D cells
    Concentration: 10 μM; 0.1, 0.5, 1, 5, or 10 μM
    Incubation Time: 24 h; 30 min
    Result: Inhibited efficiently phosphorylated Smad2.
    Inhibited the TGF-β- and activin-induced phosphorylation of Smad2 but not BMP-induced phosphorylation of Smad1.

    Apoptosis Analysis[2]

    Cell Line: A549 and HT29 cells
    Concentration: 10 μM
    Incubation Time: 24 h
    Result: Inhibited TGF-induced growth suppression and apoptosis.

    Cell Invasion Assay[2]

    Cell Line: A549 cells
    Concentration: 2, 10 μM
    Incubation Time: 21 h
    Result: Blocked TGF- induced tumor cell invasion.

    Cell Migration Assay [2]

    Cell Line: A549 cells
    Concentration: 2, 10 μM
    Incubation Time: 5 h , 30 h
    Result: Blocked TGF- induced tumor cell migration.
    體內(nèi)研究
    (In Vivo)

    SB-431542 (結(jié)膜下；0.5 和 2 mM；第 1、2、3 和 7 天) 抑制新西蘭兔青光眼濾過(guò)手術(shù)后的疤痕形成[3]。

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

    Animal Model: Rabbits (3 to 5 months, 1.8 - 2.5 kg)[3]
    Dosage: 0.5 and 2 mM
    Administration: Subconjunctival injection, on days 1, 2, 3, and 7
    Result: Showed wound healing and less severe scar formation.
    分子量

    384.39

    Formula

    C22H16N4O3
    CAS 號(hào)
    性狀

    固體

    顏色

    Off-white to yellow

    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 : ≥ 100 mg/mL (260.15 mM; 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)

    Ethanol 中的溶解度 : 11.17 mg/mL (29.06 mM; 超聲加熱助溶)

    * "≥" means soluble, but saturation unknown.

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 2.6015 mL 13.0076 mL 26.0152 mL
    5 mM 0.5203 mL 2.6015 mL 5.2030 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: ≥ 2.08 mg/mL (5.41 mM); 澄清溶液

      此方案可獲得 ≥ 2.08 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 20.8 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: ≥ 2.08 mg/mL (5.41 mM); 澄清溶液

      此方案可獲得 ≥ 2.08 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 20.8 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: 99.85%

    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
    Ethanol / DMSO 1 mM 2.6015 mL 13.0076 mL 26.0152 mL 65.0381 mL
    5 mM 0.5203 mL 2.6015 mL 5.2030 mL 13.0076 mL
    10 mM 0.2602 mL 1.3008 mL 2.6015 mL 6.5038 mL
    15 mM 0.1734 mL 0.8672 mL 1.7343 mL 4.3359 mL
    20 mM 0.1301 mL 0.6504 mL 1.3008 mL 3.2519 mL
    25 mM 0.1041 mL 0.5203 mL 1.0406 mL 2.6015 mL
    DMSO 30 mM 0.0867 mL 0.4336 mL 0.8672 mL 2.1679 mL
    40 mM 0.0650 mL 0.3252 mL 0.6504 mL 1.6260 mL
    50 mM 0.0520 mL 0.2602 mL 0.5203 mL 1.3008 mL
    60 mM 0.0434 mL 0.2168 mL 0.4336 mL 1.0840 mL
    80 mM 0.0325 mL 0.1626 mL 0.3252 mL 0.8130 mL
    100 mM 0.0260 mL 0.1301 mL 0.2602 mL 0.6504 mL
    Help & FAQs
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    Inquiry Information

    產(chǎn)品名稱(chēng)：
    SB-431542
    目錄號(hào)：
    HY-10431
    需求量：