SB505124

目錄號(hào)：S2186 Purity: 99.99%

SB505124是一種選擇性TGFβR抑制劑，作用于ALK4和ALK5，無細(xì)胞試驗(yàn)中IC50分別為129 nM和47 nM，也抑制ALK7，但不抑制ALK1，2，3或6。

SB505124 Chemical Structure

CAS: 694433-59-5

規(guī)格	價(jià)格	庫存
10mM (1mL in DMSO)	1815.87	現(xiàn)貨
10mg	1375.11	現(xiàn)貨
50mg	4662.01	現(xiàn)貨
1g	24488.1	現(xiàn)貨
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產(chǎn)品質(zhì)控

批次：純度： 99.99%

99.99

SB505124相關(guān)產(chǎn)品

相關(guān)靶點(diǎn)	ALK1 ALK2 ALK3 ALK4 TGFβRI/ALK5 ALK6 TGFβRII TGF-β Smad3 Smad4 Smad5 ALK7	點(diǎn)擊展開
相關(guān)產(chǎn)品	SB431542 LDN-193189 Galunisertib (LY2157299) LY2109761 SB525334 LDN-193189 2HCl SIS3 HCl RepSox (E-616452) LY364947 DMH1 GW788388 A-83-01 SD-208 K02288 Vactosertib (TEW-7197) SIS3 Kartogenin ITD-1 LDN-212854 LY 3200882 ML347 TP0427736 HCl SRI-011381 (C381) LDN-214117 Hesperetin Alantolactone TGFβRI-IN-3 Anti-human/mouse TGF-β-InVivo Phospho-Smad2 (S250) Rabbit Recombinant mAb	點(diǎn)擊展開
相關(guān)化合物庫	激酶抑制劑庫 PI3K/Akt 抑制劑庫 MAPK抑制劑庫細(xì)胞周期化合物庫 TGF-beta/Smad信號(hào)通路庫	點(diǎn)擊展開

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類型	給藥濃度	孵育時(shí)間	活性描述	文獻(xiàn)信息
NMuMG	Function assay	0.1 to 0.5 uM	1 hr	Inhibition of ALK5 activity in mouse NMuMG cells assessed as TGFbeta-induced phosphorylation of Smad2 at 0.1 to 0.5 uM after 1 hr by Western blot analysis	23047226
HaCaT	Function assay		24 hrs	Inhibition of ALK5 in human HaCaT cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay, IC50=0.0438μM	24786585
4T1	Function assay		24 hrs	Inhibition of ALK5 in mouse 4T1 cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay, IC50=0.0766μM	24786585
Sf9	Function assay			Inhibition of GST-fused recombinant human ALK5 expressed in baculovirus-infected insect Sf9 cells using casein as substrate by radioisotope-based assay, IC50=0.054μM	24704197
Sf9	Function assay			Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 cells, IC50=0.054μM	21435890
Sf9	Function assay			Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 insect cells using casein as substrate by proprietary radioisotopic protein kinase assay, IC50=0.0349μM	26483198
Sf9	Function assay			Inhibition of human recombinant ALK5 expressed in insect Sf9 cells using casein as substrate by radioisotopic assay, IC50=0.054μM	24786585
Sf9	Function assay			Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 cells using casein as a substrate by radioisotopic protein kinase assay, IC50=0.0544μM	23047226
Sf9	Function assay			Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 cells, IC50=0.169μM	20472445
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells	29435139
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	29435139
fibroblast cells	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells	29435139
點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

SB505124是一種選擇性TGFβR抑制劑，作用于ALK4和ALK5，無細(xì)胞試驗(yàn)中IC50分別為129 nM和47 nM，也抑制ALK7，但不抑制ALK1，2，3或6。

靶點(diǎn)

ALK5 ^[1] (Cell-free assay)	ALK4 ^[1] (Cell-free assay)
47 nM	129 nM

體外研究(In Vitro)
體外研究活性	SB-505124抑制緊密相關(guān)的ALK4,IC50為129 nM，選擇性比作用于 ALK5低2.5倍。SB-505124濃度高達(dá)10 μM時(shí)也不抑制ALK2。SB-505124 作用于COS-1細(xì)胞，也抑制內(nèi)源性Smad2磷酸化。加入SB-505124不影響組成型活性 ALK1, ALK2, ALK3, 和 ALK6 磷酸化的Smad1。ALK4和ALK5 激活Smad1和Smad2，加入SB-505124抑制激活。SB-505124作用于HepG2人類肝癌細(xì)胞，C2C12小鼠成肌細(xì)胞和Mv1Lu水貂肺細(xì)胞，抑制TGF-β誘導(dǎo)的Smad2磷酸化，這種作用存在濃度依賴性。1 μM SB-505124也抑制活化素誘導(dǎo)的Smad2磷酸化。SB-505124有效抑制TGF-β和活化素誘導(dǎo)CAGA12-熒光素酶和ARE-熒光素酶受體結(jié)構(gòu)的活力，這種作用存在濃度依賴性。^[1] SB-505124可清除TGF-β1對(duì)E-鈣粘蛋白啟動(dòng)子, mRNA和蛋白表達(dá)的抑制。^[2] SB-505124 損害Smad2磷酸化和 CTGF與α-SMA的表達(dá)。 ^[3]
激酶實(shí)驗(yàn)	體外蛋白激酶實(shí)驗(yàn)
激酶實(shí)驗(yàn)	65 nM GST-ALK5和 184 nM GST-Smad3 在50 mM HEPES, 5 mM MgCl₂, 1 mM CaCl₂, 1 mM 二硫蘇糖醇, 和 3 μM ATP，在有或無SB-505124存在時(shí)進(jìn)行激酶實(shí)驗(yàn)。反應(yīng)和 0.5 μCi [³³P]γATP在30^oC下溫育3小時(shí)。在 P-81 紙上收集磷酸化的蛋白, 使用0.5% 磷酸沖洗,然后在液體閃爍計(jì)數(shù)板上測(cè)量。另外, Smad3或Smad1蛋白覆蓋到 FlashPlate Sterile Basic 微板上。然后在FlashPlates上，在相同實(shí)驗(yàn)環(huán)境下，使用ALK5激酶域， Smad3作為底物，或者ALK6(BMP 受體)激酶域，Smad1作為底物進(jìn)行激酶實(shí)驗(yàn)。使用磷酸緩沖液沖洗實(shí)驗(yàn)板三次，然后在TopCount上計(jì)數(shù)。
細(xì)胞實(shí)驗(yàn)	細(xì)胞系	COS-1和HepG2細(xì)胞
	濃度	0.01-5 μM
	孵育時(shí)間	30分鐘
	方法	使用修正的四唑鹽WST-1測(cè)定細(xì)胞(如COS-1, HepG2 細(xì)胞系)活力。2×10³個(gè)細(xì)胞接種在96孔板上，過夜。板中為無酚紅培養(yǎng)基。用50 μL SB-505124 (獲得指定終濃度) 處理細(xì)胞30分鐘，然后使用TGF-β1和TNF-α處理，終體積為200 μL。每孔加入10 μL WST-1，在 37^oC下溫育3小時(shí)，然后在指定時(shí)間點(diǎn)測(cè)定細(xì)胞生長(zhǎng)。使用酶聯(lián)免疫吸附試驗(yàn)酶標(biāo)儀直接測(cè)量代謝活躍的細(xì)胞裂解WST-1為水溶性的甲臜。每孔中的細(xì)胞系重復(fù)處理三次。
實(shí)驗(yàn)圖片	檢測(cè)方法	檢測(cè)指標(biāo)	實(shí)驗(yàn)圖片	PMID
實(shí)驗(yàn)圖片	Western blot	p-SMAD2 / SMAD2 / Cleaved PARP / ZEB1 / Snail		30401983

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	SB-505124處理青光眼濾過手術(shù)中的濾過泡，持續(xù)10天以上，沒有任何嚴(yán)重的術(shù)后并發(fā)癥，并清楚地觀察到濾泡。第一周眼內(nèi)壓 (IOP)低于10 mmHg，然而 SB-505124處理一周后，眼內(nèi)壓漲到10 mmHg。^[4]
動(dòng)物實(shí)驗(yàn)	Animal Models	雄性Sprague-Dawley大鼠，體重300 g
	Dosages	1 μM
	Administration	外用

參考文獻(xiàn)
[1] DaCosta Byfield S, et al. Mol Pharmacol. 2004, 65(3), 744-752. [2] Hu T, et al. Am J Physiol Renal Physiol. 2005, 289(4), F816-825. [3] Misumi S, et al. Eur J Neurosci. 2008, 28(6), 1049-1059. [4] Goto N, et al. Cancer Sci. 2011, 102(8), 1501-1508. [5] Sapitro J, et al. Mol Vis. 2010 ,16, 1880-1892. [6] Chiasson VL, et al. Kidney Int. 2012 Apr 11. doi: 10.1038/ki.2012.104. + 展開

參考文獻(xiàn)

[1] DaCosta Byfield S, et al. Mol Pharmacol. 2004, 65(3), 744-752.
[2] Hu T, et al. Am J Physiol Renal Physiol. 2005, 289(4), F816-825.
[3] Misumi S, et al. Eur J Neurosci. 2008, 28(6), 1049-1059.

[4] Goto N, et al. Cancer Sci. 2011, 102(8), 1501-1508.
[5] Sapitro J, et al. Mol Vis. 2010 ,16, 1880-1892.
[6] Chiasson VL, et al. Kidney Int. 2012 Apr 11. doi: 10.1038/ki.2012.104.

+ 展開

化學(xué)信息&溶解度

分子量	335.4	分子式	C₂₀H₂₁N₃O₂
CAS號(hào)	694433-59-5	SDF	Download SB505124 SDF
Smiles	CC1=NC(=CC=C1)C2=C(N=C(N2)C(C)(C)C)C3=CC4=C(C=C3)OCO4
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1個(gè)月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 67 mg/mL ( (199.76 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Ethanol : 67 mg/mL (199.76 mM)

Water : Insoluble

DMSO : 67 mg/mL ( (199.76 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Ethanol : 67 mg/mL (199.76 mM)

Water : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑

動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計(jì)算器分子量計(jì)算器

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動(dòng)物的藥量）

給藥劑量 mg/kg 動(dòng)物平均體重 g 每只動(dòng)物給藥體積 μL 動(dòng)物數(shù)量只

第二步：請(qǐng)輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

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