ホーム 計算ツール
代理店ログイン

SB-431542

カタログ番号 T1726   CAS 301836-41-9
別名: SB 431542

SB-431542 is an inhibitor of ALK5/TGF-β type I Receptor (IC50=94 nM) and is selective. SB 431542 also has inhibitory activity against ALK4 and ALK7 but not other proteins. SB 431542 can be used for induced differentiation of stem cells.

TargetMolの製品は全て研究用試薬です。人体にはご使用できません。 また、個人の方への販売は行っておりません。
SB-431542, CAS 301836-41-9
パッケージサイズ 在庫状況 単価(税別) キャンペーン価格
サンプルについてお問い合わせ
5 mg 在庫あり ¥ 11,500 9,500
10 mg 在庫あり ¥ 18,500 15,000
25 mg 在庫あり ¥ 37,500 30,000
50 mg 在庫あり ¥ 68,000 54,500
100 mg 在庫あり ¥ 126,000 101,000
1 mL * 10 mM (in DMSO) 在庫あり ¥ 21,000 17,000
ご確認事項

1. 1研究室・グループあたり最大5製品までお申し込みいただけます。 同一製品は1回のみとなります。

2. 1回につき最大2製品までのお申し込みが可能です。

3. 2回目以降をご希望の際は、前回ご提供のサンプルの実験結果をオンラインでご提供いただく必要がございます。

4. 2023 年 1 月 20 日より前にサンプルをお申し込みいただいたお客様は、2023 年の無料申請枠にはカウントされませんが、以前の実験結果をご提供いただく必要があります。

Get quote
バッチを選択  
バッチの詳細情報はお問い合わせください
生物学的特性に関する説明
化学的特性
保存条件 & 溶解度情報
説明 SB-431542 is an inhibitor of ALK5/TGF-β type I Receptor (IC50=94 nM) and is selective. SB 431542 also has inhibitory activity against ALK4 and ALK7 but not other proteins. SB 431542 can be used for induced differentiation of stem cells.
ターゲット&IC50 ALK5:94 nM, ALK4:140 nM
In vitro METHODS: Human renal cell 293T, human colon cancer-derived non-tumorigenic cell FET, and human lung adenocarcinoma cell A549 were treated with SB-431542 (2-10 μM) and TGF-β1 (12.5 ng/mL) for 1 h. The expression levels of the target proteins were detected by Western Blot.
RESULTS: TGF-β1 induced the complex formation between Smad2/3 and Smad4, and SB-431542 blocked the complex formation by blocking TGF-β-induced phosphorylation and Smad2/3 activation in a dose-dependent manner. [1]
METHODS: Human glioblastoma cells D54MG were treated with SB-431542 (1-10 μM) for 24 h, and cell migration was detected by Transwell.
RESULTS: SB-431542 inhibited TGF-βRI signaling and blocked cell migration of D54MG cells in a concentration-dependent manner. [2]
METHODS: Human pluripotent stem cells hESCs were cultured in KSR medium containing SB-431542 (10 nM) and Noggin (500 ng/mL) for 11 days, and cell differentiation was detected using Immunofluorescence.
RESULTS: Neural induction was monitored by the expression of PAX6, an early marker of neuroectodermal differentiation. Combined treatment with Noggin and SB-431542 significantly increased the efficiency of neural induction to more than 80% of the total cells compared to less than 10% of PAX6+ cells when Noggin or SB-431542 were used alone. [3]
In vivo METHODS: To test the antitumor activity in vivo, SB-431542 (10 mg/kg in 20% DMSO/80% corn oil) was intraperitoneally injected three times a week for four weeks into Balb/c mice bearing mouse mammary cancer tumor 4T1.
RESULTS: SB-431542 significantly inhibited lung metastasis of 4T1 mammary tumors. [4]
METHODS: To investigate the treatment of tendon injuries, SB-431542 (10 mg/kg) was injected intraperitoneally into a C57B/6J mouse model with massive rotator cuff tears once daily for two or six weeks.
RESULTS: Inhibition of TGF-β1 signaling by SB-431542 reduced fibrosis, fat infiltration, and muscle weight loss. SB-431542 treatment reduced the number of FAPs in the injured muscle by promoting apoptosis of fibro/adipogenic progenitor cells (FAPs), which are an important cellular source of fibrosis and fat infiltration in the rotator cuff muscle. [5]
キナーゼ試験 Kinase assays were performed with 65 nM GSTALK5 and 184 nM GST-Smad3 in 50 mM HEPES, 5 mM MgCl2, 1 mM CaCl2, 1 mM dithiothreitol, and 3 M ATP. Reactions were incubated with 0.5 μCi of [33P]γATP for 3 h at 30°C. Phosphorylated protein was captured on P-81 paper, washed with 0.5% phosphoric acid, and counted by liquid scintillation. Alternatively, Smad3 or Smad1 protein was also coated onto FlashPlate Sterile Basic Microplates. Kinase assays were then performed in FlashPlates with same assay conditions using either the kinase domain of ALK5 with Smad3 as a substrate or the kinase domain of ALK6 (BMP receptor) with Smad1 as substrate. Plates were washed three times with phosphate buffer and counted by TopCount [2].
細胞研究 A498 cells were seeded at 5,000 to 10,000 cells/well in 96-well plates. The cells were serum-deprived for 24 h and then treated with compounds for 48 h to assess the cellular toxicity. Cell viability is determined by incubating cells for 4 h with XTT labeling and electron coupling reagent. Live cells with active mitochondria produce an orange-colored product, formazan, which is detected using a plate reader at between A450 nm and A500 nm with a reference wavelength greater than 600 nm. The absorbance values correlate with the number of viable cells [2].
動物実験 BALB/c mice received intraperitoneal (i.p.) injections of colon-26 tumor cells. Three days after tumor cell inoculation, SB-431542 (1 μM solution, 100 μl/animal) or vehicle alone was directly injected into the peritoneal cavity. CTL activities were measured by a standard 4 h 51Cr release assay after culturing spleen cells with γ-irradiated tumor cells for five days in the absence of added growth factors. In vitro experiments, cell lysate of HLA-A*2402 positive gastric cancer cell line, OCUM-8, was incubated with human DC cultures for 4 h. After washing extensively, PBMCs obtained from the same volunteer as DCs were incubated for 7 days and measured CTL activity by 51Cr release assay. NK activity was tested using 51Cr release assay against K562 [4].
別名 SB 431542
分子量 384.39
分子式 C22H16N4O3
CAS No. 301836-41-9

保存条件

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度情報

DMSO: 38.4 mg/mL (100 mM)

Ethanol: 3.8 mg/mL (10 mM)

参考文献

1. Halder SK, et al. A specific inhibitor of TGF-beta receptor kinase, SB-431542, as a potent antitumor agent for human cancers. Neoplasia. 2005 May;7(5):509-21. 2. Hjelmeland MD, et al. SB-431542, a small molecule transforming growth factor-beta-receptor antagonist, inhibits human glioma cell line proliferation and motility. Mol Cancer Ther. 2004 Jun;3(6):737-45. 3. Chambers SM, et al. Highly efficient neural conversion of human ES and iPS cells by dual inhibition of SMAD signaling. Nat Biotechnol. 2009 Mar;27(3):275-80. doi: 10.1038/nbt.1529. Epub 2009 Mar 1. Erratum in: Nat Biotechnol. 2009 May;27(5):485. 4. Sato M, et al. Differential Proteome Analysis Identifies TGF-β-Related Pro-Metastatic Proteins in a 4T1 Murine Breast Cancer Model. PLoS One. 2015 May 18;10(5):e0126483. 5. Davies MR, et al. TGF-β Small Molecule Inhibitor SB431542 Reduces Rotator Cuff Muscle Fibrosis and Fatty Infiltration By Promoting Fibro/Adipogenic Progenitor Apoptosis. PLoS One. 2016 May 17;11(5):e0155486. 6. Ma J, et al. Growth differentiation factor 11 improves neurobehavioral recovery and stimulates angiogenesis in rats subjected to cerebral ischemia/reperfusion. Brain Res Bull. 2018 Feb 9;139:38-47. 7. Duan F, Huang R, Zhang F, et al. Biphasic modulation of insulin signaling enables highly efficient hematopoietic differentiation from human pluripotent stem cells[J]. Stem cell research & therapy. 2018 Jul 27;9(1):205. 8. Xiong, Yanlu, et al. TFAP2A potentiates lung adenocarcinoma metastasis by a novel miR-16 family/TFAP2A/PSG9/TGF-β signaling pathway. . Cell Death & Disease . 12.4 (2021): 1-13. 9. Chen F, Gao Q, Wei A, et al. Histone deacetylase 3 aberration inhibits Klotho transcription and promotes renal fibrosis[J]. Cell Death & Differentiation. 2020: 1-12.

引用文献

1. Chen X, Wang P, Qiu H, et al. Integrative epigenomic and transcriptomic analysis reveals the requirement of JUNB for hematopoietic fate induction. Nature Communications. 2022, 13(1): 1-16 2. Duan F, Huang R, Zhang F, et al. Biphasic modulation of insulin signaling enables highly efficient hematopoietic differentiation from human pluripotent stem cells. Stem Cell Research & Therapy. 2018 Jul 27;9(1):205 3. Bao, Shixiang, et al. TGF-β1 Induces Immune Escape by Enhancing PD-1 and CTLA-4 Expression on T Lymphocytes in Hepatocellular Carcinoma. Frontiers in Oncology. 11 (2021): 2516. 4. Bao, Shixiang, et al. TGF-β1 Induces Immune Escape by Enhancing PD-1 and CTLA-4 Expression on T Lymphocytes in Hepatocellular Carcinoma. Frontiers in Oncology. 11 (2021): 2516. 5. Bao, Shixiang, et al. TGF-β1 Induces Immune Escape by Enhancing PD-1 and CTLA-4 Expression on T Lymphocytes in Hepatocellular Carcinoma. Frontiers in Oncology. 11 (2021): 2516. 6. Fu J, Jiang L, Yu B, et al. Generation of a Human iPSC Line CIBi010-A with a Reporter for ASGR1 Using CRISPR/Cas9. Stem Cell Research. 2022: 102800 7. Liu S, Yan X, Guo J, et al.Periodontal ligament‐associated protein‐1 knockout mice regulate the differentiation of osteoclasts and osteoblasts through TGF‐β1/Smad signaling pathway.Journal of Cellular Physiology.2023 8. Ying J, Wang P, Jin X, et al.TGF-β1 Mediates the EndoMt in High Glucose-Treated Human Retinal Microvascular Endothelial Cells.Seminars in Ophthalmology. Taylor & Francis.2024: 1-8.

関連化合物ライブラリー

この製品は下記化合物ライブラリに含まれています:
Tyrosine Kinase Inhibitor Library Highly Selective Inhibitor Library Inhibitor Library Anti-Cancer Active Compound Library TGF-beta/Smad Compound Library Kinase Inhibitor Library Anti-Pancreatic Cancer Compound Library Anti-Breast Cancer Compound Library Angiogenesis related Compound Library Bioactive Compounds Library Max

関連製品

同一標的の関連化合物
LDN-212854 Alectinib GSK1838705A Belizatinib AZD-3463 ASP3026 Entrectinib ZX-29

投与量変換

You can also refer to dose conversion for different animals. 詳細

In vivo投与量計算 (透明溶液)

ステップ1: 以下の情報を入力してください
投与量
mg/kg
動物の平均体重
g
動物あたりの投与量
ul
動物数
溶媒の組成を入力してください
% DMSO
%
% Tween 80
% ddH2O
計算する リセット

計算器

モル濃度計算機
希釈計算機
再構成計算
分子量計算機
=
X
X

モル度計算機では以下の計算が可能です

  • 既知の体積と濃度の溶液を調製するために必要な化合物の質量
  • 質量が既知の化合物を目的の濃度まで溶解させるのに必要な溶液の量
  • 特定の体積の中に既知の質量の化合物を入れて得られる溶液の濃度
参考例

モル濃度計算機を使用したモル濃度計算の例
化合物の分子量が197.13g/molである場合、10mlの水に10mMのストック溶液を作るのに必要な化合物の質量はどれくらいですか?
[分子量(MW)]の欄に[197.13]と入力してください
[濃度]ボックスに10と入力し、正しい単位(millimolar)を選択します
[容量]ボックスに10と入力し、正しい単位(milliliter)を選択します
計算を押します
答えの19.713mgが質量欄に表示されます

X
=
X

溶液を作るのに必要な希釈率の計算

溶液の調製に必要な希釈率の算出
希釈計算機は、既知の濃度の原液をどのように希釈するかを計算することができる便利なツールです。V1を計算するためにC1、C2&V2を入力します。

参考例

Tocrisの希釈計算器を用いた希釈計算の一例
50μMの溶液を20ml作るためには、10mMの原液を何ml必要ですか?
C1V1=C2V2という式を用いて、C1=10mM、C2=50μM、V2=20ml、V1を未知数とします。
濃度(開始)ボックスに10を入力し正しい単位(millimolar)を選択してください
濃度(終了)ボックスに50を入力し正しい単位(millimolar)を選択してください
体積(終了)ボックスに20を入力し正しい単位(millimolar)を選択してください
計算を押します
100 microliter (0.1 ml) という答えが体積(開始)ボックスに表示されます。

=
/

バイアルを再構成するのに必要な溶媒の量を計算する.

再構成計算機を使えば、バイアルを再構成するための試薬の量をすぐに計算することができます.
試薬の質量と目標濃度を入力するだけで計算します。

g/mol

化合物の化学式を入力して、そのモル質量や元素組成を計算します

Tヒント:化学式は大文字と小文字を区別します。: C10H16N2O2 c10h16n2o2

化合物のモル質量(分子量)を計算する手順:
化学物質のモル質量を計算するには、その化学式を入力し、「計算」をクリックしてください。.
分子質量、分子量、モル質量、モル重量の定義:
分子質量(分子量)とは、物質の1分子の質量であり、統一された原子質量単位(u)で表されます。(1uは炭素12の1原子の質量の1/12に等しい)
モル質量(molar weight)とは、ある物質の1モルの質量のことで、単位はg/molです。

bottom

技術サポート

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

SB-431542 301836-41-9 Angiogenesis Stem Cells Tyrosine Kinase/Adaptors TGF-beta/Smad ALK Transforming growth factor beta receptors inhibit SB 431542 TGF-β Receptor SB431542 Inhibitor inhibitor