SB-431542

SKU: orb1307603

特色

描述

SB-431542 is a potent and selective inhibitor of the TGF-β type I receptor ALK5 (IC50=94 nM), with additional activity against ALK4 and ALK7. It is widely used in research to study TGF-β signaling pathways, including in vitro stem cell differentiation and investigations into fibrosis and cancer biology.

研究领域

Immunology & Inflammation, Stem Cell & Developmental Biology

图片与验证

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关键属性

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CAS 号	301836-41-9
MW	384.40
纯度	>98%
分子式	C₂₂H₁₆N₄O₃
SMILES	NC(=O)c1ccc(cc1)-c1nc(c([nH]1)-c1ccccn1)-c1ccc2OCOc2c1
靶点	Kinase
溶解性	Soluble in DMSO (up to 30 mg/ml), or in Ethanol (up to 3 mg/ml).

生物活性

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靶点 IC50	ALK4:140 nM\|ALK7:2 μM\|ALK5:94 nM
体内	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. 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.
体外	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. 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. 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.
细胞研究	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 .
动物研究	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 .

储存与操作

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储存	RT
有效期	12 months from date of receipt.
免责声明	For research use only

别名

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ALK5, ALK4, ALK7, Inhibitor, inhibit, TGFb, TGF-b/Smad, TGFbeta/Smad, TGF-beta, TGFbeta, TGFβ, TGF-β/Smad, TGF-β Receptor, Smad, SB 431542, SB431542, SB-431542, Transforming growth factor beta receptors

相似产品

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SB-431542 [orb1225384]
纯度：
>98% (HPLC)
CAS 号：
301836-41-9
MW:
384.3875
分子式：
C₂₂H₁₆N₄O₃
可选规格： 50 mg, 100 mg, 200 mg, 5 mg, 10 mg, 25 mg, 500 mg, 1 g

质量保证

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our 条款与条件和选购指南.

化合物标识

PubChem CID

4521392 ↗

关键属性

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暂无计算属性。

实验方案信息

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纯度：	>98% (HPLC)
CAS 号：	301836-41-9
MW:	384.3875
分子式：	C₂₂H₁₆N₄O₃

SB-431542

描述

研究领域

图片与验证

关键属性

生物活性

储存与操作

别名

相似产品

SB-431542 [orb1225384]

质量保证

化合物标识

关键属性

实验方案信息

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