SB-431542

Rating: 5
Author: Claire Huang

SKU: orb1307603

Description

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.

Research Area

Cardiovascular Research, Cell Biology, Signal Transduction, Stem Cell & Developmental Biology

Images & Validation

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Key Properties

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CAS Number	301836-41-9
MW	384.39
Purity	>99.99% (May vary between batches)
Formula	C₂₂H₁₆N₄O₃
SMILES	NC(=O)c1ccc(cc1)-c1nc(c([nH]1)-c1ccccn1)-c1ccc2OCOc2c1
Target	ALK,TGF-beta/Smad,Apoptosis
Solubility	DMSO:48.5 mg/mL (126.17 mM);10% DMSO+90% Saline:0.1 mg/mL (0.26 mM);Ethanol:3.85 mg/mL (10.02 mM)

Bioactivity

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Target IC50	ALK4:140 nM\|ALK7:2 μM\|ALK5:94 nM
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. 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. Read more...
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. 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. Read more...
Cell Research	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 . Read more...
Animal Research	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 . Read more...

Storage & Handling

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Storage	store under nitrogen,keep away from moisture,store at low temperature \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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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

Quality Guarantee

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 Terms & Conditions and Buying Guide. Contact us at support@biorbyt.com.

Compound Identifiers

PubChem CID

4521392 ↗

Key Properties

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No computed properties available.

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SB-431542 (orb1307603)

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5 stars

Applications: Cell Culture|Reactivity: Other

"It arrived quickly, with a short waiting time. It also arrived in good quality!"

- Claire Huang

Purity:	>98% (HPLC)
CAS Number:	301836-41-9
MW:	384.4
Formula:	C₂₂H₁₆N₄O₃

SB-431542

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Research Area

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Key Properties

Bioactivity

Storage & Handling

Alternative Names

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