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SB 525334

Catalog No. T1763 CAS 356559-20-1

Synonyms: SB525334

SB-525334 is a potent and selective inhibitor of the TGF-β1R and ALK5 (IC50: 14.3 nM).

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SB 525334, CAS 356559-20-1

Pack Size	Availability	Price/USD
5 mg	In stock	$ 53.00
10 mg	In stock	$ 89.00
25 mg	In stock	$ 178.00
50 mg	In stock	$ 298.00
100 mg	In stock	$ 474.00
200 mg	In stock	$ 558.00
1 mL * 10 mM (in DMSO)	In stock	$ 59.00

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Purity: 99.86%

Purity: 99%

Purity: 98.9%

Purity: 98.39%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	SB-525334 is a potent and selective inhibitor of the TGF-β1R and ALK5 (IC50: 14.3 nM).
Targets&IC50	ALK5:14.3 nM (cell free), ALK4:58.5 nM
In vitro	SB-525334 (1 μM) blocked TGF-beta1-induced phosphorylation and nuclear translocation of Smad2/3 in renal proximal tubule cells and inhibited TGF-beta1-induced increases in plasminogen activator inhibitor-1 (PAI-1) and procollagen alpha1(I) mRNA expression in A498 renal epithelial carcinoma cells [1]. The combination with SB525334 significantly augmented the cytotoxicity of gemcitabine in both parental and gemcitabine-resistant pancreatic cancer cells. SB525334 significantly increased apoptotic cell death in gemcitabine-resistant cells [2].
In vivo	Orally administered doses of 1, 3, or 10 mg/kg/day SB-525334 for 11 days produced statistically significant reductions in renal PAI-1 mRNA [1]. SB-525334 (10 mg/kg or 30 mg/kg) was orally administered at twice a day. Lungs were isolated 5, 7, 9 and 14 days after Bleomycin (BLM) treatment. BLM treatment led to significant pulmonary fibrotic changes accompanied by significant upregulation of ECM mRNA expressions, Smad2/3 nuclear translocation, CTGF expression, myofibroblast proliferation and type I collagen deposition. SB-525334 treatment attenuated the histopathological alterations in the lung, and significantly decreased the type I and III procollagen and fibronectin mRNA expression [3].
Kinase Assay	To determine the potency of the ALK5 inhibitor SB-525334 at the enzyme level, purified GST-tagged kinase domain of ALK5 was incubated with purified GST-tagged full-length Smad3 in the presence of 33P-γATP and different concentrations of SB525334. The readout is radioactively labeled Smad3. To determine the selectivity of SB-525334, purified GST-tagged kinase domain of ALK2 and ALK4 were incubated with GST-tagged full-length Smad1 and Smad3, respectively, in the presence of different concentrations of SB-525334 (n=3). IC50 value determinations were calculated with GraphPad software using a sigmoidal dose-response curve [1].
Cell Research	RPTE cells were seeded on microscope slides. The following day, the cells were starved by removal of epidermal growth factor and serum for 24 h prior to dosing. Cells were dosed with 10 ng/ml TGF- 1 or 1 M SB-525334 or a combination of both. Slides were pretreated with SB-525334 or starve media for 3 h prior to a 1-h incubation at 37°C with TGF- 1 or starve media. The cells were then fixed for 15 min in 4% ice-cold paraformaldehyde. The cells were permeabilized for 10 min in 0.3% Triton X-100/PBS at room temperature. The slides were incubated for 30 min in a blocking solution containing 0.3% bovine serum albumin, 10% FBS, 0.3% Triton X-100/PBS, and 5% milk in PBS. A 1:200 dilution of primary mouse anti-Smad2/3 antibody was applied to each slide for overnight incubation. A 1:200 dilution of anti-mouse IgG fluorescein secondary antibody was applied to each slide for 30 min at room temperature. The slides were then viewed using an argon blue 488 nM laser in a confocal microscope. Nuclear signal intensity was analyzed using 1D Image Analysis software. The relative intensity was determined by the mean intensity of the nucleus and expressed as percent control [1].
Animal Research	To identify the optimal treatment length for puromycin aminonucleoside's effect on extracellular matrix in the kidney, 18 Sprague-Dawley (SD) rats (200 –250 g) were injected with 15 mg/100 g of puromycin aminonucleoside in 0.9% saline or sham 0.9% saline only intraperitoneally. Animals were sacrificed at 24 h (n = 3+2 control), day 4 (n=3), day 8 (n = 3), day 10 (n = 3), day 15 (n = 2), and day 20 (n = 2). A 24-h urine collection and plasma sample were taken at 9:00 AM everyday. Urine and plasma chemistry were measured at GlaxoSmithKline Laboratories Animal Science using an Olympus clinical analyzer. Proteinuria was measured as a concentration (mg/deciliter) and then converted to total protein excreted over a 24-h period using urine flow (mL/24 h). The creatinine clearance was calculated by multiplying urine creatinine levels (mg/mL) by urine flow (mg/mL/100 g b.wt.) and then dividing that product by plasma creatinine (mg/mL). To determine the effect of SB-525334 on renal disease in the PAN model, SD rats were pretreated by oral gavage with 1, 3, or 10 mg/kg/day of SB-525334 once a day. The following day, PAN was injected at 15 mg/100 g to the appropriate rats. Treatment groups continued to receive SB-525334. Ten days after PAN injection the rats were sacrificed, and blood, urine, and kidneys were collected at the termination point for analysis [1].

Synonyms	SB525334
Molecular Weight	343.42
Formula	C21H21N5
CAS No.	356559-20-1

Storage

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

Solubility Information

DMSO: 34.3 mg/mL (100 mM)

1eq. HCl: 34.3 mg/mL (100 mM)

References and Literature

1. Grygielko ET, et al. Inhibition of gene markers of fibrosis with a novel inhibitor of transforming growth factor-beta type I receptor kinase in puromycin-induced nephritis. J Pharmacol Exp Ther. 2005 Jun;313(3):943-51. 2. Kim YJ, et al. Transforming growth factor beta receptor I inhibitor sensitizes drug-resistant pancreatic cancer cells to gemcitabine. Anticancer Res. 2012 Mar;32(3):799-806. 3. Higashiyama H, et al. Inhibition of activin receptor-like kinase 5 attenuates bleomycin-induced pulmonary fibrosis. Exp Mol Pathol. 2007 Aug;83(1):39-46.

Citations

1. Peng H, Shen J, Long X, et al. Local Release of TGF‐β Inhibitor Modulates Tumor‐Associated Neutrophils and Enhances Pancreatic Cancer Response to Combined Irreversible Electroporation and Immunotherapy, Local Release of TGF‐β Inhibitor Modulates Tumor‐Associated Neutrophils and Enhances Pancreatic Cancer Response to Combined Irreversible Electroporation and Immunotherapy. Advanced Science. 2022: 2105240

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library TGF-beta/Smad Compound Library Inhibitor Library Tyrosine Kinase Inhibitor Library Angiogenesis related Compound Library HIF-1 Signaling Pathway Compound Library Anti-Fibrosis Compound Library Anti-Ovarian Cancer Compound Library Anti-Lung Cancer Compound Library Cytokine Inhibitor Library

Related Products

Related compounds with same targets

R-268712 Repotrectinib LDN193189 Lorlatinib GSK1838705A GW788388 AZD-3463 ALK2-IN-2

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Keywords

SB 525334 356559-20-1 Angiogenesis Stem Cells Tyrosine Kinase/Adaptors TGF-beta/Smad ALK SB525334 inhibit Inhibitor TGF-β Receptor Transforming growth factor beta receptors SB-525334 inhibitor

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