- SB 525334
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- $32.00
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2026-07-27
- CAS:356559-20-1
- Purity: 99.77%
- Supply Ability: 10g
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| | 6-[2-tert-Butyl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-4-yl]-quinoxaline Chemical Properties |
| Melting point | 159 °C | | Boiling point | 540.5±45.0 °C(Predicted) | | density | 1.191 | | storage temp. | 2-8°C | | solubility | DMSO: ≥20mg/mL | | form | Yellow solid | | pka | 10.24±0.10(Predicted) | | color | yellow | | Stability: | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. | | InChI | InChI=1S/C21H21N5/c1-13-6-5-7-16(24-13)19-18(25-20(26-19)21(2,3)4)14-8-9-15-17(12-14)23-11-10-22-15/h5-12H,1-4H3,(H,25,26) | | InChIKey | DKPQHFZUICCZHF-UHFFFAOYSA-N | | SMILES | N1C2C(=CC(C3=C(C4=NC(C)=CC=C4)NC(C(C)(C)C)=N3)=CC=2)N=CC=1 |
| Hazard Codes | Xn | | Risk Statements | 22-36/37/38 | | Safety Statements | 26 | | RIDADR | UN 2811 6.1/PG 3 | | WGK Germany | 3 | | HS Code | 2933.39.6190 | | Storage Class | 11 - Combustible Solids |
| | 6-[2-tert-Butyl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-4-yl]-quinoxaline Usage And Synthesis |
| Biological activity | SB525334 is a potent and selective inhibitor of TGFβ receptor I (ALK5) with IC50 of 14.3 nM in a cell-free assay, 4-fold less potent to ALK4 than ALK5 and inactive to ALK2, 3, and 6. | | In vitro | SB 525334 shows no inhibition in the enzymes ALK2, 3, and 6, with IC50 values > 10 μM. SB 525334 blocks phosphorylation induced by TGF-β1 and nuclear translocation of Smad2/3 in renal proximal tubule cells. SB 525334 also inhibits the increased mRNA expression levels of plasminogen activator inhibitor-1 (PAI-1) and procollagen α1(I) induced by TGF-β1 in A498 renal epithelial carcinoma cells at 1 μM). SB 525334 (1 μM) attenuates the heightened sensitivity to TGF-β1 exhibited by pulmonary artery smooth muscle cells (PASMCs) from patients with familial forms of idiopathic pulmonary arterial hypertension (PAH). | | In vivo | SB 525334 (10 mg/kg/day) decreases the renal mRNA levels of PAI-1, procollagen α1(I), and procollagen α1(III) in a nephritis-induced renal fibrosis rat model. Furthermore, PAN-induced proteinuria is significantly inhibited by SB 525334 (10 mg/kg/day). SB 525334 may also be efficacious in mesenchymal tumors. SB 525334 (10 mg/kg/day) significantly decreases uterine mesenchymal tumor incidence, multiplicity, and size in Eker rats. SB 525334 significantly reverses pulmonary arterial pressure and inhibits right ventricular hypertrophy in a rat model of PAH. This is revealed by a significant reduction in pulmonary arteriole muscularization induced by monocrotaline (used to induce PAH) after treatment with SB 525334 (3 or 30 mg/kg). In a Bleomycin-induced pulmonary fibrosis mice model, SB 525334 (10 mg/kg or 30 mg/kg) attenuates the histopathological alterations in the lung, and significantly decreased mRNA expression of Type I and III procollagen and fibronectin. SB 525334 also attenuates Smad2/3 nuclear translocation, myofibroblast proliferation, deposition of Type I collagen, and decreases CTGF-expressing cells. | | References | http://www.selleckchem.com/products/SB-525334.html | | Description | SB-525334 is a potent inhibitor of the TGF-β receptor 1 (TGF-β R1, ALK5) kinase (IC50 = 14.36 nM). It is ~4-fold less effective against ALK4 and inactive against ALK2, ALK3, and ALK6. SB-525334 blocks TGF-β1-induced phosphorylation and nuclear translocation of SMAD2/3 as well as TGF-β1-directed gene expression. It is effective in vivo, preventing puromycin aminonucleoside-induced renal fibrosis and bleomycin-induced pulmonary fibrosis. SB-525334 also modulates carcinogenesis and suppresses the development of pulmonary arterial hypertension in animals. | | Uses | SB-525334 is a potent activin receptor-like kinase (ALK5)/ type I TGFβ-receptor kinase inhibitor with IC50 = 14.3 nM. | | Uses | SB-525334 was used to study TGFβ1-mediated human trophoblast differentiation.7 | | Definition | ChEBI: 6-[2-tert-butyl-5-(6-methyl-2-pyridinyl)-1H-imidazol-4-yl]quinoxaline is a quinoxaline derivative. | | Biological Activity | Selective inhibitor of transforming growth factor- β receptor I (ALK5, TGF- β RI) (IC 50 = 14.3 nM). Inhibits TGF- β 1-induced smad2/3 nuclear localisation and TGF- β 1-induced mRNA expression in kidney cells. Attenuates bleomycin-induced pulmonary fibrosis. | | Biochem/physiol Actions | SB-525334 is a potent activin receptor-like kinase (ALK5)/ type I TGFβ-receptor kinase inhibitor with IC50 = 14.3 nM. | | storage | Store at -20°C | | Background | The small-molecule SB-525334 inhibits transforming growth factor-β1 receptor with an IC50 of 14.3 nM. SB-525334 also inhibits the related receptor ALK4 but is inactive against ALK2, ALK3, and ALK6. Inhibition of TGF-β downstream signaling by SB-525334 blocks phosphorylation and nuclear translocation of Smad2/3 protein and reduces PAI-1 and procollagen α1(I) mRNA expression in renal epithelial carcinoma cells. SB-525334 treatment of a bleomycin-induced pulmonary fibrosis model reduced TGF-β-mediated nuclear translocation of Smad2/3, decreased myofibroblast proliferation, and attenuated pulmonary fibrosis. Exposure of mesenchymal and epithelial tumors in Eker rats to SB-525334 reduced the size and number of mesenchymal tumors but had the opposite effect on epithelial cancer cells and lesions. Inhibition of ALK5 by SB-525334 in both human pulmonary artery smooth muscle cells and a rat model of pulmonary arterial hypertension resulted in decreased sensitivity to TGF-β, and attenuated pulmonary arterial pressure and right ventricular hypertrophy. | | References | [1] EUGENE T GRYGIELKO. Inhibition of gene markers of fibrosis with a novel inhibitor of transforming growth factor-beta type I receptor kinase in puromycin-induced nephritis.[J]. Journal of Pharmacology and Experimental Therapeutics, 2005, 313 3: 943-951. DOI:10.1124/jpet.104.082099
[2] HIROYUKI HIGASHIYAMA . Inhibition of activin receptor-like kinase 5 attenuates Bleomycin-induced pulmonary fibrosis[J]. Experimental and molecular pathology, 2007, 83 1: Pages 39-46. DOI:10.1016/j.yexmp.2006.12.003
[3] YEON JEONG KIM. Transforming growth factor beta receptor I inhibitor sensitizes drug-resistant pancreatic cancer cells to gemcitabine.[J]. Anticancer research, 2012, 32 3: 799-806. |
| | 6-[2-tert-Butyl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-4-yl]-quinoxaline Preparation Products And Raw materials |
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