SB525334 6-[2-tert-Butyl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-4-yl]-quinoxaline
SB525334
CAS: 356559-20-1
Molecular Formula: C21H21N5
SB525334 6-[2-tert-Butyl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-4-yl]-quinoxaline - Names and Identifiers
SB525334 6-[2-tert-Butyl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-4-yl]-quinoxaline - Physico-chemical Properties
| Molecular Formula | C21H21N5 |
| Molar Mass | 343.42 |
| Density | 1.191 |
| Melting Point | 159 °C |
| Boling Point | 540.5±45.0 °C(Predicted) |
| Solubility | DMSO: ≥20mg/mL |
| Appearance | Yellow solid |
| Color | yellow |
| pKa | 10.24±0.10(Predicted) |
| Storage Condition | 2-8°C |
| 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. |
| Use | SB525334 is an effective and selective TGF β receptor I (ALK5) inhibitor. IC50 is 14.3 nM. It is 4 times less effective on ALK4 than on ALK5 and can inhibit ALK2, 3, and 6 activities. |
| In vitro study | SB-525334 had little inhibitory effect on ALK2, 3, and 6 with IC50 > 10 μm. SB-525334 acts on renal proximal tubular epithelial cells, inhibiting Smad2/3 phosphorylation and nuclear translocation induced by TGF-β1; 1μM SB-525334 acts on A498 renal epithelial cancer cells, inhibition of TGF-β1 induced increased expression of plasminogen activator inhibitor -1(PAI-1) and procollagen α1(I) mRNA. SB525334 (1 μm) acts on pulmonary artery smooth muscle cells (PASMCs) obtained from patients with inherited idiopathic pulmonary arterial hypertension (PAH) to reduce sensitivity to TGF-β1. SB-525334 had little inhibitory effect on ALK2, 3, and 6, with IC50 > 10 μm. SB-525334 acts on renal proximal tubular epithelial cells, inhibiting Smad2/3 phosphorylation and nuclear translocation induced by TGF-β1; 1μM SB-525334 acts on A498 renal epithelial cancer cells, inhibition of TGF-β1 induced increased expression of plasminogen activator inhibitor -1(PAI-1) and procollagen α1(I) mRNA. SB525334 (1 μm) acts on pulmonary artery smooth muscle cells (PASMCs) obtained from patients with inherited idiopathic pulmonary arterial hypertension (PAH) to reduce sensitivity to TGF-β1. |
| In vivo study | SB-525334 at a dose of 10mg/kg per day in a murine model of nephritis-induced renal fibrosis, the levels of PAI-1, procollagen α1(I), and procollagen α1(III) mRNA in the kidney were reduced. Furthermore, SB-525334 significantly inhibited PAN-induced proteinuria. SB525334 acts on the PAH murine model, significantly reverses pulmonary artery pressure, and inhibits right ventricular hypertrophy, and after treatment with SB525334(3 or 30mg/kg), induces pulmonary artery myogenesis with monocrotaline (used to induce PAH). SB-525334 effective inhibition of interlobar cell tumor. SB-525334 at a dose of 10 mg/kg per day in Eker mice significantly reduced the incidence, diversity, and size of uterine interlobar cell tumors. SB-525334(10 mg/kg or 30 mg/kg) in Bleomycin-induced pulmonary fibrosis model, and significantly reduce the expression of type I and III procollagen and fibronectin mRNA. SB-525334 also decreased Smad2/3 nuclear translocation and translocation, and decreased CTGF-expressing cells, myofibroblast proliferation, and type I collagen precipitation. SB-525334 at a dose of 10mg/kg per day in the rat model of nephritis-induced renal fibrosis, the levels of PAI-1, procollagen α1(I), and procollagen α1(III) mRNA in the kidney were reduced. Furthermore, SB-525334 significantly inhibited PAN-induced proteinuria. SB525334 acts on the PAH murine model, significantly reverses pulmonary artery pressure, and inhibits right ventricular hypertrophy, and after treatment with SB525334(3 or 30mg/kg), induces pulmonary artery myogenesis with monocrotaline (used to induce PAH). SB-525334 effective inhibition of interlobar cell tumor. SB-525334 at a dose of 10 mg/kg per day in Eker mice significantly reduced the incidence, diversity, and size of uterine interlobar cell tumors. SB-525334(10 mg/kg or 30 mg/kg) in Bleomycin-induced pulmonary fibrosis model, and significantly reduce the expression of type I and III procollagen and fibronectin mRNA. SB-525334 also decreased Smad2/3 nuclear translocation and translocation, and decreased CTGF-expressing cells, myofibroblast proliferation, and type I collagen precipitation. |
SB525334 6-[2-tert-Butyl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-4-yl]-quinoxaline - Risk and Safety
| Hazard Symbols | Xn - Harmful |
| Risk Codes | R22 - Harmful if swallowed R36/37/38 - Irritating to eyes, respiratory system and skin. |
| Safety Description | 26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. |
| UN IDs | UN 2811 6.1/PG 3 |
| WGK Germany | 3 |
SB525334 6-[2-tert-Butyl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-4-yl]-quinoxaline - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.912 ml | 14.559 ml | 29.119 ml |
| 5 mM | 0.582 ml | 2.912 ml | 5.824 ml |
| 10 mM | 0.291 ml | 1.456 ml | 2.912 ml |
| 5 mM | 0.058 ml | 0.291 ml | 0.582 ml |
Last Update：2024-01-02 23:10:35
SB525334 6-[2-tert-Butyl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-4-yl]-quinoxaline - Reference Information
| biological activity | SB525334 is an effective, selective TGF β receptor I (ALK5) inhibitor, IC50 is 14.3 nM, the effect on ALK4 is 4 times lower than that on ALK5, and ALK2, 3, and 6 activities can be inhibited. SB525334 is an effective, selective TGF β receptor I (ALK5) inhibitor. IC50 is 14.3 nM in cell-free test. its effect on ALK4 is 4 times lower than that on ALK5, and it has no activity on ALK2,3, and 6. |
| in vitro study | SB-525334 has little inhibitory effect on ALK2, 3, and 6, IC50 > 10 μM. SB-525334 acts on renal proximal tubule epithelial cells to inhibit TGF-β1-induced Smad2/3 phosphorylation and nuclear translocation. 1μM SB-525334 acts on A498 renal epithelial cancer cells to inhibit TGF-β1-induced increased expression of plasminogen activator inhibitor -1(PAI-1) and procollagen α1(I) mRNA. SB525334 (1 μM) acts on pulmonary artery smooth muscle cells (PASMCs) obtained from patients with inherited idiopathic pulmonary hypertension (PAH) to reduce the sensitivity to TGF-β1. SB-525334 has little inhibitory effect on ALK2, 3, and 6, IC50 > 10 μ m. SB-525334 acts on renal proximal tubule epithelial cells to inhibit TGF-β1-induced Smad2/3 phosphorylation and nuclear translocation. 1μM SB-525334 acts on A498 renal epithelial cancer cells to inhibit TGF-β1-induced increased expression of plasminogen activator inhibitor -1(PAI-1) and procollagen α1(I) mRNA. SB525334 (1 μM) acts on pulmonary artery smooth muscle cells (PASMCs) obtained from patients with inherited idiopathic pulmonary hypertension (PAH) to reduce the sensitivity to TGF-β1. |
| in vivo study | SB-525334 act on nephritis-induced renal fibrosis mouse model at a dose of 10 mg/kg per day to reduce renal PAI-1, procollagen α1(I), and procollagen α1(III) mRNA levels. Moreover, SB-525334 significantly inhibited PAN-induced proteinuria. SB525334 acted on PAH mouse model, obviously reversed pulmonary artery pressure and inhibited right ventricular hypertrophy. After treatment with SB525334(3 or 30 mg/kg), monocrotaline (used to induce PAH) was used to induce pulmonary artery myosis. SB-525334 effectively inhibit interleaf cell tumor. SB-525334 acting on Eker mice at a daily dose of 10 mg/kg significantly reduced the incidence, diversity, and size of uterine interleaf cell tumors. SB-525334(10 mg/kg or 30 mg/kg) acts on the rat model of Bleomycin-induced pulmonary fibrosis, reducing the pathological variation of lung tissue and significantly reducing the expression of type I and III procollagen and fibronectin mRNA. SB-525334 also reduces Smad2/3 nuclear translocation and translocation, and reduces CTGF-expressing cells, myofibroblast proliferation and type I collagen precipitation. SB-525334 acts on nephritis-induced renal fibrosis mouse model at a dose of 10 mg/kg per day to reduce renal PAI-1, procollagen α1(I), and procollagen α1(III) mRNA levels. Moreover, SB-525334 significantly inhibited PAN-induced proteinuria. SB525334 acted on PAH mouse model, obviously reversed pulmonary artery pressure and inhibited right ventricular hypertrophy. After treatment with SB525334(3 or 30 mg/kg), monocrotaline (used to induce PAH) was used to induce pulmonary artery myometriosis. SB-525334 effectively inhibit interleaf cell tumor. SB-525334 acting on Eker mice at a daily dose of 10 mg/kg significantly reduced the incidence, diversity, and size of uterine interleaf cell tumors. SB-525334(10 mg/kg or 30 mg/kg) acts on the rat model of Bleomycin-induced pulmonary fibrosis, reducing the pathological variation of lung tissue and significantly reducing the expression of type I and III procollagen and fibronectin mRNA. SB-525334 also reduces Smad2/3 nuclear translocation and translocation, and reduces CTGF-expressing cells, myofibroblast proliferation and type I collagen precipitation. |
| features | SB-525334 effectively selectively inhibit TGF-β1 receptor (ALK5). |
| target | TargetValue TGFβR1(ALK5) (Cell-free say) 14.3 nM |
| Target | Value |
| TGFβR1(ALK5) (Cell-free assay) | 14.3 nM |
Last Update：2024-04-09 21:31:57
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Spot supply
Product Name: SB525334 Visit Supplier Webpage Request for quotationCAS: 356559-20-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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