SB-505124 hydrochloride
(Synonyms: SB 505124 hydrochloride;SB505124 hydrochloride) 目录号 : GC10421
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SB-505124 hydrochloride是一种选择性TGF-β I型受体（ALK4、ALK5、ALK7）抑制剂，对ALK4和ALK5的IC50值分别为129nM和47nM。
Cas No.:356559-13-2
Sample solution is provided at 25 µL, 10mM.
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SB-505124 hydrochloride is a selective inhibitor of TGF-β Receptor type I receptors (ALK4, ALK5, ALK7), with IC50 values of 129nM and 47nM for ALK4, ALK5, respectively[1]. SB-505124 hydrochloride can inhibit the Wnt and TGF-β1 signaling pathways, reduce inflammatory responses, and decrease the levels of fibrosis markers (such as collagen, α-SMA and fibronectin)[2]. SB-505124 hydrochloride has been widely used to inhibit the differentiation of Th17 cells and regulate inflammation in mouse models of arthritis[3].
In vitro, SB-505124 hydrochloride treatment at 3μM for 10 days significantly inhibited the osteogenic differentiation of human bone marrow mesenchymal stem cells (hBMSCs), reduced the formation of mineralized matrix, and downregulated osteogenic-related genes[4]. Treatment with SB-505124 hydrochloride (2.5μM) for 24 hours significantly enhanced the sensitivity of doxorubicin (DTX)-resistant DU 145 cells to DTX and induced cell death[5]. Pretreatment of rabbit conjunctival submucosal fibroblasts with 10µM SB-505124 hydrochloride for 1 hour significantly reduced the level of pSmad2 induced by TGF-β2 as well as the expressions of CTGF and α-SMA[6].
In vivo, SB-505124 hydrochloride treatment via intraperitoneal injection at a dose of 10mg/kg once every 12 hours for 5 days alleviated the extent of tertiary neurodegeneration and blood-brain barrier dysfunction in the perinatal mouse model with hypoxic-ischemic brain injury, and improved sensory-motor deficits[7]. SB-505124 hydrochloride treatment for 2 weeks (5mg/kg/day; i.p.) caused the increase of erythrocytes in the peripheral blood and the normalized proportion of erythroblast cell clusters in the Lewis lung carcinoma (LLC) cell-xenograft mouse models[8].
References:
[1] Byfield S D C, Major C, Laping N J, et al. SB-505124 is a selective inhibitor of transforming growth factor-β type I receptors ALK4, ALK5, and ALK7[J]. Molecular pharmacology, 2004, 65(3): 744-752.
[2] Tang Y, Liu J, Liu L. Angiotensin-converting Enzyme 2 Suppresses Pulmonary Fibrosis Associated with Wnt and TGF-β1 Signaling Pathways[J]. Discovery medicine, 2024, 36(190): 2274-2286.
[3] Aarts J, Van Caam A, Helsen M, et al. Ab0082 Inhibition Of Tgfβ Signaling Using Sb-505124 Blocks Th17 Differentiation And Restores The Th17/Treg Balance In Vivo, But Does Not Suppress Experimental Arthritis[J]. Annals of the Rheumatic Diseases, 2020, 79: 1341.
[4] Almuraikhi N. Inhibition of TGF‐β type I receptor by SB-505124 hydrochloride down‐regulates osteoblast differentiation and mineralization of human mesenchymal stem cells[J]. Cell Biochemistry and Function, 2023, 41(5): 564-572.
[5] Li Y, Zhang B, Xiang L, et al. TGF-β causes docetaxel resistance in prostate cancer via the induction of Bcl-2 by acetylated KLF5 and protein stabilization[J]. Theranostics, 2020, 10(17): 7656.
[6] Sapitro J, Dunmire J J, Scott S E, et al. Suppression of transforming growth factor-β effects in rabbit subconjunctival fibroblasts by activin receptor-like kinase 5 inhibitor[J]. Molecular Vision, 2010, 16: 1880.
[7] Kanal H D, Levison S W. Neuroprotective effects of delayed TGF-β1 receptor antagonist administration on perinatal hypoxic-ischemic brain injury[J]. Developmental Neuroscience, 2024, 46(3): 188-200.
[8] Wang B, Wang Y, Chen H, et al. Inhibition of TGFβ improves hematopoietic stem cell niche and ameliorates cancer-related anemia[J]. Stem Cell Research & Therapy, 2021, 12(1): 65.
SB-505124 hydrochloride是一种选择性TGF-β I型受体（ALK4、ALK5、ALK7）抑制剂，对ALK4和ALK5的IC50值分别为129nM和47nM[1]。SB-505124 hydrochloride能够抑制Wnt和TGF-β1信号通路，减轻炎症反应，并降低纤维化标志物（如胶原蛋白、α-SMA和纤连蛋白）的水平[2]。SB-505124 hydrochloride已被广泛用于抑制Th17细胞分化，并在关节炎小鼠模型中调节炎症[3]。
在体外，使用3µM的SB-505124 hydrochloride处理10天，显著抑制了人骨髓间充质干细胞（hBMSCs）的成骨分化，减少了矿化基质的形成，并下调了成骨相关基因的表达[4]。使用2.5µM的SB-505124 hydrochloride处理24小时，显著增强了doxorubicin（DTX）耐药的DU 145细胞对DTX的敏感性，并诱导细胞死亡[5]。用10µM的SB-505124 hydrochloride预处理兔结膜黏膜下成纤维细胞1小时，显著降低了TGF-β2诱导的pSmad2水平以及CTGF和α-SMA的表达[6]。
在体内，在围产期缺氧缺血性脑损伤小鼠模型中，每隔12小时腹腔注射一次10mg/kg剂量的SB-505124 hydrochloride，持续5天，减轻了三级神经退行性病变和血脑屏障功能障碍的程度，并改善了感觉运动缺陷[7]。SB-505124 hydrochloride治疗2周（5mg/kg/day; i.p.）导致了Lewis lung carcinoma (LLC)细胞异种移植小鼠模型中外周血红细胞数量的增加，并使成红细胞簇的比例恢复正常化[8]。
| Cell experiment [1]: | |
Cell lines | Human bone marrow mesenchymal stem cells (hBMSCs) |
Preparation Method | Human bone marrow mesenchymal stem cells (hBMSCs) were cultured in Dulbecco's Modified Eagle Medium (DMEM), supplemented with 4500mg/l D-glucose, 4mM L-glutamine, 110mg/l 10% sodium pyruvate, 10% fetal bovine serum (FBS), 1% non-essential amino acids, and 1% penicillin-streptomycin. The incubator temperature was set at 37°C, humidity at 95%, and CO2 concentration at 5% to maintain cell growth. The cells were seeded in 96-well plates, with 300μl of culture medium added to each well, and 0.3, 3, and 30μM of SB-505124 hydrochloride were added respectively. The control group cells were added with DMSO. After 72h, cell viability was analyzed. |
Reaction Conditions | 0.3, 3, and 30μM; 72h |
Applications | SB-505124 hydrochloride treatment significantly decreased the cell viability of U87MG cells at 30μM. |
| Animal experiment [2]: | |
Animal models | C57BL/6 mice |
Preparation Method | The C57BL/6 mice were raised in a standard environment and were allowed to freely consume food and water. 2×106 LLC cells were suspended in 100μl of sterile PBS, or an equal volume of PBS solution was injected subcutaneously into the left abdomen of 8-week-old male mice. From the 7th day to the 21st day after tumor implantation, 5mg/kg doses of SB-505124 hydrochloride or DMSO were injected intraperitoneally daily. Under anesthesia, blood samples were drawn from the inferior vena cava of the mice for analysis. |
Dosage form | 5mg/kg/day for 2 weeks; i.p. |
Applications | SB-505124 hydrochloride treatment attenuated the symptoms of cancer-related anemia in the LLC cell-xenograft mouse models. |
References: | |
| Cas No. | 356559-13-2 | SDF | |
| 别名 | SB 505124 hydrochloride;SB505124 hydrochloride | ||
| 化学名 | 2-[4-(1,3-benzodioxol-5-yl)-2-tert-butyl-1H-imidazol-5-yl]-6-methylpyridine | ||
| Canonical SMILES | CC1=CC=CC(=N1)C2=C(N=C(N2)C(C)(C)C)C3=CC4=C(C=C3)OCO4.Cl | ||
| 分子式 | C20H22ClN3O2 | 分子量 | 371.86 |
| 溶解度 | ≥ 9.3 mg/mL in DMSO, ≥ 87 mg/mL in EtOH | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6892 mL | 13.4459 mL | 26.8918 mL |
| 5 mM | 537.8 μL | 2.6892 mL | 5.3784 mL |
| 10 mM | 268.9 μL | 1.3446 mL | 2.6892 mL |
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动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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