SB-505124 hydrochloride
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
SB505124 是一种选择性TGFβR抑制剂，作用于ALK4和ALK5，IC50 值分别为129 nM和47 nM [ 1 ]。
间变性淋巴瘤激酶(ALK)与脑的发育有关，并影响神经系统中特定的神经元。
SB505124 是一种可逆的ATP 竞争性ALK4 和ALK5 抑制剂。用高浓度的SB505124与ALK5孵育，随后稀释至亚IC50 浓度，对下游的Smad3 磷酸化无影响[ 2 ]。浓度高至100 μM 的SB505124在48 小时处理后对肾上皮A498 细胞无毒性。证据显示100% 药品在12 h 之内释放，对体外培养兔结膜细胞未显示出细胞毒性[ 2 ] 。观察发现，在培养的成纤维细胞中，SB505124抑制包括pSmad2、CTGF以及α-SMA在内的ALK4下游效应器 [ 3 ]。
在青光眼滤过手术(GFS)兔模型中，TGF β诱导的纤维细胞减少了滤过泡周期。使用SB505124 组的GFS 中，滤过泡保持超过10 天，滤过泡存活周期相比对照组显著地延长，这表明SB505124 对ALK4 和5显著的抑制作用[ 2 ]。观察发现，ALK4 下游效应器CTGF 和α-SMA 也被SB-505124 抑制[ 3 ]。
参考文献：
[1].DaCosta B S et al. SB-505124 is a selective inhibitor of transforming growth factor-beta type I receptors ALK4, ALK5, and ALK7. Mol Pharmacol., 2004,65(3): 744-52.
[2].Sutariya V, et al. Thermoreversible gel for delivery of activin receptor-like kinase 5 inhibitor SB-505124 for glaucoma filtration surgery. Pharm Dev Technol., 2013, 18(4): 957-962.
[3].Sapitro J, et al. Suppression of transforming growth factor-β effects in rabbit subconjunctival fibroblasts by activin receptor-like kinase 5 inhibitor. Mol Vis., 2010, 16: 1880-1892.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 371.86 |
| Cas No. | 356559-13-2 |
| Formula | C20H22ClN3O2 |
| Synonyms | SB 505124 hydrochloride;SB505124 hydrochloride |
| Solubility | insoluble in H2O; ≥87 mg/mL in EtOH; ≥9.3 mg/mL in DMSO |
| Chemical Name | 2-[4-(1,3-benzodioxol-5-yl)-2-tert-butyl-1H-imidazol-5-yl]-6-methylpyridine |
| SDF | Download SDF |
| Canonical SMILES | CC1=CC=CC(=N1)C2=C(N=C(N2)C(C)(C)C)C3=CC4=C(C=C3)OCO4.Cl |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 描述 | SB-505124 盐酸盐是一种活化素受体样激酶(ALKs)抑制剂。 | |||||
| 靶点 | ALK-5 | ALK-4 | ALK-7 | |||
| IC50 | ||||||
化学结构
