SB-431542是一种有效的TGF-β 受体激酶抑制剂 (TRKI),可抑制ALK4、ALK5和ALK7的活性,IC50 值分别为 1 μM、0.75 μM 和 2 μM。SB-431542可阻断TGFβ信号向下游的传递。SB-431542还能够抑制SMAD蛋白的磷酸化,因此还能抑制TGF-β诱导的基因转录。此外,SB-431542还可提高人iPSCs重编程效率达200倍。
Theriogenology. 2024 Mar 15;219:65-74.
FEBS Open Bio. 2024 May 1.
Acta Histochem. 2022 Aug;124(6):151931.
Fibroblast-derived exosomal miRNA-133 promotes cardiomyocyte-like differentiation
分子量 | 384.39 |
分子式 | C22H16N4O3 |
CAS号 | 301836-41-9 |
溶解性 | DMSO ≥ 50 mg/mL |
储存条件 |
粉末型式 -20°C 3年;4°C 2年 溶于溶剂 -80°C 6个月;-20°C 1个月 |
运输方式 | 冰袋运输,根据产品的不同,可能会有相应调整。 |
下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前,需考虑其在不同溶剂中的溶解度限制。
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.6015 mL | 13.0076 mL | 26.0152 mL |
5 mM | 0.5203 mL | 2.6015 mL | 5.203 mL |
10 mM | 0.2602 mL | 1.3008 mL | 2.6015 mL |
*吸湿的DMSO对产品的溶解度有显著影响,请使用新开封的DMSO;
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。
细胞系 | human DCs |
方法 | Effects of SB-431542 on murine BM-DCs and human DCs. DCs were incubated in 96-well plates (5x104 cells/200 μl/well) with SB-431542 or vehicle alone and LPS in the presence of LPS at different concentrations in triplicates, and then examined for expression of co-stimulatory molecules using FACSCalibur. After 24 h of incubation, the cells were examined for surface expression of CD86 or CD83 within the CD11c+ populations, and the supernatants were tested for cytokine production by enzyme-linked immunosorbent assay (ELISA). Following 24 h of incubation with a test drug, BM-DCs were incubated for 10 min with 5 mg/ml of fluorescein isothiocyanate (FITC)-conjugated dextran (DX) (70,000 Dalton molecular weight, Sigma) at 4˚C or 37˚C, washed extensively, and then examined for FITC signals by CD11c+ cells. After drug pretreatment, BM-DC preparations (derived from BALB/c mice) were washed 3 times and then co-cultured in 96 round-bottom well plates at 4 different cell densities (0.3-10x103 cells/well) with splenic T cells purified from C57BL/6 mice (5x104 cells/well). The magnitude of T cell proliferation was assessed by 3H-thymidine uptake on day 4. Human DC cultures derived from PBMCs were examined for surface phenotype within the CD11c+ population and cytokine production by ELISA as well as for allogeneic mixed lymphocyte reaction. |
浓度 | 0~10 μM |
处理时间 | 24 hr |
* 上述方法来自公开文献,仅供相同目的实验参考。如实验目的、材料、方法不同,请参考其他文献。
建议您制定动物给药及实验方案时,尽量参考已发表的相关实验文献(溶剂种类及配比众多,简单地溶解目的化合物,并不能解决动物给药依从性、体内生物利用度、组织分布等相关问题,未必能保证目的化合物在动物体内充分发挥生物学效用)。
体内实验的工作液,建议您现用现配,当天使用;如在配制过程中出现沉淀、析出现象,可以通过超声和(或)加热的方式助溶。
切勿一次性将产品全部溶解。
请在下面的计算器中,输入您的动物实验相关数据并点击计算,即可得到该实验的总需药量和工作液终浓度。
例如您给药剂量是10 mg/kg,平均每只动物的体重为20 g,每只动物的给药体积是100 μL,动物数量为20只,则该动物实验的总需药量为4 mg,工作液终浓度为2 mg/mL。
1:鉴于实验过程的损耗,建议您至少多配1-2只动物的量;
2:为该产品最终给药时的浓度。
动物模型 | BALB/c mice received intraperitoneal (i.p.) injections of colon-26 tumor cells |
配制 | normal saline |
剂量 | 1 μM (100μL) |
给药处理 | directly injected into peritoneal cavity |
* 上述方法来自公开文献,仅供相同目的实验参考。如实验目的、材料、方法不同,请参考其他文献。