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- 产品描述: TA-02, an analog of SB 203580 (HY-10256), is a p38 MAPK inhibitor with an IC50 of 20 nM. TA-02 especially inhibits TGFBR-2. TA-02 exhibits similar cardiogenic properties as SB 203580 and SB 202190 (HY-10295
- 靶点: p38 MAPK;Autophagy;p38MAPK; Autophagy
- 体外研究:
TA-02 (5 μM) inhibits the phosphorylation of proteins downstream of p38α MAPK such as MAPKAPK2 and HSP27 during cardiogenesis. TA-02 at 5 μM concentration induces cardiogenesis, but also increases ATF-2 phosphorylation and MEF2C õexpression in contrast to what would be expected with a mechanism dependent on p38α MAPK inhibition. TA-02 induces T/Brachyury whereas SB203580 addition increased MESP1 and T/Brachyury transcripts. TA-02 significantly induces high NKX2-5 expression when applied between days 0-8. TA-02 is found to inhibit multiple targets with similar potency to p38α MAPK, such as p38α, p38β, JNK3, JNK2, CIT, CK1ε, DMPK2, JNK1, DDR1 CK1δ, MEK5, and ERBB2. TA-02 and SB203580 reduce the nuclear TCF/LEF-1 driven transcription of luciferase similar to DKK-1.TA-02 (5 nM-5 μM) inhibits p38 and increases the anti-inflammation effects of BDNF on inflammation in vitro. Western Blot Analysis Cell Line: The nerve cell line AGE1.HN. Concentration: 5 nM-5 μM. Incubation Time: 44 h (100 ng/ml LPS for 4 h at 37°C). Result: Suppressed p-38 protein expression, reduced IL-1β, IL-6, IL-18 and TNF-α levels and inhibited iNOS and COX-2 levels in an in vitro model of SCI by BDNF overexpression, compared with the BDNF overexpression group.
- 参考文献:
1. Laco F, et al. Cardiomyocyte differentiation of pluripotent stem cells with SB203580 analogues correlates with Wnt pathway CK1 inhibition independent of p38 MAPK signaling. J Mol Cell Cardiol. 2015 Mar;80:56-70. 2. Jiedong Liang, et al. The activation of BDNF reduced inflammation in a spinal cord injury model by TrkB/p38 MAPK signaling. Exp Ther Med. 2019 Mar;17(3):1688-1696.
- 溶解性: Soluble in DMSO
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 3 ml 15 ml 30 ml 5 mM 0.6 ml 3 ml 6 ml 10 mM 0.3 ml 1.5 ml 3 ml 50 mM 0.06 ml 0.3 ml 0.6 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)