| Bioactivity | 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)[1]. | ||||||||||||
| Invitro | TA-02 (5 μM) inhibits the phosphorylation of proteins downstream of p38α MAPK such asMAPKAPK2 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[1].TA-02 induces T/Brachyury whereas SB203580 addition increased MESP1 and T/Brachyury transcripts[1].TA-02 significantly induces high NKX2-5 expression when applied between days 0-8[1].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[1].TA-02 and SB203580 reduce the nuclear TCF/LEF-1 driven transcription of luciferase similar to DKK-1[1].TA-02 (5 nM-5 μM) inhibits p38 and increases the anti-inflammation effects of BDNF on inflammation in vitro[2]. Western Blot Analysis[2] Cell Line: | ||||||||||||
| Name | TA-02 | ||||||||||||
| CAS | 1784751-19-4 | ||||||||||||
| Formula | C20H13F2N3 | ||||||||||||
| Molar Mass | 333.33 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |