TA-02 是 SB 203580 (HY-10256) 的一个类似物，是p38 MAPK的抑制剂，其IC50值为 20 nM。TA-02 可抑制 TGFBR-2。TA-02 和 SB 203580、SB 202190 (HY-10295) 具有相似的心源活性。
| 生物活性 | TA-02, an analog of SB 203580 (HY-10256), is ap38 MAPKinhibitor with anIC50of 20 nM. TA-02 especially inhibits TGFBR-2. TA-02 exhibits similar cardiogenic properties as SB 203580 and SB 202190 (HY-10295)[1]. |
体外研究
(In Vitro) | 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 oexpression 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: | The nerve cell line AGE1.HN. | | Concentration: | 5 nM-5 μM. | | Incubation Time: | 44 h (100 ng/ml LPS for 4 h at 37℃). | | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 25 mg/mL(75.00 mM;Need ultrasonic) 配制储备液 | 1 mM | 3.0000 mL | 15.0002 mL | 30.0003 mL | | 5 mM | 0.6000 mL | 3.0000 mL | 6.0001 mL | | 10 mM | 0.3000 mL | 1.5000 mL | 3.0000 mL |
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