TA-02

SKU: orb1225911

Description

A potent p38 MAPK inhibitor with IC50 of 20 nM; inhibits the phosphorylation of proteins downstream of p38α MAPK such as MAPKAPK2 and HSP27 during cardiogenesis, and increases ATF-2 and MEF2C during cardiac differentiation.(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 expression 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.

Key Properties

• CAS Number: 1784751-19-4
• MW: 333.3341
• Purity: >98% (HPLC)
• Formula: C₂₀H₁₃F₂N₃
• SMILES: FC1=CC=C(C2=C(C3=CC=NC=C3)NC(C4=CC=CC=C4F)=N2)C=C1
• Target: p38 MAPK
• Solubility: 10 mM in DMSO

Bioactivity

• 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 expression 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.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

TA02 | TA 02

Quick Database Links

Gene Symbol

p38 MAPK