Tak-715
Synonym(s):N-(4-(2-Ethyl-4-(3-methylphenyl)-1,3-thiazol-5-yl)-2-pyridyl)benzamide
- CAS NO.:303162-79-0
- Empirical Formula: C24H21N3OS
- Molecular Weight: 399.51
- MDL number: MFCD17012805
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-11-19 15:53:33
What is Tak-715?
The Uses of Tak-715
TAK 715 is a p38 MAPK inhibitor for p38α and p38β but not for p38γ and p38δ.
What are the applications of Application
TAK 715 is an inhibitor of p38, Wnt/β-catenin , and CK1δ/ε
Definition
ChEBI: N-[4-[2-ethyl-4-(3-methylphenyl)-5-thiazolyl]-2-pyridinyl]benzamide is a member of benzamides.
Biological Activity
tak-715 is a selective inhibitor of p38 mapk with ic50 value of 7.1 nm [1].p38 mitogen-activated protein (map) kinases (p38 mapks) are a class of mitogen-activated protein kinases and play an important role in controlling cellular responses to cytokines and stress. four p38 mapks contain members, p38-α (mapk14), p38-β (mapk11), p38-γ (mapk12/erk6), and p38-δ (mapk13/sapk4), have been identified. abnormal expression of p38 mapks are correlated with a variety of chronic inflammatory diseases and their inhibitors are regarded as promising targets in clinical [1] [2].tak-715 is a potent p38 mapk inhibitor and has a different selectivity with the reported p38 mapk inhibitor vx-745. when tested with human monocytic thp-1 cells, administration of tak-715 exhibited inhibition on p38mapkα with ic50 value of 7.1 nm [1]. in hek293t, u2os, and f9 cells, tak-715 was used to inhibit p38 mapk activity and concluded that p38 mapk had no function in wnt/β-catenin signaling pathway [2].in adjuvant-induced rheumatoid arthritis rat model, administration of tak-715 at dose of 10 mg/kg significantly decreased lps-induced stimulated release of tnf-α (87.6%) by inhibiting p38 mapk activity [1].
storage
+4°C
References
[1]. miwatashi, s., et al., novel inhibitor of p38 map kinase as an anti-tnf-alpha drug: discovery of n-[4-[2-ethyl-4-(3-methylphenyl)-1,3-thiazol-5-yl]-2-pyridyl]benzamide (tak-715) as a potent and orally active anti-rheumatoid arthritis agent. j med chem, 2005. 48(19): p. 5966-79.
[2]. verkaar, f., et al., inhibition of wnt/beta-catenin signaling by p38 map kinase inhibitors is explained by cross-reactivity with casein kinase idelta/varepsilon. chem biol, 2011. 18(4): p. 485-94.
Properties of Tak-715
storage temp. | Sealed in dry,2-8°C |
solubility | DMSO: >15mg/mL |
form | powder |
color | faint yellow to dark yellow |
Safety information for Tak-715
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H302:Acute toxicity,oral H319:Serious eye damage/eye irritation |
Precautionary Statement Codes |
P264:Wash hands thoroughly after handling. P264:Wash skin thouroughly after handling. P270:Do not eat, drink or smoke when using this product. P280:Wear protective gloves/protective clothing/eye protection/face protection. P301+P312:IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. P337+P313:IF eye irritation persists: Get medical advice/attention. |
Computed Descriptors for Tak-715
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