U-0126 CAS: 109511-58-2
MF: C18H16N6S2
MW: 380.48

U-0126 (CAS 109511-58-2)

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別名: U-0126 is known as an MEK inhibitor and AMPK activator.
アプリケーション: U-0126 is a highly selective, non-ATP competitive MAP Kinase Kinase (MKK, MEK1 and MEK2) and ERK inhibitor.
CAS 番号: 109511-58-2
Purity: ≥97%
Molecular Weight: 380.48
Molecular Formula: C18H16N6S2
試験・研究用以外には使用しないでください。 臨床及び体外診断には使用できません。
* Refer to Certificate of Analysis for lot specific data (including water content).
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U-0126 is a selective MAPK and ERK inhibitor, displaying a preference for MEK1 and MEK2. The IC50 value for MEK1 is 72nM and MEK2 is 58nM. It is known that U-0126 binds to MAPK noncompetitive manner compared to ATP. Studies suggest that U-0126 antagonizes the transcription of AP-1, via the inhibition of MEK. In addition, U-0126 has been observed to inhibit promoters containing an AP-1 response element. Conversely, U-0126 has no effect on promoters that lack an AP-1 response group. U-0126 is also useful in neuronal studies in mice since it displays inhibitory effects against oxidative stress.


参考文献

1. Duncia, J.V., et al. 1998. Bioorg. Med. Chem. Lett. 8: 2839-2844. PMID: 9873633

2. Scherle, P.A., et al. 1998. J. Immunol. 161: 5681-5686. PMID: 9820549

3. Satoh, T., et al. 2000. Neurosci. Lett. 288: 163-166. PMID: 10876086

4. Qin, L. et al. 2015. Life Sci. 131 : 37-43. PMID: 25896660

Physical State :
Solid
Solubility :
Soluble in DMSO (>10 mg/ml), 100% ethanol (2 mg/ml), water (0.3 mg/ml at 25° C), DFM:PBS pH7.2 (1:2), and DMF.
保存方法 :
Store at -20° C
Melting Point :
278.50° C (Predicted)
Boiling Point :
~565.1° C at 760 mmHg (Predicted)
Density :
~1.4 g/cm3 (Predicted)
Refractive Index :
n20D 1.76
IC50 :
MEK1: IC50 = 72 nM; MEK2: IC50 = 58 nM
試験・研究用以外には使用しないでください。 臨床及び体外診断には使用できません。
WGK Germany :
3
PubChem CID :
SMILES :
C1=CC=C(C(=C1)N)SC(=C(C#N)C(=C(N)SC2=CC=CC=C2N)C#N)N

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U-0126 (CAS 109511-58-2)  参考文献

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引用 1 to 10 of 119 合計

PMID: # 33921748  Shi, Q.|Hu, B.|Yang, C.|Zhao, L.|Wu, J.|Qi, N.| et al. 2021. Int J Mol Sci. 22:

PMID: # 33508440  Colín-Val, Z.|López-Díazguerrero, NE.|López-Marure, R.| et al. 2021. J Steroid Biochem Mol Biol. 208: 105818.

PMID: # 33708336  Deng, S.|Liu, S.|Jin, P.|Feng, S.|Tian, M.|Wei, P.|Zhu, H.|Tan, J.|Zhao, F.|Gong, Y.| et al. 2021. Oxid Med Cell Longev. 2021: 8891373.

PMID: # 34165247  Ho, HY.|Chen, PJ.|Lo, YS.|Lin, CC.|Chuang, YC.|Hsieh, MJ.|Chen, MK.| et al. 2021. Environ Toxicol.

PMID: # 34076342  Velmurugan, BK.|Lin, JT.|Mahalakshmi, B.|Lin, CC.|Chuang, YC.|Lo, YS.|Ho, HY.|Hsieh, MJ.|Chen, MK.| et al. 2021. Environ Toxicol.

PMID: # 33578238  Ho, HY.|Lin, CC.|Chuang, YC.|Lo, YS.|Hsieh, MJ.|Chen, MK.| et al. 2021. Biomed Pharmacother. 137: 111362.

PMID: # 33686181  Amine, H.|Benomar, Y.|Taouis, M.| et al. 2021. Sci Rep. 11: 5427.

PMID: # 34062746  Hsieh, YH.|Tsai, JP.|Yu, CL.|Lee, CC.|Hsu, JC.|Chen, JC.| et al. 2021. Biology (Basel). 10:

PMID: # 33168583  Paraíso-Luna, J.|Aguareles, J.|Martín, R.|Ayo-Martín, AC.|Simón-Sánchez, S.|García-Rincón, D.|Costas-Insua, C.|García-Taboada, E.|de Salas-Quiroga, A.|Díaz-Alonso, J.|Liste, I.|Sánchez-Prieto, J.|Cappello, S.|Guzmán, M.|Galve-Roperh, I.| et al. 2020. Development. 147:

PMID: # 32602013  Kaya, Y.|Kucukvardar, S.|Yildiz, A.| et al. 2020. Mol. Cell. Biochem.

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