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Merck

662005

U0126

≥98% (HPLC), solid, MEK inhibitor, Calbiochem®

別名:

U0126, 1,4-Diamino-2,3-dicyano-1,4- bis(2-aminophenylthio)butadiene, MEK Inhibitor VI, 1,4-Diamino-2,3-dicyano-1,4-bis(2-aminophenylthio)butadiene, MEK Inhibitor VI

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この商品について

実験式（ヒル表記法）:
C18H16N6S2 · 0.5C2H6O
CAS番号:
109511-58-2
分子量:
403.52
MDL number:
MFCD09971039
UNSPSC Code:
12352200
NACRES:
NA.77

主要文書

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製品名

U0126, U0126, CAS 109511-58-2, is a potent and specific inhibitor of MEK1 (IC50 = 72 nM) and MEK2 (IC50 = 58 nM). The inhibition is noncompetitive with respect to both ATP and ERK.

SMILES string

S(c2c(cccc2)N)\C(=C(\C(=C(\Sc1c(cccc1)N)/N)\C#N)/C#N)\N

InChI

1S/C18H16N6S2/c19-9-11(17(23)25-15-7-3-1-5-13(15)21)12(10-20)18(24)26-16-8-4-2-6-14(16)22/h1-8H,21-24H2/b17-11+,18-12+

InChI key

DVEXZJFMOKTQEZ-JYFOCSDGSA-N

assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

white

solubility

DMSO: 200 mg/mL

shipped in

ambient

storage temp.

−20°C

Quality Level

100

関連するカテゴリー

Biochem/physiol Actions

Cell permeable: no
Primary Target
MEK1 and MEK2
Product does not compete with ATP.
Reversible: no
Target IC50: 72 nM, 58 nm, against MEK1, and MEK2, respectively

Disclaimer

Toxicity: Standard Handling (A)

Other Notes

Choi, Y.J., et al. 2011. Biochem. Biophys. Res. Commun.416, 232.
DeSilva, D.R., et al. 1998. J. Immunol. 160, 4175.
Duncia, J.V., et al. 1998. Biorg. Med. Chem. Lett.8, 2839.
Favata, M.F., et al. 1998. J. Biol. Chem. 273, 18623.

Packaging

Packaged under inert gas

Preparation Note

Unstable in solution; reconstitute just prior to use.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

General description

A potent and specific inhibitor of MEK1 (IC50 = 72 nM) and MEK2 (IC50 = 58 nM). The inhibition is noncompetitive with respect to both ATP and ERK. Has very little effect on other kinases such as Abl, Cdk2, Cdk4, ERK, JNK, MEKK, MKK-3, MKK-4/SEK, MKK-6, PKC, and Raf. Shown to block doxazosin-induced osteoblastic differentiation. Also acts as an immunosuppressant by effectively blocking IL-2 synthesis and T cell proliferation without affecting the long-term outcomes of either T cell activation or tolerance. Noncompetitive with respect to ATP. Also available in InSolution format (Cat. No. 662009).

保管分類

11 - Combustible Solids

wgk

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable

試験成績書（COA）

製品のロット番号・バッチ番号を入力して、試験成績書（COA） を検索できます。ロット番号・バッチ番号は、製品ラベルに「Lot」または「Batch」に続いて記載されています。

以前この製品を購入いただいたことがある場合

文書ライブラリで、最近購入した製品の文書を検索できます。

文書ライブラリにアクセスする

Gil-Ran Kim et al.
Advanced science (Weinheim, Baden-Wurttemberg, Germany), 8(14), 2004973-2004973 (2021-07-27)
Regulatory T cells play a key role in immune tolerance to self-antigens, thereby preventing autoimmune diseases. However, no drugs targeting Treg cells have been approved for clinical trials yet. Here, a chimeric peptide is generated by conjugation of the cytoplasmic
Shah Md Toufiqur Rahman et al.
The Journal of biological chemistry, 295(25), 8494-8504 (2020-05-07)
The selective pressure imposed by extrinsic death signals and stressors adds to the challenge of isolating and interpreting the roles of proteins in stress-activated signaling networks. By expressing a kinase with activating mutations and a caged lysine blocking the active
Milica Bozic et al.
Nature communications, 11(1), 1943-1943 (2020-04-25)
Kidney fibrosis is a highly deleterious process and a final manifestation of chronic kidney disease. Alpha-(α)-synuclein (SNCA) is an actin-binding neuronal protein with various functions within the brain; however, its role in other tissues is unknown. Here, we describe the
Jie-Ning Li et al.
Frontiers in cell and developmental biology, 9, 671244-671244 (2021-07-23)
MicroRNAs (miRNAs) are small non-coding RNAs which post-transcriptionally suppress target mRNAs expression and/or translation to modulate pathophyological processes. Expression and function of miRNAs are fine-tuned by a conserved biogenesis machinery involves two RNase-dependent processing steps of miRNA maturation and the
Fatmah A Mansour et al.
Oncoimmunology, 9(1), 1729299-1729299 (2020-04-22)
The T-cell inhibitory molecule PD-L1 is expressed on a fraction of breast cancer cells. The distribution of PD-L1 on the different subpopulations of breast cancer cells is not well-defined. Our aim was to study the expression level of PD-L1 on
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グローバルトレードアイテム番号

カタログ番号GTIN
662005-20MGCN04055977261004
662005-5MGCN04055977261011
662005-10MGCN04055977261691
662005-1MGCN07790788052249

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