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Merck

662005

U0126

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

동의어(들):

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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제품정보 (DICE 배송 시 비용 별도)

실험식(Hill 표기법):
C18H16N6S2 · 0.5C2H6O
CAS 번호:
Molecular Weight:
403.52
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze, protect from light
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제품 이름

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.

Quality Level

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

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

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).

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

Packaging

Packaged under inert gas

Preparation Note

Unstable in solution; reconstitute just prior to use.

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.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)


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저장 등급

11 - Combustible Solids

flash_point_f

Not applicable

flash_point_c

Not applicable



시험 성적서(COA)

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국제 무역 품목 번호

SKUGTIN
662005-1MGCN07790788052249
662005-5MGCN04055977261011
662005-10MGCN04055977261691
662005-20MGCN04055977261004