444937

MEK Inhibitor I

The MEK Inhibitor I, also referenced under CAS 297744-42-4, controls the biological activity of MEK. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• 동의어(들): MEK Inhibitor I
• 실험식(Hill 표기법): C₂₁H₁₈N₄OS
• CAS Number: 297744-42-4
• Molecular Weight: 374.46
• UNSPSC 코드: 12352200
• NACRES: NA.77

속성

• Quality Level: 100
• 분석: ≥95% (sum of two isomers, HPLC)
• 형태: solid
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; protect from light
• 색상: white
• solubility: DMSO: 10 mg/mL; methanol: 50 mg/mL
• 배송 상태: wet ice
• 저장 온도: −20°C

설명

일반 설명

A cell-permeable pyridine-containing vinylogous cyanamide compound that acts as a potent and selective inhibitor of MEK (IC₅₀ = 12 nM) with little activity towards MKK3 and MKK4 (IC₅₀ >1 µM). The inhibition is noncompetitive with respect to ERK and the compound displays significant affinity only towards ATP-bound MEK (i.e. noncompetitive with respect to ATP). Exhibits superior potency, solubility, and stability compared to U0126 (Cat. No. 662005) in aqueous solutions. Shown to protect against phorbol ester-mediated ear edema in mice (ED₅₀ of 5 mg/kg, ip.).

A cell-permeable, potent, and selective inhibitor of MEK (IC₅₀ = 12 nM) with little activity towards MKK3 and MKK4 (IC₅₀ >1 µM). The inhibition is non-competitive with respect to ERK and the compound displays significant affinity only towards ATP-bound MEK (i.e. non-competitive with respect to ATP). Exhibits superior potency, solubility, and stability compared to U0126 (Cat. No. 662005) in aqueous solutions. Shown to protect against phorbol ester-mediated ear edema in mice (ED₅₀ of 5 mg/kg, ip.).

생화학적/생리학적 작용

Cell permeable: yes

Primary Target
MEK

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 12 nM against MEK

포장

Packaged under inert gas

경고

Toxicity: Standard Handling (A)

재구성

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

기타 정보

Wityak, J., et al. 2004. Bioorg. Med. Chem. Lett.14, 1483.

법적 정보

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

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 1
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable