S5696

SKI II

≥98% (HPLC), solid

• 동의어(들): 4-[[4-(4-Chlorophenyl)-2-thiazolyl]amino]phenol
• 실험식(Hill 표기법): C₁₅H₁₁ClN₂OS
• CAS Number: 312636-16-1
• Molecular Weight: 302.78
• MDL number: MFCD00733553
• UNSPSC 코드: 12352200
• PubChem Substance ID: 24724614
• NACRES: NA.77

속성

• Quality Level: 100
• 분석: ≥98% (HPLC)
• 양식: solid
• 저장 조건: protect from light
• 색상: off-white
• solubility: DMSO: ≥20 mg/mL
• 저장 온도: 2-8°C
• SMILES string: Oc1ccc(Nc2nc(cs2)-c3ccc(Cl)cc3)cc1
• InChI: 1S/C15H11ClN2OS/c16-11-3-1-10(2-4-11)14-9-20-15(18-14)17-12-5-7-13(19)8-6-12/h1-9,19H,(H,17,18)
• InChI key: ZFGXZJKLOFCECI-UHFFFAOYSA-N

설명

애플리케이션

Human cisplatin-resistant gastric cancer cell line was treated with SKI-II to study the mechanism of reversion of multidrug resistance.¹

SKI II has been used to study the regulatory mechanism and signaling pathway induced by SKI II in inhibiting tumor growth.

생화학적/생리학적 작용

SKI II is a selective non-lipid sphingosine kinase (SK) inhibitor. IC₅₀ = 0.5 μM; does not act at ATP-binding site. Displays no inhibition of ERK2, PI 3-kinase, or PKCα at concentrations up to 60 μM. Induces apoptosis and inhibits proliferation in several other tumor cell lines in vitro (IC₅₀ = 0.9-4.6 μM).

Sphingosine kinase (SK) plays a pivotal role in regulating tumor growth and SK can act as an oncogene. Expression of SK RNA is significantly elevated in a variety of solid tumors, compared with normal tissue from the same patient. A number of novel inhibitors of human SK were identified, and several representative compounds were characterized in detail. These compounds demonstrated activity at sub- to micromolar concentrations, making them more potent than any other reported SK inhibitor, and were selective toward SK compared with a panel of human lipid and protein kinases. Kinetic studies revealed that the compounds were not competitive inhibitors of the ATP-binding site of SK. 4-[4-(4-chloro-phenyl)-thiazol-2-ylamino]-phenol (SKI-II) inhibitor is orally bioavailable, detected in the blood for at least 8 h, and showed a significant inhibition of tumor growth in mice with IC₅₀ = 0.5 μM; SKI II does not act at ATP-binding site. Displays no inhibition of ERK2, PI 3-kinase, or PKCa at concentrations up to 60 μM.SKI II induces apoptosis and inhibits proliferation in several other tumor cell lines in vitro (IC₅₀ = 0.9-4.6 μM).

특징 및 장점

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기타 정보

Product is air and light sensitive

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable
• 개인 보호 장비: Eyeshields, Gloves, type N95 (US)