341329

Fatostatin

A cell-permeable diarylthiazole compound that prevents the cellular activation of the SREBP-1/2 precursors to the active nuclear forms by blocking SREBPs-SCAP ER to Golgi translocation.

• 동의어(들): Fatostatin, 125B11, 2-Propyl-4-(4-(p-tolyl)thiazol-2-yl)pyridine, HBr, SREBP Processing Inhibitor II
• 실험식(Hill 표기법): C₁₈H₁₈N₂S · xHBr
• CAS Number: 298197-04-3
• Molecular Weight: 294.41 (free base basis)
• UNSPSC 코드: 12352200
• NACRES: NA.77

속성

• Quality Level: 100
• 분석: ≥95% (HPLC)
• 형태: solid
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; desiccated (hygroscopic); protect from light
• 색상: pale yellow
• solubility: DMSO: 10 mg/mL
• 배송 상태: ambient
• 저장 온도: 2-8°C
• InChI: 1S/C18H18N2S.BrH/c1-3-4-16-11-15(9-10-19-16)18-20-17(12-21-18)14-7-5-13(2)6-8-14;/h5-12H,3-4H2,1-2H3;1H
• InChI key: RJCFNQZVFUMORB-UHFFFAOYSA-N

설명

일반 설명

A cell-permeable diarylthiazole compound that prevents the cellular activation of the SREBP-1/2 (Sterol Regulatory Element Binding Proteins 1/2) precursors to the active nuclear forms (>95% inhibition at 20 µM in CHO-K1 cells) by blocking SREBPs-SCAP (SREBP Cleavage-Activating Protein) ER to Golgi translocation with little effect against the transcription activity of the mature SREBPs. Binding studies employing recombinant SCAP truncation constructs reveal that Fatostatin targets SCAP between aa 448 to 767 in a reversible manner and is of no effect against SREBP-SCAP interaction. Fatostatin effectively suppresses SREBPs-dependent cellular functions in vitro, such as insulin-induced 3T3-L1 adipogenesis (complete inhibition at ≤20 µg/ml) and IGF1-dependent DU-145 proliferation (IC₅₀ = 100 nM), and exhibits in vivo efficacy in lowering blood glucose level (by 70%) and body weight (by 12%) of ob/ob mice over a 28-day treatment period (30 mg/kg daily i.p.) without affecting animal food intake or apparent adverse effects.

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 6 months at -20°C.

기타 정보

Kamisuki, S., et al. 2009. Chem. Biol.16, 882.
Choi, Y., et al. 2003. J. Biol. Chem.278, 7320.

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