553210

Rapamycin

≥95% (HPLC), powder

• 동의어(들): Rapamycin, mTOR Inhibitor I
• 실험식(Hill 표기법): C₅₁H₇₉NO₁₃
• CAS Number: 53123-88-9
• Molecular Weight: 914.17
• MDL number: MFCD00867594
• UNSPSC 코드: 41116107
• NACRES: NA.77

속성

• Quality Level: 200
• 분석: ≥95% (HPLC)
• 양식: powder
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze
• 색상: clear
• solubility: DMSO: 200 mg/mL; ethanol: 50 mg/mL
• 배송 상태: ambient
• 저장 온도: −20°C
• InChI key: QFJCIRLUMZQUOT-UQKHEJQMSA-N

설명

일반 설명

Anti-fungal and immunosuppressant. Selectively inhibits the mammalian target of rapamycin (mTOR) and blocks the subsequent activation of p70 S6 kinase (IC₅₀ = 50 pM). Specifically inhibits mTORC1, but mTORC2 that phosphorylates Akt at Ser⁴⁷³ appears to be insensitive to rapamycin. Prevents the translational activation of IGF-II. Also prevents resting T-cells from entering the cell cycle, but does not directly arrest cell cycle progression. Shown to inhibit later signaling events, such as p110^Rb phosphorylation, p34^cdc2 kinase activation, and cyclin A synthesis. Exhibits strong binding to FK-506 binding proteins. Also reported to induce apoptosis in a murine B-cell line, to inhibit lymphokine-induced cell proliferation at the G₁ phase, and to irreversibly arrest Saccharomyces cerevisiae cells in the G₁ phase. A 5 mM (500 µg/109 µl) solution of Rapamycin (Cat. No. 553211) in DMSO and a 10 mM (1 mg/109 µl) solution of Rapamycin (Cat. No. 553212) in EtOH is also available.

Selectively inhibits the mammalian target of rapamycin (mTOR) and blocks the subsequent activation of p70 S6 kinase (IC₅₀ = 50 pM). Specifically inhibits mTORC1, but mTORC2 that phosphorylates Akt at Ser⁴⁷³ appears to be insensitive to rapamycin. Prevents the translational activation of IGF-II. Also prevents resting T-cells from entering the cell cycle, but does not directly arrest cell cycle progression. Shown to inhibit later signaling events, such as p110^Rb phosphorylation, p34^cdc2 kinase activation, and cyclin A synthesis. Exhibits strong binding to FK-506 binding proteins. Also reported to induce apoptosis in a murine B-cell line, to inhibit lymphokine-induced cell proliferation at the G₁ phase, and to irreversibly arrest Saccharomyces cerevisiae cells in the G₁ phase.

생화학적/생리학적 작용

Cell permeable: no

Primary Target
Mammalian target of rapamycin (mTOR)

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 50 pM against p70 S6 kinase

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

Chen, T., et al. 2011. Aging Cell.10, 908.
Powell, D.J., et al. 2003. Mol. cell Biol.23, 7794.
Braun, W., et al. 1995. FASEB J.9, 63.
Nielsen, F.C., et al. 1995. Nature 377, 358.
Aagaard-Tillery, K.M. and Jelinek, D.F. 1994. Cell. Immunol. 156, 493.
Gottschalk, A.R., et al. 1994. Proc. Natl. Acad. Sci. USA91, 7350.
Morice, W.G., et al. 1993. J. Biol. Chem.268, 3734.
Terada, N., et al. 1993. J. Biol. Chem.268, 12062.
Kuo, J., et al. 1992. Nature 358, 70.
Price, D.J., et al. 1992. Science257, 973.
Heitman, J., et al. 1991. Science253, 905.
Kay, J.E., et al. 1991. Immunology72, 544.
Schreiber, S.L. 1991. Science251, 283.
Bierer, B.E., et al. 1990. Proc. Natl. Acad. Sci. USA87, 9231.
Dumont, F.J., et al. 1990. J. Immunol.144, 251.

법적 정보

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

안전성 정보

• 픽토그램: GHS08
• 신호어: Warning
• 유해 및 위험 성명서: H351,H361fd
• 예방조치 성명서: P201 - P202 - P280 - P308 + P313 - P405 - P501
• Hazard Classifications: Carc. 2 - Repr. 2
• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 2