203811

Bryostatyna 1

≥98% (HPLC), solid,film, protein kinase C activator, Calbiochem^®

• Synonim(y): Bryo 1, aktywator PKC VII, aktywator PKC VI
• Wzór empiryczny (zapis Hilla): C₄₇H₆₈O₁₇
• Numer CAS: 83314-01-6
• Masa cząsteczkowa: 905.03
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD00893832
• Assay: ≥98% (HPLC)
• Form: film, solid
• Storage condition: OK to freeze, protect from light

Właściwości

• Nazwa produktu: Bryostatyna 1, A macrocyclic lactone with antitumor properties.
• Quality Segment: 100
• description: Merck USA index - 14, 1457
• assay: ≥98% (HPLC)
• form: film, solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: white to colorless
• solubility: DMSO: 25 mg/mL, ethanol: 25 mg/mL
• shipped in: ambient
• storage temp.: −20°C
• SMILES string: O1[C@@]2([C@H](\C(=C\C(=O)OC)\C[C@H]1CC(OC(=O)C[C@@H](CC3O[C@@](CC4O[C@H](C\C(=C/C(=O)OC)\C4)\C=C\C2(C)C)(C(C(C3)OC(=O)C)(C)C)O)O)[C@H](O)C)OC(=O)\C=C\C=C\CCC)O
• InChI: 1S/C47H68O17/c1-10-11-12-13-14-15-39(51)62-43-31(22-41(53)58-9)21-34-25-37(28(2)48)61-42(54)24-32(50)23-35-26-38(59-29(3)49)45(6,7)46(55,63-35)27-36-19-30(20-40(52)57-8)18-33(60-36)16-17-44(4,5)47(43,56)64-34/h12-17,20,22,28,32-38,43,48,50,55-56H,10-11,18-19,21,23-27H2,1-9H3/b13-12+,15-14+,17-16+,30-20+,31-22+/t28-,32-,33+,34+,35?,36?,37?,38?,43+,46+,47-/m1/s1
• InChI key: MJQUEDHRCUIRLF-BXOMOELISA-N

Opis

General description

A macrocyclic lactone that exhibits anti-tumor properties. Potently activates protein kinase C and exhibits high binding affinity (K_i = 1.35 nM). Effectively translocates protein kinase C (PKC) isozymes α, β, and ε and induces a biphasic, concentration-dependent, down-regulation of PKC δ. Reported to compete with phorbol esters in binding to PKC. Stimulates protein kinase D (PKD) activity in a biphasic, PKC-dependent manner in intact cells. Also activates Ras in Jurkat T cells and in rat2 cells.

A macrocyclic lactone with antitumor properties. Potently activates protein kinase C and exhibits a high binding affinity (K_i = 1.35 nM). Effectively translocates and down-regulates PKC isozymes α, δ, and ε. Induces a biphasic activation of PKD through a PKC-dependent pathway in intact cells. Also shown to activate Ras in Jurkat T cells and in rat2 cells.

Biochem/physiol Actions

Cell permeable: no

Primary Target
Protein kinase C

Product does not compete with ATP.

Reversible: no

Target K_i: 1.35 nM for protein kinase C

Preparation Note

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

Other Notes

Clamp, A., and Jayson, G. 2002. Anticancer Drugs13, 673.
Lorenzo, P.S., et al. 1999. Cancer Res.59, 6137.
Wang, Q.J., et al. 1999. J. Biol. Chem.274, 37233.
Wender, P.A., et al. 1998. Proc. Natl. Acad. Sci. USA95, 6624.
Matthews, S.A., et al. 1997. J. Biol. Chem.272, 20245.
Szallasi, Z., et al. 1994. Mol. Pharmacol.46, 840.
Berkow, R.L., and Kratt, A.S. 1985. Biochem. Biophys. Res. Commun.3, 1109.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

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Informacja o środkach bezpieczeństwa

• Klasa składowania: 11 - Combustible Solids
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable