203811

Bryostatin 1

≥98% (HPLC), solid,film, antitumor agent, Calbiochem^®

• Synonym(s): Bryostatin 1, Bryo 1, PKC Activator VII, PKC Activator VI
• Empirical Formula (Hill Notation): C₄₇H₆₈O₁₇
• CAS Number: 83314-01-6
• Molecular Weight: 905.03
• MDL number: MFCD00893832
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• product name: Bryostatin 1, A macrocyclic lactone with antitumor properties.
• Quality Level: 100
• 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
• 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

Description

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

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable