557370

Rottlerin

≥98% (HPLC), solid, PKC inhibitor, Calbiochem^®

• Synonym(s): Rottlerin, Mallotoxin
• Empirical Formula (Hill Notation): C₃₀H₂₈O₈
• CAS Number: 82-08-6
• Molecular Weight: 516.54
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD00017361
• Assay: ≥98% (HPLC)
• Form: solid
• Storage condition: OK to freeze

Properties

• Product Name: Rottlerin, A cell-permeable and reversible protein kinase C inhibitor that exhibits greater selectivity for PKCδ (IC₅₀ = 3-6 µM) and PKCθ.
• Quality Segment: 100
• description: Merck USA index - 14, 8272
• assay: ≥98% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze
• color: orange
• solubility: ethanol: 1 mg/mL, DMSO: 30 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• SMILES string: O1C(C=Cc2c1c(c(c(c2O)Cc4c(c(c(c(c4O)C(=O)C)O)C)O)O)C(=O)\C=C\c3ccccc3)(C)C
• InChI: 1S/C30H28O8/c1-15-24(33)19(27(36)22(16(2)31)25(15)34)14-20-26(35)18-12-13-30(3,4)38-29(18)23(28(20)37)21(32)11-10-17-8-6-5-7-9-17/h5-13,33-37H,14H2,1-4H3/b11-10+
• InChI key: DEZFNHCVIZBHBI-ZHACJKMWSA-N

Description

General description

A cell-permeable and reversible inhibitor of protein kinase C δ (PKCδ, IC₅₀ = 3-6 µM) and PKC_Θ isozymes. Also inhibits PKC_α, PKC_β, and PKC_γ isoforms, but with significantly reduced potency (IC₅₀ = 30-42 µM). Has reduced inhibitory activity on PKC_ε, PKC_η, and PKC_ξ (IC₅₀ = 80-100 µM). Also known to inhibit CaM kinase III (IC₅₀ = 5.3 µM).

A cell-permeable and reversible protein kinase C inhibitor that exhibits greater selectivity for PKC_δ (IC₅₀ = 3-6 µM) and PKC_θ. Inhibits the PKC_α, PKC_β, and PKC_γ isoforms, but with significantly reduced potency (IC₅₀ = 30-42 µM). Has reduced inhibitory activity on PKC_ε, PKC_η, and PKC_ζ (IC₅₀ = 80-100 µM). Also known to inhibit CaM kinase III (IC₅₀ = 5.3 µM).

Biochem/physiol Actions

Product does not compete with ATP.

Reversible: yes

Target IC₅₀: 3-6 µM against PKCδ; 5.3 µM against CaM kinase III

Cell permeable: yes

Primary Target
PKCδ

Preparation Note

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

Other Notes

Villalba, M., et al. 1999. J. Immunol. 163, 5813.
Gschwendt, M., et al. 1994. Biochem. Biophys. Res. Commun. 199, 93.
Gschwendt, M., et al. 1994. FEBS Lett.338, 85.
Gschwendt, M., et al. 1984. Cancer Lett.25, 177.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

Safety Information

• Storage Class: 11 - Combustible Solids
• flash_point_f: Not applicable
• flash_point_c: Not applicable