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557370

Sigma-Aldrich

Rottlerin

A cell-permeable and reversible protein kinase C inhibitor that exhibits greater selectivity for PKCδ (IC₅₀ = 3-6 µM) and PKCθ.

Synonym(s):

Rottlerin, Mallotoxin

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About This Item

Empirical Formula (Hill Notation):
C30H28O8
CAS Number:
82-08-6
Molecular Weight:
516.54
MDL number:
MFCD00017361
UNSPSC Code:
12352200

Quality Level

100

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

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

General description

A cell-permeable and reversible inhibitor of protein kinase C δ (PKCδ, IC50 = 3-6 µM) and PKCΘ isozymes. Also inhibits PKCα, PKCβ, and PKCγ isoforms, but with significantly reduced potency (IC50 = 30-42 µM). Has reduced inhibitory activity on PKCε, PKCη, and PKCξ (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 PKCδ (IC50 = 3-6 µM) and PKCθ. Inhibits the PKCα, PKCβ, and PKCγ isoforms, but with significantly reduced potency (IC50 = 30-42 µM). Has reduced inhibitory activity on PKCε, PKCη, and PKCζ (IC50 = 80-100 µM). Also known to inhibit CaM kinase III (IC50 = 5.3 µM).

Biochem/physiol Actions

Cell permeable: yes
Primary Target
PKCδ
Product does not compete with ATP.
Reversible: yes
Target IC50: 3-6 µM against PKCδ; 5.3 µM against CaM kinase III

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

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

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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