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Merck
CN

557514

Ro-31-8425

A potent, cell-permeable, reversible, ATP-competitive, and selective protein kinase C inhibitor (IC50 = 15 nM for rat brain PKC).

别名:

Ro-31-8425, 2-[8-(Aminomethyl)-6,7,8,9-tetrahydropyrido[1,2-a]indol-3-yl]-3-(1-methyl-1H-indol-3-yl)maleimide, HCl, Bisindolylmaleimide X, HCl

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关于此项目

经验公式（希尔记法）:
C26H24N4O2 · xHCl
化学文摘社编号:
131848-97-0
分子量:
424.49 (free base basis)
MDL number:
MFCD00906977
UNSPSC Code:
12352200
NACRES:
NA.77

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产品名称

Ro-31-8425, A potent, cell-permeable, reversible, ATP-competitive, and selective protein kinase C inhibitor (IC50 = 15 nM for rat brain PKC).

SMILES string

[n]21c3c(c(c2CC(CC1)CN)C4=C(C(=O)NC4=O)c5c6c([n](c5)C)cccc6)cccc3

InChI

1S/C26H24N4O2/c1-29-14-18(16-6-2-4-8-19(16)29)23-24(26(32)28-25(23)31)22-17-7-3-5-9-20(17)30-11-10-15(13-27)12-21(22)30/h2-9,14-15H,10-13,27H2,1H3,(H,28,31,32)

InChI key

QQKKPWJFHBFCTH-UHFFFAOYSA-N

assay

≥94% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

red to orange-red

solubility

DMSO: 10 mg/mL

shipped in

ambient

storage temp.

2-8°C

Quality Level

100

相关类别

Legal Information

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

Biochem/physiol Actions

Cell permeable: yes
Primary Target
PKC
Product competes with ATP.
Reversible: yes
Target IC50: 15 nM for rat brain PKC; 8 nM for PKCα, 8 nM for PKCβI, 14 nM for PKCβII, 13 nM for PKCγ, and 39 nM for PKCε

Disclaimer

Toxicity: Irritant (B)

General description

A potent, cell-permeable, reversible, ATP-competitive, and selective protein kinase C inhibitor (IC50 = 15 nM for rat brain PKC). Exhibits some degree of isozyme specificity (IC50 = 8 nM for PKCα, 8 nM for PKCβI, 14 nM for PKCβII, 13 nM for PKCγ, and 39 nM for PKCε). Shows slight selectivity for the conventional PKC isozymes PKCα, PKCβ, and PKCγ over the Ca2+-independent PKC isozyme PKCε. Upregulates CD11a expression and enhances mesenchymal stromal cell adhesion under flow.

Other Notes

Levy, O., et al. 2015. Cell Reports10, In press.
Merritt, J.E., et al. 1997. Cell Signal 9, 53.
Wilkinson, S.E., et al. 1993. Biochem. J. 294, 335.

Preparation Note

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

存储类别

11 - Combustible Solids

wgk

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable

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