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Merck

557514

Ro-31-8425

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

別名:

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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実隓匏ヒル衚蚘法:
C26H24N4O2 · xHCl
CAS番号:
分子量:
424.49 (free base basis)
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥94% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
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Quality Segment

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

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

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.

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

Preparation Note

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

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.

Legal Information

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

Disclaimer

Toxicity: Irritant (B)


保管分類

11 - Combustible Solids

WGK

WGK 1

匕火点 (F)

Not applicable

匕火点°C

Not applicable



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