203290
Bisindolylmaleimide I
A highly selective, cell-permeable, and reversible protein kinase C (PKC) inhibitor (IC₅₀ = 10 nM) that is structurally similar to staurosporine.
Szinonimák:
Bisindolylmaleimide I, 2-[1-(3-Dimethylaminopropyl)-1H-indol-3-yl]-3-(1H-indol-3-yl)-maleimide, Gö 6850, GF 109203X
Bejelentkezésa Szervezeti és Szerződéses árazás megtekintéséhez
Összes fotó(1)
About This Item
Tapasztalati képlet (Hill-képlet):
C25H24N4O2
CAS-szám:
Molekulatömeg:
412.48
MDL-szám:
UNSPSC kód:
12352111
NACRES:
NA.77
Javasolt termékek
Minőségi szint
Teszt
≥95% (HPLC)
form
solid
gyártó/kereskedő neve
Calbiochem®
tárolási körülmény
OK to freeze
protect from light
szín
deep orange
oldhatóság
DMSO: 10 mg/mL
kiszállítva
ambient
tárolási hőmérséklet
2-8°C
InChI
1S/C25H24N4O2/c1-28(2)12-7-13-29-15-19(17-9-4-6-11-21(17)29)23-22(24(30)27-25(23)31)18-14-26-20-10-5-3-8-16(18)20/h3-6,8-11,14-15,26H,7,12-13H2,1-2H3,(H,27,30,31)
Nemzetközi kémiai azonosító kulcs
QMGUOJYZJKLOLH-UHFFFAOYSA-N
Általános leírás
A highly selective cell-permeable protein kinase C (PKC) inhibitor (IC50 = 10 nM) that is structurally similar to staurosporine. Acts as a competitive inhibitor for the ATP-binding site of PKC. Shows high selectivity for PKCα, βI, βII, γ, δ, and ε isozymes. May inhibit protein kinase A at a much higher concentration (IC50 = 2 µM). Also inhibits telomerase activity in quercetin, H-89, or herbimycin A treated NPC-076 cells.
A highly selective, cell-permeable, and reversible protein kinase C (PKC) inhibitor (IC50 = 10 nM) that is structurally similar to staurosporine. Acts as a competitive inhibitor for the ATP-binding site of PKC. Shows high selectivity for PKCα-, βI-, βII-, γ-, δ-, and ε- isozymes. Potently inhibits GSK-3 in primary adipocyte lysates (IC50 = 360 nM) and in GSK-3β immunoprecipitates (IC50 = 170 nM). May inhibit protein kinase A at a much higher concentration (IC50 = 2 µM). A 1 mg/ml solution of Bisindolylmaleimide I (Cat. No. 203293) in anhydrous DMSO is also available.
Biokémiai/fiziológiai hatások
Cell permeable: yes
Primary Target
PKC
PKC
Product competes with ATP.
Reversible: yes
Target IC50: 10 nM against protein kinase C (PKC); 360 nM, 170 nM against GSK-3 in primary adipocyte lysates and in GSK-3β immunoprecipitates, respectively
Figyelmeztetés
Toxicity: Standard Handling (A)
Elkészítési megjegyzés
Further dilute with aqueous buffers just prior to use.
Feloldás
Following reconstitution, aliquot and freeze (-20°C). DMSO stock solutions are stable for up to 4 months at -20°C.
Egyéb megjegyzések
Hers, I., et al. 1999. FEBS Lett.460, 433.
Ku, W.-C., et al. 1997. Biochem. Biophys. Res. Commun. 241, 730.
Gekeler, V., et al. 1996. Br. J. Cancer 74, 897.
Kiss, Z., et al. 1995. Biochim. Biophys. Acta 1265, 93.
Toullec, D., et al. 1991. J. Biol. Chem. 266, 15771.
Ku, W.-C., et al. 1997. Biochem. Biophys. Res. Commun. 241, 730.
Gekeler, V., et al. 1996. Br. J. Cancer 74, 897.
Kiss, Z., et al. 1995. Biochim. Biophys. Acta 1265, 93.
Toullec, D., et al. 1991. J. Biol. Chem. 266, 15771.
Jogi információk
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Tárolási osztály kódja
11 - Combustible Solids
WGK
WGK 3
Analitikai tanúsítványok (COA)
Analitikai tanúsítványok (COA) keresése a termék sarzs-/tételszámának megadásával. A sarzs- és tételszámok a termék címkéjén találhatók, a „Lot” vagy „Batch” szavak után.
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Cikkek
Learn tips and tricks for how to properly use inhibitors including how to select the right inhibitor and how to plan experiments with inhibitors.
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