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Merck
CN

529598

PP1 Analog IV, 3-IB-PP1

A cell-permeable enlarged PP1 analog that acts as a potent, ATP-competitive and reversible inhibitor of asAkt1/2/3.

别名:

PP1 Analog IV, 3-IB-PP1, 3-Iodobenzyl PP1 analog

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关于此项目

经验公式(希尔记法):
C16H18IN5
化学文摘社编号:
分子量:
407.25
UNSPSC Code:
12352202
NACRES:
NA.77
MDL number:
Assay:
≥97% (HPLC)
Form:
powder
Storage condition:
OK to freeze, protect from light
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Quality Segment

assay

≥97% (HPLC)

form

powder

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

white

solubility

DMSO: 0.5 mg/mL

shipped in

ambient

storage temp.

2-8°C

SMILES string

NC1=NC=NC2=C1C(CC3=CC(I)=CC=C3)=NN2C(C)(C)C

InChI

1S/C16H18IN5/c1-16(2,3)22-15-13(14(18)19-9-20-15)12(21-22)8-10-5-4-6-11(17)7-10/h4-7,9H,8H2,1-3H3,(H2,18,19,20)

InChI key

CVRIGUMSLGSWEZ-UHFFFAOYSA-N

General description

A cell-permeable enlarged PP1 (Cat. No. 567809) analog that acts as a potent, ATP-competitive and reversible inhibitor of asAkt1/2/3 (IC50 = 28, 240 and 120 nM, respectively) over wtAkt1/2/3 (IC50 = >10 µM). Shown to hyperphosphorylate Akt-Ser473 and -Thr308 in HEK293 cells coexpressed with myr-HA-asAkt1 or myr-HA-asAkt1/2/3 with no effect on pGSK-3βSer9 levels and wtAkt expressing cells. Also, specifically blocks the inhibitory function of membrane asCsk with diminished activity towards wtCsk, induces phosphorylation of Lck-Tyr394 and ERK1/2 in primary mouse T cells (EC50 ~0.5 µM) and rapidly activates T cell receptor signaling.
A cell-permeable enlarged PP1 (Cat. No.567809) analog that acts as a potent, ATP-competitive and reversible inhibitor of asAkt1/2/3 (IC50 = 28, 240 and 120 nM, respectively) over wtAkt1/2/3 (IC50 = >10 µM). Shown to hyperphosphorylate Akt-Ser473 and -Thr308 in HEK293 cells coexpressed with myr-HA-asAkt1 or myr-HA-asAkt1/2/3 with no effect on pGSK-3βSer9 levels and wtAkt expressing cells. Also, specifically blocks the inhibitory function of membrane asCsk with diminished activity towards wtCsk, induces phosphorylation of Lck-Tyr394 and ERK1/2 in primary mouse T cells (EC50 ~0.5 µM) and rapidly activates T cell receptor signaling.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Schoenborn, J.R., et al. 2011. Sci. Signal.4, ra59.
Okuzumi, T., et al. 2009. Nat. Chem. Bio.5, 484.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)


存储类别

11 - Combustible Solids

wgk

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable



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