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.
Sinónimos:
PP1 Analog IV, 3-IB-PP1, 3-Iodobenzyl PP1 analog
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About This Item
Fórmula empírica (notación de Hill):
C16H18IN5
Número de CAS:
Peso molecular:
407.25
MDL number:
UNSPSC Code:
12352202
NACRES:
NA.77
Productos recomendados
Quality Level
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
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
Warning
Toxicity: Standard Handling (A)
Reconstitution
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.
Okuzumi, T., et al. 2009. Nat. Chem. Bio.5, 484.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class
11 - Combustible Solids
wgk_germany
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificados de análisis (COA)
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Ben F Brian et al.
Current protocols in immunology, 130(1), e104-e104 (2020-09-16)
In this article we describe the use of pharmacological and genetic tools coupled with immunoblotting (Western blotting) and targeted mass spectrometry to quantify immune signaling and cell activation mediated by tyrosine kinases. Transfer of the ATP γ phosphate to a
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