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529598

Sigma-Aldrich

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.

Synonym(s):

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

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About This Item

Empirical Formula (Hill Notation):
C16H18IN5
CAS Number:
Molecular Weight:
407.25
MDL number:
UNSPSC Code:
12352202
NACRES:
NA.77

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.

Legal Information

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

Storage Class Code

11 - Combustible Solids

WGK

WGK 2

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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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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