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.
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
UNSPSC Code:
12352202
NACRES:
NA.77
MDL number:
Assay:
≥97% (HPLC)
Form:
powder
Storage condition:
OK to freeze, protect from light
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.
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)
Storage Class
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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