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Merck

529606

PP1 Analog II, 1NM-PP1

InSolution, ≥95%, reversible PP1 analog that acts as a potent, selective, and ATP-competitive inhibitor of mutant kinases

Synonym(s):

InSolution PP1 Analog II, 1NM-PP1, 4-Amino-1- tert-butyl-3-(1ʹ-naphthylmethyl)pyrazolo[3,4-d]pyrimidine, 4-Amino-1-tert-butyl-3-(1ʹ-naphthylmethyl)pyrazolo[3,4-d]pyrimidine

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About This Item

Empirical Formula (Hill Notation):
C20H21N5
CAS Number:
221244-14-0
Molecular Weight:
331.41
MDL number:
MFCD17010191
UNSPSC Code:
12352200
NACRES:
NA.77

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Product Name

PP1 Analog II, 1NM-PP1, InSolution, ≥95%, reversible PP1 analog that acts as a potent, selective, and ATP-competitive inhibitor of mutant kinases

SMILES string

[n]1(nc(c4c1ncnc4N)Cc2c3c(ccc2)cccc3)C(C)(C)C

InChI

1S/C20H21N5/c1-20(2,3)25-19-17(18(21)22-12-23-19)16(24-25)11-14-9-6-8-13-7-4-5-10-15(13)14/h4-10,12H,11H2,1-3H3,(H2,21,22,23)

InChI key

GDQXJQSQYMMKRA-UHFFFAOYSA-N

assay

≥95% (HPLC)

form

liquid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
avoid repeated freeze/thaw cycles
desiccated (hygroscopic)
protect from light

shipped in

dry ice

storage temp.

−70°C

Quality Level

100

Related Categories

Biochem/physiol Actions

Cell permeable: yes
Primary Target
mutant c-Fyn, v-src, Cadk2, CaMKIIa, c-Abl etc.,
Reversible: yes
Target IC50: 3.2 nM for T339G, c-Fyn-as1 vs. 1.0 &micro

Disclaimer

Toxicity: Irritant (B)

General description

A cell-permeable and reversible PP1 analog that acts as a potent, selective, and ATP-competitive inhibitor of mutant kinases compared to the corresponding wild-type kinase (IC50 = 3.2 nM for T339G, c-Fyn-as1 vs. 1.0 µM for c-Fyn; 4.3 nM for I338G, v-src-as1 vs. 28 µM for v-src; 5 nM for F80G, CDK2-as1 vs. 29 µM for CDK2; 8 nM for F89G, CAMK IIa-as1 vs. 24 µM for CAMKII; 120 nM for T315A, c-Abl-as2 vs. 3.4 µM for c-Abl). Shown to activate mutants of Ire1, a transmembrane kinase.

Other Notes

Ira, G., et al. 2004. Nature431, 1011.
Papa, F.R., et al. 2003. Science302, 1533.
Bishop, A.C., et al. 2000. Nature407, 395.
Weiss, E.L., et al. 2000. Nat. Cell Biol.2, 677.
Bishop, A.C., et al. 1999. J. Am. Chem. Soc.121, 627.

Packaging

Packaged under inert gas

Physical form

A 10 mM (1 mg/302 µL) solution of PP1 Analog II, 1NM-PP1 (Cat. No. 529581) in DMSO.

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Aliquots are stable for up to 3 months at -70°C.

Legal Information

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

Storage Class

10 - Combustible liquids

wgk

WGK 1

flash_point_f

188.6 °F - closed cup - Information refers to the main ingredient.

flash_point_c

87 °C - closed cup - Information refers to the main ingredient.

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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