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1-NM-PP1

Cayman Chemical Item Number 13330

PP1 Analog II (CAS 221244-14-0)

1-NM-PP1 (CAS 221244-14-0)

See more	Inhibitors (493) Cell Biology (281) Signal Transduction (314)

Description

1-NM-PP1 is a cell permeable inhibitor of kinases that have been mutated, by a single base substitution, to become ‘analog sensitive’ (as), as compared to the wild-type kinase. 1-NM-PP1 was first developed to optimally inhibit v-Src-as1, with an I338G substitution, preferentially over v-Src (IC₅₀ = 4.2 nM versus 28 μM, respectively).¹ The homologous mutation in other kinases generated similar analog sensitivity (e.g., IC₅₀ = 3.2 nM for c-Fyn-as1 versus 1.0 μM for c-Fyn; 5.0 nM for CDK2-as1 versus 29 μM for CDK2; 8.0 nM for CAMKII-as1 versus 24 μM for CAMKII).² This approach has been used to elucidate functions of several kinases in both mammalian and yeast systems.^2,3,4,5,6

1 Bishop, A.C., Kung, C., Shah, K., et al. Generation of monospecific nanomolar tyrosine kinase inhibitors via a chemical genetic approach. J Am Chem Soc 121 627-631 (1999).

2 Bishop, A.C., Ubersax, J.A., Petsch, D.T., et al. A chemical switch for inhibitor-sensitive alleles of any protein kinase. Nature 407 395-401 (2000).

3 Weiss, E.L., Bishop, A.C., Shokat, K.M., et al. Chemical genetic analysis of the budding-yeast p21-activated kinase Cla4p. Nat Cell Biol 2 677-685 (2000).

4 Ira, G., Pellicioli, A., Balijja, A., et al. DNA end resection, homologous recombination and DNA damage checkpoint activation require CDK1. Nature 431 1011-1017 (2004).

5 Larochelle, S., Merrick, K.A., Terret, M., et al. Requirements for Cdk7 in the assembly of Cdk1/cyclin B and activation of Cdk2 revealed by chemical genetics in human cells. Mol Cell 25(6) 839-850 (2007).

6 Van den Broeke, C., Radu, M., Deruelle, M., et al. Alphaherpesvirus US3-mediated reorganization of the actin cytoskeleton is mediated by group A p21-activated kinases. Proc Natl Acad Sci USA 106(21) 8707-8712 (2009).

Synonyms	PP1 Analog II
Formal Name	1-(1,1-dimethylethyl)-3-(1-naphthalenylmethyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
CAS Number	221244-14-0
Molecular Formula	C₂₀H₂₁N₅
Formula Weight	331.4
Formulation	A crystalline solid
Purity	≥95%
Stability	2 years
Storage	-20°C
Shipping	Room temperature in continental US; may vary elsewhere
SMILES	Copy SMILES to clipboard NC1=NC=NC2=C1C(CC3=CC=CC4=C3C=CC=C4)=NN2C(C)(C)C

Background Reading

Van den Broeke, C., Radu, M., Deruelle, M., et al. Alphaherpesvirus US3-mediated reorganization of the actin cytoskeleton is mediated by group A p21-activated kinases. Proc Natl Acad Sci USA 106(21) 8707-8712 (2009).

Larochelle, S., Merrick, K.A., Terret, M., et al. Requirements for Cdk7 in the assembly of Cdk1/cyclin B and activation of Cdk2 revealed by chemical genetics in human cells. Mol Cell 25(6) 839-850 (2007).

Ira, G., Pellicioli, A., Balijja, A., et al. DNA end resection, homologous recombination and DNA damage checkpoint activation require CDK1. Nature 431 1011-1017 (2004).

Weiss, E.L., Bishop, A.C., Shokat, K.M., et al. Chemical genetic analysis of the budding-yeast p21-activated kinase Cla4p. Nat Cell Biol 2 677-685 (2000).

Bishop, A.C., Ubersax, J.A., Petsch, D.T., et al. A chemical switch for inhibitor-sensitive alleles of any protein kinase. Nature 407 395-401 (2000).

Bishop, A.C., Kung, C., Shah, K., et al. Generation of monospecific nanomolar tyrosine kinase inhibitors via a chemical genetic approach. J Am Chem Soc 121 627-631 (1999).

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1-NM-PP1 is available in the following screening library:

Bio-active Lipid I Screening Library (96-Well)

Size	Price	Quantity	Subtotal
1 mg	$86.00		$0.00
5 mg	$387.00		$0.00
10 mg	$688.00		$0.00
25 mg	$1,505.00		$0.00
Bulk	Contact
		Cart Total	$0.00

Pricing updated 2012-02-11. Prices are subject to change without notice.

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Related Products

PP2

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