1-Naphthyl PP1 CAS: 221243-82-9
MF: C19H19N5
MW: 317.39
A selective inhibitor of v-Src and c-Fyn as well as c-Abl.

1-Naphthyl PP1 (CAS 221243-82-9)

1-Naphthyl PP1 | CAS 221243-82-9 is rated 5.0 out of 5 by 1.
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Application: 1-Naphthyl PP1 is a selective inhibitor of v-Src and c-Fyn as well as c-Abl
CAS Number: 221243-82-9
Purity: ≥98%
Molecular Weight: 317.39
Molecular Formula: C19H19N5
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data (including water content).

1-Naphthyl PP1 selectively inhibits c-Src family kinases v-Src and Fyn (c-Fyn) as well as c-Abl tyrosine kinase (IC50 values are 1.0, 0.6, 0.6, 18 and 22 μM for v-Src, Fyn (c-Fyn), c-Abl, CDK2 and CAMK II respectively). 1-Naphthyl PP1 preferentially inhibits mutant over wild-type kinases (IC50 values are 1.5 vs 1000 nM for I338G v-src and v-src respectively).


References

1. Bishop et al (1999) Generation of monospecific nanomolar tyrosine kinase inhibitors via a chemical genetic approach. J.Am.Chem.Soc. 121 627.
2. Bishop, A.C. et al. 2000. Nature. 407(6802): 395-401. PMID: 11014197
3. Kenski, D.M. et al. 2005. J. Biol. Chem. 280(41): 35051-35061. PMID: 16081410
4. Endo, S. et al. 2006. Biochem. Biophys. Res. Commun. 341(1): 261-265. PMID: 16431218
5. Reboutier, D. et al. 2013. J. Cell Biol. 201(1): 65-79. PMID: 23547029

Physical State :
Solid
Solubility :
Soluble in DMSO (~20 mg/ml), chloroform, ethanol (~2 mg/ml), DMF (~30 mg/ml), and 1: 5 solution of DMF: PBS (pH 7.2) (~0.15 mg/ml).
Storage :
Store at 4° C
Melting Point :
219-222° C
Boiling Point :
527.82° C at 760 mmHg (Predicted)
Density :
1.28 g/cm3 (Predicted)
Refractive Index :
n20D 1.69 (Predicted)
IC50 :
c-Fyn: IC50 = 0.6 µM; c-Abl: IC50 = 0.6 µM; v-Src: IC50 = 1.0 µM; CDK2: IC50 = 18 µM; CAMK II: IC50 = 22 µM
pK Values :
pKb: 4.19 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
4877
MDL Number :
MFCD03425471
Beilstein Registry :
8275174
SMILES :
CC(C)(C)N1C2=C(C(=N1)C3=CC=CC4=CC=CC=C43)C(=NC=N2)N

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Certificate of Analysis

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1-Naphthyl PP1 (CAS 221243-82-9)  Product Citations

See how others have used 1-Naphthyl PP1 (CAS 221243-82-9). Click on the entry to view the PubMed entry .

Citations 1 to 2 of 2 total

PMID: # 27525436  Matsushima, S. et al. 2016. J. Clin. Invest. 126: 3403-16.

PMID: # 32518085  J. Am. Soc. Nephrol.

Citations 1 to 2 of 2 total
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Rated 5 out of 5 by from Reboutier Reboutier, D. et al. (PubMed 23547029) reported the design of the first human Aurora A kinase (as-AurA) engineered by chemical genetics techniques. This kinase is fully functional biochemically and in cells, and is rapidly and specifically inhibited by the ATP analogue 1-Naphthyl-PP1 (1-Na-PP1). By treating cells exclusively expressing the as-AurA with 1-Na-PP1, they discovered that Aurora A is required for central spindle assembly in anaphase through phosphorylation of Ser 19 of P150Glued. -SCBT Publication Review
Date published: 2015-06-27
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