| Identification | Back Directory | [Name]
1 NM-PP1 | [CAS]
221244-14-0 | [Synonyms]
1 NM-PP1
Chebi:52309
PP1 ANALOG II
PP1 Analog II, 1NM-PP1
MUTANT KINASES INHIBITOR II
4-AMINO-1-TERT-BUYTL-3-(1-NAPHTHYLMETHYL)PYRAZOLO[3,4-D]PYRIMIDINE
4-AMINO-1-TERT-BUTYL-3-(1'-NAPHTHYLMETHYL)PYRAZOLO[3,4-D]PYRIMIDINE
1-tert-Butyl-3-(naphthalen-1-ylmethyl)-1H-pyrazolo[3,4-D]pyrimidin-4-amine
1-(1,1-Dimethylethyl)-3-(1-naphthalenylmethyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine | [Molecular Formula]
C20H21N5 | [MDL Number]
MFCD03425470 | [MOL File]
221244-14-0.mol | [Molecular Weight]
331.41 |
| Chemical Properties | Back Directory | [Appearance]
White Cyrstalline Solid | [Melting point ]
175-176°C | [Boiling point ]
545.7±45.0 °C(Predicted) | [density ]
1.25±0.1 g/cm3(Predicted) | [storage temp. ]
-20°C Freezer | [solubility ]
Chloroform (Slightly), Methanol (Slightly, Heated) | [form ]
White solid | [pka]
4.50±0.30(Predicted) | [color ]
White to Beige |
| Hazard Information | Back Directory | [Chemical Properties]
White Cyrstalline Solid | [Uses]
A highly potent (IC50=4.3 nM) and uniquely specific tyrosine kinase inhibitor of a rationally engineered v-Src tyrosine kinase | [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 | [Definition]
ChEBI: 1-NM-PP1 is a pyrazolopyrimidine. It has a role as a tyrosine kinase inhibitor. | [References]
[1] bishop ac1, ubersax ja, petsch dt, matheos dp, gray ns, blethrow j, shimizu e, tsien jz, schultz pg, rose md, wood jl, morgan do, shokat km. a chemical switch for inhibitor-sensitive alleles of any protein kinase. nature. 2000 sep 21; 407 (6802): 395-401. |
|
|