529606

PP1 Analog II, 1NM-PP1

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

• Synonyme(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
• Formule empirique (notation de Hill): C₂₀H₂₁N₅
• Numéro CAS: 221244-14-0
• Poids moléculaire : 331.41
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Pureté: ≥95% (HPLC)
• Forme: liquid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; avoid repeated freeze/thaw cycles; desiccated (hygroscopic); protect from light
• Conditions d'expédition: dry ice
• Température de stockage: −70°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)
• Clé InChI: GDQXJQSQYMMKRA-UHFFFAOYSA-N

Description

Description générale

A cell-permeable and reversible PP1 analog (>Cat. No. 529579) 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.

A cell-permeable and reversible PP1 analog (>Cat. No. 529579) 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.

Actions biochimiques/physiologiques

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

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Irritant (B)

Forme physique

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

Reconstitution

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

Autres remarques

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.

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 10 - Combustible liquids
• Classe de danger pour l'eau (WGK): WGK 1
• Point d'éclair (°F): 188.6 °F - closed cup - Information refers to the main ingredient.
• Point d'éclair (°C): 87 °C - closed cup - Information refers to the main ingredient.