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

Properties

• Quality Level: 100
• 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
• 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

Description

General description

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.

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

Packaging

Packaged under inert gas

Warning

Toxicity: Irritant (B)

Physical form

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.

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.

Legal Information

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

Safety Information

• Storage Class Code: 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.