529606
PP1 Analog II, 1NM-PP1
InSolution, ≥95%, reversible PP1 analog that acts as a potent, selective, and ATP-competitive inhibitor of mutant kinases
别名:
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
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关于此项目
经验公式（希尔记法）:
C20H21N5
化学文摘社编号:
分子量:
331.41
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥95% (HPLC)
Form:
liquid
Storage condition:
OK to freeze, avoid repeated freeze/thaw cycles, desiccated (hygroscopic), protect from light
Quality Segment
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
SMILES string
[n]1(nc(c4c1ncnc4N)Cc2c3c(ccc2)cccc3)C(C)(C)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
General description
A cell-permeable and reversible PP1 analog 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.,
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 µ
Packaging
Packaged under inert gas
Physical form
A 10 mM (1 mg/302 µL) solution of PP1 Analog II, 1NM-PP1 (Cat. No. 529581) in DMSO.
Preparation Note
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.
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
Disclaimer
Toxicity: Irritant (B)
存储类别
10 - Combustible liquids
wgk
WGK 1
flash_point_f
188.6 °F - closed cup - Information refers to the main component.
flash_point_c
87 °C - closed cup - Information refers to the main component.