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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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P341313-1mg | 1mg | In stock | $29.90 | |
P341313-5mg | 5mg | In stock | $122.90 | |
P341313-25mg | 25mg | In stock | $553.90 | |
P341313-50mg | 50mg | In stock | $757.90 |
a cell-permeable PP1 analog that acts as a potent and selective inhibitor of mutant kinases
Synonyms | MLS001065852 | SR-01000781016 | HMS3648M20 | Mutant Kinases Inhibitor II | SCHEMBL1964002 | EX-A868 | SMR000486341 | 1-tert-butyl-3-(naphthalen-1-ylmethyl)pyrazolo[3,4-d]pyrimidin-4-amine | CCG-206782 | 1-(tert-butyl)-3-(naphthalen-1-ylmethyl)-1H-pyrazolo |
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Specifications & Purity | Moligand™, ≥98% |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Product Description | PP1 Analog II, 1NM-PP1 is a cell-permeable PP1 analog that acts as a potent and selective inhibitor of mutant kinases over their wild-type progenitors. 1-NM-PP1 is a cell permeable inhibitor of kinases that have been mutated, by a single base substitution, to become 'analog sensitive', 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 (IC|50|= 4.2 nM versus 28 μM, respectively). The homologous mutation in other kinases generated similar analog sensitivity (e.g., IC|50|= 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). This approach has been used to elucidate functions of several kinases in both mammalian and yeast systems. In addition it has been shown to activate mutants of Ire1, a transmembrane kinase. |
pKa | pKₐ: 4.50 |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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Pubchem Sid | 488195123 |
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Pubchem Sid Url | https://pubchem.ncbi.nlm.nih.gov/substance/488195123 |
IUPAC Name | 1-tert-butyl-3-(naphthalen-1-ylmethyl)pyrazolo[3,4-d]pyrimidin-4-amine |
INCHI | 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 |
Canonical SMILES | CC(C)(C)N1C2=NC=NC(=C2C(=N1)CC3=CC=CC4=CC=CC=C43)N |
Isomeric SMILES | CC(C)(C)N1C2=NC=NC(=C2C(=N1)CC3=CC=CC4=CC=CC=C43)N |
PubChem CID | 5154691 |
Molecular Weight | 331.41 |
Beilstein | 8278642 |
PubChem CID | 5154691 |
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ChEMBL Ligand | CHEMBL573578 |
ChEBI | CHEBI:52309 |
CAS Registry No. | 221244-14-0 |
RCSB PDB Ligand | 0JN |
PubChem SID | 488195123 |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
Lot Number | Certificate Type | Date | Item |
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D2320664 | Certificate of Analysis | Mar 27, 2023 | P341313 |
D2320665 | Certificate of Analysis | Mar 27, 2023 | P341313 |
D2320673 | Certificate of Analysis | Mar 27, 2023 | P341313 |
D2320689 | Certificate of Analysis | Mar 27, 2023 | P341313 |
D2320798 | Certificate of Analysis | Mar 27, 2023 | P341313 |
D2320804 | Certificate of Analysis | Mar 27, 2023 | P341313 |
D2320805 | Certificate of Analysis | Mar 27, 2023 | P341313 |
D2320809 | Certificate of Analysis | Mar 27, 2023 | P341313 |
Solubility | Soluble in ethanol (2 mg/ml), DMSO (20 mg/ml), DMF (20 mg/ml), 1:5 DMF:PBS(pH 7.2) (0.15 mg/ml), dichloromethane, ethyl acetate, and methanol. |
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Refractive Index | n20D1.68 |
Boil Point(°C) | ~545.7° C at 760 mmHg (Predicted) |
Melt Point(°C) | 175-176° C |
1. Saghatelian A, Cravatt BF. (2005) Assignment of protein function in the postgenomic era.. Nat Chem Biol, 1 (3): (130-42). [PMID:16408016] [10.1021/op500134e] |