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AB287015

1-NM-PP1

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MW 331.4 Da, Purity >98%. 1-NM-PP1 is a cell-permeable PP1 analog that acts as a potent and selective inhibitor of mutant kinases over their wild-type progenitors. Inhibits multiple tyrosine kinase targets, such as v-Src (IC50 = 1 μM), c-Fyn (IC50 = 0.6 μM), c-Abl (IC50 = 0.6 μM), CDK2 (IC50: 18 μM), and CaMK II (IC50 = 22 μM). Addiitonally, 1-NM-PP1 is reported to be a potent and specific inhibitor of TrkB-F616A and TrkA-F592A signaling (IC50 values ~ 3 nM).

Key facts

CAS number

221244-14-0

Purity

>98%

Form

Solid

form

Molecular weight

331.4 Da

Molecular formula

C<sub>2</sub><sub>0</sub>H<sub>2</sub><sub>1</sub>N<sub>5</sub>

PubChem

5154691

Nature

Synthetic

Solubility

Soluble in DMSO to 75 mM

Biochemical name

1-tert-butyl-3-(naphthalen-1-ylmethyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine

Biological description

1-NM-PP1 is a cell-permeable PP1 analog that acts as a potent and selective inhibitor of mutant kinases over their wild-type progenitors. Inhibits multiple tyrosine kinase targets, such as v-Src (IC50 = 1 μM), c-Fyn (IC50 = 0.6 μM), c-Abl (IC50 = 0.6 μM), CDK2 (IC50: 18 μM), and CaMK II (IC50 = 22 μM). Addiitonally, 1-NM-PP1 is reported to be a potent and specific inhibitor of TrkB-F616A and TrkA-F592A signaling (IC50 values ~ 3 nM).

Canonical smiles

CC(C)(C)N1C2=NC=NC(=C2C(=N1)CC3=CC=CC4=CC=CC=C43)N

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)

InChiKey

GDQXJQSQYMMKRA-UHFFFAOYSA-N

IUPAC Name

1-tert-butyl-3-(naphthalen-1-ylmethyl)pyrazolo[3,4-d]pyrimidin-4-amine

Properties and storage information

Shipped at conditions
Blue Ice
Appropriate long-term storage conditions
-20°C
Storage information
This product is air and light sensitive and impurities can occur as a result of air oxidation or due to metabolism by microbes

Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

The targets JNK1 Src RIP2 CSK PKC mu/PKD Lck cAMP Protein Kinase Catalytic subunit and Calmodulin 1/2/3 are proteins involved in various cellular processes. JNK1 also known as c-Jun N-terminal kinase 1 plays a role in signaling cascades that regulate cell growth differentiation and apoptosis. It has a molecular mass of approximately 48 kDa. Src a non-receptor tyrosine kinase is essential in controlling several aspects of cell behavior. RIP2 or receptor-interacting protein kinase 2 facilitates signal transduction processes from the cell surface to the cytoplasm. These proteins are expressed in a wide range of tissues emphasizing their significance in multiple cellular functions.
Biological function summary

These proteins participate in significant regulatory roles in cells. JNK1 contributes to stress response mechanisms and is a part of the mitogen-activated protein kinase (MAPK) complex. Src impacts cytoskeletal arrangement and cellular adhesion making it influential in cellular mechanics. RIP2 engages in the innate immune response and functions alongside other innate immunity pathways. Calmodulin existing in three isoforms acts as a calcium-binding messenger protein influencing numerous enzymatic activities by working with its target proteins.

Pathways

These target proteins integrate into major cellular signaling pathways. JNK1 plays a critical role in the MAPK signaling pathway influencing the activity of transcription factor AP-1. Src is involved in the integrin signaling pathway impacting focal adhesion dynamics and cell motility. These proteins interact with others like ERK and PI3K within these pathways highlighting their interconnectivity in signal relay and propagation. Such associations illustrate the importance of these targets in maintaining cellular homeostasis and responding to external stimuli.

The dysfunction of these target proteins links to various pathological conditions. JNK1 involves in the progression of neurodegenerative disorders like Alzheimer's disease where abnormal signaling can lead to neuronal cell death. Src has implications in cancer with its overactivation contributing to tumor progression and metastasis. In these conditions the interplay between these proteins and others like TRAF2 and Ras further exemplifies the intricate networks that influence disease pathology highlighting potential areas for therapeutic intervention.

Product protocols

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