NP1 peptide
NP1 peptide is a cyclic peptide (CHSHGTRAC) and TK-EGFR inhibitor (IC50 = 0.58 nM, Kd = 18.40 μM). NP1 peptide blocks kinase activity by binding to the ATP-binding pocket of TK-EGFR and inhibits autophosphorylation at the EGFR Y1173 site, and it also serves as a pH-responsive nanocarrier for siRNA delivery. NP1 peptide is used in cancer research.
For research use only. We do not sell to patients.
- Formula: C162H245N81O25·xC2HF3O2
- Molecular Weight:3727.21 (free base)
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All EGFR Isoforms
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Biological Activity
Description
IC50 & Target
[3]|
TK-EGFR 0.58 nM (IC50) |
TK-EGFR 18.40 μM (Kd) |
In Vitro
NP1 peptide (1 mg/mL dispase; 10 passages; 16 days) supports the maintenance of pluripotency in H1 hESCs and f-hiPSCs over multiple passages with or without Y-27632, but is inferior to VBO1 peptide for long-term stemness maintenance[1].
NP1 peptide potently inhibits TK-EGFR activity with an IC50 of 0.58 nM, and its selectivity for TK-EGFR over TK-HER2 is more than 100-fold[3].
NP1 peptide (1.25-5 µM; 1.5 min association) binds to TK-EGFR with a Kd of 18.40 µM[3].
NP1 peptide (up to 200 µM; 72 h) exhibits no cytotoxicity against A431, A549, and HeLa cell lines even at a concentration of 200 µM[3].
NP1 peptide (100 ns) binds to TK-EGFR by forming hydrogen bonds with Thr766, Met769, Pro770, Cys773, Asp776, and Asp831, and through hydrophobic interactions with Phe699 and Val702[3].
NP1 peptide (50 nM) requires the Ser3, His4, and Gly5 residues to exert its inhibitory activity against TK‑EGFR.[3].
NP1 peptide is equally well recognized by C2 and H1 hybridomas, confirming their specificity for the NP264 epitope[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:H1 hESCs and f-hiPSCs
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Concentration:1 mg/mL dispase
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Incubation Time:10 passages; 5-7 min; 8 days; 8 days; 16 days
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Result:Maintained unaltered morphology with intact karyotypes.
Confirmed that the majority of cells expressed the pluripotency markers OCT-4 and SSEA-3.
Showed high levels of OCT-4 and SSEA-3 expression throughout the cell colonies.
Demonstrated that embryoid bodies derived from these f-hiPSCs could generate cells representing all three germ layers after 16 days of culture.
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Cell Line:A431, A549, and HeLa
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Concentration:0.28, 0.56, 1.12 mM
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Incubation Time:72 h
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Result:Exhibited no cytotoxic effects on EGFR-expressing cells (A431, HeLa, and A549) even at a high concentration of 200 µM.
Could not determine an IC50 for NP1 against these cell lines.
Chemical Information
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Molecular Weight 3727.21 (free base)
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Formula C162H245N81O25·xC2HF3O2
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SMILES
O=C([C@@H](NC(CCCCCCCCCCCCCCCCC)=O)CC1=CNC=N1)N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N)=O)CCCNC(N)=N)=O)CCCNC(N)=N)=O)CCCNC(N)=N)=O)CCCNC(N)=N)=O)CCCNC(N)=N)=O)CCCNC(N)=N)=O)CCCNC(N)=N)=O)CCCNC(N)=N)=O)CC2=CNC=N2)=O)CC3=CNC=N3)=O)CC4=CNC=N4)=O)CC5=CNC=N5)=O)CC6=CNC=N6)=O)CC7=CNC=N7)=O)CC8=CNC=N8)=O)CC9=CNC=N9)=O)CC%10=CNC=N%10)=O)CC%11=CNC=N%11)=O)CC%12=CNC=N%12)=O)CC%13=CNC=N%13)=O)CC%14=CNC=N%14)=O)CC%15=CNC=N%15)=O)CC%16=CNC=N%16
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Sequence
{Stearyl}-His-His-His-His-His-His-His-His-His-His-His-His-His-His-His-His-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-NH2
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Sequence Shortening
{Stearyl}-HHHHHHHHHHHHHHHHRRRRRRRR-NH2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Kinase activity and phosphorylation assays
Kinase activity assays measure the ability of kinases to transfer phosphate groups from ATP to specific substrates, while phosphorylation assays detect the presence and levels of phosphorylated proteins. Common methods include radiolabeled ATP incorporation (e. g. ,), ADP release detection via bioluminescence (e. g. ,[3]), enzyme-linked immunosorbent assays (ELISA) for phospho-specific epitopes (e. g. ,[6]), and microtiter-based formats for high-throughput screening (e. g. ,[8]). The ADP-Glo assay quantifies kinase activity by measuring ADP produced during phosphorylation using a luciferase-based system. Radiometric assays involve autoradiography or scintillation counting after incorporation of 32P-labeled ATP into substrate proteins. ELISA-based approaches rely on phospho-specific antibodies to detect activated kinases in cell lysates or purified samples.
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RNA interference technology
RNA interference (RNAi) is a cellular mechanism that inhibits gene expression by suppressing gene transcription or activating RNA degradation. This mechanism was discovered in plants in 1998 by Andrew Fire and Craig Mello. Today, this phenomenon can be observed in almost all eukaryotes, including protozoa, flies, nematodes, insects, parasites, and mammals.
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Protocol for Kinase activity and phosphorylation assays
Kinase activity assays measure transfer of phosphate from ATP to a protein or peptide substrate, generating phosphorylated substrate, ADP, or incorporated radiolabeled phosphate as the readout; phosphorylation assays measure site-specific phosphorylation in cells or tissues as a proxy for kinase-pathway activation, inhibition, or substrate regulation. Phosphorylation can be detected by phospho-specific Western blot, immunoprecipitation kinase assay, phospho-immunofluorescence, phospho-flow cytometry, luminescent ADP detection, radiolabeled ATP incorporation, or reporter-based pathway assays, and these readouts can be applied to cancer cells, primary neurons, mouse tumors, organoids, inflammatory macrophages, ferroptosis studies, and mitophagy studies when the kinase target is biologically relevant.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)