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.
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- Formule: C162H245N81O25·xC2HF3O2
- Masse moléculaire:3727.21 (free base)
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Activité biologique
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Chemical Information
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- Pureté et documentation
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Activité biologique
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.
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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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Masse moléculaire 3727.21 (free base)
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NP1 peptide Related Classifications
HY-P12278 Related Classifications
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