NCP26
NCP26 is an ATP-competitive ProRS inhibitor (with a KD of 271 nM in the absence of proline, and a KD of 0.35 nM in the presence of 100 μM proline). NCP26 activates AAR, induces G0/G1 phase arrest, Apoptosis, Caspase cleavage, and PARP cleavage. NCP26 downregulates MYC, TCF3, and CCND1. NCP26 inhibits the growth of multiple myeloma cells. NCP26 can be used for the research of multiple myeloma.
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- CAS 番号: 2396683-89-7
- 分子式: C20H23N5O2
- 分子量:365.44
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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NCP26 is an ATP-competitive inhibitor of recombinant ProRS. Its binding affinity increases by more than 750-fold in the presence of 100 μM proline, with a KD of 0.35 nM[1].
NCP26 (0.5 μM; 48 h) maintains antiproliferative activity against AMO1 and RPMI 8226 multiple myeloma (MM) cells over a proline concentration range of 0 to 20 mM, with no reduction in its potency at high proline levels[1].
NCP26 (0.01-10 μM; 96 h) is 10-fold more potent against AMO1 multiple myeloma (MM) cells than against peripheral blood mononuclear cells (PBMCs) from healthy donors, with an EC50 of 0.1 μM for the former and approximately 1 μM for the latter after 96 h of treatment[1].
NCP26 potently inhibits the growth of most multiple myeloma (MM) cell lines, with EC50 values ranging from 135 nM to 1.1 μM[1].
NCP26 (0.5 μM; 6-48 h) induces G0/G1 cell cycle arrest and caspase-dependent apoptosis in AMO1 and RPMI 8226 multiple myeloma (MM) cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:AMO1, RPMI 8226 MM cell lines
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Concentration:0.5 μM
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Incubation Time:6 h, 24 h, 48 h
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Result:Induced G0/G1 cell cycle arrest in both cell lines at 6 h, with enhanced arrest observed at 24 h.
Induced apoptotic cell death, evidenced by increased Annexin-V+ cells, sub-G1 populations, and mitochondrial damage.
Induced time- and dose-dependent cleavage of caspases-3, -8, -9, and PARP.
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Cell Line:AMO1, RPMI 8226 MM cell lines
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Concentration:0-1 μM
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Incubation Time:6 h
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Result:Dose-dependently reduced protein levels of MYC, PIM2, CCND1, and TCF3 in both cell lines.
Mirrored the effects of EPRS shRNA knockdown on MYC, PIM2, CCND1, and TCF3 protein levels.
NCP26 (10 mg/kg; q.d. [daily]) significantly inhibits multiple myeloma tumor growth (P = 0.005) and prolongs host survival (P < 0.001) in an AMO1 xenograft mouse model without inducing weight loss[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CB17 SCID (5-week-old female, subcutaneously inoculated with AMO1 cells)[1]
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Dosage:2.5 mg/kg; 10 mg/kg
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Administration:i.p.; once daily; 21 days
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Result:Significantly inhibited AMO1 tumour growth compared to vehicle control (control vs.
2.5 mg/kg, P = 0.01; control vs.
10 mg/kg, P < 0.001).
Resulted in greater tumour growth inhibition at 10 mg/kg dose than 2.5 mg/kg dose.
Caused no significant body weight loss in either treatment cohort.
Significantly prolonged overall survival compared to vehicle control (control vs.
2.5 mg/kg, P = 0.01; control vs.
10 mg/kg, P < 0.001).
Downregulated MYC, CCND1, and TCF3, and induced p-GCN2 and DDIT3 in treated tumours.
化学情報
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CAS 番号 2396683-89-7
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分子量 365.44
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分子式 C20H23N5O2
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SMILES
O=C(NC1CC=2C=CC=CC2C1)C3=NC=CN=C3NC(=O)N4CCCCC4
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
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