NCP26 TFA
Based on 1 Customer Validation
NCP26 TFA 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 TFA activates AAR, induces G0/G1 phase arrest, Apoptosis, Caspase cleavage, and PARP cleavage. NCP26 TFA downregulates MYC, TCF3, and CCND1. NCP26 TFA inhibits the growth of multiple myeloma cells. NCP26 TFA can be used for the research of multiple myeloma.
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- Fòrmula: C22H24F3N5O4
- Peso molecular:479.45
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
Caspase 8 |
Caspase 9 |
Caspase 3 |
In Vitro
NCP26 TFA 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) TFA 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) TFA 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 TFA 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) TFA 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.
In Vivo
NCP26 (10 mg/kg; q.d. [daily]) TFA 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.
Chemical Information
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Appearance Solid
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Peso molecular 479.45
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Fòrmula C22H24F3N5O4
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SMILES
O=C(C1=NC=CN=C1NC(N2CCCCC2)=O)NC3CC4=C(C3)C=CC=C4.O=C(O)C(F)(F)F
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NCP26 TFA Related Classifications
HY-183004A Related Classifications
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