PTC-IN-1
PTC-IN-1 is a human ribosomal peptidyl transferase center (PTC) inhibitor. PTC-IN-1 forms stable interactions with 28S rRNA and undergoes steric-hindrance electrostatic interactions with nascent polypeptide chains, thereby inducing context-dependent translation arrest. PTC-IN-1 activates the ribotoxic stress response through phosphorylation of p46 and p54 JNK, triggers ribosome collisions, and activates the integrated stress response via phosphorylation of eIF2α. PTC-IN-1 inhibits the proliferation of cancer cells. PTC-IN-1 can be used in the research of triple-negative breast cancer, prostate cancer, colorectal cancer.
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- CAS. Nr.: 3079914-21-6
- Formel: C20H23FN2O4
- Molecular Weight:374.41
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
eIF2-α |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| 22Rv1 | EC50 |
0.077 μM
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Antiproliferative activity against human 22Rv1 prostate cancer cells assessed as reduction in cell viability incubated for 72 hrs by fluorescent cell viability assay.
Antiproliferative activity against human 22Rv1 prostate cancer cells assessed as reduction in cell viability incubated for 72 hrs by fluorescent cell viability assay.
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41735331 |
| HCC1143 | EC50 |
0.140 μM
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Antiproliferative activity against human HCC-1143 triple-negative breast cancer cells assessed as reduction in cell viability incubated for 72 hrs by fluorescent cell viability assay.
Antiproliferative activity against human HCC-1143 triple-negative breast cancer cells assessed as reduction in cell viability incubated for 72 hrs by fluorescent cell viability assay.
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41735331 |
| LS-411N | EC50 |
0.191 μM
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Antiproliferative activity against human LS411N colorectal cancer cells assessed as reduction in cell viability incubated for 72 hrs by fluorescent cell viability assay.
Antiproliferative activity against human LS411N colorectal cancer cells assessed as reduction in cell viability incubated for 72 hrs by fluorescent cell viability assay.
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41735331 |
| MCF7 | EC50 |
0.295 μM
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Antiproliferative activity against human MCF7 breast cancer cells assessed as reduction in cell viability incubated for 72 hrs by fluorescent cell viability assay.
Antiproliferative activity against human MCF7 breast cancer cells assessed as reduction in cell viability incubated for 72 hrs by fluorescent cell viability assay.
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41735331 |
| MRC5 | EC50 |
0.456 μM
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Antiproliferative activity against human MRC-5 normal fibroblasts assessed as reduction in cell viability incubated for 72 hrs by fluorescent cell viability assay.
Antiproliferative activity against human MRC-5 normal fibroblasts assessed as reduction in cell viability incubated for 72 hrs by fluorescent cell viability assay.
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41735331 |
In Vitro
PTC-IN-1 (IDB-002) (0.08-10 μM; 60 min) induces context-dependent translational elongation arrest in HCC-1143 cells, with a preference for aliphatic residues at position -1 of nascent polypeptide chains[1].
PTC-IN-1 (0.3-30 μM) exhibits sequence-specific translational inhibitory activity in vitro, with its potency toward the aliphatic-rich tetramer motif reporter gene being up to 18-fold higher than that toward the acidic motif-rich reporter gene[1].
PTC-IN-1 (50 μM; 30 min) binds to the PTC of human 80S ribosomes and forms sequence-specific spatial interactions with the aliphatic residues of the FPAK nascent polypeptide chain[1].
PTC-IN-1 (0.001-100 μM; 15 min for HCC-1143, 15 min to 8 h for MCF7) activates ribotoxic stress responses in HCC-1143 and MCF7 cells via rapid and sustained JNK phosphorylation, a process associated with increased ribosome collisions[1].
PTC-IN-1 (72 h) inhibits the proliferation of various MYC-dependent cancer cell lines with EC50 values of 0.077, 0.14, 0.191, 0.295, and 0.456 μM against 22RV1, HCC-002, LS411N, MCF7, and MRC-5, respectively, and shows weak potency against normal MRC-5 fibroblasts[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCC-1143, MCF7
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Concentration:0.001, 0.01. 0.1, 1, 10, 100 μM (HCC-1143 cells, 15 min incubation); 10 μM (MCF7 cells)
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Incubation Time:15 min (HCC-1143 cells; MCF7 cells: 15 min, 2 h, 4 h, 8 h)
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Result:Rapidly induced robust phosphorylation of both p46 and p54 JNK isoforms within 15 min in HCC-1143 cells.
Maintained strong JNK phosphorylation over 8 h in MCF7 cells.
Induced modest p38 phosphorylation in MCF7 cells after 2 h of treatment.
Detected eIF2α phosphorylation in MCF7 cells after 8 h of treatment.
Revealed a peak suggestive of ribosome collisions upstream of pause sites via metagene analysis of ribosome footprints, indicating higher collision frequency compared to IDB-001.
Chemical Information
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CAS. Nr. 3079914-21-6
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Molecular Weight 374.41
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Formel C20H23FN2O4
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SMILES
FC1=CC=CC(CNC(O[C@H]([C@H](CN2)O)[C@H]2CC3=CC=C(C=C3)OC)=O)=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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