BJP-06-005-3
BJP-06-005-3 is a selective Pin1 inhibitor with a Ki value of 48 nM. BJP-06-005-3 induces the degradation of mutant KRAS. BJP-06-005-3 inhibits pancreatic ductal adenocarcinoma via the Pin1-mediated pathway. BJP-06-005-3 is used in studies related to KRAS-mutant pancreatic ductal adenocarcinoma.
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- CAS No.: 2400958-08-7
- Formule: C37H48ClN7O7
- Masse moléculaire:738.27
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Description
IC50 & Target
[1]|
K-RAS |
In Vitro
BJP-06-005-3 is a highly selective peptide-based covalent Pin1 inhibitor that achieves potent Pin1 inhibition with an IC50 of 48 nM through specific covalent modification of the active site Cys113 residue[1].
BJP-06-005-3 (12 h) is a high-affinity covalent binder of recombinant Pin1 with an apparent Ki of 15 nM following 12 h incubation[2].
BJP-06-005-3 (12 h) potently inhibits the enzymatic isomerase activity of recombinant Pin1 with an apparent Ki of 48 nM[2].
BJP-06-005-3 (4 days) impairs 3D spheroid transformation in a Pin1-selective manner in PATU-8988T PDAC cells[2].
BJP-06-005-3 (10 μM; 4 h) induces broad transcriptional remodeling in PATU-8988T PDAC cells after 4 h of treatment, with Myc target genes ranked among the most highly enriched transcription factor-associated gene sets[2].
BJP-06-005-3 potently impairs KRAS-mutated PDAC cell function by disrupting Pin1-dependent downstream pathways and driving degradation of oncogenic mutant KRAS[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2400958-08-7
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Masse moléculaire 738.27
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Formule C37H48ClN7O7
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SMILES
O=C([C@H]1N(CCCC1)C([C@@H](N(C)C(CCl)=O)CC2=CC=CC=C2)=O)N[C@H](C(N[C@H](C(OCC)=O)CCCNC(N)=O)=O)CC3=CNC4=CC=CC=C34
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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)