WRN-IN-26
WRN-IN-26 is an orally active Werner syndrome helicase (WRN) inhibitor with a human Ki value of 58.7 μM and an IC50 value of 0.026 μM. WRN-IN-26 selectively targets the cysteine residues of WRN. WRN-IN-26 induces the expression of p21 protein in MSI-H tumor cells. WRN-IN-26 inhibits the growth of MSI-H tumor cells and exhibits potent in vivo efficacy in MSI-H xenograft tumor models. WRN-IN-26 can be used for the research of microsatellite instability-high (MSI-H) cancers.
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- CAS. Nr.: 3059172-54-9
- Formel: C28H27F3N2O5S
- Molecular Weight:560.58
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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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Helicase 58.7 μM (Ki) |
Helicase 0.026 μM (IC50) |
WRN-IN-26 (compound 26) inhibits WRN helicase DNA unwinding activity with an IC50 of 0.026 μM[1].
WRN-IN-26 inhibits wild-type WRN helicase ATPase activity with an IC50 of 0.023 μM[1].
WRN-IN-26 irreversibly inhibits WRN helicase with an inactivation rate constant (k_inact/Ki) of 459 M-1s-1[1].
WRN-IN-26 induces p21 protein expression in HCT116 MSI-H colorectal tumor cells with an EC50 of 1.8 μM[1].
WRN-IN-26 inhibits viability of HCT116 MSI-H colorectal tumor cells with an IC50 of 0.674 μM, while showing no inhibition of viability in SW620 MSS colorectal tumor cells up to 50 μM, demonstrating synthetic lethality for MSI-H cells[1].
WRN-IN-26 (2 μM; 2 hours) exclusively engages WRN at residue C727 in HCT116 MSI-H colorectal tumor cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | CL | T1/2 | Vss | Bioavailability |
|---|---|---|---|---|---|---|
| Mice[1] | 100 mg/kg | p.o. | 99 mL/min/kg | 0.3 h | 4.9 L/kg | 46 % |
WRN-IN-26 (300 mg/kg; p.o.; twice daily; 21 days) achieves 90% tumor growth inhibition in HCT116 MSI-H xenograft tumors with good tolerability[1].
WRN-IN-26 (300 mg/kg; p.o.; twice daily; 18 days) does not inhibit tumor growth in SW620 MSS xenograft tumors, demonstrating synthetic lethality specific to MSI-H tumors in vivo[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 3059172-54-9
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Molecular Weight 560.58
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Formel C28H27F3N2O5S
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SMILES
O=C(N([C@H]1CS(=O)(C=C1)=O)CC2=CC=NC(C(C)(O)C)=C2)[C@@H](C3=CC=C(C4=CC=C(F)C(F)=C4)C=C3F)OC
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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)
WRN-IN-26 Related Classifications
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