OICR-41103
OICR-41103 is a selective DCAF1 WDR domain binder with Kd <2 nM. OICR-41103 has no effect on the p53/MDM2 protein-protein interaction. OICR-41103 can be used for HIV research.
For research use only. We do not sell to patients.
- Formula: C28H26Cl2F2N4O3
- Molecular Weight:575.43
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[2]|
DCAF1 <2 nM (Kd) |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| NCI-H460 | EC50 |
165 nM
|
Thermal stabilization of Flag-HiBiT-tagged DCAF1 WDR domain in NCI-H460 cells after 3 hrs incubation measured by cellular thermal shift assay with luminescence readout.
Thermal stabilization of Flag-HiBiT-tagged DCAF1 WDR domain in NCI-H460 cells after 3 hrs incubation measured by cellular thermal shift assay with luminescence readout.
|
40683980 |
| HEK-293T | EC50 |
128 nM
|
Displacement of DCAF1 tracer in HEK293T cells expressing NanoLuc-tagged DCAF1 WDR domain after 1 hr incubation measured by NanoBRET.
Displacement of DCAF1 tracer in HEK293T cells expressing NanoLuc-tagged DCAF1 WDR domain after 1 hr incubation measured by NanoBRET.
|
40683980 |
In Vitro
OICR-41103 (20 µM) has a thermal stabilizing effect on the DCAF1 WDR domain, with a maximum ΔTm of 23.0 °C at 20 µM[2].
OICR-41103 (up to 20 µM) shows no significant binding to WDR61, WDR92, WDR5, DDB1, FBXW7, or PAFAH1B1 at concentrations up to 20 µM[2].
OICR-41103 (3 h) exerts a thermal stabilizing effect on the DCAF1 WDR domain in NCI-H460 cells, with an EC50 of 165 nM[2].
OICR-41103 (1 h) displaces the DCAF1 tracer with an EC50 of 128 nM in HEK293T cells[2].
OICR-41103 (3 h) disrupts the DCAF1 WDR-Vpr interaction in HEK293EMT cells with an EC50 of 1 µM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293T, MCF7, U2OS, and HCT116 cells
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Concentration:Up to 3 µM
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Incubation Time:5 days (topped up after 3 days)
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Result:Cell confluency was not affected in HEK293T, MCF7, U2OS, or HCT116 cells up to 3 µM over 5 days.
Chemical Information
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Molecular Weight 575.43
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Formula C28H26Cl2F2N4O3
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SMILES
NC(C[C@@H](C1=CC=C(C(Cl)=C1)F)NC(C2=CNC(/C=C/C(N3CCCCC3)=O)=C2C4=C(C=C(C=C4)Cl)F)=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)