And1 degrader 1
And1 degrader 1 is an acidic nucleoplasmic DNA-binding protein 1 (And1) molecular glue-like degrader. And1 degrader 1 binds to the WD40 domain of And1 in a 'V' conformation to induce And1 degradation via the ubiquitin-proteasome pathway. And1 degrader 1 exhibits antiproliferative activity via synthetic lethal interaction with a PARP1 inhibitor to inhibit proliferation of cancer cells. And1 degrader 1 can be used for the research of non-small cell lung cancer (NSCLC).
For research use only. We do not sell to patients.
- CAS No.: 3029132-46-2
- Formula: C26H27Cl2N3O
- Molecular Weight:468.42
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Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
Description
In Vitro
And1 degrader 1 (A15) (1-10 μM; 3-48 h) induces time- and dose-dependent degradation of And1 in A549 and H460 NSCLC cells via the ubiquitin-proteasome pathway, with 5 μM reducing And1 levels by 19-38% after 48 h[1].
And1 degrader 1 (5 μM; 24-96 h) acts synergistically with 1 μM Olaparib (HY-10162) to significantly inhibit proliferation of A549 and H460 NSCLC cells, despite showing no significant activity when used alone[1].
And1 degrader 1 (5 μM; 2 weeks) combined with 1 μM Olaparib reduces clone formation by 50% in A549 and H460 NSCLC cells, despite showing minimal activity when used alone[1].
And1 degrader 1 (5 μM; 48 h) reduces BRCA1 and BRCA2 expression and increases DNA damage (γ-H2AX foci) in A549 NSCLC cells, with enhanced effects observed when combined with 1 μM Olaparib[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human NSCLC cell lines A549 and H460
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Concentration:1 μM (48 h); 2.5 μM (48 h); 5 μM (48 h); 10 μM (3 h, 6 h, 12 h, 24 h, 48 h)
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Incubation Time:3 h, 6 h, 12 h, 24 h, 48 h
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Result:Induced dose-dependent degradation of And1 in both cell lines at 48 h, with degradation detectable at 1 μM.
Reduced And1 levels by 38% in H460 cells and 19% in A549 cells at 5 μM and 48 h.
Had its And1-degrading effect blocked when co-treated with MG132.
Induced detectable And1 degradation as early as 3 h at 10 μM, with significant degradation observed up to 48 h.
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Cell Line:human NSCLC cell lines A549 and H460
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Concentration:5 μM; 5 μM in combination with 1 μM Olaparib
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Incubation Time:24 h, 48 h, 72 h, 96 h
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Result:Showed no significant antiproliferative activity in A549 or H460 cells when used alone compared to controls.
Significantly inhibited cell proliferation in both cell lines when combined with 1 μM Olaparib.
Exhibited synergistic activity with CDI values of 0.77 for A549 cells and 0.92 for H460 cells at 48 h.
Chemical Information
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CAS No. 3029132-46-2
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Molecular Weight 468.42
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Formula C26H27Cl2N3O
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SMILES
OC1=CC=C(/C=C/C2=CC=C(Cl)C(Cl)=C2)C=C1CNC3=CC=C(N4CCN(C)CC4)C=C3
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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)
And1 degrader 1 Related Classifications
HY-162896 Related Classifications
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