LO-3-61
LO-3-61, a JQ-1 (HY-13030) analog bearing a truncated fumaramide handle, is a PROTAC (proteolysis-targeting chimeras)-like BRD4 degrader. LO-3-61 degrades both the long and short isoforms of BRD4 CUL4DcAr16-dependently in cells. LO-3-61 shows selectivity for BRD3 and BRD4 degradation in MDA-MB-231 cells.
For research use only. We do not sell to patients.
- Formula: C32H30Cl2N8O3S
- Molecular Weight:677.60
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
LO-3-61 (0.1-1 μM, 24 h) leads to the proteasome mediated degradation of BRD4 in HEK293T cells (WT, CUL4DCAF16 C173S, CUL4DCAF16 C178S), an effect that can be inhibited in DCAF16 KO cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293T cells (WT, CUL4DCAF16 C173S, CUL4DCAF16 C178S, DCAF16 KO)
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Concentration:0.1, 1 μM
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Incubation Time:24 h
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Result:Degraded BRD4 when BTZ (1 μM) for 1 h prior to treatment in HEK293T cells (WT, CUL4DCAF16 C173S, CUL4DCAF16 C178S).
Did not affect the degradation of BRD4 in DCAF16 KO cells.
Chemical Information
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Molecular Weight 677.60
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Formula C32H30Cl2N8O3S
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SMILES
O=C(NC1=CC(Cl)=CN=C1)/C=C/C(N2CCN(C(C[C@H]3C4=NN=C(C)N4C5=C(C(C)=C(C)S5)C(C6=CC=C(Cl)C=C6)=N3)=O)CC2)=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)
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