1. Epigenetics Metabolic Enzyme/Protease
  2. Epigenetic Reader Domain E1/E2/E3 Enzyme
  3. 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.

LO-3-61

LO-3-61 Chemical Structure

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Description

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[1].

In Vitro

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.

Western Blot Analysis[1]

Cell Line: HEK293T cells (WT, CUL4DCAF16 C173S, CUL4DCAF16 C178S, DCAF16 KO)
Concentration: 0.1, 1 μM
Incubation Time: 24 h
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.
Molecular Weight

677.60

Formula

C32H30Cl2N8O3S

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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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
LO-3-61
Cat. No.:
HY-175179
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