2. PROTAC Epigenetics
  3. PROTACs Epigenetic Reader Domain
  4. LGF308

LGF308 is a PROTAC degrader of BRD4 that exhibits selective cytotoxicity toward cancer cells over normal cells. LGF308 mediates the formation of a ternary complex between BRD4 and DCAF11 to achieve BRD4 degradation. LGF308 induces tumor cell apoptosis by upregulating apoptosis-related proteins. LGF308 inhibits tumor cell proliferation and migration in breast cancer and triple-negative breast cancer cell lines. LGF308 can be used for the research of breast cancer.
(Pink: BRD4 ligand (HY-78695); Blue: DCAF11 ligand (HY-W288798); Black: linker).

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LGF308

LGF308 Chemical Structure

CAS No. : 3061406-69-4

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LGF308 Related Antibodies

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Description

LGF308 is a PROTAC degrader of BRD4 that exhibits selective cytotoxicity toward cancer cells over normal cells. LGF308 mediates the formation of a ternary complex between BRD4 and DCAF11 to achieve BRD4 degradation. LGF308 induces tumor cell apoptosis by upregulating apoptosis-related proteins. LGF308 inhibits tumor cell proliferation and migration in breast cancer and triple-negative breast cancer cell lines. LGF308 can be used for the research of breast cancer[1]. (Pink: BRD4 ligand (HY-78695); Blue: DCAF11 ligand (HY-W288798); Black: linker).

In Vitro

LGF308 (10 nM-1 μM; 12 h) potently induces BD1 degradation in BD1-HEK293T reporter cells at concentrations as low as 10 nM for 12 h[1].
LGF308 (0.1-5 μM; 3-9 h) induces time- and concentration-dependent degradation of BRD4 in MDA-MB-231 cells, with DC50 values of 0.50 μM (long isoform) and 0.23 μM (short isoform) and maximal degradation of >90% at 5 μM for 9 h[1].
LGF308 (1 μM) induced BRD4 degradation in MDA-MB-231 cells is dependent on the ubiquitin-proteasome pathway, not the lysosomal pathway[1].
LGF308 (0.1-10 μM; 12 h) induces BRD4/BD1 degradation in BD1-HEK293T and CRISPRi HEK293T cells that is DCAF11-dependent[1].
LGF308 (1 μM; 6 h) promotes formation of a ternary complex between BD1 and DCAF11 in HEK293T cells[1].
LGF308 (gradient concentrations; 48 h) selectively inhibits proliferation of breast cancer cell lines, with the highest potency in MDA-MB-468 cells (IC50 = 0.70 μM) and lower potency in normal HEK293T cells (IC50 = 16.01 μM) after 48 h treatment[1].
LGF308 (1 μM) induces apoptosis in MDA-MB-231 cells, as shown by upregulated c-PARP-1 and c-Caspase-7 levels[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

LGF308 Related Antibodies

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.1 μM, 0.5 μM, 1 μM, 2 μM, 5 μM (9 h treatment); 1 μM (3 h, 6 h, 9 h treatments)
Incubation Time: 3 h, 6 h, 9 h (1 μM treatment); 9 h (0.1-5 μM treatments)
Result: Reduced BRD4 levels to ~60% of control after 3 h of 1 μM treatment.
Dropped BRD4 levels to ~40% of control by 6 h of 1 μM treatment.
Degraded over 90% of both long and short BRD4 isoforms at 5 μM, with a DC50 of 0.50 μM for the long isoform and 0.23 μM for the short isoform.

Cell Proliferation Assay[1]

Cell Line: MCF-7, T-47D, MDA-MB-231, MDA-MB-157, MDA-MB-468, HCC1937, BT-549 (breast cancer cell lines), HEK293T (normal cell line)
Concentration: Gradient concentrations
Incubation Time: 48 h
Result: Inhibited proliferation of breast cancer cell lines with IC50 values of 2.86 μM (MCF-7), 2.22 μM (T-47D), 1.31 μM (MDA-MB-231), 3.10 μM (MDA-MB-157), 0.70 μM (MDA-MB-468), 1.45 μM (HCC1937), 1.60 μM (BT-549).
Resulted in an IC50 of 16.01 μM for normal HEK293T cells, significantly higher than cancer cell lines.
Parmacokinetics
Species Dose Route T1/2 Vdss MRT0-inf CL Cmax AUC0-t AUC0-∞
Rat[1] 3 mg/kg i.v. 3.84 h 0.08 L/kg 1.72 h 0.73 mL/min/kg 30,833.3 ng/mL 114,985 115,124
Molecular Weight

732.27

Formula

C35H34ClN7O5S2
CAS No.
SMILES

O=C(N1CCCCCCNC(C[C@@H]2N=C(C3=C(N4C2=NN=C4C)SC(C)=C3C)C5=CC=C(C=C5)Cl)=O)/C(SC1=O)=C/C6=CC([N+]([O-])=O)=CC=C6
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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LGF308 Related Classifications

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Help & FAQs
  • 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.

Keywords:

LGF3083061406-69-4LGF 308LGF-308PROTACsEpigenetic Reader DomainHEK293T cellsMDA-MB-468 cellsbreast cancerDCAF11triple-negative breast cancerE3 ligaseMDA-MB-231 cellsproteasomal pathwayBRD4apoptosisInhibitorinhibitorinhibit

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