2. Epigenetics PROTAC
  3. Epigenetic Reader Domain PROTACs
  4. GXF-111

GXF-111, a PROTAC molecule, can promote selective degradation of cellular BRD3 and BRD4-L. GXF-111 has binding affinities for BRD3 BD1 and BRD3 BD2 with Ki values of 11.97 nM and 2.35 nM, respectively. GXF-111 can be used for the research of cancer.

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GXF-111 Chemical Structure

GXF-111 Chemical Structure

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GXF-111 Related Antibodies

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Description

GXF-111, a PROTAC molecule, can promote selective degradation of cellular BRD3 and BRD4-L. GXF-111 has binding affinities for BRD3 BD1 and BRD3 BD2 with Ki values of 11.97 nM and 2.35 nM, respectively. GXF-111 can be used for the research of cancer[1].

IC50 & Target

Ki: 11.97 nM (BRD3 BD1); 2.35 nM (BRD3 BD2) [1].
IC50: 6.31 nM (MV4-11 cell); 95.2 nM (MM.1 S cell) [1].
In Vitro

GXF-111 (Compound 24) has binding affinities for BRD3 BD1 and BRD3 BD2 with Ki values of 11.97 nM and 2.35 nM, respectively[1].
GXF-111 has cellular activities in MV4-11 and MM.1 S cell lines with IC50 values of 6.31 nM and 95.2 nM, respectively[1].
GXF-111 (2, 10 nM; 24 h) has potent cell growth inhibition activities for degradation of BET family proteins in MM.1 S cells[1].
GXF-111 (4 days) has anti-proliferative activity in 7 human cancer cell lines with IC50 values range from 6.31 nM to 17.25 μM[1].

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

GXF-111 Related Antibodies

Western Blot Analysis[1]

Cell Line: MM.1 S cells；MM.1 S, HGC-27, and MCF-7 cells；Multiple cancer cell lines
Concentration: 2, 10 nM; 0.1, 0.3, 1, 3 nM; 30 nM; 3, 10, 30, 100, 300 nM
Incubation Time: 24 h; 8 h; 1, 3, 6, 8, 24 h; 24 h
Result: Efficiently depleted BRD3 and BRD4-L in MM.1 S cells at 2 nM.
Dose-dependently depleted BRD3 and BRD4-L and partially depleted BRD2 at 10 nM.
Had good degradation kinetics of BET proteins in three selected cancer cell lines, i.e. MM.1S, MCF-7, and HGC-27 cells.
Only BRD3 and BRD4-L, were depleted dose-dependently in five cancer cell lines, i.e. HGC27, MCF-7, A549, Hela, and HepG2 cells.

Cell Cycle Analysis[1]

Cell Line: MM.1 S cell
Concentration: 1, 3, 10, 30, 100, 300 nM
Incubation Time: 24 h
Result: Dose-dependently induced cell cycle arrest at G1 phase.
Molecular Weight

728.28

Formula

C42H42ClN7O3
SMILES

O=C1N(C2C(NC(CC2)=O)=O)CC3=C1C=CC=C3CCCCNCC4=CC=C(C5=CC=C6C(C(NC7=CC=C(Cl)C=C7)CCC8=NN=C(C)N86)=C5)C=C4
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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GXF-111 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:

GXF-111GXF111GXF 111Epigenetic Reader DomainPROTACsPROTACBRD3BRD4-Lcanceranti-tumorInhibitorinhibitorinhibit

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