79-6 (CID5721353, BCL6 inhibitor)

Catalog No.S8250

79-6 (CID5721353, BCL6 inhibitor) Chemical Structure

Molecular Weight(MW): 457.28

79-6 (CID5721353) is a BCL6 inhibitor with Kd value of 138 μM.

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Biological Activity

Description 79-6 (CID5721353) is a BCL6 inhibitor with Kd value of 138 μM.
Targets
Bcl-6 [3]
()
138 μM(Kd)
In vitro

Small molecular BCL6 inhibitor 79-6 is a cell-permeable oxindole compound that selectively inhibits the transcriptional repression activity of BCL6 but does not affect BCL6 protein levels[2]. 79-6 binds an aromatic pocket situated in the BTB domain lateral groove, induces disruption of BCL6 transcriptional complexes, reactivation of BCL6 target genes and selective killing of BCL6-dependent DLBCL cells[1]. BCL6 can also interact with MTA3 through its RD2 domain and represses the terminal differentiation. It recruits CtBP through its DBD domain and represses its own expression. 79-6 suppresses invasive ability and colony-forming ability in both of MCF-7 and MDA231 cells. The inhibition of BCL6 with 79-6 enhanced the mRNA expression of E-cadherin in both of MCF-7 and MDA231 cells. 79-6 reverses the functions of BCL6 in the positive regulation of EMT, invasion and transcriptional repression of E-cadherin in breast cancer cells[2].

In vivo

Administration of 50 mg/kg/day 79-6 to SCID mice induced a 65-70% reduction in the size of established BCL6-dependent DLBCL xenografts, but had no effect on BCL6-independent DLBCLs[1]. Therapeutic targeting of BCL6 with the small molecule 79-6 is an effective antilymphoma strategy in vivo[3].

Protocol

Cell Research:

[2]

+ Expand
  • Cell lines: MCF-7 and MDA231 cells
  • Concentrations: 200 μM
  • Incubation Time: 48 h
  • Method:

    MCF-7 and MDA231 cells were plated on the upper chamber of the filters and were treated with vehicle (DMSO) or 79-6 (200 µmol/L) for 48 hours respectively. The cells invaded to the underside of the filter were counted (magnification, ×200).


    (Only for Reference)
Animal Research:

[3]

+ Expand
  • Animal Models: SCID mice injected (s.c.) with BCL6-dependent DLBCL cell lines (OCI-Ly7 and SU-DHL6) to form tumors
  • Formulation: 10% DMSO
  • Dosages: 50 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 91 mg/mL (199.0 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 457.28
Formula

C15H9BrN2O6S2

CAS No. 301356-95-6
Storage powder
in solvent
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID