Home Apoptosis Bcl-6 inhibitor 79-6 (CID5721353) For research use only.

79-6 (CID5721353)

Synonyms: BCL6 inhibitor

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

79-6 (CID5721353) Chemical Structure

79-6 (CID5721353) Chemical Structure

CAS No. 301356-95-6

Purity & Quality Control

Batch: S825001 DMSO]91 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.06%
99.06

79-6 (CID5721353) Related Products

Biological Activity

Description 79-6 (CID5721353) (BCL6 inhibitor) is a BCL6 inhibitor with Kd value of 138 μM.
Targets
Bcl-6 [3]
138 μM(Kd)
In vitro
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].
Cell Research 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).
In Vivo
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].
Animal Research Animal Models SCID mice injected (s.c.) with BCL6-dependent DLBCL cell lines (OCI-Ly7 and SU-DHL6) to form tumors
Dosages 50 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 457.28 Formula

C15H9BrN2O6S2
CAS No. 301356-95-6 SDF --
Smiles C1=CC2=NC(=O)C(=C2C=C1Br)C3=C(N(C(=S)S3)C(CC(=O)O)C(=O)O)O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 91 mg/mL ( (199.0 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

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.

Handling Instructions

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