Home Apoptosis Bcl-6 inhibitor 79-6 (CID5721353)

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79-6 (CID5721353) Bcl-6 inhibitor

Cat.No.S8250

79-6 (CID5721353), a BCL6 inhibitor, has a Kd value of 138 μM.
79-6 (CID5721353) Bcl-6 inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 457.28

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 91 mg/mL (199.0 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 457.28 Formula

C15H9BrN2O6S2

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 301356-95-6 -- Storage of Stock Solutions

Synonyms BCL6 inhibitor Smiles C1=CC2=NC(=O)C(=C2C=C1Br)C3=C(N(C(=S)S3)C(CC(=O)O)C(=O)O)O

Mechanism of Action

Targets/IC50/Ki
Bcl-6
138 μM(Kd)
In vitro

Small molecular BCL6 inhibitor 79-6 (CID5721353) is a cell-permeable oxindole compound that selectively inhibits the transcriptional repression activity of BCL6 but does not affect its protein levels. It 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. 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. This compound 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. It reverses the functions of BCL6 in the positive regulation of EMT, invasion and transcriptional repression of E-cadherin in breast cancer cells.
In vivo

Administration of 50 mg/kg/day 79-6 (CID5721353) 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. Therapeutic targeting of BCL6 with this compound is an effective antilymphoma strategy in vivo.
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