79-6 (CID5721353)

製品コードS8250 バッチS825001

印刷

化学情報

Chemical Structure Synonyms BCL6 inhibitor Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C15H9BrN2O6S2
分子量 457.28 CAS No. 301356-95-6
Solubility (25°C)* 体外 DMSO 91 mg/mL (199.0 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or 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.

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生物活性

製品説明 79-6 (CID5721353) (BCL6 inhibitor)は、Kd値138 μMのBCL6阻害剤です。
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.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 MCF-7 and MDA231 cells
濃度 200 μM
反応時間 48 h
実験の流れ

MCF-7 and MDA231 cells were plated on the upper chamber of the filters and were treated with vehicle (DMSO) or 79-6 (CID5721353) for 48 hours respectively. The cells invaded to the underside of the filter were counted (magnification, ×200).
動物実験 動物モデル SCID mice injected (s.c.) with BCL6-dependent DLBCL cell lines (OCI-Ly7 and SU-DHL6) to form tumors
投薬量 50 mg/kg
投与方法 i.p.

参考

  • https://pubmed.ncbi.nlm.nih.gov/27881582/
  • https://pubmed.ncbi.nlm.nih.gov/26049022/
  • https://pubmed.ncbi.nlm.nih.gov/27856253/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Balance between immunoregulatory B cells and plasma cells drives pancreatic tumor immunity [ Cell Rep Med, 2022, 3(9):100744] PubMed: 36099917

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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