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Synonyms | BCL6 inhibitor | Storage (From the date of receipt) |
3 years -20°C powder | |
化学式 | C15H9BrN2O6S2 |
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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 | |||
* <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. |
製品説明 | 79-6 (CID5721353) (BCL6 inhibitor) is a BCL6 inhibitor with Kd value of 138 μM. |
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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]. |
細胞アッセイ | 細胞株 | MCF-7 and MDA231 cells |
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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 (200 µmol/L) for 48 hours respectively. The cells invaded to the underside of the filter were counted (magnification, ×200). |
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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. |
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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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