A small molecule stimulator of SRC-1

MCB-613 – 25 mg

Brand:
Cayman
CAS:
296792-62-6
Storage:
-20
UN-No:
Non-Hazardous - /

The p160 steroid receptor coactivator (SRC) family, SRC-1/NCOA1, SRC-2/NCOA2/TIF2/GRIP1, and SRC-3/NCOA3/AIB1/RAC3/ACTR/pCIP, interact with nuclear receptors and other transcription factors to drive target gene expression and integrate growth signaling pathways on which cancer cells rely. MCB-613 is a small molecule stimulator of SRC-1, SRC-2, and SRC-3 that has been used to disrupt cancer cell homeostatic dependence on SRCs.{29318} MCB-613 can increase the interaction of SRCs with the coactivators CBP and CARM1 and can induce ER stress coupled to the generation of reactive oxygen species.{29318} Overactivation of SRCs by 1-7 µM MCB-613 was shown to selectively and dose dependently induce paraptosis in a variety of cancer cells in vitro but not in normal cells.{29318} At 20 mg/kg, MCB-613 was also shown to inhibit tumor growth in an MCF-7 breast cancer xenograft model in mice.{29318}  

 

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Description

A small molecule stimulator of SRC-1, SRC-2, and SRC-3 that selectively induces paraptosis in a variety of cancer cells in vitro and reduces tumor growth in a xenograft mouse model; can increase the interaction of SRCs with the coactivators CBP and CARM1 and can induce ER stress coupled to the generation of reactive oxygen species

Formal name: 4-​ethyl-​2,​6-​bis(3-​pyridinylmethylene)​-cyclohexanone

Synonyms: 

Molecular weight: 304.4

CAS: 296792-62-6

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|SRC Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Death||Research Area|Cell Biology|Endomembrane System & Vesicular Trafficking||Research Area|Epigenetics, Transcription, & Translation|Transcription Factors

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