An inhibitor of SRE activation in PC3 cells (IC50 = 6.4 μM)

CCG-203971 – 25 mg

Brand:
Cayman
CAS:
1443437-74-8
Storage:
-20
UN-No:
Non-Hazardous - /

Signaling through small G proteins of the RhoA subfamily, including RhoC, induces actin-regulated cytosolic-to-nuclear translocation of the oncogene product megakaryoblastic leukemia 1 (MKL1), which binds to serum response factor (SRF).{15012} The MKL1/SRF complex, in turn, activates the transcription of serum response element (SRE) regulated genes, stimulating cell migration, a process that is central to metastasis.{15012} CCG-203971 is an inhibitor of SRE activation in the prostate cancer cell line PC-3 (IC50 = 6.4 μM), with 87% inhibition of SRE activation achieved at 100 μM.{25536} This compound also inhibits PC-3 cell migration (IC50 = 4.2 μM), as determined by a scratch wound assay.{25536} CCG-203971 causes no cytotoxicity when evaluated by WST-1 assay.{25536} It is well tolerated in normal mice up to doses of 100 mg/kg given intraperitoneally over five days.{25536}  

 

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Description

An inhibitor of SRE activation in PC3 cells (IC50 = 6.4 μM), with 87% inhibition of SRE activation achieved at 100 μM; inhibits PC3 cell migration (IC50 = 4.2 μM), as determined by a scratch wound assay; causes no cytotoxicity when evaluated by WST-1 assay

Formal name: N-(4-chlorophenyl)-1-[3-(2-furanyl)benzoyl]-3-piperidinecarboxamide

Synonyms: 

Molecular weight: 408.9

CAS: 1443437-74-8

Purity: ≥90%

Formulation: A crystalline solid

Product Type|Biochemicals||Research Area|Cancer|Cell Migration & Metastasis

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