SMI-4a

• Background:

  The serine/threonine Pim kinases have been suggested to promote the activity of the rapamycin-sensitive mammalian target of rapamycin (mTORC1), which regulates cell growth and survival. Pim kinases are overexpressed in solid cancers and hematologic malignancies, and as such have become targets of small molecule inhibitors to prevent the progression of various cancers. SIM-4a is a Pim kinase inhibitor that blocks mTORC1 activity via activation of AMPK.1 SMI-4a has been found to inhibit prostate cancer cell growth and induce G1 phase cell-cycle arrest in precursor T-cell lymphoblastic leukemia/lymphoma cell lines.

• Description:

  SMI-4a is a potent inhibitor of Pim1 with IC50 = 17 -21 nM. It does not significantly inhibit other serine/threonine- or tyrosine-kinases. It induces G1 phase cell cycle arrest and induces apoptosis through the mitocondrial pathway. It downregulates c-myc and induces p27Kip1 expression. Inhibits PRAS40 phosphorylation and mTOR activity, as well as the mammalian target of rapamycin C1 (mTORC1) pathway. SMI-4a is a potential anti-cancer compound that blocks prostate cancer growth.

• Format:

  White to beige powder

• Solubility:

  Soluble in DMSO

• Molecular Formula:

  C11H6F3NO2S

• Shipping Conditions:

  Room Temperature (continental US) or Gel Packs

• Storage Conditions:

  Store at or below –20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.

• Calculated Molecular Weight:

  273.2 Da

• CAS Number:

  438190-29-5