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Updated: Jan 30, 2026

Anticancer Metal Complexes: Synthesis and Cytotoxicity Evaluation by the MTT Assay
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CB-6644 Is a Selective Inhibitor of the RUVBL1/2 Complex with Anticancer Activity

Victoria A Assimon1, Yangzhong Tang1, Jesse D Vargas1

  • 1Cleave Biosciences, Inc. , Burlingame , California 94010 , United States.

ACS Chemical Biology
|January 15, 2019
PubMed

Insights

Targeting RUVBL1/2 ATPases with CB-6644 shows therapeutic potential in cancer. This novel inhibitor induces cancer cell death and reduces tumor growth in preclinical models, highlighting RUVBLs as promising drug targets.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • RUVBL1 and RUVBL2 are ATPases associated with diverse cellular activities (AAAs) crucial for chromatin remodeling and gene expression.
  • Overexpression of RUVBL1/2 is linked to oncogenesis, tumor growth, and poor prognosis in various cancers.

Purpose of the Study:

  • To investigate the therapeutic potential of inhibiting the RUVBL1/2 complex in cancer treatment.
  • To evaluate the efficacy and specificity of the small-molecule inhibitor CB-6644.

Main Methods:

  • Utilized CB-6644, an allosteric inhibitor targeting RUVBL1/2 ATPase activity.
  • Assessed drug-induced cell death and characterized resistance mechanisms via mutations in RUVBL1 or RUVBL2.
  • Tested CB-6644 efficacy in xenograft models of acute myeloid leukemia and multiple myeloma.

Main Results:

  • CB-6644 specifically interacts with RUVBL1/2 in cancer cells, leading to cell death.
  • Acquired resistance mutations in RUVBL1 or RUVBL2 confirm on-target activity.
  • CB-6644 significantly reduced tumor growth in leukemia and myeloma xenograft models with no apparent toxicity.

Conclusions:

  • Targeting RUVBL1/2 with CB-6644 demonstrates significant therapeutic potential for cancer treatment.
  • CB-6644 is a valuable chemical tool for further research into RUVBL biology and cancer therapeutics.

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