Name: Ro 3306
Price: 220.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    RO-3306 is an ATP-competitive, potent cyclin-dependent kinase (CDK) 1 inhibitor with Ki values of 35 and 110 nM for cdk1/cyclin B1 and cdk1/cyclin A, respectively.Cell cycle progression is regulated by a series of CDKs. Cdk1 controls the cell cycle entry into mitosis. It forms a bipartite complex with cyclin B and phosphorylates a spectrum of substrates that coordinate nuclear envelope breakdown, chromosome condensation, assembly of the mitotic spindle and activation of the spindle assembly checkpoint. CDK1 inhibitor RO-3306 was reported to impair BRCA1 localization to DSBs, and consistent with this, suppressed RAD51 focus formation in DU145 cells when applied at the GI50 (1μM). Co-treatment of 100 nM AZ12253801 and 1 μM RO-3306 manifested a marked increase in pre-G1DNA, indicating apoptosis induction. In viability assays, RO-3306 induced a significant shift to the left of the AZ12253801 dose-response curve, with 2.4-fold reduction in GI50, comparable to RAD51 depletion or inhibition. At sub-50nM AZ12253801 concentrations there was more striking sensitization, with 13-fold reduction in GI80. Paralleling effects of RAD51 knockdown, RO-3306 did not affect AZ12253801 sensitivity of PC3 or LNCaP cells, but did sensitize 22Rv1 cells.
    
    [1]. Lodhia KA, Gao S, Aleksic T, et al. Suppression of homologous recombination sensitizes human tumor cells to IGF-1R inhibition. Int J Cancer. 2014 Nov 12.
- Properties
  - Alternative Name
    
    (Z)-5-(quinolin-6-ylmethylene)-2-((thiophen-2-ylmethyl)amino)thiazol-4(5H)-one
    
    CAS Number
    
    872573-93-8
    
    Molecular Formula
    
    C18H13N3OS2
    
    Molecular Weight
    
    351.45
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in EtOH; insoluble in H2O; ≥4.39 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Macheret M, Bhowmick R, et al. "High-resolution mapping of mitotic DNA synthesis regions and common fragile sites in the human genome through direct sequencing." Cell Res. 2020;10.1038/s41422-020-0358-x. PMID:32561860
    2. Wu W, Bhowmick R, et al. "RTEL1 suppresses G-quadruplex-associated R-loops at difficult-to-replicate loci in the human genome." Nat Struct Mol Biol. 2020;27(5):424-437. PMID:32398827
    3. Venegas AB, Natsume T, et al. "Inducible Degradation of the Human SMC5/6 Complex Reveals an Essential Role Only during Interphase." Cell Rep. 2020;31(3):107533. PMID:32320646
    4. Liu JC, Granieri L, et al. "Identification of CDC25 as a Common Therapeutic Target for Triple-Negative Breast Cancer." Cell Rep. 2018 Apr 3;23(1):112-126. PMID:29617654
    5. Özer Ö, Bhowmick R, et al. "Human cancer cells utilize mitotic DNA synthesis to resist replication stress at telomeres regardless of their telomere maintenance mechanism." Oncotarget. 2018 Mar 23;9(22):15836-15846. PMID:29662610
    6. Azimi A, Caramuta S, et al. "Targeting CDK2 overcomes melanoma resistance against BRAF and Hsp90 inhibitors." Mol Syst Biol. 2018 Mar 5;14(3):e7858. PMID:29507054
    7. Arpita Mukherjee, Upayan Patra, et al. "Rotaviral non‐structural protein 4 triggers Dynamin related protein 1‐dependent mitochondrial fragmentation during infection." CELLULAR MICROBIOLOGY.2018.February 28.

Ro 3306

Ro 3306

Background

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