Name: CX-4945 (Silmitasertib)
Price: 244.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    CX-4945 (Silmitasertib) is a potent and selective casein kinase 2 (CK2) inhibitor with IC50 value of 1 nM. It is ATP-competitive and can be taken orally [1].
    CX-4945 has been reported to have antiproliferative activity against a wide range of tumor cell lines. It is suggested that CX-4945 suppresses the CK2 regulated PI3K/Akt signaling pathway by inhibiting Akt phosphorylation at Serine 129, but not by activating PTEN. Additionally, cells treated with CX-4945 had a reduction of p21 phophorylation and an up-regulations of total p21 and p27. CX-4945 has been shown to induce cell-cycle arrest at G2/M phase in breast cancer cell line BT-474. It also causes cell-cycle arrest at G1 phase the breast cancer cell line BxPC-3) [1].
    In CX-4945 and BxPC-3 derived mouse xenograft model, CX-4945 induced a reduction of phos-p21 expression along with anti-carcinoma effects [1]
    
    [1] Siddiqui-Jain A1, Drygin D, Streiner N, Chua P, Pierre F, O'Brien SE, Bliesath J, Omori M, Huser N, Ho C, Proffitt C, Schwaebe MK, Ryckman DM, Rice WG,Anderes K. CX-4945, an orally bioavailable selective inhibitor of protein kinase CK2, inhibits prosurvival and angiogenic signaling and exhibits antitumor efficacy. Cancer Res. 2010 Dec 15; 70 (24): 10288-98.
- Properties
  - Alternative Name
    
    CX 4945; CX4945; 5-(3-chloroanilino)benzo[c][2,6]naphthyridine-8-carboxylic acid
    
    CAS Number
    
    1009820-21-6
    
    Molecular Formula
    
    C19H12ClN3O2
    
    Molecular Weight
    
    349.77
    
    Appearance
    
    A solid
    
    Purity
    
    98.98%
    
    Solubility
    
    ≥103.5 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Swati Mishra, Chizuru Kinoshita, et al. "Evaluation of a Selective Chemical Probe Validates That CK2 Mediates Neuroinflammation in a Human Induced Pluripotent Stem Cell-Derived Mircroglial Model." Front Mol Neurosci. 2022 Jun 14;15:824956. PMID: 35774866
    2. Silva-Pavez E, Villar P, et al. "CK2 inhibition with silmitasertib promotes methuosis-like cell death associated to catastrophic massive vacuolization of colorectal cancer cells." Cell Death Dis.2019 Jan 25;10(2):73. PMID: 30683840
    3. Zhao Z, Wang L, et al."Regulation of MLL/COMPASS stability through its proteolytic cleavage by taspase1 as a possible approach for clinical therapy of leukemia." Genes Dev. 2019 Jan 1;33(1-2):61-74. PMID: 30573454
    4. Tanghe G, Urwyler-Rösselet C, et al. "RIPK4 activity in keratinocytes is controlled by the SCF(β-TrCP) ubiquitin ligase to maintain cortical actin organization." Cell Mol Life Sci. 2018 Feb 12. PMID: 29435596
    5. Wu F, Qiu J, et al. "Apelin-13 attenuates ER stress-mediated neuronal apoptosis by activating Gα(i)/Gα(q)-CK2 signaling in ischemic stroke." Exp Neurol. 2018 Apr;302:136-144. PMID: 29337146
    6. Krentz Gober, Madeline J. "GENE EXPRESSION PROFILES REVEAL ALTERNATIVE TARGETS OF THERAPEUTICINTERVENTION FOR THE TREATMENT OF DRUG-RESISTANT NON-SMALL CELL LUNG CANCERS" (2017).Thesesand Dissertations--Pharmacy. 78.
    7. Korb E, Herre M, et al. "Excess Translation of Epigenetic Regulators Contributes to Fragile X Syndrome and Is Alleviated by Brd4 Inhibition." Cell. 2017 Aug 12. PMID: 28823556
    8. Viscarra JA, Wang Y, et al. "Transcriptional activation of lipogenesis by insulin requires phosphorylation of MED17 by CK2." Sci Signal. 2017 Feb 21;10(467). pii: eaai8596. PMID: 28223413
    9. Kubiński K, Masłyk M, Orzeszko A. "Benzimidazole inhibitors of protein kinase CK2 potently inhibit the activity of atypical protein kinase Rio1." Mol Cell Biochem. 2017 Feb;426(1-2):195-203. PMID: 27909846
    10. Dubois N, Willems M, et al. "Constitutive activation of casein kinase 2 in glioblastomas: Absence of class restriction and broad therapeutic potential." Int J Oncol. 2016 Jun;48(6):2445-52. PMID: 27098015