CX-5011 free base
CX-5011 free base is an ATP-competitive, selective CK2 inhibitor with an IC50 of 0.97 nM for nCK2. CX-5011 free base reduces Bin1, CKB, Tubb3, and Pxn levels. CX-5011 free base impairs myogenic differentiation, myotube formation, muscle markers, myofiber growth, and zebrafish muscle development/locomotion. CX-5011 free base can be used for breast cancer research.
For research use only. We do not sell to patients.
- CAS No.: 1009821-06-0
- Formula: C20H12N4O2
- Molecular Weight:340.33
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[2]|
CK2 0.97 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BXPC-3 | EC50 |
0.27 μM
Compound: 7e
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Inhibition of CK2 in human BxPC3 cells assessed as reduction of Akt phosphorylation at Ser129
Inhibition of CK2 in human BxPC3 cells assessed as reduction of Akt phosphorylation at Ser129
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[PMID: 21316963] |
In Vitro
CX-5011 (1-10 μM; 48 h) does not significantly reduce MDA-MB-231 cell viability[6].
CX-5011 (1 μM; 5 days) does not reduce the viability of AMO-1 or L363 parental multiple myeloma cells[6].
CX-5011 (0.5 μM) is highly selective for CK2, with Gini coefficients of 0.735 (102 kinases) and 0.794 (235 kinases), respectively, and 11 kinases are inhibited by more than 50% at 0.5 μM[2].
CX-5011 (100 nM) significantly reduces CK2-dependent GST-HDGF phosphorylation in C2C12 WT myoblast lysates, while leaving a detectable residual phosphorylation band[3].
CX-5011 (3 μM; 24-48 h) decreases Bin1, CKB, Tubb3, and Pxn levels in C2C12 WT myoblasts, whereas CK2β and DecR1 remain unchanged[3].
CX-5011 impairs myogenic differentiation and cell fusion in primary mouse muscle precursor cells[4].
CX-5011 (2 μM; 2-6 d after transfection; WT proliferating cells 4 d), despite inhibiting CK2 activity, does not affect proliferation or MyoD expression in CK2β-silenced C2C12 myoblasts[4].
CX-5011 inhibits late muscle-specific gene expression in differentiating CK2α′−/− C2C12 myoblasts but does not affect MyoD[4].
CX-5011 is a potent and selective inhibitor of CK2 in cell-free kinase assays[5].
CX-5011 binds to CK2α and CK2α′ in cells with IC50 values of 350 nM and 66 nM, respectively[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 cells
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Concentration:1, 2, 5, and 10 µM
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Incubation Time:48 h
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Result:Compounds 7, CX-5011, and CX-4945 similarly did not exhibit cytotoxicity.
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Cell Line:JJN3, AMO-1 (parental and pomalidomide-resistant), and L363 (parental, carfilzomib-resistant, and bortezomib-resistant) multiple myeloma cell lines
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Concentration:1 μM
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Incubation Time:5 days
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Result:The viability of AMO-1 and L363 parental lines was not reduced by CX-5011.
JJN3 cells were not responsive to any compound.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD1 (male, 3 months of age)[4]
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Dosage:90 µg per injection in 50 µl saline
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Administration:intramuscular; starting at 3 d after injury; repeated every 3 d
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Result:Reduced CK2 activity in regenerating muscles by approximately 70% up to 14 d without affecting expression of CK2 subunits.
At 7 d postinjury, expression of late muscle-specific markers was reduced.
MyoD and myogenin remained unchanged in CX-5011-exposed regenerating mouse muscle at 7 d.
Myofiber growth was impaired, with reduced fiber cross-sectional area in CX-5011-exposed regenerating muscles compared with vehicle-exposed contralateral muscles.
CX-5011-exposed regenerating fibers showed decreased myonuclei content at 14 d.
Inhibited regenerating fiber-type switching, with decreased mature regenerating fibers and persistence of embryonic myosin-heavy-chain-positive immature fibers at both 7 and 14 d postinjury.
At 4 d of regeneration, CX-5011 did not affect general cell proliferation (Ki67-positive nuclei) but reduced the percentage of Ki67-positive myonuclei within the basal lamina and shifted proliferating myonuclei distribution toward fibers with fewer than 3 nuclei.
Total (Pax7-positive) and activated (MyoD-positive) satellite cell numbers were not affected by CX-5011.
Chemical Information
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CAS No. 1009821-06-0
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Molecular Weight 340.33
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Formula C20H12N4O2
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SMILES
C#CC1=CC(NC2=NC3=CC(C(O)=O)=CC=C3C4=CN=CN=C42)=CC=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[2]. Battistutta R, et al. Unprecedented selectivity and structural determinants of a new class of protein kinase CK2 inhibitors in clinical trials for the treatment of cancer. Biochemistry. 2011 Oct 04;50(39):8478-88. [Content Brief]
[6]. Davis-Gilbert ZW, et al. Discovery of a Potent and Selective Naphthyridine-Based Chemical Probe for Casein Kinase 2. ACS medicinal chemistry letters. 2023 Apr 13;14(4):432-441. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CX-5011 free base Related Classifications
HY-50733 Related Classifications
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