CX-5011

CX-5011 is an ATP-competitive, selective CK2 inhibitor with an IC₅₀ of 0.97 nM for nCK2. CX-5011 reduces Bin1, CKB, Tubb3, and Pxn levels. CX-5011 impairs myogenic differentiation, myotube formation, muscle markers, myofiber growth, and zebrafish muscle development/locomotion. CX-5011 can be used for breast cancer research^{[1][2][3][4][5][6]}. In Vitro:CX-5011 is a low-nanomolar ATP-competitive CK2 inhibitor that inhibits nCK2, recombinant CK2α, and the V66A/I174A CK2α mutant, with IC₅₀ values of 0.97-2.50 nM^[2].
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].
CX-5011 (4 days) reduces the viability of the tested cancer cell lines after 4 days, with IC₅₀ values ranging from 1.6 to 9.8 μM, among which K-562 and H1299 are the most sensitive (1.6 μM)^[2].
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 produces antiproliferative effects across a panel of 16 cancer cell lines and induces apoptosis in BXPC3 cells and G1 phase accumulation in MDA-MB-231 cells^[5]. In Vivo:CX-5011 (90 µg; intramuscular injection; repeated every 3 days) impairs skeletal muscle regeneration in the mouse tibialis anterior muscle by reducing CK2 activity, late muscle-specific marker expression, myofiber growth, myonuclear incorporation, and fiber maturation, without affecting general proliferation or satellite cell number^[4].