CK2 Inhibitor

Silmitasertib (CX-4945) is an orally bioavailable, highly selective and potent CK2 inhibitor, with IC₅₀ values of 1 nM against CK2α and CK2α'.

Emodin (Frangula emodin), an anthraquinone derivative, is an anti-SARS-CoV compound. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 (ACE2) interaction. Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects. Emodin is a potent selective 11β-HSD1 inhibitor with the IC₅₀ of 186 and 86 nM for human and mouse 11β-HSD1, respectively. Emodin ameliorates metabolic disorder in diet-induced obese mice.

Ellagic acid is a natural antioxidant, and acts as a potent and ATP-competitive inhibitor of CK2 and SHP2, with an IC₅₀ of 40 nM and a K_i of 20 nM.

LY294002 hydrochloride is a potent and broad-spectrum PI3K inhibitor, with IC₅₀ values of 0.5, 0.57, and 0.97 μM for P110α, P110δ and P110β, respectively. LY294002 hydrochloride also inhibits CK2 with an IC₅₀ of 98 nM. LY294002 hydrochloride can be used for pancreatic cancer research.

TBB is a cell-permeable and ATP-competitive CK2 inhibitor with an IC₅₀ of 0.15 μM for rat liver CK2.

Emodin (Standard) is the analytical standard of Emodin. This product is intended for research and analytical applications. Emodin (Frangula emodin), an anthraquinone derivative, is an anti-SARS-CoV compound. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 (ACE2) interaction. Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects. Emodin is a potent selective 11β-HSD1 inhibitor with the IC₅₀ of 186 and 86 nM for human and mouse 11β-HSD1, respectively. Emodin ameliorates metabolic disorder in diet-induced obese mice.

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.

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.

Silmitasertib sodium salt is an orally bioavailable, highly selective and potent CK2 inhibitor, with IC₅₀ values of 1 nM against CK2α and CK2α'.

SGC-CK2-1 is a highly potent, ATP-competitive, and cell-active CK2 chemical probe with exclusive selectivity for both human CK2 isoforms, with IC₅₀s of 36 and 16 nM for CK2α and CK2α′respectively in the nanoBRET assay. SGC-CK2-1 can be used for the research of neurodegenerative diseases.

DMAT is a potent and specific CK2 inhibitor with an IC₅₀ value of 130 nM.

BioE-1115 is a highly selective and potent PAS kinase (PASK) inhibitor with an IC₅₀ of ~4 nM. BioE-1115 is also a potent casein kinase 2α inhibitor with an IC₅₀ of ~10 μM.

Hematein is a oxidation product of hematoxylin acted as a dye. Hematein is an allosteric casein kinase II inhibitor with an IC₅₀ of 0.74 μM. Hematein inhibits Akt/PKB Ser129 phosphorylation, the Wnt/TCF pathway and increases apoptosis in lung cancer cells.

CK2/ERK8-IN-1 is a dual casein kinase 2 (CK2) (K_i of 0.25 µM) and ERK8 (MAPK15, ERK7) inhibitor with IC₅₀s of 0.50 μM. CK2/ERK8-IN-1 also binds to PIM1, HIPK2 (homeodomain-interacting protein kinase 2), and DYRK1A with K_is of 8.65 µM, 15.25 µM, and 11.9 µM, respectively. CK2/ERK8-IN-1 has pro-apoptotic efficacy.

CK2 inhibitor 2 is a potent, selective and orally active inhibitor of CK2, with an IC₅₀ of 0.66 nM. CK2 inhibitor 2 shows high selectivity for Clk2 (IC₅₀=32.69 nM)/CK2. CK2 inhibitor 2 exhibits favorable antiproliferative and antitumor activity.

TBCA is a highly selective CK2 (casein kinase II) inhibitor with an IC₅₀ of 110 nM and a K_i of 77 nM. TBCA shows selectivity for CK2 over CK1, DYRK1A and a panel of 27 other kinases.

TTP 22 is a potent CK2 inhibitor, with an IC₅₀ of 100 nM and a K_i of 40 nM.

ON 108600 (108600) is a CK2 (CK2α1: IC₅₀ = 50 nM; CK2α2 = 5 nM), TNIK (IC₅₀ = 5 nM) and DYRK (DYRK1A: IC₅₀ = 16 nM; DYRK1B = 7 nM; DYRK2: = 28 nM). ON 108600 suppresses the growth of CD44high/CD24low breast cancer stem cell (BCSC) populations, induces G2/M arrest and apoptosis in triple negative breast cancer (TNBC) cells, and inhibits tubulin polymerization. ON 108600 can be used for the study of chemotherapy-resistant and metastatic TNBC.

PI-828 is a dual PI3K and casein kinase 2 (CK2) inhibitor with IC₅₀s of 173 nM, 149 nM, and 1127 nM for p110α, CK2, and CK2α2 in lipid kinase assay, respectively.

Quinalizarin is a protein kinase CK2 inhibitor with a K_i of 0.052 μM. Quinalizarin exhibits antifungal and anticancer activities. Quinalizarin induces ROS production, apoptotic signaling, mitochondrial pathway activation, cell cycle arrest, and cytotoxicity in cancer cells. Quinalizarin inhibits hyphal growth, biofilm formation, and mature biofilm integrity of Candida albicans. Quinalizarin can be used in research related to cancer and fungal infections.