Casein Kinase Inhibitor

CK1-IN-1 (Compound 1c) is a casein kinase 1 (CK1) inhibitor with IC₅₀ values of 15 nM and 16 nM for CK1δ and CK1ε, respectively. CK1-IN-1 inhibits p38α MAPK with an IC₅₀ of 73 nM. CK1-IN-1 can be used to study cardiomyogenesis.

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.

BTX161, a Thalidomide (HY-14658) analog, is a molecular glue degrader targeting CK1α. BTX161 recruits CK1α and the CK1α-FAM83 complex to the Cul4ACRBN E3 ligase complex, thereby driving ubiquitination and proteasomal degradation. BTX161 reduces FAM83G abundance through CK1α-FAM83G co-stability, slightly decreases FAM83H levels, but has no effect on the expression of FAM83B. BTX161 activates DNA damage response (DDR) and upregulates Wnt target genes including MYC. BTX161 can be used in research related to colorectal cancer, type b myelomonocytic leukemia and acute myeloid leukemia.

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

TA-01 is a potent CK1 and p38 MAPK inhibitor, with IC₅₀s of 6.4 nM, 6.8 nM, 6.7 nM for CK1ε, CK1δ and p38 MAPK, respectively. TA-01 acts as a cardiogenic inhibitor.

Epiblastin A is an ATP-competitive casein kinase 1 (CK1) inhibitor that inhibits CK1α, CK1δ, and CK1ε. Epiblastin A inhibits the kinase activity of STK10, BRSK1, EEF2K, EGFR, MKNK2, and RIPK2. Epiblastin A inhibits Ki-67 expression, induces Oct4-GFP expression, and enhances the conversion of mouse epiblast stem cells to embryonic stem cells. Epiblastin A selectively reduces the cell viability of colorectal cancer cell lines HCT116, HT29, and DLD1. Epiblastin A can be used in colorectal cancer-related research.

IWP-3 is a Wnt production inhibitor with an IC₅₀ of 40 nM. IWP-3 also acts as a CK1δ inhibitor, with an IC₅₀ of 1.89 μM against rat full-length CK1δ. IWP-3 inhibits the function of Porcupine (Porcn), thereby blocking the palmitoylation of Wnt proteins, suppressing the canonical Wnt signaling pathway, reducing the proliferative capacity of cancer cells, promoting the differentiation of mesoderm into cardiomyocytes and increasing cardiomyocyte yield. IWP-3 reduces embryonic cell division, alters the cell movement along the anterior-posterior axis of embryos, and causes embryonic shortening. IWP-3 can be used in studies related to cancers such as pancreatic cancer.

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.

CKI-7 is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC₅₀ of 6 μM and a K_i of 8.5 μM. CKI-7 is a selective Cdc7 kinase inhibitor. CKI-7 also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 has a much weaker effect on casein kinase II and other protein kinases.

AH078 is a PROTAC-based CK1δ/ε degrader (DC₅₀=0.55 μM, D_max=70%) that lacks subtype selectivity between CK1δ and CK1ε. AH078 induces target protein degradation either by recruiting the CUL4-CRBN E3 ligase complex and proteasome, or via the VHL- and ubiquitin-dependent pathway. AH078 also exhibits selectivity for CK1α, and is widely applicable to research related to colon cancer, pancreatic cancer, breast cancer, ovarian cancer, chronic lymphocytic leukemia, acute myeloid leukemia, glioma, and metastatic breast adenocarcinoma.

LH846 is a selective inhibitor of CKIδ, with an IC₅₀ of 290 nM, and less potently inhibits CKIα and CKIε, with IC₅₀s of 2.5 μM and 1.3 μM, respectively.

TMX-4113 is a FPFT-2216 (HY-145319) (Molecular glue) analog and degrader of PDE6D and CK1α. TMX-4113 does not inhibit the growth of KRAS^G12C-dependent cancer cells. TMX-4113 can be used in the research of multiple myeloma, pancreatic ductal adenocarcinoma, non-small cell lung cancer and gastric adenocarcinoma.

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.

CSNK2A-IN-1 (compound 7C) is a selective CSNK2A inhibitor. CSNK2A-IN-1 has antiviral activity and improved selectivity over PIM3.

CK2α-IN-1 (compound 2) is a selective CK2α inhibitor (IC₅₀=7.0 µM; K_i=1.6 µM) that exhibits a non-ATP-competitive mode of action. CK2α-IN-1 exhibits good potential for anticancer studies.

Rhodiolin, a flavonoid, is an orally active glucose 6-phosphate isomerase (GPI) inhibitor. Rhodiolin inhibits papillary thyroid cancer (PTC) by targeting glycolysis enzyme glucose 6-phosphate isomerase GPI and suppressing PI3K/AKT/mTOR phosphorylation and induce apoptosis. Rhodiolin as a NS2B-NS3 protease inhibitor can disrupt dengue viral replication. Rhodiolin is also a potential candidate for developing anticancer strategies inhibiting CK1ε kinase. Rhodiolin can be used for the study of anti-tumor and anti-viral .

Casein Kinase inhibitor A86 is a potent and orally active casein kinase 1α (CK1α) inhibitor. Casein Kinase inhibitor A86 also inhibits of CDK7 (TFIIH) and CDK9 (P-TEFb). Casein Kinase inhibitor A861 induces leukemia cell apoptosis, and has potent anti-leukemic activities.

CX-5011 is a CK2 inhibitor. CX-5011 also induces Rac1 activation. CX-5011 induces apoptosis and induces cancer cell death.