Casein Kinase Inhibitor

AMG-548 dihydrochloride (Standard) is the analytical standard of AMG-548 (dihydrochloride) (HY-108642B). This product is intended for research and analytical applications. AMG-548 dihydrochloride, an orally active and selective p38α inhibitor (K_i=0.5 nM), shows slightly selective over p38β (K_i=36 nM) and >1000 fold selective against p38γ and p38δ. AMG-548 dihydrochloride is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC₅₀=3 nM). AMG-548 dihydrochloride inhibits Wnt signaling by directly inhibiting Casein K_inase 1 isoforms δ and ε.

D4476 (Standard) is the analytical standard of D4476 (HY-10324). This product is intended for research and analytical applications. D4476 is a potent, selective and cell-permeable inhibitor of casein kinase 1(CK1) with an IC₅₀ value of 0.3 μM in vitro.

Umbralisib (Standard) is the analytical standard of Umbralisib. This product is intended for research and analytical applications. Umbralisib (TGR-1202) is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib can be used for haematological malignancies reseach.

Ac-ESMD-CHO is an inhibitor of caspase-3 and caspase-7. Ac-ESMD-CHO inhibits proteolytic cleavage of the caspase-3 precursor peptide (CPP32) at the Glu-Ser-Met-Asp (ESMD) site.

LY294002 (hydrochloride) (Standard) is the analytical standard of LY294002 (hydrochloride). This product is intended for research and analytical applications. 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.

PI-828 (Standard) is the analytical standard of PI-828 (HY-108606). This product is intended for research and analytical applications. PI-828 is a dual PI3K and casein K_inase 2 (CK2) inhibitor with IC₅₀s of 173 nM, 149 nM, and 1127 nM for p110α, CK2, and CK2α2 in lipid K_inase assay, respectively.

Casein kinase 1δ-IN-30 (Compound 581) is a Casein kinase 1δ (CK1δ) inhibitor. Casein kinase 1δ-IN-30 can be used in the research of neurodegenerative diseases.

CK1δ-IN-5 (Compound 24) is a Casein kinase 1δ (CK1δ) inhibitor. CK1δ-IN-5 can be used in the research of neurodegenerative diseases.

TBCA (Standard) is the analytical standard of TBCA (HY-110052). This product is intended for research and analytical applications. TBCA is a highly selective CK2 (casein K_inase 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 K_inases.

Casein K_inase II Inhibitor IV (Standard) is the analytical standard of Casein K_inase II Inhibitor IV (HY-111378). This product is intended for research and analytical applications. Casein K_inase II Inhibitor IV is a potent, ATP-competitive of casein K_inase II inhibitor with an IC₅₀ of 9 nM. Casein K_inase II Inhibitor IV ia also a human keratinocytes (NHEK) differentiation inducer.

CK1-IN-1 (Standard) is the analytical standard of CK1-IN-1 (HY-111820). This product is intended for research and analytical applications. CK1-IN-1 (Compound 1c) is a casein K_inase 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.

CK2-IN-12 (Compound 39) is an inhibitor for protein kinase CK2 with an IC₅₀ of 0.8 μM.

Silmitasertib (sodium salt) (Standard) is the analytical standard of Silmitasertib (sodium salt). This product is intended for research and analytical applications. Silmitasertib sodium salt is an orally bioavailable, highly selective and potent CK2 inhibitor, with IC50 values of 1 nM against CK2α and CK2α'.

IWP-2 (Standard) is the analytical standard of IWP-2 (HY-13912). This product is intended for research and analytical applications. IWP-2 is an inhibitor of Wnt processing and secretion with an IC₅₀ of 27 nM. IWP-2 targets the membrane-bound O-acyltransferase porcupine (Porcn) and thus preventing a crucial Wnt ligand palmitoylation. IWP-2 is also an ATP-competitive CK1δ inhibitor with an IC₅₀ of 40 nM for the gatekeeper mutant ^M82FCK1δ.

CK2-IN-18 is a protein kinase CK2 inhibitor with an IC₅₀ of > 30 μM against protein kinase CK2. CK2-IN-18 can be used in studies related to CK2-mediated signaling pathways, such as various cancers including lung cancer and breast cancer.

GW461484A is a small-molecule inhibitor targeting Candida albicans Yck2, with an IC₅₀ of 0.11 µM. It exhibits antifungal activity against C. albicans with a MIC₈₀ of 12.5 µM. GW461484A holds potential for research on fungal diseases, such as drug-resistant Candida infections.

CK1-IN-5 (compound B-AZ) is an inhibitor of CK1. CK1-IN-5 lengthened the circadian period by inhibits AtCKL3/AtCKL4 activity.

Yck2-IN-1 (Compound 2a) is an inhibitor of the fungal Candida albicans Yck2 kinase. It exhibits an IC₅₀ of approximately 80 nM against Yck2 and a MIC₈₀ of 12.5 µM against C. albicans, with good metabolic stability (66% remaining in mouse liver microsomes). In a mouse model of drug-resistant candidiasis, Yck2-IN-1 significantly reduced fungal burden in the kidneys. Yck2-IN-1 holds promise for research in the field of antifungal infection.

CSNK2-IN-2 (compound 2) is an orally active CSNK2 inhibitor. CSNK2-IN-2 has an IC₅₀ of 29 μM against CLK11. CSNK2-IN-2 has a half-life of 2.5 h and an AUC of 10,100 h × nM. CSNK2-IN-2 can be used in antiviral studies.

Silmitasertib (Standard) is the analytical standard of Silmitasertib. This product is intended for research and analytical applications. Silmitasertib (CX-4945) is an orally bioavailable, highly selective and potent CK2 inhibitor, with IC50 values of 1 nM against CK2α and CK2α'.