Casein Kinase Inhibitor

CK2-IN-6 is a potent protein kinase CK2 inhibitor that can be used in the study of cancer as well as other kinase-related conditions, including inflammation, pain and certain immune diseases.

CK1δ-IN-9 (Compound 8) is the inhibitor for casein kinase 1 that inhibits CK1δ with IC₅₀ of 1.4 nM. CK1δ-IN-9 inhibits p38α and p38β with IC₅₀ of 0.25 μM and 0.78 μM. CK1δ-IN-9 exhibits pharmacokinetic characteristics with a good oral bioavailability (70%) and a moderate clearance.

CAM4066 is a potent CK2α inhibitor, with an IC₅₀ value of 300 nM. CAM4066 exhibits high selectivity, with IC₅₀ values of 22.35, 43.55, and > 50 μM for HIPK3, DAPK3, and CLK2, respectively. CAM4066 shows no cell activity. CAM4066 can be used for the development of highly potent CK2 inhibitors.

CX-5279 is an efficient and selective CK2 inhibitor with IC₅₀ values for nCK2 and CK2α of 2.73 and 0.91 nM, respectively. CX-5279 is sensitive to mutations at Val66, Ile174, and V66I174AA, with IC₅₀ values of 13.8, 12.5, and 23.35 nM, respectively. CX-5279's inhibitory activity against PIM1 is very weak, with a IC₅₀ value of 8.52 μM. CX-5279 exhibits anti-proliferative activity in various cancer cell lines. CX-5279 can be used for research on cancers such as pancreatic cancer and leukemia.

CK1δ-IN-6 (Compound 303) is a Casein kinase 1δ inhibitor. CK1δ-IN-6 is promising for research of Alzheimer's disease.

Tyrphostin AG1112 is a potent inhibitors of CK II. Tyrphostin AG1112 inhibits p210^bcr-abl tyrosine kinase, with IC₅₀ values of 2, 15, 20 μM in p210^bcr-abl, EGFR and PDGFR cells, respectively.

TMCB is a selective, ATP-competitive CK2 (casein kinase II) inhibitor with distinct K_i values of 83 nM and 21 nM for the two different catalytic CK2 subunits α and α', respectively.

CK2 inhibitor 3 is a potent CK2 inhibitor with IC₅₀ value of 280 nM. CK2 inhibitor 3 inhibits endocellular CK2, significantly affects viability of tumour cells and shows remarkable selectivity on a panel of 320 kinases.

Casein kinase 1δ-IN-31 (Compound 16) is the inhibitor for casein kinase (CK) that inhibits CK1α, CK1δ, and p38α with IC₅₀s of 196, 17, and 18 nM, respectively. Casein kinase 1δ-IN-31 inhibits Double Homeobox 4 (DUX4) with IC₅₀ of 1200 nM.

p38α inhibitor 8 (Compound 1) exhibits inhibitory activity against p38α MAPK and CK1δ with IC₅₀ of 0.21 µM and 0.202 µM^[1]>.

4,5,6,7-Tetrabromobenzimidazole is a selective and ATP competitive CK2 (casein kinase 2) inhibitor.

p38α MAPK/CK1δ inhibitor-1 (Compound 3) exhibits inhibitory activity against p38α MAPK and CK1δ with IC₅₀s of 0.185 µM and 0.089 µM.

CK2-IN-14 (Compound 10b) is an inhibitor for cyclin kinase 2α with an IC₅₀ of 36.7 nM. CK2-IN-14 inhibits the growth of cancer cell 786-O and U937 with GI₅₀ of 7.3 μM and 7.5 μM.

Umbralisib (hydrochloride) (Standard) is the analytical standard of Umbralisib (hydrochloride). This product is intended for research and analytical applications. Umbralisib (TGR-1202) hydrochloride 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 hydrochloride exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib hydrochloride can be used for haematological malignancies reseach.

CX-5279 free acid is an efficient and selective CK2 inhibitor with IC₅₀ values for nCK2 and CK2α of 2.73 and 0.91 nM, respectively. CX-5279 free acid is sensitive to mutations at Val66, Ile174, and V66I174AA, with IC₅₀ values of 13.8, 12.5, and 23.35 nM, respectively. CX-5279 free acid's inhibitory activity against PIM1 is very weak, with a IC₅₀ value of 8.52 μM. CX-5279 free acid exhibits anti-proliferative activity in various cancer cell lines. CX-5279 free acid can be used for research on cancers such as pancreatic cancer and leukemia.

CK1δ-IN-7 (Compound 488) is the inhibitor for casein kinase 1δ (CK1δ).

TAK-715 (Standard) is the analytical standard of TAK-715 (HY-10456). This product is intended for research and analytical applications. TAK-715 is an orally active and potent p38 MAPK inhibitor with IC₅₀s of 7.1 nM, 200 nM for p38α and p38β, respectively. TAK-715 inhibits casein kinase I (CK1δ/ε) to regulate activation of Wnt/β-catenin signaling. TAK-715 shows good significant efficacy in a rat arthritis model.

CZP-IN-1 (compound SH-1) is an inhibitor targeting the pathogen Trypanosoma cruzi cruzipain (CZP) and does not inhibit cathepsin L (IC₅₀=28 nM). CZP-IN-1 can be used for the research of Chagas disease.

PLK1-IN-17 is a potent PLK1 inhibitor with an IC₅₀ of 2 nM. PLK1-IN-17 shows high selectivity for PLK2 and CDK2/A, moderate selectivity for PLK3, only weak activity against CK2, FLT3 and NEK6, and no activity against PDGFR, ALK and another 37 kinases. PLK1-IN-17 inhibits the proliferation of ovarian cancer cells and can be used in ovarian cancer-related research.

CK1δ-IN-8 (Compound 429) is a CK1δ inhibitor that can be used in Alzheimer's disease research.