CDK2 Inhibitor

Anticancer agent 30 (compound 6f-Z), a 3-arylidene-2-oxindole derivative, is a selective CDK2 inhibitor with potent anticancer activity.

CDK-IN-14 (B34) is a CDK2 inhibitor (IC₅₀=0.097 μM) with anti-hepatocellular carcinoma activity. CDK-IN-14 blocks the cell cycle of HepG-2 cancer cells through a caspase-mediated mechanism and induces apoptosis.

CDK2-IN-57 is a selective Cdk2/CycE inhibitor with an IC₅₀ of 2.8 nM. CDK2-IN-57 inhibits Cdk1/2 kinase activity, blocks cell cycle progression, induces G₀-phase cell cycle arrest, and prevents S-phase entry. CDK2-IN-57 can be used for the research of colon carcinoma.

CAIX/CDK-2-IN-1 is a dual-acting inhibitor of carbonic anhydrase IX (CA IX) and cyclin-dependent kinase-2 (CDK-2) with IC₅₀ values of 0.29 μM and 0.32 μM. The zein nanoparticls of CAIX/CDK-2-IN-1 can induce cancer cells apoptosis. CAIX/CDK-2-IN-1 can be used for the research of cancer, such as lung cancer.

KB-0742 hydrochloride is a potent, selective and orally active CDK9 inhibitor with an IC₅₀ of 6 nM for CDK9/cyclin T1. KB-0742 hydrochloride is selective for CDK9/cyclin T1 with >50-fold selectivity over other CDK kinases. KB-0742 hydrochloride has potent anti-tumor activity.

EF-4-177 is an orally active and allosteric CDK2 inhibitor with the IC₅₀ of 87 nM. EF-4-177 can disrupt spermatogenesis.

MM129 is an anticancer agent. MM129 inhibits key oncogenic signaling molecules such as AKT, mTOR, and CDK2, and downregulates the expression of PD-L1. MM129 induces cell cycle arrest. MM129 induces Apoptosis. MM129 induces DNA damage. MM129 induces oxidative stress. MM129 exhibits chemosensitizing properties. MM129 restores the expression of E-cadherin. MM129 can be used in the research of colorectal cancer.

CDK2-IN-48 (Compound 109) is a CDK2 inhibitor with IC₅₀ values for CDK2 and CDK1 of respectively < 0.05 and > 1 μM. CDK2-IN-48 can be used for the study of CDK2-dependent cancers.

CDK2-IN-50 is a CDK2 inhibitor (IC₅₀ = 0.77 nM). CDK2-IN-50 can induce G1 phase arrest, indicating that it has an effective CDK2/cyclin E targeting mechanism. CDK2-IN-50 also has a significant pro-apoptotic effect. CDK2-IN-50 can be used for the study of breast cancer.

ARUK2010694 (Compound 20) is a potent and selective NUAK1 inhibitor with a pIC₅₀ of 8.7. ARUK2010694 also inhibits CDK2, CDK4 and CDK6 activity, with inhibitory rate of 13%, 63% and 32% at 1 μM. ARUK2010694 can be used for the research of neurological disease, such as Alzheimer’s disease (AD).

Multi-kinase-IN-7 is a multikinase inhibitor with IC₅₀s of 2.19, 2.95, 3.59 and 9.31 μM against EGFR, VEGFR2, TrKA and CDK2, respectively. Multi-kinase-IN-7 shows moderate and weaker activity against FAK, AKT1, GSK3β and CDK5 with IC₅₀ values of 6.3, 9.2, 11.7 and 23.4 μM, respectively. Multi-kinase-IN-7 displays broad spectrum anti­proliferative potential against NCI cancer cell lines. Multi-kinase-IN-7 induces cell cycle arrest, apoptosis and necrosis. Multi-kinase-IN-7 Inhibitor can be used for the study of breast cancer.

BLINK15 is a BBB-penetrant CDK5 inhibitor. BLINK15 lowers CDK5 activity for both complexes CDK5/p35 (IC₅₀ = 29.34 nM) and CDK5/p25 (IC₅₀ = 12.08 nM). BLINK15 offers anti-diabetic and neuroprotective benefits. BLINK15 lowers blood glucose, enhances cognition, and reduces neurodegeneration in T2D mice.

CDK2-IN-29 (Compound 13q) is an inhibitor for cyclin-dependent kinase (CDK), with IC₅₀ of 96 nM and 360 nM, for CDK 2 and CDK 4, respectively.

IRAK4-IN-35 is an orally active IRAK4 inhibitor with an IRAK4 IC₅₀ of 9.88 nM. IRAK4-IN-35 also inhibits JAK3, EGFR, CDK2 with IC₅₀ values of 6.72 nM, 32.35 nM, and 39.08 nM, respectively. IRAK4-IN-35 inhibits the production of proinflammatory cytokines, blocks inflammatory signaling pathways, and reduces serum TNF-α levels and spleen index in mouse models of acute inflammation. IRAK4-IN-35 decreases the disease activity index, paw swelling degree, and spleen index in a collagen-induced arthritis mouse model. IRAK4-IN-35 can be used for the research of rheumatoid arthritis.

CDK8-IN-19 (Compound 3d) is a CDK8 inhibitor with an IC₅₀ of 25.08 nM. CDK8-IN-19 has a broad-spectrum anticancer activity, such as leukemia, melanoma and breast cancer, without significant cytotoxic effect on the normal Vero cells (mean IC₅₀s of 2.87, 3.65, 3.79 and 45.48 μM, respectively).

3-Methylthienyl-carbonyl-JNJ-7706621 is a potent and selective inhibitor of cyclin-dependent kinase (CDK), with IC₅₀s of 6.4 nM and 2 nM for CDK1/cyclin B and CDK2/cyclin A, respectively. 3-Methylthienyl-carbonyl-JNJ-7706621 also shows potent inhibition of GSK-3 (IC₅₀=0.041 μM) and modest potency against CDK4, VEGF-R2, and FGF-R2 (IC₅₀=0.11, 0.13, 0.22 μM, respectively). 3-Methylthienyl-carbonyl-JNJ-7706621 can be used for the research of cancer.

SY-5102 is a potent, selective, and orally active cyclin-dependent kinase (CDK7) inhibitor with a K_d value of 0.03 nM. SY-5102 occupies the ATP-binding pocket of CDK7 via non-covalent binding to inhibit CDK7 activity, and downregulates its phosphorylation of cyclin CDK and RNA polymerase II. SY-5102 inhibits cancer cell proliferation, and induces tumor growth inhibition and regression. SY-5102 can be used in research related to triple-negative breast cancer.

CDK2/PIM1-IN-1 is an inhibitor of CDK2 (IC₅₀: 0.27 μM) and PIM1 (IC₅₀: 0.67 μM) kinases. CDK2/PIM1-IN-1 induces apoptosis and reduces tumor-promoting TNF-α expression. CDK2/PIM1-IN-1 has antitumor activity.

BMS-357075 is a pan-CDK inhibitor with CDK1 IC₅₀ 18 nM, CDK2 IC₅₀ 3 nM, CDK4 IC₅₀ 26 nM. BMS-357075 induces cytotoxicity in human ovarian cancer A2780 cells. BMS-357075 exhibits anticancer activity in mice against P388 murine leukemia. BMS-357075 can be used for the research of leukemia.

ZLWT-37 is a potent, orally active CDKs inhibitor with IC₅₀ values of 0.002 μM and 0.054 μM against CDK9 and CDK2, respectively. ZLWT-37 induces apoptosis and arrests the cell cycle in the G2/M phase in HCT116 cells.