CDK2 Inhibitor

CDK2-IN-20 (compound 3b) is an inhibitor of CDK2. CDK2-IN-20 has cytotoxicity on tumor cells presenting an IC₅₀ range of 5.52-17.09 µM. CDK2-IN-20 arrests the MCF-7 cell cycle at the S phase and induces apoptosis.

CDK4/6-IN-14 is a potent and highly selective CDK4 and CDK6 (CDK) inhibitor with IC₅₀s of 10 nM and 16 nM, respectively. CDK4/6-IN-14 exhibits more than 60-fold selectivity over CDKs 1, 2, 7, and 9, and shows high selectivity among other 205 kinases.

CDK2-IN-60 is an orally active, ATP-competitive selective CDK2 inhibitor with a K_i of 77 pM. CDK2-IN-60 has high selectivity for both CDK4 and CDK1. CDK2-IN-60 blocks G1/S cell cycle progression to suppress proliferation of CCNE1-amplified tumor cells. CDK2-IN-60 serves as a lead chemical probe for investigating CCNE1-amplified cancers and CDK4/6 inhibitor-resistant HR-positive breast cancer.

BLINK11 is a BBB-penetrant CDK5 inhibitor. BLINK11 lowers CDK5 activity for both complexes CDK5/p35 (IC₅₀ = 17.09 nM) and CDK5/p25 (IC₅₀ = 14.69 nM). BLINK11 offers anti-diabetic and neuroprotective benefits. BLINK11 lowers blood glucose, enhances cognition, and reduces neurodegeneration in T2D mice.

IIIM-290 is a potent and oral CDK inhibitor with IC₅₀s of 90 and 94 nM for CDK2/A and CDK9/T1.

CDK/HDAC-IN-2 is a potent HDAC/CDK dual inhibitor with IC₅₀ of 6.4, 0.25, 45, >1000, 8.63, 0.30, >1000 nM for HDAC1, HDAC2, HDAC3, HDAC6,8, CDK1, CDK2, CDK4,6,7, respectively. CDK/HDAC-IN-2 shows excellent antiproliferative activities. CDK/HDAC-IN-2 induces apoptosis and cell cycle arrest at G2/M phase. CDK/HDAC-IN-2 shows potent antitumor efficacy.

ZLHQ-5f is a dual CDK2 and Topo I inhibitor with an IC₅₀ of 0.145 μM against CDK2/CycA2. ZLHQ-5f arrests the cell cycle in S-phase, triggers apoptosis in HCT116 cells, and has a good safety profile.

CDK2-IN-62 is a predicted CDK2 inhibitor. CDK2-IN-62 induces apoptosis in breast cancer cells and reduces their colony-forming ability. CDK2-IN-62 can be used for the research of breast cancer, ovarian cancer and colorectal cancer.

CDK2-IN-43 (Compound 3a) is a CDK2-cyclin E2 inhibitor with an IC₅₀ value of 6.0 nM. CDK2-IN-43 can be used in the research of the anti-cancer field.

CDK2-IN-36 (compound1) is a CDK2 inhibitor with anticancer activity.

ARUK2010489 (Compound 23) is a potent, selective and brain-penetrant NUAK1 inhibitor with a pIC₅₀ of 8.7. ARUK2010489 also inhibits CDK2, CDK4 and CDK6 activity, with inhibitory rate of 7%, 39% and 26% at 1 μM. ARUK2010489 can be used for the research of neurological disease, such as Alzheimer’s disease (AD).

CDK2-IN-18 (compound 8q) is a potent inhibitor of CDK2/E and CDK4/D1, with IC₅₀s of 8 nM and 46 nM, respectively. CDK2-IN-18 inhibits the proliferation of tumor cells.

CDK2/9-IN-1 (compound 20a) is an orally active dual inhibitor of CDK2 and CDK9 with IC₅₀ values are 0.004 μM and 0.009 μM respectively. CDK2/9-IN-1 induces apoptosis by regulating G2/M cell cycle arrest. CDK2/9-IN-1 has antitumor activity.

EGFR/CDK2-IN-5 is a potent dual EGFR and CDK2 inhibitor with IC₅₀s of 17.30 and 212.10 nM, respectively. EGFR/CDK2-IN-5 also inhibits EGFR^T790M with an IC₅₀ of 123.8 nM. EGFR/CDK2-IN-5 exhibits potent anticancer activity. EGFR/CDK2-IN-5 induces G1 and S cell cycle arrest and apoptosis, accompanied by increased levels of caspase-3/9 and Bax, as well as decreased Bcl-2 levels. EGFR/CDK2-IN-5 can be used for the research of cancers, such as lung cancer, breast cancer, and leukemia.

CDK7-IN-20 is a potent, selective and irreversible CDK7 (CDK) inhibitor with an IC₅₀ value of 4 nM. CDK7-IN-20 displays >206-fold selectivity for CDK7 over CDK1, CDK2, CDK3, CDK5, CDK6, CDK9 and CDK12 . CDK7-IN-20 has the potential for autosomal dominant polycystic kidney disease (ADPKD) research.

NU6310 is a non-covalent, ATP-competitive CDK2 inhibitor with an IC₅₀ of 0.16 μM against CDK2. NU6310 can be used for research on cell cycle regulation related to tumors.

CDK2-IN-47 is a potent CDK2 inhibitor with an IC₅₀ of 0.21 μM. CDK2-IN-47 exhibits outstanding anticancer activity against MCF-7, HCT-116, and MGC-803 cell lines. CDK2-IN-47 effectively induces G1 cell cycle arrest, retinoblastoma protein (Rb) dephosphorylation, and significant apoptosis. CDK2-IN-47 can be used for the studies of breast cancer, colorectal cancer and gastric cancer.

CDK2-IN-7 is a CDK2 inhibitor for researching cancer (IC₅₀ < 50 nM).

CDK2-IN-55 (Compound 12c) is a CDK2 inhibitor with an IC₅₀ value of 4.7 nM. CDK2-IN-55 also has a strong inhibitory effect on CDK1 (IC₅₀ = 26.3 nM), moderate inhibitory effects on Aurora A (IC₅₀ = 92.0 nM) and CDK9 (IC₅₀ = 288 nM), and very weak inhibitory activities on CDK4, CDK6, DYRK1A, and GSK3β (IC₅₀ > 1000 nM). CDK2-IN-55 shows strong anti-proliferative activity against various cancer cell lines, inducing cell cycle arrest and apoptosis. CDK2-IN-55 can be used for research on colorectal cancer, lung cancer, and cervical cancer.

8‑Acetonyldihydronitidine is a naturally occurring benzophenanthridine alkaloid with antibacterial, antifungal, and anti-proliferative activities against colorectal cancer cells. 8‑Acetonyldihydronitidine inhibits Staphylococcus aureus and exerts a potent antifungal effect against Cladosporium cladosporioides. 8‑Acetonyldihydronitidine activates the p53 signaling pathway, upregulates the expression of target genes including p21, BAX, and FAS, downregulates cyclin A and cyclin B, and induces cell cycle arrest and apoptosis, thereby suppressing the proliferation of colorectal cancer cells. 8‑Acetonyldihydronitidine is used in research related to colorectal cancer, fungal infections, and bacterial infections.