CDK Inhibitor

rel-(2S,3R)-Voruciclib is the (2S,3R)-enantiomer of Voruciclib. (2S,3R)-Voruciclib is an orally active CDK inhibitor.

PROTAC BCL6/GSPT1 Degrader-1 is a dual-target PROTAC degrader that targets BCL6 and GSPT1. PROTAC BCL6/GSPT1 Degrader-1 inhibits cell proliferation, promotes DNA damage, and induces cell cycle arrest and apoptosis in diffuse large B-cell lymphoma. PROTAC BCL6/GSPT1 Degrader-1 can be used for research on tumors such as lymphoma.

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.

CDK7-IN-25 (CY-16-1) is a CDK-7 inhibitor (IC₅₀<1nM) that can be used in cancer research.

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.

KRAS G13D-IN-2 (compound 8B) is a potent orally active KRAS G13D inhibitor with IC₅₀ values of 1.95 μM (HCT-116^G13D) and 2.16 μM (HCT-15^G13D). KRAS G13D-IN-2 induces G1-phase arrest and mitochondrial membrane depolarization. KRAS G13D-IN-2 induces senescence through CDK6/TWIST1 inhibition. KRAS G13D-IN-2 inhibits tumor growth in murine models. KRAS G13D-IN-2 can be used for KRAS^G13D-mutant colorectal cancer research.

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

CDK4/6-IN-21 (compound I-52) is a CDK4/6 inhibitor with IC₅₀ values of 3.88 and 3.31 nM for CDK4 and CDK6, respectively. CDK4/6-IN-21 has antitumor activity.

CDK9-IN-27 (Compound 6a) is a CDK9 inhibitor (IC₅₀s: 0.424 μM). CDK9-IN-27 induces apoptosis and cell cycle arrest at S stage. CDK9-IN-27 has cytotoxic action against HepG2, HCT-116 and MCF-7 cell lines, with IC₅₀s of 10.31-40.34 μM. CDK9-IN-27 can be used for cancer research.

CDK2-IN-19 (Compound 32) is a selective and orally active CDK2 inhibitor (K_i: 0.18 nM). CDK2-IN-19 shows anticancer activity in mice bearing OVCAR3 tumors.

CDK2-IN-11 (compound 9d) is a potent CDK2 inhibitor with an IC₅₀ of 6.4 μM, and K_I values of 23.4 nM, 56.3 nM and 44.3 nM for hCA II, hCA IX and hCA XII, respectively. CDK2-IN-11 can be used for researching anticancer.

ZJC-11 is a CDK7 inhibitor with an IC₅₀ of 5.4 nM. ZJC-11 binds covalently to CDK7, inhibits CDK7-dependent phosphorylation of RNAPII at Ser2, Ser5 and Ser7 sites, and suppresses transcriptional processes. ZJC-11 acts as a cell cycle inhibitor, inhibits the G2/M checkpoint pathway, and induces G2/M phase arrest. ZJC-11 induces DNA damage-driven cellular senescence and cell death. ZJC-11 exhibits antiproliferative activity against triple-negative breast cancer both in vitro and in vivo. ZJC-11 can be used for research related to triple-negative breast cancer

SHP2/CDK4-IN-1 (compound 10) is an orally active and potent SHP2 and CDK4 dual inhibitor, with IC₅₀ values of 4.3 and 18.2 nM, respectively. SHP2/CDK4-IN-1 effectively induces G0/G1 arrest to prevent the proliferation of TNBC cell lines. SHP2/CDK4-IN-1 shows significant antitumor efficacy in the EMT6 syngeneic mouse model. SHP2/CDK4-IN-1 can be used for triple-negative breast cancer (TNBC) research.

CDK4/6-IN-5 is a potent CDK4 and CDK6 inhibitor with K_is of 0.2 and 4.4 nM for CDK4/Cyclin D1 and CDK6/Cyclin D3, respectively. (from patent WO2019207463A1 example A93).

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.

CDK4 Human Pre-designed siRNA Set A contains three designed siRNAs for CDK4 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

CDK8-IN-5 is a potent CDK8 inhibitor with an IC₅₀ of 72 nM. CDK8-IN-5 shows anti-inflammatory activities with 43% IL-10 enhancement rate. CDK8-IN-5 has the potential for the research of inflammatory bowel disease.

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.

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

BMI-1026 is a cyclin-dependent kinase 1 (Cdk1) inhibitor with IC₅₀ of 2.3 nM. BMI-1026 induces apoptosis by arresting the G2-M phase.