CDK Inhibitor

CDK12/13-IN-1 (Compound 4) is a CDK12/13 inhibitor. CDK12/13-IN-1 has antitumor activity .

Cdk5 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Cdk5 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

PROTAC BRD4 Degrader-27 is a selective cereblon-mediated BRD4 PROTAC degrader. PROTAC BRD4 Degrader-27 exhibits anticancer activity, induces G1 phase arrest, and inhibits DNA synthesis and colony formation. PROTAC BRD4 Degrader-27 suppresses HCC1806 tumor growth in xenograft mouse models. PROTAC BRD4 Degrader-27 can be used in breast cancer-related research.

EGFR/CDK2-IN-1 (Compound 3b) is an EGFR/CDK2 inhibitor. EGFR/CDK2-IN-1 shows good cytotoxicity against MCF7 and HepG2 cells. EGFR/CDK2-IN-1 can be used in cancer research.

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

Dalpiciclib (isethionate) is a CDK4/6 inhibitor. Dalpiciclib (isethionate) inhibits the kinase activity of CDK4 and CDK6, thereby blocking the G1-to-S phase transition of the cell cycle and suppressing abnormal cell proliferation. Dalpiciclib (isethionate) can be used for the study of breast cancer.

CDK-IN-10 (example 54) is a cyclin dependent kinase (CDK) inhibitor that can be used in cancer research.

TMLB-C16 is a potent and orally active B3GAT3 inhibitor with a K_D of 3.962 μM. TMLB-C16 suppresses proliferation and migration, and induces cell cycle arrest and apoptosis in MHCC-97H (IC₅₀ = 6.53 μM) and HCCLM3 cells (IC₅₀ = 6.22 μM). TMLB-C16 inhibits tumor growth in both MHCC-97H and HCCLM3 xenograft tumor mouse models without causing obvious toxicity. TMLB-C16 can be used for hepatocellular carcinoma research.

CDK4/6/HDAC-IN-1 (Compound N14) is a dual-targeting inhibitor of CDK4/6 and HDAC (IC₅₀: CDK4 = 7.23 nM, CDK6 = 13.20 nM, HDAC1 = 55.66 nM, HDAC6 = 48.38 nM). CDK4/6/HDAC-IN-1 induces cell Apoptosis and G0/G1 phase arrest through HDAC-p21-CDK signaling pathway. CDK4/6/HDAC-IN-1 inhibits hepatocellular carcinoma.

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.

CDK9-IN-18 is a potent CDK9 inhibitor. CDK9-IN-18 blocks the phosphorylation function of kinase CDK9. CDK9-IN-18 exhibits both good anticancer activity and low cellular activity. CDK9-IN-18 induces apoptosis.

CDK8-IN-10 (compound 2) is a potent, selective cyclin-dependent kinase (CDK8) inhibitor with an IC₅₀ value of 8.25 nM. CDK8-IN-10 can be used for research of cancer.

AG-12275 is a cyclin-dependent kinase (CDK) inhibitor. AG-12275 can be used for the research of cancer.

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.

CLK1/4-IN-2 is a selective CLK1/4 inhibitor, with an IC₅₀ of 7 nM against CLK1 and an IC₅₀ of 2.3 nM against CLK4. CLK1/4-IN-2 induces protein depletion in cancer cells and exhibits anticancer activity. CLK1/4-IN-2 can be used in research related to breast cancer, monocytic leukemia, bladder cancer, mammary adenocarcinoma and hepatocellular carcinoma.

CDK9-IN-46 (Compound Formula I) is a CDK9 inhibitor. CDK9-IN-46 can be used for the research of cancer.

CDK9-IN-42 is a potent and selective CDK9 inhibitor with an IC₅₀of 3.8 nM. CDK9-IN-42 can inhibit the growth of cancer cells and induce apoptosis by downregulating Myc-1 and c-Myc. CDK9-IN-42 can be used for the research of cancer, such as breast and lungcancer.

CDK9-IN-40 is a potent and orally active CDK9 inhibitor with an IC₅₀ of 5.5 nM. CDK9-IN-40 shows high selectivity for CDK9 versus CDK1, CDK2, CDK4, and CDK6, respectively. CDK9-IN-40 can arrest cell cycle, induce cell apoptosis and inhibit tumor growth. CDK9-IN-40 exhibits strong anti-cancer activity.

CDK4/6-IN-16 (example 195) is a potent CDK4 and CDK6 inhibitor, with an IC₅₀ of 0.013 μM for CDK4. CDK4/6-IN-16 can be used for the research of CDK4-mediated disorders, such as cancer.

(S)-Cdc7-IN-18 is a potent inhibitor of CDC7. Overexpression of huCdc7 promotes overactivation of MCM2, an important marker of tumor cells, and thus promotes aberrant proliferation of tumor cells. (S)-Cdc7-IN-18 has the potential for the research of cancer diseases (extracted from patent WO2020239107A1, compound 1-1).