CDK4 Inhibitor

GSK3-IN-10 (Compound 4) is a multi-target inhibitor, that mainly targets GSK3α and GSK3β with IC₅₀ of 1.0 nM and 2.0 nM. GSK3-IN-10 inhibits the activation of β-catenin, promotes the neuronal survival, and exhibits a protective effect against endoplasmic reticulum stress.

NUAK1-IN-1 (Compound 9) is a NUAK1 (IC₅₀ of 5.012 nM) and CDK4 inhibitor. NUAK1-IN-1 can be used in cancer, neurodevelopmental disorders and Alzheimer's disease research.

USP10-IN-4 is a potent ubiquitin-specific protease 10 (USP10) inhibitor with an IC₅₀ of 10.87 μM and a K_d of 365 nM. USP10-IN-4 effectively inhibits USP10-mediated proteasomal degradation of downstream proteins YAP and p53, leading to the subsequent downregulation of CDK4 in the p53 signaling pathway. USP10-IN-4 promotes apoptosis in HCC cells and inhibits the onset and progression of liver cancer. USP10-IN-4 can used for the study of hepatocellular carcinoma (HCC).

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.

CDK4/6/BRD4-IN-1 (B15) is an inhibitor of CDK4, CDK6 and BRD4, with IC₅₀ values of 220 nM, 146 nM, 106 nM and 85 nM for BRD4-BD2, BRD4-BD1, CDK6 and CDK4, respectively. CDK4/6/BRD4-IN-1 (B15) can be used in the study of NSCLC (Non-Small Cell Lung Cancer). CDK4/6/BRD4-IN-1 (B15) induces cell cycle arrest and apoptosis.

PROTAC BRD4 Degrader-16 is a BRD4 PROTAC degrader. PROTAC BRD4 Degrader-16 induces sustained degradation of both long and short isoforms of BRD4 in cancer cells, causes cell cycle arrest, and exhibits only extremely low apoptosis effects. PROTAC BRD4 Degrader-16 can be used in studies related to acute myeloid leukemia.

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.

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.

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.

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.

YY173 is a dual inhibitor for CDK4 and CDK6 with IC₅₀ of 7.7 and 88 nM. YY173 inhibits the proliferation of cell Jurkat with an IC₅₀ of 1.46 μM. YY173 can be used for synthesis of PROTAC CDK4/6 degrader 1 (HY-163786).

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-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.

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.

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.

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.

CDK4/6-IN-27 (Example 12) is a CDK4/6 inhibitor. CDK4/6-IN-27 can be used for researching diseases such as 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).