CDK2 Inhibitor

CDK1-IN-9 is an orally active and selective CDK1 inhibitor with an IC₅₀ of 5.5 nM. CDK1-IN-9 exhibits broad antiproliferative activity, particularly against HCT116 colon cancer cells. CDK1-IN-9 induces G2/M phase arrest and downregulates CDK1, cyclin B1, and the replication initiation factor CDC45. CDK1-IN-9 induces severe DNA replication stress, subsequently activating the p53 signaling pathway to trigger apoptosis. CDK1-IN-9 can be used for research on colon cancer, liver cancer and gastric cancer.

HS-36 is a highly selective and orally active dual inhibitor of CDK4 and CDK9 with IC₅₀ values of 18.9 and 4.2 nM respectively. HS-36 exhibits nanomolar-level potent activity against various cancer cells, inducing G0/G1 phase arrest and promoting cell apoptosis. HS-36 efficiently inhibits tumor growth in a mouse model of MV-4-11 tumors. HS-36 can be used for the study of acute myeloid leukemia.

CDK2-IN-15 (Compound 19) is an inhibitor of CDK2 with an IC₅₀ of 2.9 μM. CDK2-IN-15 can be used for cancer research.

LS-Q2 is a highly selective CDK4/9 inhibitor with IC₅₀ values of 1.4 nM and 6.2 nM. LS-Q2 inhibits cancer cells proliferation, induces G2/M phase arrest, apoptosis and reduces pSer2 RNA polymerase II expression. LS-Q2 interacts synergistically with BET and Bcl-2 inhibitors to drive antitumor activity. LS-Q2 can be used for the research of cancer, such as malignant solid tumors.

CDK2-IN-45 (Compound 8f) is a CDK2 inhibitor (IC₅₀: 0.64 μM). CDK2-IN-45 inhibits the proliferation of DU-145 and PC-3 cell lines with IC₅₀ of 2.20 μM and 4.17 μM, respectively. CDK2-IN-45 induces G0/G1 cell cycle arrest and apoptosis. CDK2-IN-45 can be used in prostate cancer research.

BMK-Y101 is a potent CDK kinase inhibitor. BMK-Y101 induces tumor cell apoptosis by inhibiting CDK kinases. BMK-Y101 can be used for research on hepatocellular carcinoma.

CDK2-IN-52 (Compound Cpb No 39) is a selective cyclin-dependent kinase 2 (CDK2) inhibitor with a DC₅₀ value of 1-10 nM. CDK2-IN-52 induces cell cycle arrest and suppresses tumor cell proliferation. CDK2-IN-52 is promising for research of CDK2-overexpressing malignancies such as breast and ovarian cancers.

PLK2-IN-1 is a selective PLK2 inhibitor (IC₅₀ 0.78 μM). PLK2-IN-1 induces Apoptosis and cell cycle arrest, reduces AKT and mTOR phosphorylation, and decreases Cyclin E expression as well as downregulates the CDK2/Rb/E2F1 axis. PLK2-IN-1 inhibits tumor growth in colorectal cancer xenograft models. PLK2-IN-1 can be used for research on colorectal cancer.

CDK2-IN-44 (Compound 46) is an inhibitor of cyclin-dependent kinase 2 (CDK2). CDK2-IN-44 can effectively inhibit the proliferation of cancer cells and exert its activity in inhibiting cancer cell growth by arresting the cell cycle, promoting Apoptosis, and inducing cellular senescence. CDK2-IN-44 holds promise for use in the research of ovarian cancer and breast cancer.

CDK2-IN-56 (compound 39) is a pyrazoloquinazoline-3-carboxamide and CDK2/CyA inhibitor. CDK2-IN-56 can be used for the research of cancer.

CDK2-IN-14-d₃ is a potent and selective CDK2 inhibitor. CDK2-IN-14-d₃ can be used in research of cancer.

CDK7-IN-27 (Compound 37) is a selective inhibitor for cyclin-dependent kinase 7 (CDK7), with K_i of 3 nM. CDK7-IN-27 arrests the cell cycle at G0/G1 phase.

UNC10112785 is a serine/threonine kinase inhibitor with a human GSK-3β IC₅₀ of 0.031 μM, human CDK-2 IC₅₀ of 0.016 μM, and human CDK-4 IC₅₀ of 1.99 μM. UNC10112785 can be used for the research of type 2 diabetes.

VEGFR2-IN-86 is a dual VEGFR2/CDK2 inhibitor, with an IC₅₀ of 0.06 μM against VEGFR2 and an IC₅₀ of 0.78 μM against CDK2. VEGFR2-IN-86 induces G-phase cell cycle arrest, reduces colony-forming ability and tumor cell migration capacity, and exerts antiproliferative activity in cancer cells. VEGFR2-IN-86 can be used for the research of breast cancer and prostate cancer.

CDK2-IN-59 is a CDK2 inhibitor with a IC₅₀ of 66.33 μM. CDK2-IN-59 stably interacts within the CDK2 active site and induces apoptosis in breast cancer cells. CDK2-IN-59 can be used for the research of breast cancer.

Isosilybin B (Standard) is the analytical standard of Isosilybin B (HY-N7045). This product is intended for research and analytical applications. Isosilybin B is a flavonolignan. Isosilybin B can be isolated from Silybum marianum. Isosilybin B can regulate cell cycle-related proteins (e.g., reduce cyclins (D3, D1, A, E), Cdk4, Cdk2, Cdc25A), and activate Caspases (Caspase-9 and Caspase-3). Isosilybin B can promote Apoptosis, reduce androgen receptor (AR) and PSA. Isosilybin B has anticancer activity against prostate cancer.

CDK1-IN-4 (10d) is a selective CDK1 inhibitor with IC₅₀s of 44.52, 624.93 and 135.22 nM for CDK1, CDK2 and CDK5, respectively. CDK1-IN4 inhibits the growth of cancer cells by affecting cell cycle. CDK1-IN-4 can be used for the research of cancer.

BRD4/AKT-IN-1 is a BRD4/AKT inhibitor with BRD4 IC₅₀ 66.12 nM and AKT1 IC₅₀ 143.81 nM. BRD4/AKT-IN-1 blocks BRD4-mediated c-Myc transcriptional regulation, modulates AKT1 signaling, decouples AKT phosphorylation from pro-survival effectors. BRD4/AKT-IN-1 induces G0/G1 cell cycle arrest via downregulated phosphorylated RB, cyclin E1, CDK2. BRD4/AKT-IN-1 elevates LC3B levels to promote autophagy. BRD4/AKT-IN-1 promotes apoptosis in cancer cells. BRD4/AKT-IN-1 can be used for the research of metastatic castration-resistant prostate cancer.

VEGFR-2-IN-69 (Compound 5A) is a dual inhibitor of VEGFR-2 and Telomerase, which upregulates the expression of caspase 3, caspase 8 and caspase 9, while downregulating CDK-2, CDK-4 and CDK-6. VEGFR-2-IN-69 exhibits an IC₅₀ of 15.46 µM against HCT116 cells.