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.

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.

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.

Tyrphostin AG17 is an orally active CDK2 inhibitor and EGFR tyrosine kinase antagonist. Tyrphostin AG17 reduces the levels of p21 and p16. Tyrphostin AG17 induces G1 phase cell cycle arrest, Apoptosis, mitochondrial dysfunction, decreased ATP levels, and inhibits DNA, RNA and protein synthesis, adipogenesis, and lipid synthesis. Tyrphostin AG17 inhibits fat accumulation, white adipose tissue hypertrophy, and alterations of glycogen and lipid inclusions in hepatocytes in obese mice without changing their serum biochemical parameters. Tyrphostin AG17 exhibits anticancer effects. Tyrphostin AG17 can be used in research related to immunoblastic lymphoma, leukemia, ovarian cancer, glioblastoma, colon cancer, breast cancer, melanoma, obesity and hepatic steatosis.

PHA-793887 hydrochloride is a CDK inhibitor (with IC₅₀ values of 8 nM for Cdk2, 60 nM for Cdk1, 62 nM for Cdk4, 138 nM for Cdk9). PHA-793887 hydrochloride inhibits purified GSK3β (IC₅₀ 79 nM). PHA-793887 hydrochloride reduces the phosphorylation level of nucleophosmin/cdc6, induces G1/G2/M phase arrest, and triggers Apoptosis by activating Caspase-3. PHA-793887 hydrochloride exhibits anticancer activity against leukemia. PHA-793887 hydrochloride can be used in research related to acute leukemia, chronic myeloid leukemia, and advanced/metastatic solid tumors.