CDK Inhibitor

FKA-9i is an orally active anticancer agent. FKA-9i directly binds to and promotes the degradation of oncoproteins LRPPRC (k_d: 7.387 μM), YBX1 (k_d: 16.52 μM) and RPN1 (k_d: 26.82 μM). FKA-9i inhibits the MAPK signaling pathway and mitochondrial oxidative phosphorylation. FKA-9i also induces cancer cell cycle arrest, apoptosis, mitochondrial dysfunction and ROS accumulation. FKA-9i can be used in the research of tumors such as gastric cancer.

CDK4-IN-2 (A17) is a CDK4 inhibitor, with K_i and IC₅₀ values of <10 nM. Used in cancer research.

CDK9-IN-36 (Compound T7) is a potent, selective and metabolically stable CDK9 inhibitor with an IC₅₀ value of 1.2 nM. CDK9-IN-36 effectively suppresses cell proliferation, reduces colony formation, and induces apoptosis in Osimertinib (HY-15772)-resistant NSCLC cells by downregulating Mcl-1. CDK9-IN-36 also demonstrates antitumor efficacy in a tumor xenograft model.

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.

CDK7-IN-29 (compound 20) is an inhibitor of CDK7 with an IC₅₀ value of 1.4 nM. CDK7-IN-29 has oral activity and good pharmacokinetic (PK) properties.

MRTX849-amide-C4-(o)-carborane is a KRAS^G12C inhibitor with mutation selectivity for cells expressing KRAS^G12C. MRTX849-amide-C4-(o)-carborane shows low intrinsic cytotoxicity in cancer cells. MRTX849-amide-C4-(o)-carborane covalently binds to Cys12 of KRAS^G12C, recruits Hsp70, promotes ubiquitination, and induces proteasome-dependent degradation of the target protein. MRTX849-amide-C4-(o)-carborane inhibits the activity of the downstream ERK signaling pathway and induces apoptosis signaling in cancer cells. MRTX849-amide-C4-(o)-carborane is applicable for the research of KRAS^G12C-positive cancers.

CDK8-IN-9 (compound 22) is a potent type II CDK8 inhibitor with an IC₅₀ value of 48.6 nM. CDK8-IN-9 can inhibit tumor growth and is used in colorectal cancer studies.

CDK9/PARP-IN-1 (compound 37) is a CDK9/PARP inhibitor. CDK9/PARP-IN-1 inhibits CDK9 and PARP1 with IC₅₀s of 118 and 107 nM, respectively. CDK9/PARP-IN-1 exhibits broad-spectrum antiproliferative effects across multiple cancer cell lines.

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.

Cdc7-IN-9 is a potent Cdc7 inhibitor and can be used for cancer research.

ARN25499 (compound 15) is a CDC42 inhibitor. ARN25499 can be used in cancer-related research.

Antitumor agent-104 (Compound 9) is an antitumor agent by inhibiting DNA damage repair in tumors. Antitumor agent-104 inhibits PARP1 enzymatic activity and the PAR protein level. Antitumor agent-104 also inhibits the expression of CDK12.

PARP-1/2-IN-2-IN-1 (Compound 12e) is a PARP1/2/CDK12 inhibitor (IC₅₀: 34, 30 and 285 nM respectively). PARP-1/2-IN-2 inhibits DNA damage repair, promotes cell cycle arrest and apoptosis. PARP-1/2-IN-2 inhibits the growth of TNBC cells and TNBC xenograft tumor.

EGFR/HER2/CDK9-IN-2 (Compound 9) is a potent inhibitor of EGFR/HER2/CDK9 with IC₅₀s of 145.35, 129.07, and 117.13 nM, respectively. EGFR/HER2/CDK9-IN-2 exhibits remarkable antitumor activity.