retinoblastoma protein

TPCK is an irreversible inhibitor of chymotrypsin-like proteases that affect cell proliferation, apoptosis, and tumorigenesis

NU6300 is an inhibitor of the first covalent ATP-competitive CDK2.

CDK4/6-IN-15 hydrochloride is an orally active selective inhibitor of CDK4/6. It effectively restrains the growth of cancer cells by arresting the cell cycle at the G1 phase. Additionally, CDK4/6-IN-15 hydrochloride inhibits phosphorylation of the retinoblastoma tumor suppressor protein (Rb) at site S780 and suppresses E2 factor (E2F)-regulated gene expression.

A-83586C is a depsipeptide antibiotic from Streptomyces karnatakensis with potent against Gram-positive activity in vitro. A-83586C acts as a highly potent inhibitor of beta-catenin/TCF4 signaling within cancer cells, while simultaneously downregulating o

CDK-IN-9 (compound 24) is a potent inhibitor of CDK and acts on CDK2/E (IC50: 4 nM). It functions as a molecular gel that induces interaction between CDK12 and DDB1, and can dephosphorylate retinoblastoma protein and RNA polymerase II, thereby inducing apoptosis.

D-erythro-Sphingosine hydrochloride, also known as Erythrosphingosine, serves as a specific TRPM3 activator and induces retinoblastoma protein dephosphorylation.

CDK4/6-IN-15, an orally active and selective inhibitor of CDK4/6, effectively halts the growth of cancer cells by arresting the cell cycle at the G1 phase and inhibiting the phosphorylation of the retinoblastoma tumor suppressor protein (Rb) at S780, as well as suppressing E2 factor (E2F)-regulated gene expression.

PAWI-2 functions as both a p53 activator and a Wnt inhibitor. It suppresses β3-KRAS signaling independently of KRAS and selectively inhibits the phosphorylation of TBK1. Additionally, PAWI-2 triggers apoptosis (activation of caspase-3/7) and induces PARP cleavage. It facilitates the translocation of retinoblastoma protein into the nucleus, leading to G2/M cell cycle arrest. PAWI-2 reverses the cancer stem cell-like properties of KRAS-dependent human pancreatic cancer stem cells (hPCSC) and overcomes drug resistance. Moreover, it inhibits the growth of hPCSC tumors in an orthotopic xenograft mouse model.

Dalpiciclib (SHR-6390) is a highly selective, orally bioavailable, and comparable potency inhibitor of CDK4 and CKD6 with IC50s of 12.4 nM and 9.9 nM, respectively. Dalpiciclib exerts potent antitumor activity in esophageal squamous cell carcinoma by inhibiting phosphorylated tumor suppressor retinoblastoma protein (Rb) and inducing G1 cell cycle arrest.