early 2 factor (e2f)

HLM006474 is a pan inhibitor of E2F. This inhibits E2F4 DNA-binding (IC50: 29.8 µM in A375 cells).

MRT00033659 is an effective broad-spectrum kinase inhibitor of CK1 (IC50=0.9 µM for CK1δ) and CHK1 (IC50=0.23 µM). MRT00033659 is a pyrazolo-pyridine analogue. It also induces p53 pathway activation and E2F-1 destabilization.

Dth is a proteolysis-targeting chimera (PROTAC) composed of the fluorescent RNA probe DFHBI and the immunomodulatory compound thalidomide.

Edifoligide sodium is a decoy oligonucleotide that binds to the E2F transcription factor, inhibiting its activity, which may help prevent neointimal hyperplasia and vein graft failure.

Edifoligide is a decoy oligonucleotide that binds to the E2F transcription factor, inhibiting its activity, which may help prevent neointimal hyperplasia and vein graft failure.

Ly101-4B is an apoptosis (apoptosis) inducer and multi-target inhibitor with antiproliferative, antitumor, and cytotoxic effects. It reduces HSF1 expression, inhibits microRNA-214 synthesis, and downregulates the expression of HSP27, HSP70, and HSP90. Additionally, Ly101-4B represses E2F-dependent transcriptional activity and downregulates its target genes. By decreasing DNA synthesis, inhibiting the cell cycle, and hindering the G1/S phase transition, Ly101-4B induces caspase3/7-mediated apoptosis without affecting RNA synthesis or causing necrosis. The compound demonstrates selectivity towards pancreatic ductal adenocarcinoma cells with varying genotypes and degrees of E2F dependency. Moreover, Ly101-4B is applicable in research related to epithelial ovarian cancer and pancreatic ductal adenocarcinoma.

JR4-187 is an orally active copper-dependent anti-cancer agent. It downregulates genes involved in oxidative phosphorylation, MYC targets, and E2F targets, while upregulating genes associated with the TNF-α signaling pathway, p53 pathway, and KRAS signaling pathway, in addition to reducing CTR1 protein levels. JR4-187 induces ROS production, apoptosis (apoptosis), and copper-dependent cytotoxicity, with selective cytotoxicity towards KRAS mutant cancer cells. It exhibits good tolerability in pancreatic cancer mouse models. JR4-187 is applicable for research in pancreatic ductal adenocarcinoma, colon cancer, rectal cancer, and other related cancers.

LL-K8-22 is a potent, selective, and durable dual degrader of CDK8-cyclin C, demonstrating DC50 values of 2.52 and 2.64 μM, respectively. This compound effectively suppresses STAT1 Ser 727 phosphorylation and inhibits carcinogenic transcriptional programs driven by E2F and MYC. LL-K8-22 is specifically utilized in research for triple-negative breast cancer (TNBC) [1].

INX-315 is an orally active, selective CDK2 inhibitor that induces cell cycle arrest and senescence in solid tumours, suppresses E2F target gene expression, and exhibits anticancer activity in ccne1-amplified cancers and cdk4/6i-resistant intraductal breast cancer models.