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Early 2 Factor (E2F)

E2F (Early 2 Factor) constitutes a family of transcription factors playing a pivotal role in cell cycle regulation. E2F proteins bind to specific promoter regions within DNA, thereby activating gene expression associated with cell cycle progression, DNA replication, and apoptosis. Within normal cells, E2F activity is primarily regulated by the retinoblastoma protein (pRB) and its associated proteins, ensuring the orderly progression of the G1/S phase transition. Defects in the RB pathway or excessive E2F activation lead to abnormal cell proliferation and promote tumourigenesis.

HLM006474
T15486353519-63-8
HLM006474 is a pan inhibitor of E2F. This inhibits E2F4 DNA-binding (IC50: 29.8 µM in A375 cells).
  • $38
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ll-k8-22
T74784
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].
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MRT00033659
T161411401731-54-1
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.
  • $68
5 days
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