2. Signaling Pathways
  3. Cell Cycle/DNA Damage
  4. Early 2 Factor (E2F)

Early 2 Factor (E2F)

The Early 2 Factors (E2Fs) are a family of eight winged-helix transcription factors that are key to regulating cell cycle progression from G1 to S phase among other functions. E2F1, E2F2, and E2F3a are expressed in early G1 through S phase and are believed to promote S phase initiation by activating genes involved in the G1 to S phase transition18. E2F3b, E2F4, E2F6, E2F5, E2F7, and E2F8 act as repressors and are expressed later in the cell cycle. E2Fs participate in myriad cell biological processes including: the cell cycle, DNA repair, apoptosis, development, differentiation, and metabolism.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-16667
    HLM006474
    		Inhibitor 99.57%
    HLM006474 is a pan E2F inhibitor, which inhibits E2F4 DNA-binding with an IC50 of 29.8 μM in A375 cells.
    HLM006474
  • HY-149209
    LL-K8-22
    		Inhibitor 99.76%
    LL-K8-22 is a potent, selective and durable PROTAC CDK8-cyclin C dual degrader, with DC50 values of 2.52 and 2.64 μM, respectively. LL-K8-22 also suppresses STAT1 Ser 727 phosphorylation. LL-K8-22 inhibits E2F- and MYC-driven carcinogenic transcriptional programs. LL-K8-22 can be used for triplenegative breast cancer (TNBC) research. (Pink: Ligand for target protein (HY-168683); Black: Linker (HY-Y0340); Blue: Ligand for E3 ligase (HY-N2427)) .
    LL-K8-22
  • HY-117857
    MRT00033659
    		Inhibitor 99.77%
    MRT00033659 is a potent broad-spectrum kinase inhibitor of CK1 (IC50=0.9 μM for CK1δ) and CHK1 (IC50=0.23 μM). MRT00033659, a pyrazolo-pyridine analogue, induces p53 pathway activation and E2F-1 destabilisation.
    MRT00033659
  • HY-175397
    Dth
    		Degrader
    Dth is a RNA aptamer-based PROTAC degrader. Dth can degrade a range of endogenous proteins (such as mCherry, p50, p65 and E2F1) by simply replacing the 3′ module on the RNA scaffold with the corresponding RNA aptamer of target protein (target aptamer). Pink: Target aptamer ligand (HY-176801); Blue: CRBN ligase ligand (HY-41547); Black: linker (HY-79577)
    Dth
Cat. No. Product Name / Synonyms Application Reactivity