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WDR5-IN-1

" in MedChemExpress (MCE) Product Catalog:
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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-133121
    WDR5-IN-1

    		Histone Methyltransferase Apoptosis Cancer
    WDR5-IN-1 is a potent and selective WD repeat domain 5 (WDR5) inhibitor, with a Kd of <0.02 nM. WDR5-IN-1 inhibits MLL1 histone methyltransferase (HMT) activity with an IC50 of 2.2 nM. WDR5-IN-1 diminishes MYC recruitment at WDR5-displaced genes and exhibits potent anti-proliferative effects in CHP-134 (neuroblastoma) and Ramos (Burkitt’s lymphoma) lines .
    WDR5-IN-1
  • HY-148817
    WDR5-0102

    		WDR5 Cancer
    WDR5-0102 is an inhibitor targeting WDR5-MLL1 interface (Kdis=7 μM, Kd=4 μM). WDR5-0102 suppresses MLL1 HMT activity, but not human H3K4 methyltransferase SETD7 and six other HMTs: G9a, EHMT1, SUV39H2, SETD8, PRMT3, and PRMT5 .
    WDR5-0102
  • HY-162014
    WDR5 degrader-1

    		PROTACs Cancer
    WDR5 degrader-1 (compound 25) is a cereblon (CRBN)-recruiting WDR5 degrader. WDR5 degrader-1 selectively degraded WDR5 over the CRBN neo-substrate IKZF1 .
    WDR5 degrader-1
  • HY-157659
    WDR5-MLL1 antagonist 1

    		Others Others
    WDR5-MLL1 antagonist 1 (compound 47) is a compound optimized through protein crystal structure guidance. It has stronger antagonistic activity against WDR5-MLL interaction with a dissociation constant (Kd) of 0.3μM.
    WDR5-MLL1 antagonist 1
  • HY-163774
    WDR5-MYC-IN-1

    		Histone Methyltransferase Cancer
    WDR5-MYC-IN-1 (compound 4o) is a potent WDR5-MYC interaction inhibitor with a Ki value of 1.0 µM. WDR5-MYC-IN-1 shows antiproliferative activity .
    WDR5-MYC-IN-1
  • HY-153331
    DDO-2213

    		WDR5 Cancer
    DDO-2213 is an orally active and potent WDR5-MLL1 inhibitor, with an IC50 of 29 nM and a Kd value of 72.9 nM for the WDR5 protein. DDO-2213 selectively inhibits MLL (mixed lineage leukemia) histone methyltransferase activity and the proliferation of MLL translocation-harboring cells. DDO-2213 can be used for MLL fusion leukemia research .
    DDO-2213

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