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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

    		Apoptosis WDR5 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-162014
    WDR5 degrader-1

    		PROTACs WDR5 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-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-157659
    WDR5-MLL1 antagonist 1

    		WDR5 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

    		WDR5 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-168475
    DD0-2363

    		Apoptosis WDR5 HDAC Cancer
    DD0-2363 (Compound 32d) is a dual-target inhibitor of WDR5-MLL1/HDAC. DD0-2363 inhibits cells proliferation and induces apoptosis in acute myeloid leukemia cells. DD0-2363 has antitumor activity and can be used in the research of acute myeloid leukemia .
    DD0-2363
  • 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
  • HY-168488
    WDR5 ligand 2

    		WDR5 Ligands for Target Protein for PROTAC Cancer
    WDR5 ligand 2 is the ligand for WDR5 and can be used for synthesis of PROTAC WDR5 degrader 1 (HY-168487) .
    WDR5 ligand 2
  • HY-168487
    PROTAC WDR5 degrader 1

    		DNA/RNA Synthesis PROTACs WDR5 Others
    PROTAC WDR5 degrader 1 (compound 8g) is a PROTAC degrader targeting WDR5. PROTAC WDR5 degrader 1 is composed of a target protein ligand (red part) WDR5 ligand 2 (HY-168488), a VHL-type E3 ligase ligand (blue part) (S,R,S)-AHPC (HY-125845), and a PROTAC linker (balck part) 5-Aminovaleric acid (HY-W015878), in which the VHL ligand and the PROTAC linker form a conjugate (HY-114176A) .
    PROTAC WDR5 degrader 1

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