2. Signaling Pathways
  3. Epigenetics
  4. WDR5

WDR5

WD repeat protein-5; WD40 repeat domain protein 5

WDR5 is a highly conserved WD40 repeat-containing protein that is essential for proper regulation of multiple cellular processes. WDR5 is best characterized as a core scaffolding component of histone methyltransferase complexes. WDR5 also plays a crucial role in mediating protein-protein interactions that sustain oncogenesis in human cancers. One prominent example is the interaction between the transcription factor MYC and WDR5, which is essential for oncogenic processes.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-157332
    WDR5-IN-7
    		Inhibitor 98.10%
    WDR5-IN-7 (Compound 22) is an orally bioavailable benzoxazepinone-based WD repeat domain 5 (WDR5) inhibitor. WDR5-IN-7 can be used for the research of anti-cancer.
    WDR5-IN-7
  • HY-153331
    DDO-2213
    		Inhibitor 98.84%
    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-162014
    WDR5 degrader-1
    		Degrader 98.00%
    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-100869A
    MM-589 TFA
    		Inhibitor 98.67%
    MM-589 TFA is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction. MM-589 binds to WDR5 with an IC50 of 0.90 nM and inhibits the MLL H3K4 methyltransferase activity with an IC50 of 12.7 nM.
    MM-589 TFA
  • HY-175802
    HBI-2375
    		Inhibitor 98.06%
    HBI-2375 (HYBI-084) is a brain-penetrant WDR5 inhibitor with an IC50 of 4.48 nM. HBI-2375 binds to the WINR5 and disrupts MLL1-WDR5 protein-protein interactions. HBI-2375 inhibits cancer cells proliferation and shows anti-tumor activity in AML mouse models, and increases tumor CD8+ cytotoxic T lymphocyte infiltration. HBI-2375 inhibits hERG with an IC50 of 17 µM.
    HBI-2375
  • HY-P10948A
    CS-VIP 8 hydrochloride
    		Inhibitor
    CS-VIP 8 hydrochloride is a selective allosteric WDR5 protein inhibitor (Ki= 0.008 μM). CS-VIP 8 hydrochloride induces conformational changes in the MLL1 complex, leading to the dissociation of MLL1 from the complex, inhibiting MLL1 histone methyltransferase activity and regulating HOX gene expression. CS-VIP 8 hydrochloride is promising for research of hematological diseases such as leukemia.
    CS-VIP 8 hydrochloride
  • HY-148817
    WDR5-0102
    		Inhibitor
    WDR5-0102 is an inhibitor of WDR5. WDR5-0102 specifically targets the WIN site of WDR5, disrupts the WDR5-MLL1 interaction, and reduces the histone methyltransferase activity of MLL1. WDR5-0102 exerts dose-dependent toxicity on MDSC-like cells and reduces their osteopontin levels, while showing extremely low cytotoxicity to pancreatic cancer cells. WDR5-0102 can be used in the research of related diseases such as acute myeloid leukemia, lymphoid leukemia, biphenotypic leukemia and pancreatic cancer.
    WDR5-0102
  • HY-100869
    MM-589
    		Inhibitor
    MM-589 is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction. MM-589 binds to WDR5 with an IC50 of 0.90 nM and inhibits the MLL H3K4 methyltransferase activity with an IC50 of 12.7 nM.
    MM-589
  • HY-132233
    DDO-2093
    		Inhibitor
    DDO-2093 is a potent MLL1-WDR5 protein-protein interaction inhibitor (IC50=8.6 nM; Kd=11.6 nM) with antitumor activity. DDO-2093 selectively inhibits the catalytic activity of MLL complex.
    DDO-2093
  • HY-141797
    MS33
    		Degrader 99.38%
    MS33 is a potent WDR5 degrader, with Kds of 870 nM and 120 nM for VCB and WDR5, respectively. MS33 induces WDR5 degradation in an E3 ligase VHL, and proteasome-dependent manner. MS33 can be used for the research of acute myeloid leukemia.
    MS33
  • HY-100869B
    MM-589 (racemic mixture ) TFA
    		Inhibitor 99.83%
    MM-589 (racemic mixture) TFA, is a racemic mixture of MM-589 TFA (HY-100869A). MM-589 TFA is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction. MM-589 binds to WDR5 with an IC50 of 0.90 nM and inhibits the MLL H3K4 methyltransferase activity with an IC50 of 12.7 nM.
    MM-589 (racemic mixture ) TFA
  • HY-141798
    OICR-9429-N-C2-NH2
    		Ligand
    OICR-9429-N-C2-NH2 is a ligand for Wd40 repeat domain protein 5 (WDR5) extracted from patent WO2019246570A1, intermediate 2. OICR-9429-N-C2-NH2 can be used in the synthesis of PROTACs.
    OICR-9429-N-C2-NH2
  • HY-150403
    XF067-68
    		Degrader 99.56%
    XF067-68 (example 132) is a PROTAC for targeted degradation of WD40 repeat domain protein 5 (WDR5). XF067-68 can be usde for the study of WDR5-mediated diseases. (Pink: target protein ligand (HY-141799); Blue: E3 ligase ligand (HY-173627); Black: linker (HY-Y0966); E3 ligase ligand + linker: HY-176517).
    XF067-68
  • HY-N1983R
    Caudatin (Standard)
    Caudatin (Standard) is the analytical standard of Caudatin (HY-N1983). This product is intended for research and analytical applications. Caudatin is an orally active and brain-penetrant C-21 steroidal found in Cynanchum bungei decne with a variety of biological activities. Caudatin can inhibit cell proliferation, migration, invasion, cause cell phase arrest, induce apoptosis, autophagy, ROS prodution and loss of mitochondrial membrane potential. Caudatin activates PARP, caspase-3, -7, -9, upregulates pro-apoptotic Bad and Bax and downregulates anti-apoptotic Bcl-2 and Bcl-XL. Caudatin suppresses VEGF, FAK phosphorylation, upregulates p21, p27, DR5 protein expression, activates the p38 MAPK, JNK and PPARα/TFEB-mediated autophagy-lysosomal signaling pathways. Caudatin can be used for the research of cancer, inflammation and neurological disease, such as glioma and Alzheimer's disease.
    Caudatin (Standard)
  • HY-157659
    WDR5-47
    		Antagonist 98.34%
    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.
    WDR5-47
  • HY-153728A
    (R)-WM-586
    		Inhibitor 99.07%
    (R)-WM-586 is the R-enantiomer of WM-586.
    (R)-WM-586
  • HY-179099
    WDR5 probe 1
    Multi-target kinase-IN-8 (compound 16) is an efficient and highly selective WDR5 chemical probe. Multi-target kinase-IN-8 is a pharmaceutical intermediate. Multi-target kinase-IN-8 can be used for cancer research.
    WDR5 probe 1
  • HY-169415
    DBL-6-13
    		Inhibitor
    DBL-6-13 is an inhibitor for WDR5 with a moderate binding affinity of 6.8 μM (microscale thermophoresis assay) and 9.1 μM (fluorescence polarization assay).
    DBL-6-13
  • HY-169389
    OICR41114
    		Degrader
    OICR41114 is a WDR5 PROTAC degrader with an EC50 of 40 nM. OICR41114 binds both DCAF1 and WDR5, and its binding affinity for DCAF1 is significantly enhanced in the presence of WDR5 (KD increases from 59 nM to 5 nM). OICR41114 exerts antiproliferative effects on MV4-11 cells. OICR41114 can be used for the research of acute myeloid leukemia.
    OICR41114
  • HY-RS15789
    WDR5B Human Pre-designed siRNA Set A
    		Degrader

    WDR5B Human Pre-designed siRNA Set A contains three designed siRNAs for WDR5B gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    WDR5B Human Pre-designed siRNA Set A
Cat. No. Product Name / Synonyms Application Reactivity