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-16993
    OICR-9429
    		Inhibitor 99.71%
    OICR-9429 is high affinity WD repeat domain 5 (WDR5) inhibitor, competitively blocks WDR5 interaction with MLL protein via binding the central peptide-binding pocket of WDR5. OICR-9429 can suppress histone H3K4 trimethylation and can be used for the research of various cancers including non-MLL-rearranged leukaemia, colon, pancreatic, prostate cancer and bladder cancer (BCa) .
    OICR-9429
  • HY-141796
    MS67
    		Degrader 98.73%
    MS67 is a potent and selective WD40 repeat domain protein 5 (WDR5) degrader with a Kd of 63 nM. MS67 is inactive against other protein methyltransferases, kinases, GPCRs, ion channels, and transporters. MS67 shows potent acticancer effects.
    MS67
  • HY-19347
    WDR5-0103
    		Antagonist 99.93%
    WDR5-0103 (WD-Repeat Protein 5-0103) is a potent and selective WD repeat-containing protein 5 (WDR5) antagonist with a Kd of 450 nM. WDR5-0103 competitively binds to the peptide-binding pocket of WDR5, blocking the interaction between WDR5 and mixed-lineage leukemia (MLL) protein and inhibiting the methyltransferase activity of MLL. WDR5-0103 is mainly used in the research of cancer and neurodegenerative diseases.
    WDR5-0103
  • HY-12220
    MM-102
    		Inhibitor 99.39%
    MM-102 (HMTase Inhibitor IX) is a cell-permeable and tightly binding inhibitor of MLL1-WDR5 interaction (IC50=2.4 nM). MM-102 can specifically inhibit the growth and induce apoptosis of leukemia cells containing MLL1 fusion protein, and reduce renal fibrosis and inflammation in mice with ischemia-reperfusion injury. In addition, MM-102 also acts as an H3K4 histone methyltransferase inhibitor to improve the development of porcine somatic cell nuclear transfer (SCNT) embryos.
    MM-102
  • HY-133121
    WDR5-IN-1
    		Inhibitor ≥98.0%
    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-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 (PROTAC 4) is a WDR5-targeting PROTAC degrader. OICR41114 degrades endogenous WDR5 with an EC50 and Dmax values of 40 nM and 49%, respectively. OICR41114 degrades HiBiT-tagged WDR5 in a proteasome-dependent manner. OICR41114 is composed of target protein ligand (red part) Dimethyl-F-OICR-9429-COOH (HY-141799), E3 ligase ligand (blue part) OICR-8268-acrylic acid (HY-169390) and PROTAC linker (black part) Amino-PEG9-amine (HY-140210). The conjugate of E3 ligase ligand and linker is OICR-8268-acrylic acid-amino-PEG9-amine (HY-169391).
    OICR41114
  • HY-159993
    MR44397
    		Inhibitor
    MR44397 is a WD40 repeat (WDR) 5 ligand, can be used for cancer research.
    MR44397
  • HY-150654
    WDR5-IN-5
    		Inhibitor 98.92%
    WDR5-IN-5 is an orally active and selective inhibitor of WIN site of WD repeat domain 5 (WDR5). WDR5-IN-5 exhibits anti-proliferative activity towards cancer cells and good pharmacokinetics profile in mice. WDR5-IN-5 shows high affinity to WDR5 and the binding affinity Ki value <0.02 nM.
    WDR5-IN-5
  • HY-111753A
    WDR5-IN-4 TFA
    		Inhibitor 99.87%
    WDR5-IN-4 TFA is an inhibitor of the WIN site of chromatin-associated WD repeat-containing protein 5 (WDR5), with a Kd of 0.1 nM. WDR5-IN-4 TFA displaces WDR5 from chromatin and decreases the expression of associated genes, causing translational inhibition, nucleolar stress. Anti-cancer activity.
    WDR5-IN-4 TFA
  • HY-12220A
    MM-102 TFA
    		Inhibitor 99.68%
    MM-102 TFA (HMTase Inhibitor IX TFA) is a potent WDR5/MLL interaction inhibitor, achieves IC50 = 2.4 nM with an estimated Ki < 1 nM in WDR5 binding assay, which is >200 times more potent than the ARA peptide.
    MM-102 TFA
  • HY-154949
    WDR5-IN-6
    		Inhibitor 99.89%
    WDR5-IN-6 is a WDR5 inhibitor, targeting to WBM site. WDR5-IN-6 inhibits cell proliferation of neuroblastoma cell lines with potent anti-tumor activity. WDR5-IN-6 shows high synergy with OICR-9429 (HY-16993), a WDR5 inhibitor targeting to WIN site. WDR5-IN-6 can be used for reasearch in neuroblastoma.
    WDR5-IN-6
  • HY-19554A
    MM-401 TFA
    		Inhibitor 99.62%
    MM-401 (TFA) is a MLL1 H3K4 methyltransferase inhibitor. MM-401 inhibits MLL1 activity (IC50 = 0.32 μM) by blocking MLL1-WDR5 interaction. MM-401 can induce cell cycle arrest, apoptosis and differentiation. MM-401 can be used for the research of MLL leukemia.
    MM-401 TFA
  • HY-16994
    OICR-0547
    		Inhibitor 99.93%
    OICR-0547 is a negative control, closely related derivative of OICR-9429 (HY-16993). OICR-9429 is a novel small-molecule antagonist of the Wdr5-MLL interaction. OICR-0547 is an inactive control compound that no longer binds to WDR5.
    OICR-0547
  • HY-141799
    Dimethyl-F-OICR-9429-COOH
    		Ligand 98.05%
    Dimethyl-F-OICR-9429-COOH a ligand for WD40 repeat domain protein 5 (WDR5) extracted from patent WO2019246570A1 intermediate 19. Dimethyl-F-OICR-9429-COOH can be used in the synthesis of PROTACs.
    Dimethyl-F-OICR-9429-COOH
  • HY-153728
    WM-586
    		Inhibitor 98.74%
    WM-586 is a covalent WDR5 inhibitor that disrupts the binding of WDR5 to MYC. WM-586 specifically decreases cellular WDR5 and MYC interaction with the IC50 of 101 nM in HTRF assay.
    WM-586
  • HY-154847
    WM-662
    		Inhibitor 99.48%
    WM-662 is a WDR5-MYC interaction inhibitor, with an IC50 of 18 μM. WM-662 has potential for the research of cancer, aging, and neurodegenerative disorders.
    WM-662
  • HY-149873
    Anticancer agent 126
    		Inhibitor ≥98.0%
    Anticancer agent 126 (compound 12) is a WDR5 inhibitor with anticancer effects. Anticancer agent 126 disrupts WDR5-MYC interaction in cells and reduce MYC target gene expression.
    Anticancer agent 126
  • 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-148817
    WDR5-0102
    		Inhibitor
    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
Cat. No. Product Name / Synonyms Application Reactivity