wdr 5

WDR5-0103 hydrochloride[890190-22-4(free base)] (WD-Repeat Protein 5-0103) is an effective and specific WD repeat-containing protein 5 (WDR5) antagonist (Kd: 450 nM).

WDR5-0103 (WD-Repeat Protein 5-0103) is an effective and specific WD repeat-containing protein 5 (WDR5) antagonist (Kd: 450 nM).

WDR5-IN-6 is a WDR5 inhibitor targeting the WBM locus and is highly synergistic with OICR-9429, a WDR5 inhibitor that targets the WIN locus. It exhibits potent antitumor activity and inhibits cell proliferation in neuroblastoma cell lines, making WDR5-IN-6 suitable for neuroblastoma research.

WIN site inhibitor 1 is a WIN site of chromatin-associated WD repeat-containing protein 5 (WDR5) inhibitor (Kd: 0.1 nM), with anti-cancer activity.

WDR5ligand 2 is a ligand for WDR5 and can be utilized in the synthesis of PROTAC WDR5degrader 1.

WDR5-IN-7 (Compound 22) is an orally bioavailable benzoxazinone-based inhibitor of the WD repeat domain 5 (WDR5). It is useful in cancer research.

WDR5degrader-1 is a cereblon (CRBN) degrader that recruits WDR5. It selectively targets CRBN's new substrate IKZF1 for the degradation of WDR5.

WDR5-IN-8 is a WDR5 inhibitor with an IC50 value of 15.5 nM. It displays significant antiproliferative activity in two human acute leukemia cell lines and possesses antitumor properties.

WDR5-MYC-IN-2 is an inhibitor of the WDR5-MYC protein-protein interaction (PPI) with an IC50 of 0.59 μM. It is utilized in research on MYC-driven cancers and in the development of other potent WDR5-MYC PPI inhibitors.

WDR5-IN-5 is a selective, orally active inhibitor targeting the WD repeat domain 5 (WDR5) WIN site.WDR5-IN-5 exhibits high affinity for WDR5 (Ki<0.02 nM).WDR5-IN-5 exhibits anti-cancer cell proliferation and a good pharmacokinetic profile.

WDR5-0102 is a compound that inhibits the WDR5-MLL1 interface (K dis = 7 μM, K d = 4 μM), selectively reducing MLL1 HMT activity without affecting the human H3K4 methyltransferase SETD7 or other HMTs, including G9a, EHMT1, SUV39H2, SETD8, PRMT3, and PRMT5.

WDR5-IN-4 TFA is an inhibitor of the WIN site of chromatin-associated WD repeat-containing protein 5 ( WDR5 ), with a K d 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 [1] .

MM-589 is a potent WD repeat domain 5 (WDR5) inhibitor and mixed lineage leukemia (MLL) protein-protein interaction.

MM-589 TFA is a potent inhibitor of WD repeat domain 5 (WDR5) and a modulator of mixed lineage leukemia (MLL) protein-protein interaction.

OICR-9429 is a potent antagonist of the interaction that WDR5 effect with peptide regions of MLL and Histone 3. It reduces the viability of acute myeloid leukemia cells in vitro.

WDR5-47 is a potent small molecule to disturb the interaction of MLL1-WDR5 with IC50 value of 0.3μM.

Homer is a specific probe targeting WDR5. In MV4-11 cells, Homer induces the degradation of WDR5 protein with a DC50 of 53 nM. At a concentration of 1 µM, Homer reduces WDR5 protein levels in MV4-11 cells without affecting its mRNA expression.

WDR5-MYC-IN-1 (compound 4o) is an effective inhibitor of the WDR5-MYC interaction, demonstrating a Ki value of 1.0 µM and exhibiting antiproliferative activity.

MS67 is a potent and selective degrader of WD40 repeat domain protein 5 (WDR5) with a dissociation constant (Kd) of 63 nM, exhibiting no activity against protein methyltransferases, kinases, G-protein-coupled receptors (GPCRs), ion channels, and transporters, and notably demonstrating significant anticancer properties.

MS33 is a highly effective degrader of the WDR5 protein, exhibiting Kd values of 870 nM and 120 nM for VCB and WDR5, respectively. It induces degradation of WDR5 through an E3 ligase VHL-mediated and proteasome-dependent mechanism. MS33 holds promise for furthering research in the field of acute myeloid leukemia.

MR44397 is a ligand for WD40 repeat (WDR) 5 and is applicable in cancer research.