wdr5

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.

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.

WDR5-0103 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).

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

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-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] .

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.

OICR-0547 is an inactive derivative of OICR-9429 and is commonly used as a negative control for OICR-9429. OICR-9429 is an inhibitor of the interaction between WDR5 and the mixed leukaemia (MLL) protein.

WIN site inhibitor 1 TFA is a WIN site of chromatin-associated WD repeat-containing protein 5 (WDR5) inhibitor (Kd: 0.1 nM).

MS40 is a WDR5 PROTAC that selectively degrades WDR5 and serves as a novel degrader for immune-modulating compounds (IMiDs), including the new substrates CRBN and Ikaros zinc finger (IKZF) transcription factors IKZF1 and IKZF3. MS40 facilitates the degradation of WDR5, resulting in the dissociation of the MLL/KMT2A complex from chromatin, thereby reducing H3K4me2 levels. In vitro, MS40 inhibits the growth of primary leukemia patient cells, and in vivo, it suppresses the expansion of patient-derived xenografts.

OICR41114 (PROTAC4) is a PROTAC degrader targeting WDR5. It effectively degrades endogenous WDR5 with an EC50 of 40 nM and a Dmax of 49%. The degradation of HiBiT-tagged WDR5 by OICR41114 occurs in a proteasome-dependent manner. This compound is composed of a target protein ligand, Dimethyl-F-OICR-9429-COOH, an E3 ligase ligand, OICR-8268-acrylic acid, and a PROTAC linker, Amino-PEG9-amine. Notably, the conjugate of the E3 ligase ligand and the linker is OICR-8268-acrylic acid-amino-PEG9-amine.

DBL-6-13 is an inhibitor of WDR5, displaying moderate binding affinity with dissociation constants (Kd) of 6.8 μM and 9.1 μM as determined by microscale thermophoresis analysis and fluorescence polarization analysis, respectively.

DD0-2363 (Compound 32d) is a dual-target inhibitor of WDR5-MLL1/HDAC. It can suppress the proliferation of acute myeloid leukemia cells and induce apoptosis. With its antitumor properties, DD0-2363 is applicable for research on acute myeloid leukemia.

CS-VIP 8 TFA is a selective allosteric inhibitor of the WDR5 protein (Ki= 0.008 μM). It induces a conformational change in the MLL1 complex, leading to the dissociation of MLL1 from the complex, thereby inhibiting the MLL1 histone methyltransferase activity and modulating HOX gene expression. CS-VIP 8 TFA shows potential for research in hematological disorders such as leukemia.