Catalog No.
Product Name
Application
Product Information
Citations
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WDR5 antagonist
WDR5-0103 is a small molecule that binds a peptide-binding pocket on WDR5 (Kd = 450 nM), inhibiting the catalytic activity of the MLL core complex in vitro (IC50 = 39 M).- Nicolas A Fraunhoffer, .et al. , EBioMedicine, 2023, Jun;92:104602 PMID: 37148583
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WDR5 and MLL protein-protein interaction inhibitor
MM-589 TFA is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction. -
WDR5/MLL interaction inhibitor
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. -
WDR5 Degrader
MS67 is a highly potent and selective PROTAC degrader of WD40 repeat domain protein 5 (WDR5), exhibiting minimal activity against other protein methyltransferases, kinases, GPCRs, ion channels, and transporters. Its strong anticancer activity highlights its utility as a targeted tool for studying WDR5-related epigenetic regulation and cancer therapy. -
MLL1-WDR5 Interaction Inhibitor
HBI-2375 is a selective inhibitor of the MLL1-WDR5 interaction, exhibiting a strong binding affinity with an IC50 of 4.48 nM. This compound effectively inhibits proliferation in MV4;11 leukemia cells, with an IC50 of 3.17 µM. Additionally, HBI-2375 disrupts histone methyltransferase activity, making it a valuable tool for research on leukemia, glioma, and glioblastoma. Its ability to penetrate the blood-brain barrier and its oral bioavailability further enhance its potential for in vivo studies. -
WDR5 Degrader
MS33 is a potent WDR5 degrader that functions through E3 ligase VHL-mediated degradation. It exhibits binding affinities of 870 nM for VCB and 120 nM for WDR5, effectively targeting this protein for proteasomal degradation. MS33 is primarily utilized in research related to acute myeloid leukemia, aiding in the understanding of WDR5's role in cancer biology. -
MLL1 Inhibitor
MM-401 TFA is a selective inhibitor of the MLL1 H3K4 methyltransferase, functioning primarily by disrupting the interaction between MLL1 and WDR5 (IC50 = 0.32 μM). This compound has demonstrated the capability to induce cell cycle arrest, promote apoptosis, and facilitate differentiation in various cell types. Its unique mechanism makes MM-401 TFA a valuable tool for investigating the role of MLL1 in MLL leukemia research. -
WDR5 Inhibitor
WDR5-IN-1 is a highly selective inhibitor of WD repeat domain 5 (WDR5), demonstrating a binding affinity (Kd) of less than 0.02 nM. It effectively inhibits the MLL1 histone methyltransferase activity with an IC50 of 2.2 nM, leading to reduced MYC recruitment at WDR5-displaced genes. This compound exhibits significant anti-proliferative effects in neuroblastoma (CHP-134) and Burkitt’s lymphoma (Ramos) cell lines, making it a valuable tool for research in cancer biology and epigenetics. -
WDR5 Inhibitor
WDR5-IN-4 is a selective inhibitor of the WDR5 protein, which plays a crucial role in chromatin regulation. With a Kd value of 0.1 nM, WDR5-IN-4 effectively displaces WDR5 from chromatin, leading to decreased expression of associated genes and subsequent inhibition of translation, resulting in nucleolar stress. This compound demonstrates potential anti-cancer effects, making it a valuable tool for research into gene regulation and cancer therapeutics. -
WDR5 Inhibitor
WDR5-IN-4 TFA is a potent inhibitor targeting the WIN site of the chromatin-associated protein WDR5, exhibiting a Kd of 0.1 nM. This compound effectively displaces WDR5 from chromatin, leading to a reduction in the expression of WDR5-associated genes, resulting in translational inhibition and nucleolar stress. Its significant anti-cancer activity makes WDR5-IN-4 TFA a valuable tool for research in cancer biology and therapy modulation. -
MLL1 Inhibitor
MM-401 is a potent inhibitor of MLL1, a methyltransferase that targets H3K4. By interfering with the MLL1-WDR5 interaction, MM-401 effectively inhibits MLL1 activity with an IC50 of 0.32 μM. This compound has been shown to induce cell cycle arrest, promote apoptosis, and facilitate differentiation. MM-401 is particularly relevant for research focused on MLL leukemia. -
DNA/RNA Synthesi
PROTAC WDR5 degrader 1 is a bifunctional degrader that selectively targets WDR5, promoting its proteasomal degradation via a VHL-type E3 ligase mechanism. This compound consists of a WDR5 ligand, a VHL ligand, and a PROTAC linker, facilitating the targeted degradation of WDR5 in cellular environments. Its distinct mechanism of action makes it a valuable tool for investigating WDR5-related biological pathways and their involvement in various diseases, including cancer and developmental disorders. Researchers can utilize this reagent for studies in targeted protein degradation and gene regulation. -
WDR5-MYC PPI Inhibitor
WDR5-MYC-IN-2 is a potent inhibitor of the WDR5-MYC protein-protein interaction, exhibiting an IC50 of 0.59 μM. This compound is valuable for investigating MYC-driven cancers and facilitates the development of novel WDR5-MYC PPI inhibitors. Its mechanism of action offers insights into therapeutic strategies targeting MYC in oncogenesis. -
WDR5 Inhibitor
WDR5-IN-5 is a selective inhibitor targeting the WIN site of the WD repeat domain 5 (WDR5). This compound demonstrates significant anti-proliferative activity against various cancer cell lines and possesses favorable pharmacokinetic properties in murine models. With a high binding affinity to WDR5, the Ki value is recorded at less than 0.02 nM, making it a valuable tool for research into cancer biology and potential therapeutic applications. -
WDR5 Inhibitor
WDR5-IN-6 is a selective inhibitor of WDR5, acting primarily at the WBM site. This compound demonstrates significant anti-tumor activity by inhibiting cell proliferation in neuroblastoma cell lines. Additionally, WDR5-IN-6 exhibits notable synergy with OICR-9429, another WDR5 inhibitor that targets the WIN site. This compound is valuable for research applications focused on neuroblastoma and related oncological studies. -
WDR5 Inhibitor
WM-586 is a covalent inhibitor of WDR5, effectively disrupting the interaction between WDR5 and MYC with an IC50 value of 101 nM. This compound demonstrates significant potential in cancer research, particularly in the study of neuroblastoma, breast cancer, bladder cancer, and colorectal cancer. Its ability to target the WDR5-MYC complex makes it a valuable tool for exploring therapeutic strategies in various malignancies. -
WDR5-MYC Interaction Inhibitor
WM-662 is an inhibitor targeting the WDR5-MYC interaction, exhibiting an IC50 of 18 μM. This compound is particularly relevant for investigations into cancer biology, aging processes, and neurodegenerative disorders. Its ability to disrupt the WDR5-MYC interaction positions WM-662 as a valuable tool in studying dysregulated gene expression associated with these conditions. -
WDR5-MYC Interaction Inhibitor
Anticancer agent 126 is a specific inhibitor of the WDR5-MYC interaction, targeting the critical role of this complex in oncogenic signaling. This compound effectively disrupts the binding of WDR5 to MYC, leading to a reduction in MYC target gene expression. It is suitable for research applications focused on elucidating the mechanisms of cancer biology and developing therapeutic strategies against MYC-driven malignancies. -
WDR5 Inhibitor
WDR5-IN-7 is a potent inhibitor of WD repeat domain 5 (WDR5), utilizing a benzoxazepinone structure. This compound exhibits significant anti-cancer activity and is particularly useful in the study of various tumor models. WDR5-IN-7 serves as a valuable tool for elucidating the role of WDR5 in oncogenic processes and for exploring therapeutic strategies in cancer research. -
WDR5-MLL1 Inhibitor
DDO-2213 is a potent inhibitor of the WDR5-MLL1 complex, exhibiting an IC50 of 29 nM and a Kd value of 72.9 nM for WDR5. This compound selectively targets MLL histone methyltransferase activity, effectively inhibiting the proliferation of cells containing MLL translocations. DDO-2213 is a valuable tool for research focused on MLL fusion leukemia and its underlying mechanisms. -
CRBN Degrader
WDR5 Degrader-1 is a cereblon (CRBN)-recruiting compound designed to selectively induce degradation of the WDR5 protein. This degrader effectively targets WDR5 while sparing the CRBN neo-substrate IKZF1, facilitating precise manipulation of WDR5 levels in cellular systems. It is a valuable tool for investigating the biological roles of WDR5 in transcriptional regulation and potential therapeutic strategies in diseases associated with dysregulated WDR5 expression. -
WDR5-MLL1 Inhibitor
WDR5-0102 is a selective inhibitor of the WDR5-MLL1 complex, exhibiting a dissociation constant (Kd) of 4 μM and a competitive inhibition constant (Kdis) of 7 μM. This compound effectively suppresses the H3K4 methyltransferase activity of MLL1 without affecting other human methyltransferases, including SETD7 and several others such as G9a, EHMT1, SUV39H2, SETD8, PRMT3, and PRMT5. WDR5-0102 is a valuable tool for investigating the role of MLL1 in various biological processes and its implications in cancer research. -
MLL1-WDR5 PPI Inhibitor
DDO-2093 is a selective inhibitor of the MLL1-WDR5 protein-protein interaction, exhibiting a potent IC50 of 8.6 nM and a dissociation constant (Kd) of 11.6 nM. This compound demonstrates significant antitumor activity by selectively targeting and inhibiting the catalytic function of the MLL complex. DDO-2093 is useful in research focused on understanding MLL-related oncogenesis and potential therapeutic strategies in cancer treatment. -
WDR5 Ligand
OICR-9429-N-C2-NH2 is a selective ligand for WDR5, a key protein involved in the regulation of gene expression and crucial in oncogenic pathways. This compound facilitates the design and synthesis of PROTACs (Proteolysis Targeting Chimeras), allowing for targeted protein degradation. Its unique properties make it a valuable tool for cancer research and the development of innovative therapeutic strategies. -
PROTAC WDR5 Degrader
XF067-68 is a PROTAC designed for the targeted degradation of the WD40 repeat domain protein 5 (WDR5). This compound facilitates the specific elimination of WDR5, making it a valuable tool for investigating diseases associated with WDR5 dysregulation. Researchers can employ XF067-68 to elucidate the biological roles of WDR5 and explore potential therapeutic interventions in related disorders. -
WDR5 Antagonist
WDR5-47 is a potent WDR5 antagonist that specifically disrupts the WDR5-MLL1 interaction. This compound demonstrates significant biological activity with a dissociation constant (Kd) of 0.3 μM, showcasing its effectiveness in inhibiting WDR5-mediated functions. WDR5-47 is ideal for research applications focusing on epigenetic regulation and will aid in the investigation of oncogenic processes involving the MLL1 complex. -
WDR5 Degrader
XF056-132 free base is a potent WDR5 (WD40 repeat domain protein 5) degrader that utilizes the proteolysis-targeting chimeric (PROTAC) mechanism. This compound effectively promotes the selective degradation of WDR5, which is implicated in various cancers and transcriptional regulation processes. XF056-132 serves as a valuable tool for research into targeted protein degradation and its therapeutic potential in oncological studies. -
WDR5-MLL1 Ligand
Z88418521 is a ligand targeting the WDR5-MLL1 complex, acting to disrupt its interaction. This compound demonstrates potential inhibitory effects on pathways associated with oncogenesis, particularly in leukemia research. Z88418521 serves as a valuable tool for investigating the molecular mechanisms underlying various cancer pathologies. -
WDR5 PROTAC Degrader
MS40 is a WDR5 PROTAC degrader with a Kd of 125 nM, which facilitates the ubiquitination and subsequent degradation of the WDR5 protein. The degradation of WDR5 causes the dissociation of the MLL/KMT2A complex from chromatin, leading to reduced levels of H3K4me2. This compound is instrumental in investigating the mechanistic pathways involved in primary leukemia. -
WDR5 Ligand
WDR5 ligand 2 is a specific ligand for the WDR5 protein, which plays a crucial role in regulating gene expression and chromatin dynamics. This compound can be utilized in the synthesis of PROTAC WDR5 degrader 1, facilitating targeted protein degradation studies. Its application is valuable in research focusing on epigenetic regulation and cancer biology. -
WDR5 Ligand
Dimethyl-F-OICR-9429-COOH is a potent ligand for the WD40 repeat domain protein 5 (WDR5), functioning as a critical component in the synthesis of proteolysis-targeting chimeras (PROTACs). Its specific binding to WDR5 facilitates the targeted degradation of associated proteins, making it a valuable tool in chemical biology research. This compound is instrumental in the exploration of protein interactions and the development of innovative therapeutic strategies. -
WDR5-MLL1 Interaction Disruptor
Z116334910 is a potent disruptor of the WDR5-MLL1 interaction. It exhibits significant biological activity in inhibiting the assembly of MLL1 complexes, making it valuable in cancer research. This compound can be applied to investigate the role of WDR5-MLL1 interactions in oncogenic processes and therapeutic strategies targeting these pathways.
