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WDR5 inhibitors and degraders act on WD repeat domain 5 (WDR5), a chromatin scaffold protein. WDR5 is a core subunit of the mixed-lineage leukemia (MLL) complexes that methylate lysine 4 of histone H3 (H3K4). A 2005 study showed that WDR5 binds methylated H3K4 and is required for this methylation and for vertebrate development. In 2015 WDR5 was also shown to help the transcription factor c-Myc recognize its target genes. OICR-9429, MM-589 and WDR5-0103 block the interaction between WDR5 and MLL. MS67 and MS33 are degraders that remove WDR5 protein from cells instead of only occupying a binding site.
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).
OICR-9429 is a novel small-molecule antagonist of the Wdr5-MLL interaction with IC50 of 5 uM. inhibit proliferation and induce differentiation .
MM-589 is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction.
OICR-0547 is a closely related derivative of OICR-9429. OICR-9429 is a novel small-molecule antagonist of the Wdr5-MLL interaction, while OICR-0547 cannot bind to WDR5.
Synonyms: MM589
MM-589 TFA is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction.
Synonyms: HMTase Inhibitor IX TFA; MM102
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.
Synonyms: HYBI-084
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.
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-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-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-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.
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.
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.
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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-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.
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.
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.
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-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.
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.
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.
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.
WDR5-47 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.
