mll1-wdr5

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.

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

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.

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

Z116334910 is a competitive WDR5-MLL1 interaction disruptor, where WDR5 (WD Repeat-containing protein 5) is crucial for the methyltransferase activity of the MLL1 (mixed lineage leukemia 1) complex, and can be used for cancer research.

HBI-2375 (HYBI-084) is a selective inhibitor that penetrates the blood-brain barrier and is orally active, targeting the MLL1-WDR5 interaction. It inhibits WDR5 with an IC50 of 4.48 nM and demonstrates antiproliferative activity in MV4;11 leukemia cells with an IC50 of 3.17 µM. Furthermore, HBI-2375 disrupts histone methyltransferase activity in cancer cells and is useful for researching leukemia, glioma, and glioblastoma.

Z88418521 is a ligand for the WDR5-MLL1 complex. It may aid in disrupting the interaction of the WDR5-MLL1 complex. Z88418521 is applicable in cancer research, particularly for leukemia.

DDO-2093, a powerful inhibitor of the MLL1-WDR5 protein-protein interaction (IC50 = 8.6 nM; Kd = 11.6 nM), exhibits prominent antitumor effects. Notably, DDO-2093 selectively hampers the catalytic activity of the MLL complex.

MM-102 (HMTase Inhibitor IX) is a potent inhibitor of WDR5/MLL interaction with IC50 of 2.4 nM and Ki of less than 1 nM in a WDR5 binding assay. MM-102 can also specifically inhibit cell growth and induce apoptosis in leukemia cells carrying MLL1 fusion protein.

DC_M5_2 is a novel inhibitor of wdr5-mll1 interaction

DDO-2093 dihydrochloride, a potent inhibitor of MLL1-WDR5 protein-protein interactions (IC50=8.6 nM; Kd=11.6 nM), exhibits antitumor activity. It selectively inhibits the catalytic activity of the MLL complex.

MM-401 (TFA), an MLL1 H3K4 methyltransferase inhibitor, effectively impedes MLL1 activity (IC 50 = 0.32 µM) by preventing MLL1-WDR5 interaction. It can induce cell cycle arrest, apoptosis, and differentiation, offering potential for MLL leukemia research [1].

MM-102 TFA (HMTase Inhibitor IX TFA) is a potent WDR5/MLL interaction inhibitor with an IC50 of 2.4 nM. This compound prevents the interaction between mixed lineage leukemia 1 (MLL1) and WD Trp-Asp repeat domain 5 (WDR5), inhibiting MLL1 H3K4 histone methyltransferase (HMT) activity and down-regulating H3K4me3, which facilitates the epigenetic reprogramming of porcine somatic cell nuclear transfer embryos.