mll1

Piribedil (Trivastan) is a dopamine D2 agonist, used in the treatment of Parkinson's disease.

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.

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.

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.

MI-3454 is an orally active, selective and potent inhibitor of Menin-MLL1 interaction that inhibits the proliferation and induces differentiation of acute leukemia cells with MLL1 translocation or NPM1 mutation.MI-3454 induces complete remission or regression of leukemia in a mouse model of leukemia with MLL1 rearrangement or NPM1 mutation through the down-regulation of key genes involved in leukemogenesis. complete remission or remission.

W4022 (compound 16) is an efficient dual inhibitor of the lysine methyltransferases G9a/NSD2, with IC50 values of 0.241 μM for G9a and 0.017 μM for NSD2. It exhibits potent antiproliferative properties, including the ability to suppress colony formation, induce apoptosis, and inhibit metastasis of cancer cells. W4022 effectively curtails the catalytic activities of G9a and NSD2 within cells and demonstrates significant antitumor efficacy in PANC-1 xenograft models.

TC-5115 is a highly potent, selective inhibitor of the SET domain of the histone lysine methyltransferase MLL1 (KMT2A), with an IC₅₀ value of 16 nM. TC-5115 exhibits weak inhibitory activity against other methyltransferases such as SET7/9, DOT1L, and EZH2 (IC₅₀ > 1 μM). TC-5115 induces differentiation and growth arrest in leukemia cells and can be used in leukemia research.

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

AS-254s is an inhibitor of absent, small, or homeotic-like 1 protein (ASH1L), with an IC50 of 94 nM (FP assay). It exhibits antiproliferative activity against leukemia cells with MLL1 rearrangement, with a GI50 of less than 1 μM. Additionally, AS-254s can induce differentiation in MLL1-r leukemia cells.

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.

METTL3-IN-11 is a highly selective METTL3 inhibitor (IC50 = 45.31 nM), demonstrating greater selectivity for METTL3 over DNMT1, EZH1, MLL1, and PRMT1. It reduces m6A levels in total RNA of MOLM-13 and SKOV3 cells, inducing apoptosis and inhibiting migration. METTL3-IN-11 also decreases expression of m6A downstream target genes (c-MYC and BCL2). It is applicable in ovarian cancer and acute myeloid leukemia research.

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.

MI-1481 is an effective MML1 inhibitor (IC50: 3.6 nM). MI-1481 showed very potent inhibition of the menin-MLL1 interaction (IC50: 3.6 nM). MI-1481 also demonstrates pronounced activity in MLL leukemia cells and in vivo in MLL leukemia models.

MM-401 is a specific inhibitor of histone H3K4 methyltransferase MLL1 activity that acts by reprogramming mouse epiblast stem cells to naive pluripotency.

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.

Piribedil hydrochloride can be used in the parkinson's disease, circulatory disorders, cancers research. Piribedil hydrochloride inhibits MLL1 methyltransferase activity with EC50 value of 0.18 μM. Piribedil hydrochloride is a potent and orally active agonist of dopamine D2 and dopamine D3 as well as the antagonist of α2-adrenoceptors [1] [2] [3] [4].

DC_M5_2 is a novel inhibitor of wdr5-mll1 interaction

Sekikaic acid is a phenolic lichen metabolite that has been found in H. obscurata and has diverse biological activities. It scavenges superoxide and DPPH radicals in cell-free assays when used at a concentration of 0.5 µM. Sekikaic acid is active against the rg recombinant strain of respiratory syncytial virus (RSV; IC50 = 5.69 µg/ml). It inhibits the protein-protein interaction between mixed lineage leukemia 1 (MLL1) and the GACKIX domain of CREB-binding protein (CBP; IC50 = 34 µM).

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].