mll1

Piribedil (Trivastan) 是多巴胺 D2受体激动剂，对 hα1A-肾上腺素受体也显示出拮抗作用。

MM-102 (HMTase Inhibitor IX) 是一种有效的 WDR5 MLL 相互作用抑制剂，在 WDR5 结合检测中，IC50为 2.4 nM，Ki 小于 1 nM，MM-102 还能特异性抑制细胞生长并诱导携带 MLL1 融合蛋白的白血病细胞凋亡。

MM-102 TFA (HMTase Inhibitor IX TFA) 是一种有效的 WDR5 MLL 相互作用抑制剂，在 WDR5 结合检测中，IC50为 2.4 nM，Ki 小于 1 nM。

WDR5-47是一种干扰MLL1-WDR5相互作用的有效小分子，IC50值为0.3μM。

WDR5-0102为针对WDR5-MLL1的抑制剂(Kdis=7 μM, Kd=4 μM)。该化合物有效抑制MLL1活性，而对人类H3K4甲基转移酶SETD7及其他六种HMT（G9a、EHMT1、SUV39H2、SETD8、PRMT3、PRMT5）不表现出抑制作用。

MI-3454 是一种具有口服活性，选择性和高效性的 Menin-MLL1 相互作用抑制剂，可抑制具有 MLL1 易位或 NPM1 突变的急性白血病细胞增殖并诱导分化。MI-3454 通过下调参与白血病发生的关键基因，诱导MLL1重排或NPM1突变白血病小鼠模型中白血病的完全缓解或消退。

WDR5-IN-1 is a potent and selective inhibitor of WD repeat domain 5 (WDR5) (Kd <0.02 nM), and also inhibits MLL1 histone methyltransferase (HMT) activity (IC50: 2.2 nM).

AS-254s 是 absent, small, or homeotic-like 1 protein (ASH1L) 的抑制剂，IC50 为 94 nM (FP 测定)。对于 MLL1 重排的白血病细胞，AS-254s 显示出抗增殖活性，GI50 < 1 μM，并能诱导 MLL1-r 白血病细胞的分化。

DD0-2363 (Compound 32d) 是一种同时靶向WDR5-MLL1和HDAC的抑制剂。能够抑制急性髓系白血病细胞的增殖，并诱导细胞凋亡 (apoptosis)。DD0-2363 展现出抗肿瘤活性，可应用于急性髓细胞白血病的研究。

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 可用于帕金森病，循环系统疾病，癌症等的研究。Piribedil hydrochloride 以0.18 μM 的EC50值抑制 MLL1 甲基转移酶的活性。Piribedil hydrochloride 是口服有效的多巴胺 D2 和 多巴胺 D3 激动剂，也是 α2-肾上腺素能受体的拮抗剂。

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).

TC-5115 is a potent inhibitor of MLL methyltransferase with IC50 value of 16 nM. TC-5115 may lead to the development of a new therapy for the treatment of human MLL leukemia. The mixed-lineage leukemia (MLL) protein, also known as MLL1, is a lysine methyltransferase specifically responsible for methylation of histone 3 lysine 4. MLL has been pursued as an attractive therapeutic target for the treatment of acute leukemia carrying the MLL fusion gene or MLL leukemia.

DDO-2093 dihydrochloride 是一种有效的MLL1和WDR5蛋白-蛋白相互作用抑制剂 (IC50=8.6 nM ; Kd=11.6 nM)，具有抗肿瘤活性。DDO-2093 dihydrochloride 选择性抑制 MLL 复合物的催化活性。

MM-401 (TFA) 是一种针对MLL1 H3K4甲基转移酶的抑制剂，通过阻断MLL1与WDR5的相互作用，有效抑制MLL1活性，其IC50值为0.32 µM。此化合物能够诱导细胞周期停滞、凋亡及分化，主要用于MLL白血病的研究。

DDO-2213是一口服有效的WDR5-MLL1抑制剂，具有29 nM的IC50和72.9 nM的Kd值针对WDR5蛋白。该化合物对MLL组蛋白甲基转移酶活性及MLL易位细胞增殖具有选择性抑制作用，可用于研究MLL融合型白血病。

W4022 (compound 16) 作为一种有效的赖氨酸甲基转移酶G9a NSD2双重抑制剂，其对G9a和NSD2的IC50值分别是0.241 μM和0.017 μM。此化合物不仅具有显著的抗增殖特性，还能抑制菌落形成、诱导细胞凋亡以及阻止癌细胞转移。在PANC-1异种移植模型中，W4022有效地抑制了G9a和NSD2的催化活性，展现出其抗肿瘤的潜力。