Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T3278 |
Piribedil
EU-4200,Trivastan,ET-495,Trivastal |
Dopamine Receptor; Histone Methyltransferase; Adrenergic Receptor | Chromatin/Epigenetic; GPCR/G Protein; Neuroscience |
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。 | |||
T39584 |
MI-3454
|
||
MI-3454 is a highly potent, orally active, and selective inhibitor of the interaction between menin and MLL1, with an IC50 of 0.51 nM. This compound effectively inhibits the proliferation of leukemic cells and promotes their differentiation, leading to the regression or complete remission of leukemia in mouse models featuring MLL1 rearrangements or NPM1 mutations. This remarkable therapeutic effect is achieved through the downregulation of key genes involved in the development of leukemia. | |||
T8768 |
MM-102 TFA
HMTase Inhibitor IX TFA |
Histone Methyltransferase | Chromatin/Epigenetic |
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。 | |||
T6333 |
MM-102
MM102,HMTase Inhibitor IX |
Histone Methyltransferase | Chromatin/Epigenetic |
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。 | |||
T67947 |
WDR5-0102
|
Histone Methyltransferase | Chromatin/Epigenetic |
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。 | |||
T67697 |
WDR5-47
|
Histone Methyltransferase | Chromatin/Epigenetic |
WDR5-47是一种干扰MLL1-WDR5相互作用的有效小分子,IC50值为0.3μM。 | |||
T68821 |
DC_M5_2
|
||
DC_M5_2 is a novel inhibitor of wdr5-mll1 interaction | |||
T75258 | MM-401 TFA | ||
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。 | |||
T13334 | WDR5-IN-1 | Others | Others |
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). | |||
T24489 |
MM-401
MM401 |
||
MM-401 is a specific inhibitor of histone H3K4 methyltransferase MLL1 activity that acts by reprogramming mouse epiblast stem cells to naive pluripotency. | |||
T39769 |
DDO-2093
|
||
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. | |||
T24463 |
MI-1481
MI 1481 |
||
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. | |||
T72239 |
DDO-2093 dihydrochloride
|
||
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。 | |||
T69624 |
TC-5115
|
||
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. | |||
T82598 |
DDO-2213
|
||
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。 | |||
T61027 |
Piribedil hydrochloride
|
||
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。 | |||
T69014 |
Sekikaic Acid
|
||
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). |