lineage

Y-27632 dihydrochloride (Y-27632 2HCl) 是一种 ROCK-I 和 ROCK-II 抑制剂，具有口服有效性、ATP 竞争性。Y-27632 dihydrochloride 还抑制分离诱导的小鼠前列腺干或祖细胞凋亡。

GW806742X 是ATP 模拟物，是MLKL 抑制剂，可结合 MLKL 假激酶结构域，Kd 值为 9.3μM。它对VEGFR2的IC50为 2 nM，延缓 MLKL 膜移位并抑制坏死。

URMC-099 是一种具有优异的血脑屏障穿透性的，可口服的混合谱系激酶 3 抑制剂，IC50为14 nM。

Necrosulfonamide ((E)-Necrosulfonamide) 是一种坏死性凋亡抑制剂，靶向 MLKL，具有选择性。Necrosulfonamide 阻止 MLKL-RIP1-RIP3 坏死小体复合体与其下游效应子相互作用。

L-Pyrrolysine 是一种存于古细菌谱系的特殊氨基酸，可响应少数古细菌和细菌中的琥珀色 （TAG） 密码子。

Cbl-b-IN-3是一种有效的casitas b 系淋巴瘤原癌基因-b (Cbl-b)抑制剂（ic50 < 1 nM）。

Eltrombopag Olamine (Eltrombopag diethanolamine salt) 是 Eltrombopag 的口服活性乙醇胺盐，是一种血小板生成素(TPO)受体激动剂，用于血小板减少的某些病症研究。

SGC0946是一种组蛋白甲基转移酶DOT1L 高选择性抑制剂，IC50值为0.3nM，可选择性地杀死混合谱系白血病细胞。

M-89 可抑制 Menin-MLL 蛋白之间的相互作用，有研究混合谱系白血病的潜力。它是一种强特异性 menin 抑制剂，结合到 menin 的Kd 值为 1.4 nM。

Menin-MLL inhibitor 4 has antitumor activity.Menin-MLL inhibitor 4 is an inhibitor of Menin- MLL (mixed-lineage leukemia protein) interaction .

MM-589 is a potent WD repeat domain 5 (WDR5) inhibitor and mixed lineage leukemia (MLL) protein-protein interaction.

MM-589 TFA is a potent WD repeat domain 5 (WDR5)inhibitor and mixed lineage leukemia (MLL) protein-protein interaction.

TC13172 is an inhibitor of mixed lineage kinase domain-like protein (EC50: 2 nM for HT-29 cells).

Enzomenib (DSP5336) 是一种针对多发性内分泌腺瘤 (MEN) 基因所编码的menin蛋白的抑制剂。它能阻断menin蛋白与混合谱系白血病 (MLL) 融合蛋白之间的相互作用，应用于血液系统恶性肿瘤的研究领域。

PROTAC MLKL Degrader-2 是针对MLKL（Mixed Lineage Kinase）的靶向PROTAC。该化合物由PROTAC MLKLDegrader-2靶蛋白配体、Thalidomide做为E3连接酶配体以及N-Methylpiperazine做为PROTAC Linker组合而成，其E3 泛素连接酶配体与Linker的偶联产物是Thalidomide-N-methylpiperazine。PROTAC MLKL Degrader-2 在人类细胞系中具有抗坏死性凋亡活性，且能有效地在小鼠HT-29异种移植模型中降解MLKL。

MLK3-IN-1 (Compound 37) 是一种专门针对混合谱系激酶 3 (MLK3) 的抑制剂，其 IC50 值小于 1 nM。该化合物对 FAK 的抑制作用的 IC50 为 15.5 μM。此外，MLK3-IN-1 在小鼠与人类的肝微粒体中显示出优良的代谢稳定性。

MIV-6 is an inhibitor of the menin-mixed lineage leukemia interaction.

BOP is anantagonist of alpha4beta1/alpha9beta1 integrins. BOP rapidly mobilizes long-term multi-lineage reconstituting hematopoietic stem cells (HSC).

RX-37 is a potent BET inhibitor with Ki values of 3.2-24.7 nM for BRD2, BRD3 and BRD4. RX-37 demonstrates high selectivity over other non-BET bromodomain-containing proteins. RX-37 potently and selectively inhibits cell growth in human acute leukemia cell

Selenodicysteine is the 21st proteinogenic amino acid. Selenocysteine exists naturally in all three domains of life, but not in every lineage.

GW841819X is an analogue of (+)-JQ1 and a novel inhibitor of BET bromodomains. GW841819X was a single enantiomer but of undefined chirality at the 4-position of the benzodiazepine ring3. GW841819X and JQ1 were recently discovered that bind to the acetyl-lysine binding pocket of BET bromodomains with Kd ranges from 50 to 370 nM [1]. GW841819X bounded to both the individual BD1 and BD2 domains with affinities of 46 and 52.5 nM, respectively. GW841819X-Brd3 interaction was estimated to be around 70 nM4. GW841819X displayed activity in vivo against NUT-midline carcinoma, multiple myeloma, mixed-lineage leukemia, and acute myeloid leukemia1. It also potent induced the ApoA1 reporter gene with an EC50 of 440 nM. It had very little effect on LDL-R luciferase activity at the concentrations at which it induces ApoA1 expression, suggesting that the effect is indeed specific3. GW841819X competed directly with GATA1 site for BD1 binding and also specifically blocked the interaction between Brd3 and acetylated GATA14. Recent findings reported that GW841819X are chose as an interest compound to further develop into potential drugs against diseases including cancer, HIV infection and heart disease2.

Ara-G 是一种脱氧鸟苷 (GdR) 类似物和核苷类似物，可被 T 淋巴谱系细胞迅速转化为其相应的阿拉伯糖基鸟嘌呤核苷酸三磷酸 (araGTP)，从而抑制 DNA 合成和对 T 淋巴母细胞的选择性体外毒性细胞系以及来自 T 细胞急性淋巴细胞白血病 (ALL) 患者的新鲜分离的白血病细胞。

MLK-IN-1 (US20140256733A1, compound 68) is a highly potent and selective inhibitor of mixed lineage kinase 3 (MLK-3). It exhibits excellent brain penetration and specifically targets MLK-3.

Cbl-b-IN-2 是一种口服具有活力的生物化合物，能够抑制泛素蛋白酶体通路中的 E3 酶Casitas b 系淋巴瘤原癌基因-b (Cbl-b)，可以用于调节免疫系统和易受免疫系统调节疾病的研究。Cbl-b-IN-2 也能够单独或与一种或多种免疫检查点抑制剂，抗肿瘤剂和放射剂联合应用于癌症的研究。