human myeloid cell

G150 是高选择性h-cGAS 抑制剂，IC50值为 10.2 nM，用于抑制 dsDNA 引发的干扰素表达。

Neriifolin (17β-Neriifolin) 是一种从 Cerbera manghas 未熟果实中提取的强心苷，是一种 Na+K+-ATPase 抑制剂，具有抗癌活性，通过抑制 HOXA9 依赖性基因表达和诱导人急性髓细胞系 THP-1 细胞凋亡抑制细胞增殖。Neriifolin 诱导人肝癌 HepG2 细胞周期阻滞和凋亡，可用于研究前列腺癌。

FLT3-ITD-IN-2 (Compound A1) 是一种FLT3-ITD激酶的抑制剂，其IC50为2.12 nM。FLT3-ITD-IN-2 可有效抑制FLT3依赖的人AML细胞系MOLM-13的增殖，IC50为25.65 nM，并对急性髓系白血病展现抗肿瘤作用。

Rotundifuran 是从 Vitex rotundifolia 的果实中提取的。 Rotundifuran 抑制细胞周期进程并诱导人髓性白血病细胞凋亡。

Tpl2 kinase inhibitor is an inhibitor of tumor progression locus 2 (Tpl2; IC50= 0.05 μM).1It is selective for Tpl2 over MEK, p38 MAPK, Src, MK2, and PKC (IC50s = >40, 180, >400, 110, and >400 μM, respectively). Tpl2 kinase inhibitor inhibits LPS-induced TNF-α production in isolated human monocytes and whole blood (IC50s = 0.7 and 8.5 μM, respectively). It enhances differentiation induced by calcitriol in HL-60 and U937 leukemia cells when used at a concentration of 5 μM.2Tpl2 kinase inhibitor (5 μM) inhibits the proliferation of KG-1a leukemia cells.3 1.Garvin, L.K., Green, N., Hu, Y., et al.Inhibition of Tpl2 kinase and TNF-α production with 1,7-naphthyridine-3-carbonitriles: Synthesis and structure-activity relationshipsBioor. Med. Chem. Lett.15(23)5288-5292(2005) 2.Wang, X., and Studzinski, G.P.Expression of MAP3 kinase COT1 is up-regulated by 1,25-dihydroxyvitamin D3 in parallel with activated c-jun during differentiation of human myeloid leukemia cellsJ. Steroid. Biochem. Mol. Biol.121(1-2)395-398(2010) 3.Wang, X., Gocek, E., Novik, V., et al.Inhibition of Cot1/Tlp2 oncogene in AML cells reduces ERK5 activation and up-regulates p27Kip1 concomitant with enhancement of differentiation and cell cycle arrest induced by silibinin and 1,25-dihydroxyvitamin D3Cell Cycle9(22)4542-4551(2010)

Nargenicin is a macrolide antibiotic that selectively inhibits the growth of S. aureus, methicilin resistant S. aureus (MRSA), and M. luteus (MICs = 0.6, 0.3, and 2.5 μg ml, respectively) over a panel of 11 Gram-positive and Gram-negative bacteria (MICs = >80 μg ml). [1] It dose-dependently inhibits S. aureus DnaE in the presence of DNase I-activated DNA and E. coli DnaE when used at concentrations of 0.00001-0.1 and 0.01-100 μg mL, respectively. [2] In murine BV-2 microglial cells, nargenicin (1 μM) inhibits cytokine expression and nitric oxide production induced by LPS.[3] Nargenicin (200 μM), when used in combination with 1,25-dihydroxyvitamin D3 or all-trans retinoic acid , reduces cell proliferation by 37-47% and increases cell differentiation by 82-85% in HL-60 human myeloid leukemia cells.[4]

Sorafenib N-oxide is an active metabolite of sorafenib , an inhibitor of Raf-1, B-RAF, and receptor tyrosine kinases. Sorafenib N-oxide inhibits FLT3 that contains the internal tandem duplication mutation (FLT3-ITD; Kd = 70 nM) and inhibits proliferation of MV4-11 acute myeloid leukemia (AML) cells expressing FLT3-ITD (IC50 = 25.8 nM). It is selective for AML cell lines containing FLT3-ITD over lines containing wild-type FLT3 (IC50s = 3.9-13.3 μM). Sorafenib N-oxide is also a linear-mixed inhibitor of the cytochrome P450 (CYP) isoform CYP3A4 (Ki = 15 μM in human liver microsomes).

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。

Solasodine (Purapuridine) 是存在于茄科植物中的一种类固醇生物碱。它具有神经保护、降压、抗真菌、抗癌、抗动脉粥样硬化、抗雄激素和抗炎活性。

Kirenol (Kirel) 是分离自 Siegesbeckia orientalis 中的，具有抗氧化、抗炎、抗过敏、抗关节炎活性，可用于缓解疼痛的研究。

PC-046 is a potent tubulin-binding agent, which was originally identified for development based on selective activity in deleted in pancreas cancer locus 4 (DPC4 SMAD4) deficient tumors. PC-046 has growth inhibitory activity in a variety of tumor types in vitro, and efficacy in SCID mice was shown in human tumor xenografts of MV-4-11 acute myeloid leukemia, MM.1S multiple myeloma, and DU-145 prostate cancer. Pharmacokinetic studies demonstrated relatively high oral bioavailability (71 %) with distribution to both plasma and bone marrow. No myelosuppression was seen in non-tumor bearing SCID mice given a single dose just under the acute lethal dose. The COMPARE algorithm in the NCI-60 cell line panel demonstrated that PC-046 closely correlated to other known tubulin destabilizing agents (correlation coefficients ≈0.7 for vincristine and vinblastine). Mechanism of action studies showed cell cycle arrest in metaphase and inhibition of tubulin polymerization. Overall, these studi......

Ulocuplumab (BMS-936564) 是一种完全人 抗 CXCR4 的 IgG4  抗体。Ulocplumab 在急性髓系白血病 (AML)，非霍奇金淋巴瘤 (NHL) 和多发性骨髓瘤移植模型中展现出抗肿瘤活性。Ulocplumab 对 CXCL12 介导的慢性淋巴细胞白血病 (CLL) 细胞在 CXCR4 激活下的迁移有抑制作用，诱导癌细胞凋亡 (apoptosis)，。

CML-IN-1（compound 7）是一种高效抗癌药物，针对人类慢性粒细胞白血病（CML）细胞系K562，能有效诱导凋亡（apoptosis）。该化合物主要通过显著抑制PI3K Akt信号通路的蛋白磷酸化来发挥作用，同时CML-IN-1（compound 4）也能通过抑制结直肠癌的MEK ERK信号通路来阻止细胞增殖。

ZG36是一种人类Caseinolytic protease P(ClpP)激动剂，具有非选择性地降解呼吸链复合物和减少线粒体DNA的能力，从而导致线粒体功能衰竭及白血病细胞死亡。此外，ZG36能够抑制异种移植小鼠模型中急性髓细胞性白血病的发展。

EP4 antagonist 14是一种前列腺素E2（PGE2）受体亚型EP4的拮抗剂，其在使用表达人源受体的HEK293细胞的报告基因测定中的IC50值为1.1 nM。它还能抑制PGE2诱导的同种细胞中的β-阿雷斯汀招募（IC50 = 0.9 nM）。EP4 antagonist 14（10 µM）能减少RAW 264.7巨噬细胞中PGE2诱导的mRNA表达，这些mRNA编码Il-4、巨噬细胞甘露糖受体1（Mrc1）、几丁质酶样蛋白3（Chil3）、趋化因子（C-X-C）基序配体1（Cxcl1）、表达在髓样细胞上的触发受体2（Trem2）和精氨酸酶-1（Arg1）。在体内，EP4 antagonist 14（每天30 mg/kg），结合抗PD-1抗体，能够在CT26小鼠结肠癌模型中抑制肿瘤生长并增加CD8+ T细胞对肿瘤的浸润。

HA-14-1, a small molecule, binds the surface pocket of Bcl-2 proteins (IC50= ~ 9 µM), including Bcl-xl and Bcl-W, and disrupts their interaction with the Bak peptide. This action induces apoptosis by activating Apaf-1 and caspase-9 and -3. Additionally, HA-14-1 effectively induces apoptosis in human acute myeloid leukemia (HL-60) cells, with a 50 µM concentration resulting in a 90% loss of cell viability.

Pim-1 2 kinase inhibitor 2 (compound 5b) 作为一种PIM-1和PIM-2激酶的竞争性抑制剂，其IC50值分别为1.31 μM和0.67 μM。该化合物在正常的人类肺成纤维细胞系Wi-38中表现出较低的细胞毒性，并且在体外对多种癌细胞系如骨髓性白血病(NFS-60)、肝癌(HepG-2)、前列腺癌(PC-3)和结肠癌(Caco-2)显示出有效的抗癌活性。

UR778Br 是一种针对IQGAP1蛋白的GTPase活化蛋白相关结构域(GRD 结构域)的靶向化合物。该化合物能够抑制人类急性髓系白血病(AML)细胞的增殖，通过引发G2 M期的细胞周期阻滞以及诱导细胞凋亡(apoptosis)。此外，UR778Br能够抑制原代细胞和AML细胞的集落形成，而对正常骨髓细胞不产生显著影响。