myeloid-derived

SX-682 是口服有效的 CXCR1和 CXCR2变构抑制剂，可以阻断肿瘤髓系抑制细胞募集并增强 T 细胞活化和抗肿瘤免疫，具有治疗去势抵抗性前列腺癌的潜力。

TLR7 agonist 29 (Compound 1) 是一种TLR7激动剂，人TLR7的EC50为5.2 nM（小鼠TLR7的EC50为48.2 nM）。它可以激活骨髓来源的巨噬细胞 (BMDM)，刺激肿瘤微环境中的髓系细胞，并促进PD-L1、CD86和IFN-α的表达。TLR7 agonist 29 还可用作合成ADC的有效载荷。

HEMTACWEE1degrader-1 是一种靶向WEE1的HSP90介导嵌合降解剂 (HEMTAC)，其HSP90酶抑制活性呈现IC50: 16.76 nM。它能诱导WEE1的泛素化和降解，并有效阻断G2/M细胞周期。在急性髓系白血病 (AML) 患者来源的异种移植 (PDX) 模型中，HEMTACWEE1degrader-1 展现了抗癌活性。该化合物可应用于AML研究。

PAD4-IN-4 (compound 28) 是一种高效的PAD4抑制剂 (IC50=0.79±0.09 μM)。它通过改变中性粒细胞表型、提高树突状细胞和 M1 巨噬细胞的比例、减少髓源性抑制细胞的数量，改善肿瘤免疫微环境。此化合物可用于三阴性乳腺癌的研究。

Quizartinib, also know as AC220 and AC010220, is an orally available FLT3 / STK1 inhibitor with potential antineoplastic activity. Class III receptor tyrosine kinase inhibitor AC220 selectively inhibits class III receptor tyrosine kinases, including FMS-related tyrosine kinase 3 (FLT3/STK1), colony-stimulating factor 1 receptor (CSF1R/FMS), stem cell factor receptor (SCFR/KIT), and platelet derived growth factor receptors (PDGFRs), resulting in inhibition of ligand-independent leukemic cell proliferation and apoptosis. Mutations in FLT3, resulting in constitutive activation, are the most frequent genetic alterations in acute myeloid leukemia (AML) and occur in approximately one-third of AML cases.

EVT801是一种高选择性和低毒性VEGFR-3抑制剂，抑制VEGF-C诱导的肿瘤淋巴和血管生成，降低循环中重要的免疫抑制因子（CCL4、CCL5）和髓源性抑制细胞（MDSC）。

Flotetuzumab (MGD006; S80880) 是一种双特异性 CD123/CD3双亲和再靶向 (DART) 抗体。Flotetuzumab 通过同时结合靶细胞的 CD123和效应 T 细胞的CD3，而重新激活 T 细胞，导致 T 细胞介导的靶细胞的细胞毒性。Flotetuzumab 对小鼠中急性髓系白血病 (AML) 患者来源异种移植物 (PDX) 模型具有抑制效力。

LQVTDSGLYRCVIYHPP（LP17）是一种多肽和TREM-1(Triggering Receptor Expressed on Myeloid cells 1)抑制剂，序列来源于小鼠和人类TREM-1和TLT-1胞外结构域之间的高度保守序列，通过类似于诱饵受体的机制抑制肌动蛋白激活TREM-1，具有可穿透大脑屏障的优点，能够减轻神经元损伤和炎症反应。

Gemtuzumab ozogamicin为抗体药物偶联物，由针对CD33单克隆抗体与Calicheamicin细胞毒性衍生物构成，用于急性髓系白血病研究。

TAT-CIRP为小肽，指Tat融合的冷诱导RNA结合蛋白。作为骨髓分化蛋白2（MD2）的抑制剂，该化合物对小鼠缺血性及出血性中风显示出显著的神经保护效果。

PMAP-23为具有生物活性的抗菌肽(AMP)，源自猪骨髓。

BMAP 28是一种合成抗菌肽，对应牛防御素-5的132-158氨基酸。对大肠杆菌(E. coli)、金黄色葡萄球菌(S. aureus)、耐甲氧西林金黄色葡萄球菌(MRSA)、表皮葡萄球菌(S. epidermidis)及白色念珠菌(C. albicans)具有活性(MICs分别为2、2、4、1和8 µM)。在200 nM浓度下，BMAP 28能够使大肠杆菌的内膜渗透。在5 µM浓度下，减少Vero 76细胞中单纯疱疹病毒1型(HSV-1)的复制。在30 µM浓度下，对分离的人类红细胞引起溶血，并对分离的人类嗜中性粒细胞具有细胞毒性。BMAP 28 (0.8 mg/kg)可提高大肠杆菌或MRSA感染的小鼠的生存率，但对铜绿假单胞菌(P. aeruginosa)感染的小鼠无效。

Prostaglandin D2 (PGD2) is a primary enzymatic prostaglandin derived from PGH2 and is abundantly produced in the cerebrospinal fluid (CSF) by the lipocalin-type PGD synthase, and peripherally by myeloid cells such as mast cells and basophils via a hematopoietic-type PGD synthase. PGD2 is chemically unstable and presents challenges for use and analysis due to its brief in vivo half-life. Δ12-PGD2, an initial decomposition product of PGD2, acts as an intermediate in the pathway to Δ12-PGJ2, a cyclopentenone prostaglandin known for its antimitotic and carcinogenic properties. The metabolism of Δ12-PGD2 involves the addition of thiol nucleophiles, a common pathway for many cyclopentenone prostaglandins.

Prostaglandin D2 (PGD2) is one of the five principal prostaglandins enzymatically derived from PGH2. It is abundantly generated in the cerebrospinal fluid (CSF) by lipocalin-type PGD synthase and in peripheral regions by myeloid cells, such as mast cells and basophils, via leukocyte-type PGD synthase. The compound 1,25-trans-PGD2 is an isomer of PGD2, characterized by the alteration of the double bond between carbons 5 and 6 from cis(Z) to trans(E). This trans isomer, found as a 2-5% impurity in most commercial PGD2 bulk drug preparations, is primarily synthesized as an analytical standard to identify and quantify this impurity. Based on existing studies of trans isomers of F-type prostaglandins, 5-trans-PGD2 likely exhibits biological activity comparable to its cis isomer, although no specific published reports confirm this for 5-trans-PGD2.

OPBP-1 是通过噬菌体展示筛选、分子对接及分子动力学模拟获得的一种 D 肽。它具有高度稳定性、强效的抗肿瘤活性以及口服活性。OPBP-1 可选择性结合PD-L1蛋白，有效阻断PD-1/PD-L1的相互作用，从而恢复并增强 T 淋巴细胞功能，降低骨髓源抑制细胞 (MDSCs) 的比例，抵御肿瘤诱导的免疫逃逸。这使得 OPBP-1 可用于癌症免疫疗法的研究。