CD11b

Dexamethasone (Hexadecadrol) 是一种糖皮质激素受体激动剂和一种 IL 受体调节剂。Dexamethasone 具有抗炎和免疫抑制活性，可诱导自噬。Dexamethasone 抑制 LPS 诱导的巨噬细胞炎症反应。

BMS-813160 是CCR2 CCR5双重拮抗剂。有用于心血管的研究潜力。

Elubrixin (SB-656933) 是一种有效和特异性的 CXCR2 和 IL-8 受体拮抗剂。 Elubrixin 可用于炎症性疾病的研究，例如炎症性肠病和气道炎症。

ADH-503 (GB1275) 是一种可口服的变构CD11b的小分子激动剂，可以导致肿瘤相关巨噬细胞的复极化、肿瘤浸润免疫抑制性髓系细胞数量的减少以及增强树突状细胞反应。

(Z)-Leukadherin-1 (ADH-503 free base) 是 CD11b 的变构激动剂。

Enoximone 是一种选择性的，具有口服活性的磷酸二酯酶 III 抑制剂，也是正性肌力血管舒张剂。它通过抑制 cGMP 抑制的 PDE 来诱导血管舒张并增加细胞内 cAMP 水平。它还表现出 PDE4抑制作用，对心肌 PDE4A 的 IC50为 21.1 μM。它用于充血性心力衰竭的研究，并具有支气管扩张，抗哮喘和抗炎作用。

Anti-Mouse CD11b Antibody 为针对小鼠CD11b的IgG2b subtype 抗体，其宿主来源为Rat。

Leukadherin-1 是 CD11b CD18 的变构激活剂，可增加 CD11b CD18 依赖性细胞对纤维蛋白原的粘附，减少白细胞运动和跨内皮迁移，具有抗炎作用。

Pulrodemstat (CC-90011) 是一种具有口服活性、选择性和高效性的赖氨酸特异性脱甲基酶-1 (LSD1) 抑制剂，具有抗癌抗肿瘤活性，抑制 HNSCC 细胞增殖和迁移，通过触发细胞凋亡来抑制头颈部鳞状细胞癌的生长。

Adriforant (PF-3893787,ZPL-3893797,阿屈仑特)是一种竞争性的H4(histamine receptor 4)拮抗剂，拮抗组胺诱导的ERK磷酸化，使肥大细胞中组胺诱导的转录变化正常化，并降低神经元中组胺依赖性Ca 2+ 通量，可减轻小鼠瘙痒和皮肤

Pulrodemstat HCl 是一种具有口服活性、选择性和高效性的赖氨酸脱甲基酶-1 （LSD1） 抑制剂，也是选择性 KDM1A 抑制剂，具有抗癌抗、增殖活性，抑制 HNSCC 细胞增殖和迁移通过触发细胞凋亡来抑制头颈部鳞状细胞癌的生长。

VAF347 是细胞可渗透且高度亲和力的芳烃受体激动剂，可诱导AhR 信号传导，具有抗炎作用。它抑制颗粒单核细胞 (GM 期) 前体中 CD14+CD11b+单核细胞的发育。

10-Methoxy-canthin-6-one (Mtx-C) 作为一种有效的DNA损伤诱导剂，主要通过嵌入DNA促使细胞周期在G2 M期停滞。这一机制有助于诱导急性髓性白血病细胞 (AML) 以及白血病干细胞 (LSC) 的髓系分化。在AML和LSC细胞中，髓系分化主要通过髓过氧化物酶、CD15、CD11b及CD14的表达增强以及p38 MAPK的激活来体现。因此，10-Methoxy-canthin-6-one 在白血病研究领域具有重要应用价值。

ORY-1001 is a KDM1A inhibitor (IC50 <20nM) with high selectivity against related FAD dependent aminoxidases (MAO-A B, IL4I1, KDM1B >100uM, SMOX 7uM). Treatment of THP-1 (MLL-AF9) cells with ORY-1001, results in a time dose dependent me2H3K4 accumulation a

(R,R)-CXCR2-IN-2, diastereoisomer of CXCR2-IN-2 (compound 68), is a brain penetrant CXCR2 antagonist with a pIC50 of 9 and 6.8 in the Tango assay and d in the HWB Gro-α induced CD11b expression assay, respectively[1]. [1]. Lu H, et al. Discovery of Novel 1-Cyclopentenyl-3-phenylureas as Selective, Brain Penetrant, and Orally Bioavailable CXCR2 Antagonists. J Med Chem. 2018;61(6):2518-2532.

TEI-9648, a Vitamin D3 Lactone analogue, is a potent and specific vitamin D receptor (VDR) antagonist. TEI-9648 inhibits VDR/VDRE-mediated genomic actions of 1α,25(OH)2D3. TEI-9648 also inhibits HL-60 cell differentiation induced by of 1α,25(OH)2D3. TEI-9648 has the potential for bone metabolism research[1][2]. TEI-9648 (10-1000 nM) dose-dependently blocks the reciprocal changes of CD11b and CD71 expression associated with HL-60 cell differentiation induced by 1α,25(OH)2D3[1]. TEI-9648 has consistently weaker suppressive effect than TEI-9647[1]. TEI-9648 can not induce cell differentiation even after treatment at 1 μM in HL-60 cell[1]. TEI-9648 alone can not induce activation of NBT-reducing activity or α-NB esterase activity. In contrast, TEI-9648 markedly suppresses the up-regulation induced by 1α,25(OH)2D3 (0.1 nM) in HL-60 cells[1]. [1]. Miura D, et al. Antagonistic action of novel 1α,25-dihydroxyvitamin D3-26, 23-lactone analogs on differentiation of human leukemia cells (HL-60) induced by 1α,25-dihydroxyvitamin D3. J Biol Chem. 1999 Jun 4;274(23):16392-9. [2]. Kazuya Takenouchi, et al. Synthesis and structure-activity relationships of TEI-9647 derivatives as Vitamin D3 antagonists. J Steroid Biochem Mol Biol. 2004 May;89-90(1-5):31-4.

CXCR2-IN-2 is a selective, brain penetrant, and orally bioavailable CXCR2 antagonist (IC50=5.2 nM 1 nM in β-arrestin assay CXCR2 Tango assay, respectively). CXCR2-IN-2 displays ~730-fold selectivity over CXCR1 and >1900-fold selectivity over all other chemokine receptors. CXCR2-IN-2 inhibits human whole blood Gro-α induced CD11b expression with an IC50 of 0.04 μM[1]. CXCR2-IN-2 (compound 68) (1-10 mg kg; p.o.; twice daily for 3 days) dose-dependently reduces neutrophil infiltration in vivo in rat and mouse air pouch models[1]. [1]. Lu H, et al. Discovery of Novel 1-Cyclopentenyl-3-phenylureas as Selective, Brain Penetrant, and Orally Bioavailable CXCR2 Antagonists. J Med Chem. 2018;61(6):2518-2532.

CAY10503 is a proapoptotic, antiproliferative compound that is able to arrest cell cycle progression in the G0-G1 phase. CAY10503 inhibits the growth of HL60, multidrug resistant HL60R, and K562 cells with IC50 values of 7.0, 23, and 20 μM, respectively. Accumulation of HL60 cells in G0-G1 occurred within eight hours following treatment with 50 μM CAY10503, whereas 10 μM CAY10503 required 96 hours for cell cycle arrest to appear. CAY10503 also induces differentiation of HL60 cells into the following positive cells: CD14 (monocytic marker) as well as CD11b and CD11c (granulocytic markers). Approximately 60% of HL60 cells exposed to 10 μM CAY10503 expressed these markers within 72 hours.

15(R)-15-methyl Prostaglandin D2 (15(R)15methyl PGD2) 是一种 PGD2 合成类似物，也是一种具有选择性和强效性的 CRTH2 DP2 受体激动剂，可调节嗜酸性粒细胞 CD11b 表达、肌动蛋白聚合和趋化。

Elubrixin tosylate (SB-656933 tosylate) is a high-potency, selective, competitive, and reversible CXCR2 antagonist, as well as an antagonist of the IL-8 receptor. It effectively inhibits upregulation of neutrophil CD11b (with an IC50 of 260.7 nM) and shape change (with an IC50 of 310.5 nM). This compound holds promise for the study of inflammatory diseases, including inflammatory bowel disease and airway inflammation.

Flavipin 是一种芳香烃受体(Ahr)激动剂，可诱导小鼠 CD4+T 细胞和 CD11b+巨噬细胞表达 Ahr 下游基因。Flavipin 抑制 Arid5a 在 Il23a3'UTR 上的稳定功能，这是一种新发现的靶 mRNA。Flavipin 具有清除 DPPH 自由基的能力，IC50值为7.2 μM，对α-葡萄糖苷酶具有较强的抑制作用，IC50值为 33.8 μM。

BAY-155 is a powerful and selective menin-MLL inhibitor, exhibiting an IC 50 of 8 nM. It significantly down-regulates MEIS1 gene expression while up-regulating CD11b and MNDA genes. BAY-155 also demonstrates anti-proliferative effects in AML ALL (acute myeloid lymphoblastic leukemia) models [1].

Macluraxanthone (3-Hydroxyblancoxanthone) 具有许多生物活性，包括抗胆碱酯酶、抗氧化、抗癌、抗疟疾、抗炎和免疫调节作用。Macluraxanthone 通过增加表达CD86的巨噬细胞的百分比，同时减少其CD14、CD11b 和CD80的表达，来促进M1类促炎症巨噬细胞的极化。Macluraxanthone 在促炎症刺激物脂多糖的存在下明显减少了TNF-α和IL-10细胞因子的产生。