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17

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T83039	Anti-Mouse CD11b Antibody (M1/70)
	Anti-Mouse CD11b Antibody 为针对小鼠CD11b的IgG2b subtype 抗体，其宿主来源为Rat。
T8462	Enoximone 依诺昔酮,烯氟酮	PDE	Metabolism
	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。
T4584	BMS-813160 BMS 813160	CCR	Immunology/Inflammation; Microbiology/Virology
	BMS-813160 是CCR2/CCR5双重拮抗剂。有用于心血管的研究潜力。
T7776	ADH-503 GB1275	Complement System	Immunology/Inflammation
	ADH-503 (GB1275) 是一种可口服的变构CD11b 激动剂，可以导致与肿瘤相关的巨噬细胞重新极化，可减轻骨髓细胞的免疫抑制，并增强树突状细胞的反应。
T11179	Elubrixin SB-656933	IL Receptor; CXCR	Autophagy; GPCR/G Protein; Immunology/Inflammation
	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。
T1076	Dexamethasone MK 125,Prednisolone F,NSC 34521,Hexadecadrol,地塞米松	Glucocorticoid Receptor; Mitophagy; IL Receptor; SARS-CoV; Antibacterial; Antibiotic; Autophagy; Complement System	Autophagy; Endocrinology/Hormones; Immunology/Inflammation; Microbiology/Virology
	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。
T13379	(Z)-Leukadherin-1 ADH-503 free base	Complement System	Immunology/Inflammation
	(Z)-Leukadherin-1 (ADH-503 free base) 是 CD11b 的变构激动剂。
T3638	Leukadherin-1	Integrin; Complement System	Cytoskeletal Signaling; Immunology/Inflammation
	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。
T13276	VAF347 4-(3-氯苯基)-N-[4-(三氟甲基)苯基]嘧啶-2-胺	Aryl Hydrocarbon Receptor	Immunology/Inflammation
	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。
T15613	JHU-083	Others	Others
	JHU-083 is a selective glutaminase antagonist. JHU-083 blocks glutaminase activity in brain CD11b+ cells. JHU-083 also experimental cerebral malaria (ECM) resulting in a net decrease of glutamate levels in the animals.
T37264	15(R)-15-methyl Prostaglandin D2 15(R)15methyl PGD2	GPR	Endocrinology/Hormones; GPCR/G Protein
	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。
T36443	(R,R)-CXCR2-IN-2 (R,R)-CXCR2-IN-2
	(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.
T41121	Elubrixin tosylate SB-656933 tosylate,Elubrixin tosylate
	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.
T36923	CXCR2-IN-2 CXCR2-IN-2
	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 ra...
T36963	CAY10503
	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 follo...
T28269	ORY-1001 free base RG 6016,ORY-1001,ORY 1001,ORY1001,RG-6016,RG6016
	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
T36593	TEI-9648
	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 cons...

化合物

Anti-Mouse CD11b Antibody (M1/70)

Cat.No: T83039

Cat.No: T8462

Synonym: 依诺昔酮,烯氟酮

Target: PDE

Cat.No: T4584

Synonym: BMS 813160

Target: CCR

Cat.No: T7776

Synonym: GB1275

Target: Complement System

Cat.No: T11179

Synonym: SB-656933

Target: IL Receptor, CXCR

Cat.No: T1076

Synonym: MK 125,Prednisolone F,NSC 34521,Hexadecadrol,地塞米松

Target: Glucocorticoid Receptor, Mitophagy, IL Receptor, SARS-CoV, Antibacterial, Antibiotic, Autophagy, Complement System

(Z)-Leukadherin-1

Cat.No: T13379

Synonym: ADH-503 free base

Target: Complement System

Cat.No: T3638

Target: Integrin, Complement System

Cat.No: T13276

Synonym: 4-(3-氯苯基)-N-[4-(三氟甲基)苯基]嘧啶-2-胺

Target: Aryl Hydrocarbon Receptor

Cat.No: T15613

Target: Others

15(R)-15-methyl Prostaglandin D2

Cat.No: T37264

Synonym: 15(R)15methyl PGD2

Target: GPR

(R,R)-CXCR2-IN-2

Cat.No: T36443

Synonym: (R,R)-CXCR2-IN-2

Elubrixin tosylate

Cat.No: T41121

Synonym: SB-656933 tosylate,Elubrixin tosylate

Cat.No: T36923

Synonym: CXCR2-IN-2

Cat.No: T36963

ORY-1001 free base

Cat.No: T28269

Synonym: RG 6016,ORY-1001,ORY 1001,ORY1001,RG-6016,RG6016

Cat.No: T36593

Cat. No.	Product Name	Target	Signaling Pathways
T73402	Flavipin
	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。
TN5912	Macluraxanthone 3-Hydroxyblancoxanthone	Antioxidant; TNF	Apoptosis; oxidation-reduction
	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。

天然产物

Cat.No: T73402

Macluraxanthone

Cat.No: TN5912

Synonym: 3-Hydroxyblancoxanthone

Target: Antioxidant, TNF

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