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26

抑制剂 & 化合物

8

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T11344	G150	DNA; cGAS	DNA Damage/DNA Repair; Immunology/Inflammation
	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。
T27730	KGP94 KGP-94,KGP 94	Cysteine Protease	Proteases/Proteasome
	KGP94 是一种有效的、选择性的和竞争性的溶酶体内肽酶抑制剂。
T36573	NHWD-870	Apoptosis; Epigenetic Reader Domain	Apoptosis; Chromatin/Epigenetic
	NHWD-870 是一种有效且特异性的 BET 家族溴结构域抑制剂，仅与 BRD2、BRD3、BRD4 (IC50 = 2.7 nM) 和 BRDT 结合。 NHWD-870 具有强大的抗肿瘤功效，并通过增加肿瘤细胞凋亡和抑制肿瘤增殖来抑制癌细胞-巨噬细胞相互作用。
T4412	Roquinimex Linomide,罗喹美克,LS2616,FCF89,ABR212616	TNF	Apoptosis
	Roquinimex (FCF89) 是一种喹啉衍生物免疫刺激剂，可增加 NK 细胞活性和巨噬细胞的细胞毒性，抑制血管生成并减少 TNF α 的分泌。
T77493	Murlentamab 3C23K,GM102	Others	Others
	Murlentamab (GM102) 是一种人源化抗 AMHRII 抗体。Murlentama 具有潜在的抗肿瘤活性，可诱导巨噬细胞介导的抗体依赖的细胞介导的细胞毒性作用 (ADCC)。Murl可通过募，集、活化T细胞激发促炎和抗肿瘤内环境。Murlentama 通过促进幼稚的巨噬细胞定向，促进肿瘤相关巨噬细胞 (TAM) 重编程来发挥抗肿瘤活性。
T60388	MIF098	Others	Others
	MIF098 是一种巨噬细胞迁移抑制因子 (MIF) 拮抗剂。MIF098，抑制与 SLE 相关的肺动脉高压，抑制肺平滑肌细胞(PASMC)增殖和迁移。MIF098 可用于研究特发性肺动脉高压。
T60336	CCR4 antagonist 3-1	CCR	Immunology/Inflammation; Microbiology/Virology
	CCR4 antagonist 3-1 是一种具有较低活性的趋化因子受体 4 (CCR4) 拮抗剂，对 [125I]TARC (胸腺和活化调节趋化因子) 具有抑制作用，IC50 值为 1.7 μM。CCR4 antagonist 3-1 对放射标记的[125I]TARC和巨噬细胞来源的趋化因子(MDC) 与 CEM 细胞表面的CCR4 受体的结合有抑制作用，并对 TARC 介导的 CEM 细胞的体外迁移有抑制作用，IC50 值为 6.4 μM。
T77125	Otilimab GSK 3196165,MOR103	CSF-1R	Tyrosine Kinase/Adaptors
	Otilimab (GSK 3196165) 是一种人源化抗粒细胞-巨噬细胞集落刺激因子 (GM-CSF) 单克隆抗体。Otilimab 具有抗炎活性，通过阻断 GM-CSF 与其细胞表面受体的相互作用来调节 GM-CSF 的生物学功能，可用于研究治疗重症 COVID-19 肺炎。
T3614	Inosine pranobex Groprinosin,Isoprinosine,异丙肌苷,Immunovir,Delimmun	IL Receptor; HIV Protease	Immunology/Inflammation; Microbiology/Virology; Proteases/Proteasome
	Inosine pranobex (Delimmun) 是一种免疫增强剂，它是一种广谱抗病毒剂，用于 HIV 感染。
T11449L	Golotimod Gamma-D-glutamyl-L-tryptophan,SCV 07	Antibiotic	Microbiology/Virology
	Golotimod (SCV 07) 是一种具有抗菌活性的二肽，具有免疫调节活性，能显著提高抗结核治疗的疗效，诱导胸腺和脾脏细胞增殖，调节巨噬细胞功能，抑制 STAT3 信号传导。Golotimod 可用于研究复发性生殖器单纯疱疹病毒 2 （HSV-2）感染和口腔黏膜炎。
T61705	MIF-IN-6
	MIF-IN-6 (compound 2d) is an effective inhibitor of macrophage migration inhibitory factor (MIF), exhibiting an IC50 of 1.4 μM and a Ki value of 0.96 μM. MIF-IN-6 effectively reduces MIF-induced ERK phosphorylation and impedes A549 cell proliferation [1].
TP2115	SAH-EZH2
	EZH2/EPP interaction inhibitor (Kd = 320 nM). Suppresses EZH2 expression and H3K27 trimethylation by PCR2 complex. Arrests proliferation and induces monocyte to macrophage differentiation of MLL-AF9 leukemia cell line.
T69205	GGTI-2166
	GGTI-2166 is a geranylgeranyl transferase I inhibitor. GGTI-2166 inhibit the pOC formation induced by RANKL or TNF-alpha in cultures of both mouse marrow-derived macrophage-colony-stimulating factor (M-CSF) dependent monocytes (MD cells) and the mouse monocyte cell line RAW 264.7 (RAW cells). GGTI-2166 inhibited TRAP activity induced by RANKL or TNF-alpha in both cell cultures and prevented the incorporation of [3H]all-trans geranylgeraniol into prenylated proteins in RAW cells.
T78901	PPM-3	PROTACs	PROTAC
	PPM-3是一种高效的选择性PROTAC ERK5降解剂，不会直接作用于肿瘤细胞生长，而是通过调控巨噬细胞分化来间接影响肿瘤发展。
T78277	ATG-031
	ATG-031是一款人源化抗CD24单克隆抗体，能有效激活巨噬细胞介导的吞噬作用，阻断多种癌症细胞表面的“不要吃我”信号，诱导癌细胞清除。此抗体适用于血液恶性肿瘤和实体瘤研究。
T77110	Amivantamab
	Amivantamab (JNJ-61186372) 是一种人源 EGFR-MET 双特异性抗体，具有免疫抗癌活性。Amivantamab 可以抑制配体结合，促进受体-抗体复合物的内吞作用和降解，并诱导巨噬细胞的 Fc 依赖性胞吞作用和自然杀伤细胞的抗体依赖性细胞毒性。
T79634	LYP-IN-3	Phosphatase	Metabolism
	LYP-IN-3（compound D34）作为一种淋巴酪氨酸磷酸酶（LYP）的选择性抑制剂（Ki=0.93 μM），通过调节T细胞受体（TCR）信号通路发挥在肿瘤进展中的作用。它能够激活T细胞，抑制M2型巨噬细胞的极化，并上调PD-1/PD-L1表达，适合与PD-1/PD-L1抑制剂联合使用，为癌症免疫治疗提供进一步的疗效潜力。
T82994	Anzurstobart BMS-986351,CC-95251
	Anzurstobart (CC-95251; BMS-986351) 是具有高亲和力的SIRPα全人源单克隆抗体，能够阻断CD47与SIRPα的结合。联合应用抗体利妥昔单抗时，Anzurstobart能增强巨噬细胞在共培养模型中对DLBCL细胞系的吞噬作用，显示出在实体和血液恶性肿瘤研究中的应用潜力。
T78716	MKA031
	MKA031（compound 6y）作为一种非竞争性MIF抑制剂，展现出1.7 μM的IC50。该化合物能够阻断MIF/AIF相互作用、抑制MIF核内转移，并干预MNNG所诱发的细胞死亡。MKA031主要用于研究慢性丙型肝炎病毒感染。
T38073	Thiocarlide Isoxyl
	Thiocarlide (isoxyl) is a thiourea derivative that was used in the 1960s to successfully treat tuberculosis (TB). It has considerable antimycobacterial activity in vitro and is effective against multi-drug resistant strains of Mycobacterium tuberculosis in the range of 1-10 &#181g/ml. [1] [2] At concentrations of 10 &#181M, isoxyl inhibits the synthesis of M. bovis during six hours of exposure which is similar to isoniazid (INH) and ethionamide (ETH), two other predominant anti-tuberculosis drug...
T79635	LYP-IN-4	Phosphatase	Metabolism
	LYP-IN-4（compound D14）是一种针对淋巴酪氨酸磷酸酶（LYP）的可逆且特异性抑制剂，具有Ki值1.34 μM和IC50值3.52 μM。该化合物通过抑制LYP来调控TCR信号传递，并上调PD-1/PD-L1的表达，以此增强抗肿瘤免疫反应。此外，LYP-IN-4能够激活T细胞、抑制M2型巨噬细胞的极化，并在MC38同基因小鼠模型中抑制肿瘤生长。
T11449	Golotimod hydrochloride (229305-39-9 free base) Golotimod hydrochloride,Gamma-D-glutamyl-L-tryptophan hydrochloride,SCV 07 hydrochloride	STAT	JAK/STAT signaling; Stem Cells
	Golotimod (SCV 07) hydrochloride 是一种免疫调节肽，具抗菌活性，能显著提升抗结核疾病研究效果。该化合物通过刺激胸腺和脾细胞增殖、改善巨噬细胞功能，展现其生物调节能力。此外，Golotimod hydrochloride 通过抑制STAT3信号传导，有效调节接受放疗或与顺铂联用治疗动物模型中的口腔粘膜炎持续时间和严重程度。还显示出对研究复发性生殖器单纯疱疹病毒 2 型 (HSV-2) 具有潜在应用价值。
T38100	Betamethasone 21-phosphate (sodium salt hydrate)
	Betamethasone 21-phosphate is a synthetic glucocorticoid.1It prevents increases in macrophage and eosinophil numbers in bronchoalveolar lavage fluid (BALF) and decreases in blood leukocyte numbers in a guinea pig model of parainfluenza-3 viral infection when administered at a dose of 8 mg/kg but does not prevent airway hyperresponsiveness after infection.2Betamethasone 21-phosphate inhibits cell infiltration into the aqueous humor in a rat model of endotoxin-induced uveitis when administered top...
T83779	EP4 Antagonist 14 Prostaglandin E2 Receptor 4 Antagonist 14,PGE2 Receptor 4 Antagonist 14
	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。
T37861	Talabostat
	Talabostat (PT100, Val-boroPro) is a potent, nonselective and orally available dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 0.18 nM. Talabostat is a nonselective DPP-IV inhibitor, inhibiting DPP8/9, FAP, DPP2 and some other DASH family enzymes essentially as potently as it inhibits DPP-IV[1]. Talabostat stimulates the immune system by triggering a proinflammatory form of cell death in monocytes and macrophages known as pyroptosis. The inhibition of two serine proteases, DPP8 and DPP9,...
T38106	JC-171
	JC-171 is a selective NLRP3 inflammasome inhibitor, with an IC50 of 8.45 μM for inhibiting LPS/ATP-induced interleukin-1β (IL-1β) release from J774A.1 macrophages[1]. JC-171 (0-100 μM) blocks NLRP3 inflammasome activation and IL-1β production in primary macrophages dose dependently[1]. ...

化合物

Cat.No: T11344

Target: DNA, cGAS

Cat.No: T27730

Synonym: KGP-94,KGP 94

Target: Cysteine Protease

Cat.No: T36573

Target: Apoptosis, Epigenetic Reader Domain

Cat.No: T4412

Synonym: Linomide,罗喹美克,LS2616,FCF89,ABR212616

Target: TNF

Cat.No: T77493

Synonym: 3C23K,GM102

Target: Others

Cat.No: T60388

Target: Others

CCR4 antagonist 3-1

Cat.No: T60336

Target: CCR

Cat.No: T77125

Synonym: GSK 3196165,MOR103

Target: CSF-1R

Inosine pranobex

Cat.No: T3614

Synonym: Groprinosin,Isoprinosine,异丙肌苷,Immunovir,Delimmun

Target: IL Receptor, HIV Protease

Cat.No: T11449L

Synonym: Gamma-D-glutamyl-L-tryptophan,SCV 07

Target: Antibiotic

Cat.No: T61705

Cat.No: TP2115

Cat.No: T69205

Cat.No: T78901

Target: PROTACs

Cat.No: T78277

Cat.No: T77110

Cat.No: T79634

Target: Phosphatase

Cat.No: T82994

Synonym: BMS-986351,CC-95251

Cat.No: T78716

Cat.No: T38073

Synonym: Isoxyl

Cat.No: T79635

Target: Phosphatase

Golotimod hydrochloride (229305-39-9 free base)

Cat.No: T11449

Synonym: Golotimod hydrochloride,Gamma-D-glutamyl-L-tryptophan hydrochloride,SCV 07 hydrochloride

Target: STAT

Betamethasone 21-phosphate (sodium salt hydrate)

Cat.No: T38100

EP4 Antagonist 14

Cat.No: T83779

Synonym: Prostaglandin E2 Receptor 4 Antagonist 14,PGE2 Receptor 4 Antagonist 14

Cat.No: T37861

Cat.No: T38106

Cat. No.	Product Name	Target	Signaling Pathways
T3383	Cimifugin 升麻素,Cimitin	Others	Others
	Cimifugin (Cimitin) 是中草药Saposhnikovia divaricate 的一种生物活性成分。它能够调节紧密连接减少上皮衍生的主动关键因子，对过敏性炎症产生抑制作用。
T1257	Bestatin Ubenimex,乌苯美司	Others; Aminopeptidase; Antibacterial; Antibiotic; LTR	Immunology/Inflammation; Metabolism; Microbiology/Virology; Others
	Bestatin (Ubenimex) 是 CD13 (Aminopeptidase N)/APN 和 leukotriene A4 hydrolase 抑制剂，可用于癌症研究。
TN4146	Glutinol acetate	TNF	Apoptosis
	Glutinol acetate shows significant cytotoxic activity against four human cancer cell lines (HL-60, SK-OV-3, A549, and HT-29), with GI(50) in the range of 11.1-17.9microM; it also has anti-inflammatory effect, exhibits moderate inhibitory activity of TNF-alpha secretion in the lipopolysaccharide (LPS)-stimulated murine RAW264.7 macrophage cell line.
T35614	D-Trimannuronic acid
	D-Trimannuronic acid is an alginate oligomer that originates from seaweed. It can induce TNF-α secretion by mouse macrophage cell lines, making it valuable in pain and vascular dementia research [1][2][3].
T69446	Cochlioquinone A
	Cochlioquinone A is an inhibitor of diacylglycerol kinase (DGK) and diacylglycerol acyltransferase (DGAT). It has been shown to reduce the concentration of phosphatidic acid in T cell lymphoma and has also been shown to compete with macrophage inflammatory protein-1α for binding to human CCR5 chemokine receptors.
TN4050	Fargesone A	NOS	Immunology/Inflammation
	Fargesone A shows inhibitory effects on nitric oxide (NO) production in the lipopolysaccharide plus interferon-gamma activated-murine macrophage cell line, J774.1.
TN4089	Futokadsurin C	Others	Others
	Futokadsurin C can inhibit nitric oxide production by a murine macrophage-like cell line (RAW 264.7), which is activated by lipopolysaccharide and interferon-gamma.
TN6062	1,3,9-Trimethyluric acid
	1,3,9-Trimethyluric acid exhibits in vitro cytotoxic activity against breast cancer (MCF-7), human neuroblastoma (SHSY5Y), human non-small cell lung cancer (A549) and human liver cancer (HEPG2) with IC50 value in the range of 1-3 uM. 1,3,9-Trimethyluric a

天然产物

Cat.No: T3383

Synonym: 升麻素,Cimitin

Target: Others

Cat.No: T1257

Synonym: Ubenimex,乌苯美司

Target: Others, Aminopeptidase, Antibacterial, Antibiotic, LTR

Glutinol acetate

Cat.No: TN4146

Target: TNF

D-Trimannuronic acid

Cat.No: T35614

Cochlioquinone A

Cat.No: T69446

Cat.No: TN4050

Target: NOS

Cat.No: TN4089

Target: Others

1,3,9-Trimethyluric acid

Cat.No: TN6062

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