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18

抑制剂 & 化合物

8

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T24437	MCP110 MCP-110,MCP 110	Raf; Ras	GPCR/G Protein; MAPK
	MCP110 是 Ras 与 Raf-1 相互作用的抑制剂，可用于治疗人类肿瘤的研究。
T13114	CCR2 antagonist 4 Teijin compound 1	CCR	Immunology/Inflammation; Microbiology/Virology
	CCR2 antagonist 4 (Teijin compound 1) 是高效的、特异性的CCR2拮抗剂，对 CCR2b 的IC50为 180 nM，抑制 MCP-1 诱导的趋化作用的 IC50为 24 nM。
T8316	1V209 TLR7 agonist T7	TLR	Immunology/Inflammation
	1V209 (TLR7 agonist T7) 是一种 Toll 样受体 7 (TLR7) 激动剂，可与各种多糖缀合，以改善其水溶性，增强功效并保持低毒性，具有抗肿瘤作用。
T11079	NMI 8739 n-docosahexaenoyl dopamine,Dha-DA conjugate	Dopamine Receptor	GPCR/G Protein; Neuroscience
	NMI 8739 (n-docosahexaenoyl dopamine) 是 D2 自身受体的激动剂。 NMI 8739 减少 NO 的产生并引起 CCL-20、MCP-1 和 IL-6 释放的浓度依赖性抑制。
T16091	MK-0812 Succinate	Others; CCR	Immunology/Inflammation; Microbiology/Virology; Others
	MK-0812 Succinate 是一种选择性CCR2拮抗剂。
T11648	INCB 3284	Others	Others
	INCB 3284, a potent and selective human CCR2 antagonist with an oral bioavailability, is utilized in the study of acute liver failure. It effectively inhibits the binding of monocyte chemoattractant protein-1 (MCP-1) to hCCR2, demonstrating an IC50 of 3.7 nM.
T19230	CCR2 antagonist 4 hydrochloride Teijin compound 1 hydrochloride	Others	Others
	CCR2 antagonist 4 hydrochloride is a specific CCR2 antagonist (IC50s: 180 nM for CCR2b). It potently inhibits MCP-1-induced chemotaxis (IC50: 24 nM).
T78806	PPARδ agonist 9	PPAR	DNA Damage/DNA Repair; Metabolism
	PPARδ agonist9 (compound 21) 作为PPARδ激动剂，展现出EC50为3.6 nM的活性。在体内实验中，PPARδ agonist9能有效降低小鼠血清中MCP-1水平，并在LDLr-KO模型中显著抑制动脉粥样硬化的发展，其抑制率达50-60%。
T80059	Complement factor I	Endogenous Metabolite	Metabolism
	Complement factor I，一丝氨酸蛋白酶，可与辅助因子H (FH)、补体受体1 (CR1/CD35)、C4结合蛋白 (C4BP) 或膜辅助因子蛋白 (MCP/CD46) 结合，调控液相及/或细胞表面补体系统的活性。
T68721	Cantharidin imide
	Cantharidin imide is a PP1/2A inhibitor found in Canarthis vesicatoria. It inhibits proliferation of colorectal cancer cells, increases MCP-1, IL-6, and IL-β levels, and inhibits differentiation and resorptive activity of osteoclasts. This compound can produce severe skin inflammation, and is extremely toxic if ingested orally.
T36198	Avenanthramide-C methyl ester
	Avenanthramide-C methyl ester is an inhibitor of NF-κB activation that acts by blocking the phosphorylation of IKK and IκB (IC50 ~ 40 μM). Through this mechanism, avenanthramide-C methyl ester dose dependently inhibits the expression and secretion of IL-6, IL-8, and MCP-1 in human aortic endothelial cells.
T82233	HCAR2 agonist 1
	HCAR2 agonist 1 (Compound 9n) 是一种偏向Gi蛋白的变构调节剂，能够激活Gi蛋白相关的信号传导通路。该化合物展现了明显的抗炎效果，能够显著降低促炎细胞因子（TNF-α、IL-1β、IL-6 和 MCP-1）的mRNA表达水平，并在结肠炎小鼠模型中增强正位激动剂的抗炎作用。
T36130	22(S)-hydroxy Cholesterol 22(S)-hydroxy Cholesterol,22β-hydroxy Cholesterol
	22(S)-hydroxy Cholesterol is a synthetic oxysterol and a modulator of the liver X receptor (LXR). [1] t prevents monocyte chemoattractant protein 1 (MCP-1) expression induced by the LXR agonist GW 3965 in primary hepatocytes and downregulates mRNA expression of the LXR target genes CD36, ACSL1, and SCD-1 in human myotubes. It decreases triacylglycerol and diacylglycerol synthesis from labeled palmitate and acetate, respectively, in human myoblasts by 50% when used at a concentration of 10 uM. 22...
T71884	ß-Carboline-1-carboxylic acid
	β-Carboline-1-carboxylic acid is an alkaloid that has been found in P. quassioides and has diverse biological activities. It reduces LPS-induced increases in MCP-1, TNF-α, IL-6, and IL-1β levels in RAW 264.7 cells when used at a concentration of 15 µg/ml and inhibits the epithelial-to-mesenchymal transition (EMT) induced by TGF-β1 in A549 cells. β-Carboline-1-carboxylic acid induces cytotoxicity in CT26.WT, K562, and SGC-7901 cells (IC50s = 14.96, 22.11, and 19.7 µg/ml, respectively) but not Hep...
T11647	INCB 3284 dimesylate	Others	Others
	INCB 3284 dimesylate is a selective and orally bioavailable human CCR2 antagonist, inhibiting monocyte chemoattractant protein-1 binding to hCCR2 (IC50: 3.7 nM). It can be used in the research of acute liver failure.
T7499	TAK-779 Takeda 779	HIV Protease; CXCR; CCR	Autophagy; GPCR/G Protein; Immunology/Inflammation; Microbiology/Virology; Proteases/Proteasome
	TAK-779 (Takeda 779) 是一种非肽类CCR5和CXCR3 拮抗剂，对CCR5的Ki 值为 1.1 nM，并选择性抑制R5 HIV-1。
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,...
T14845	BX471 hydrochloride ZK-811752 hydrochloride	Others	Others
	BX471 hydrochloride (ZK-811752 hydrochloride) is a potent, selective non-peptide CCR1 antagonist (Ki: 1 nM for human CCR1). It shows 250-fold selectivity for CCR1 over CCR2, CCR5, and CXCR4.

化合物

Cat.No: T24437

Synonym: MCP-110,MCP 110

Target: Raf, Ras

CCR2 antagonist 4

Cat.No: T13114

Synonym: Teijin compound 1

Target: CCR

Cat.No: T8316

Synonym: TLR7 agonist T7

Target: TLR

Cat.No: T11079

Synonym: n-docosahexaenoyl dopamine,Dha-DA conjugate

Target: Dopamine Receptor

MK-0812 Succinate

Cat.No: T16091

Target: Others, CCR

Cat.No: T11648

Target: Others

CCR2 antagonist 4 hydrochloride

Cat.No: T19230

Synonym: Teijin compound 1 hydrochloride

Target: Others

PPARδ agonist 9

Cat.No: T78806

Target: PPAR

Complement factor I

Cat.No: T80059

Target: Endogenous Metabolite

Cantharidin imide

Cat.No: T68721

Avenanthramide-C methyl ester

Cat.No: T36198

HCAR2 agonist 1

Cat.No: T82233

22(S)-hydroxy Cholesterol

Cat.No: T36130

Synonym: 22(S)-hydroxy Cholesterol,22β-hydroxy Cholesterol

ß-Carboline-1-carboxylic acid

Cat.No: T71884

INCB 3284 dimesylate

Cat.No: T11647

Target: Others

Cat.No: T7499

Synonym: Takeda 779

Target: HIV Protease, CXCR, CCR

Cat.No: T37861

BX471 hydrochloride

Cat.No: T14845

Synonym: ZK-811752 hydrochloride

Target: Others

Cat. No.	Product Name	Target	Signaling Pathways
T6413	Bindarit 宾达利,AF2838	CCR	Immunology/Inflammation; Microbiology/Virology
	Bindarit (AF2838) 是单核细胞趋化蛋白MCP-1/CCL2，MCP-3/CCL7和MCP-2/CCL8的选择性抑制剂，具有抗炎作用。
TC0036	Compound Lup-20(29)-en-3-yl acetate	IL Receptor; VEGFR; Others; TNF; COX	Angiogenesis; Apoptosis; Immunology/Inflammation; Neuroscience; Others; Tyrosine Kinase/Adaptors
	Lup-20(29)-en-3-yl acetate 是 Lupeol 的衍生物，通过下调 TNF-α、IL-1β、MCP-1、COX-2、VEGF 和颗粒酶 B 来抑制类风湿性关节炎的进展。
T4S0795	Berberrubine chloride 9-Berberoline Chloride,Beroline,Beroline Chloride,小檗红碱,Berberrubine,9-Berberoline	IL Receptor	Immunology/Inflammation
	Berberrubine chloride (9-Berberoline Chloride) 是一种黄连素的有效代谢物，能够改善动物模型中溃疡性结肠炎的症状。
T5688	Micheliolide	NOS; NF-κB; COX	Immunology/Inflammation; Neuroscience; NF-κB
	Micheliolide 是一种倍半萜内酯，能够抑制各种炎症反应。它能减弱高糖刺激的NF-κB 活化，IκBα的降解，和MCP-1，TGF-β1，FN 在鼠系膜细胞的表达。
T4S0350	Licochalcone B 甘草查尔酮 B,甘草查尔酮B	Beta Amyloid; Others	Neuroscience; Others
	Licochalcone B 是从Glycyrrhiza inflate 根中提取的。它能够抑制淀粉样蛋白 β 自聚集作用 (IC50=2.16 μM) ，分解预先形成的 Aβ42原纤维，并通过螯合金属离子抑制金属诱导的 Aβ42聚集。
TN1154	Nepetin 6-Methoxyluteolin,泽兰黄酮,6-甲氧基藤黄菌素	Calcium Channel; Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Neuroscience
	Nepetin (6-Methoxyluteolin) 是一种分离自Eupatorium ballotaefoliumHBK 中的天然类黄酮，具有有效的抗炎作用。它在 ARPE-19 细胞中能够抑制IL-6(IC50:4.43 μM) 、IL-8 (IC50:43.42 μM) 、MCP-1 (IC50:4.17 μM) 的分泌。
TN5593	Euphohelioscopin A
	Euphohelioscopin A, an activator of protein kinase C (PKC), it inhibits proliferation and induces differentiation of the myeloid leukemia cell lines THP-1 and HL-60. Euphohelioscopin A has anti-inflammary activity, it exhibits moderate inhibitory activity
T38285	C24:1 3'-sulfo Galactosylceramide (d18:1/24:1(15Z)) C24:1 3'-sulfo Galactosylceramide (d18:1/24:1(15Z))	Others	Others
	C24:1 3'-sulfo Galactosylceramide (d18:1/24:1(15Z))是成熟髓鞘中主要的硫酸盐类化合物。C24:1 3'-sulfo Galactosylceramide (d18:1/24:1(15Z)) 在大鼠小脑中发现活跃的髓发生鞘化反应时积累率高于C24 3'-sulfo 半乳糖甘油酰胺。C24:1 3'-sulfo Galactosylceramide (d18:1/24:1(15Z))与C 型凝集素和免疫球蛋白样受体相互作用使对LMIR5的亲和力高。C24:1 3'-sulfo Galactosylceramide (d18:1/24:1(15Z))诱导嗜碱细胞产生MCP-1，可通过增加LMIR5激活NFAT，但不能诱导肥大细胞。C24:1 3'-sulfo Galactosylceramide (d18:1/24:1(15Z))在体外与CD1d 结合，并增加游离小鼠脾细胞的增殖。

天然产物

Cat.No: T6413

Synonym: 宾达利,AF2838

Target: CCR

Compound Lup-20(29)-en-3-yl acetate

Cat.No: TC0036

Target: IL Receptor, VEGFR, Others, TNF, COX

Berberrubine chloride

Cat.No: T4S0795

Synonym: 9-Berberoline Chloride,Beroline,Beroline Chloride,小檗红碱,Berberrubine,9-Berberoline

Target: IL Receptor

Cat.No: T5688

Target: NOS, NF-κB, COX

Cat.No: T4S0350

Synonym: 甘草查尔酮 B,甘草查尔酮B

Target: Beta Amyloid, Others

Cat.No: TN1154

Synonym: 6-Methoxyluteolin,泽兰黄酮,6-甲氧基藤黄菌素

Target: Calcium Channel, Histamine Receptor

Euphohelioscopin A

Cat.No: TN5593

C24:1 3'-sulfo Galactosylceramide (d18:1/24:1(15Z))

Cat.No: T38285

Synonym: C24:1 3'-sulfo Galactosylceramide (d18:1/24:1(15Z))

Target: Others

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