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30

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T15055	DB04760 MMP-13 Inhibitor	MMP	Proteases/Proteasome
	DB04760 是一种高选择性和有效的 MMP-13 非锌螯合抑制剂（IC50：8 nM）。DB04760 能明显降低紫杉醇的神经毒性，并具有抗癌活性。
T16124	MMP13-IN-3	MMP	Proteases/Proteasome
	MMP13-IN-3 是口服有效的MMP-13选择性抑制剂，IC50为 1 nM，比其他 MMP 的选择性高 1000倍多。MMP13-IN-3在用于骨关节炎方面有研究的价值。
T37172	MMP-9/MMP-13 Inhibitor I
	MMP-9/MMP-13 Inhibitor I 是 MMP-9 和 MMP-13 双重抑制剂，IC50 均为 0.9 nM。MMP-9/MMP-13 Inhibitor I 对 MMP-9/MMP-13 的选择性是其他 MMP 的 20 倍以上。
T76077	MMP-13 Substrate
	MMP-13Substrate 是MMP-13的底物。MMP-13Substrate 可用于骨关节炎 (OA) 的研究。
T41079	MMP13-IN-2 MMP13-IN-2
	MMP13-IN-2 is a highly potent, selective, and orally active inhibitor of MMP-13. It demonstrates exceptional potency against MMP-13, with an IC50 value of 0.036 nM, and exhibits selectivities greater than 1,500-fold over MMP-1, 3, 7, 8, 9, 14, and TACE. Moreover, MMP13-IN-2 possesses the capability to effectively inhibit collagen release from cartilage in vitro. Consequently, MMP13-IN-2 holds great potential for advancing research on collagenase-related diseases.
T20563	PD-166793 PD-166793-0000,PD 166793,PD166793	MMP	Proteases/Proteasome
	PD-166793是一种具有口服活性、有效性和选择性的 MMP 抑制剂，对 MMP-2，MMP-3 和 MMP-13 具有抑制作用。PD-166793 在大鼠心力衰竭模型中改善心肌缺血和再灌注损伤。
T14978	CL-82198	MMP	Proteases/Proteasome
	CL-82198 是 MMP-13选择性抑制剂。它能够与 MMP-13 的整个 S1' 口袋结合，这是其对 MMP-13 选择性和对其他 MMP 缺乏抑制活性的基础。它可用于研究骨关节炎。
T5361	T-26c	MMP	Proteases/Proteasome
	T-26c 是高效的、选择性的基质金属蛋白酶-13 抑制剂，IC50=6.75 pM。
T6885	Marimastat BB2516,马立马司他,KB-R8898,TA2516	MMP	Proteases/Proteasome
	Marimastat (BB2516) 是一种血管生成和转移抑制剂，限制血管的生长和生成。它是一种广谱的，具有口服活性的MMPs 抑制剂，有效抑制 MMP-9 , MMP-1, MMP-2, MMP-14, MMP-7，用于癌症的研究。
T5416	T-5224	MMP	Proteases/Proteasome
	T-5224 是选择性的转录因子c-Fos/activator protein (AP)-1抑制剂，具有抗炎作用，能够特异性抑制 c-Fos/c-Jun 的 DNA 结合活性，但对其他转录因子的结合活性无影响。它抑制 IL-1β 诱导的 Mmp-3、Mmp-13、Adamts-5 转录上调。
T29150	WAY-151693 WAY151693,WAY 151693
	WAY-151693 is an inhibitor of human collagenase-3 (MMP-13).
T22685	CP-471474 CP 471474	Others	Others
	Broad spectrum MMP inhibitor (IC<sub>50</sub> values are 0.7, 0.9, 13, 16 and 1170 nM for MMP-2, MMP-13, MMP-9, MMP-3 and MMP-1 respectively). Attenuates early left ventricular dilation after experimental myocardial infarction in mice.
T78775	MMP13-IN-5	MMP	Proteases/Proteasome
	MMP13-IN-5 (compound 13m) 作为具有针对性的MMP-2/MMP-13 抑制剂，显示出高效的抑制活性（IC50=3.6 μM/14.6 μM），适用于骨关节炎疼痛的研究。
T13358	XL-784	MMP	Proteases/Proteasome
	XL-784 is a selective inhibitor of matrix metalloproteinases (MMP)(IC50s of ~1900, 0.81, 120, 10.8, 18, 0.56 nM for MMP-1,MMP-2,MMP-3,MMP-8,MMP-9,MMP-13,respectively).
T24775	SD-2590 HCl SD2590 HCl,SD-2590 Hydrochloride,SD2590 Hydrochloride,SD 2590 Hydrochloride
	SD-2590 HCl is an MMP-2,-3, -9, -8, 13, and -14 inhibitor.
T16986	Tanomastat BAY 12-9566	MMP	Proteases/Proteasome
	Tanomastat is an orally bioavailable and non-peptidic biphenyl matrix metalloproteinases inhibitor. For MMP-2, MMP-3, MMP-9, MMP-13 the Ki values are 11, 143, 301, and 1470 nM respectively.
T13357	XL-784 free base	Others	Others
	XL-784 free base is a selective inhibitor of matrix metalloproteinases (MMP), (IC50s of ~1900, 0.81, 120, 10.8, 18, 0.56 nM for MMP-1,MMP-2,MMP-3,MMP-8,MMP-9,MMP-13,respectively).
T38800	MMPI-1154
	MMPI-1154 is a highly promising imidazole-carboxylic acid (ICA) MMP-2 inhibitor (IC 50 = 6.6 μM) with excellent cardio-cytoprotective properties. It is specifically designed for the study of acute myocardial infarction. Additionally, MMPI-1154 exhibits significant inhibitory effects on MMP-13, MMP-1, and MMP-9 activities with IC 50 values of 1.8 μM, 10 μM, and 13 μM, respectively.
T78774	MMP13-IN-4	MMP	Proteases/Proteasome
	MMP13-IN-4（compound 13）作为MMP-13抑制剂，具备强效性和选择性，其IC50值为14.6 μM，可用于骨关节炎疼痛的研究。
T60551	MMP2-IN-2
	MMP2-IN-2 (化合物 42) 是一种有效且选择性的MMP-2(基质金属蛋白酶)抑制剂，其IC50值为 4.2 μM。它对MMP-13、MMP-9和MMP-8也具有抑制活性，IC50值分别为 12、23.3 和 25 μM。
T41179	CL 82198 hydrochloride
	CL 82198 hydrochloride is a selective inhibitor of MMP-13 (89% inhibition at 10μg/mL) that displays no activity at MMP-1, MMP-9 or TACE. Inhibitsin vitroinvasion by the human pituitary adenoma cell line HP75. Rescues paclitaxel induced axon degradation and reduces associated neurotoxicity in zebrafish.
T37983	GM 1489
	GM 1489 is a broad-spectrum inhibitor of matrix metalloproteinases (MMPs) with Ki values of 0.002, 0.1, 0.5, 0.2, and 20 μM for MMP-1, MMP-8, MMP-2, MMP-9, and MMP-3, respectively. It reduces 5-aza-2'-deoxycytidine-induced increases in MMP-1, MMP-2, MMP-3, MMP-7, MMP-9, and MMP-14 expression as well as cell invasion in AsPC-1, BxPC-3, Hs766T, MiaPaCa2, and PANC-1 cancer cells. Topical administration of GM 1489 (100 μg) inhibits increases in ear thickness and epidermal hyperplasia induced by phor...
T16291	NF157	COX	Immunology/Inflammation; Neuroscience
	NF157 significantly decreases the expression of metalloproteinase (MMP)-3, MMP-13, which can be used in the treatment of osteoarthritis (OA). NF157 is a highly selective nanomolar P2Y11 antagonist (pKi: 7.35). The IC50s are 463 nM, 1811 µM, 170 µM for P2Y
T78436	Mca-Lys-Pro-Leu-Gly-Leu-Dap(Dnp)-Ala-Arg-NH2	MMP	Proteases/Proteasome
	Mca-Lys-Pro-Leu-Gly-Leu-Dap(Dnp)-Ala-Arg-NH2 (FS-6) 是一种用于实时定量测定基质金属蛋白酶(MMP)酶活性的猝灭荧光肽底物。该化合物是MMP底物(FS-1)的衍生物，对胶原酶MMP-1、MMP-8、MMP-13及MT1-MMP的特异性常数更高，具备较强的底物特异性。荧光激发与发射波长分别为325 nm和400 nm。
T37726	MMP-9 Inhibitor I
	MMP-9 inhibitor I is an inhibitor of matrix metalloproteinase-9 (MMP-9) that is selective over MMP-1 and MMP-13 (IC50s = 5, 1,050, and 113 nM, respectively). It also decreases the activity of TNF-α converting enzyme (TACE) in a dose-dependent manner (IC50 = 0.54 μM). MMP-9 inhibitor I decreases TNF-α secretion stimulated by LPS in BV-2 microglial cells when used at concentrations of 50 and 100 μM.
T62090	(Rac)-Tanomastat
	Rac)-Tanomastat ((Rac)-BAY 12-9566) 是 Tanomastat 的外消旋体。其中 Tanomastat (BAY 12-9566) 是一种口服具有活力的、含锌羧基的非肽联苯基质金属蛋白酶(MMPs)抑制剂，能够抑制 MMP-2 (Ki: 11 nM)、MMP-3 (Ki: 143 nM)、MMP-9 (Ki: 301 nM)、MMP-13 (Ki: 1470 nM)。在几种实验性肿瘤模型中，Tanomastat 表现出抗侵袭和抗转移作用。
T69230	AZD-1236
	AZD1236 is a potent and reversible inhibitor of human MMP-9 and MMP-12 (IC50 = 4.5 and 6.1nM, respectively), with >10-fold selectivity to MMP-2 and MMP-13 and >350-fold selectivity to other members of the enzyme family. AZD1236 activity is approximately 20 to 50-fold lower at the rat, mouse, and guinea pig orthologues. In acute models of lung injury, AZD1236 inhibited the haemorrhage and inflammation induced by instillation of human MMP-12 into rat lungs by ~80% at 0.81mg/kg, and also abolished ...
T80242	TNO211	MMP	Proteases/Proteasome
	TNO211为具备生物活性的肽，主要研究对象是基质金属蛋白酶（MMP），一类能够降解多种细胞外基质蛋白并调控诸多生物活性分子的肽链内切酶家族。MMP在细胞表面受体裂解、凋亡配体释放及趋化因子/细胞因子失活等过程中起作用，同时与细胞增殖、迁移（粘附/分散）、分化、血管生成、细胞凋亡及宿主防御等生物行为密切相关。TNO211可靶向MMP-2、8、12、13和14，包含MMP特定可裂解的Gly-Leu键，并具有EDANS/DABCYL荧光标记，其荧光检测在监测内皮细胞培养基和患者滑液中的MMP活性方面表现出高灵敏度。吸光度/电磁场测量参数为340/490 nm。
T37860	T 26c disodium salt
	Highly potent and selective MMP13 inhibitor (IC50 = 6.9 pM). Exhibits >2600-fold selectivity for MMP13 over related MMPs. Inhibits degradation of bovine nasal septum cartilage explants in vitro . Orally bioavailable. Nara et al (2014) Thieno[2,3-d]pyrimidine-2-carboxamides bearing a carboxybenzene group at 5-position: highly potent, selective, and orally available MMP-13 inhibitors interacting with the S1 binding site. Bioorg.Med.Chem. 22 5487 PMID:25192810"
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,...

化合物

Cat.No: T15055

Synonym: MMP-13 Inhibitor

Target: MMP

Cat.No: T16124

Target: MMP

MMP-9/MMP-13 Inhibitor I

Cat.No: T37172

MMP-13 Substrate

Cat.No: T76077

Cat.No: T41079

Synonym: MMP13-IN-2

Cat.No: T20563

Synonym: PD-166793-0000,PD 166793,PD166793

Target: MMP

Cat.No: T14978

Target: MMP

Cat.No: T5361

Target: MMP

Cat.No: T6885

Synonym: BB2516,马立马司他,KB-R8898,TA2516

Target: MMP

Cat.No: T5416

Target: MMP

Cat.No: T29150

Synonym: WAY151693,WAY 151693

Cat.No: T22685

Synonym: CP 471474

Target: Others

Cat.No: T78775

Target: MMP

Cat.No: T13358

Target: MMP

Cat.No: T24775

Synonym: SD2590 HCl,SD-2590 Hydrochloride,SD2590 Hydrochloride,SD 2590 Hydrochloride

Cat.No: T16986

Synonym: BAY 12-9566

Target: MMP

XL-784 free base

Cat.No: T13357

Target: Others

Cat.No: T38800

Cat.No: T78774

Target: MMP

Cat.No: T60551

CL 82198 hydrochloride

Cat.No: T41179

Cat.No: T37983

Cat.No: T16291

Target: COX

Mca-Lys-Pro-Leu-Gly-Leu-Dap(Dnp)-Ala-Arg-NH2

Cat.No: T78436

Target: MMP

MMP-9 Inhibitor I

Cat.No: T37726

(Rac)-Tanomastat

Cat.No: T62090

Cat.No: T69230

Cat.No: T80242

Target: MMP

T 26c disodium salt

Cat.No: T37860

Cat.No: T37861

Cat. No.	Product Name	Target	Signaling Pathways
T5S1026	Apigenin-7-glucuronide Apigenin 7-O-glucuronide,芹菜素-7-葡萄糖醛酸	MMP	Proteases/Proteasome
	Apigenin-7-glucuronide (Apigenin 7-O-glucuronide) 能够抑制基质金属蛋白酶的活性，其对 MMP-3 (IC50:12.87 μM)，MMP-8 (IC50:22.39 μM)，MMP-9 (IC50:17.52 μM)，MMP-13 (IC50:0.27 μM)。
T3850	Luteolin 7-O-glucuronide Luteolin-7-glucuronide,木犀草素-7-O-葡萄糖醛酸苷	MMP	Proteases/Proteasome
	Luteolin 7-O-glucuronide (Luteolin-7-glucuronide) 是一种自由基清除剂，能够抑制基质金属蛋白酶的活性，其对 MMP-1，MMP-3，MMP-8，MMP-9，MMP-13的IC50值分别为 17.63，7.99，11.42，12.85，0.03 μM。

天然产物

Apigenin-7-glucuronide

Cat.No: T5S1026

Synonym: Apigenin 7-O-glucuronide,芹菜素-7-葡萄糖醛酸

Target: MMP

Luteolin 7-O-glucuronide

Cat.No: T3850

Synonym: Luteolin-7-glucuronide,木犀草素-7-O-葡萄糖醛酸苷

Target: MMP

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