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24

抑制剂 & 化合物

5

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T8310	MMP-9-IN-1	MMP	Proteases/Proteasome
	MMP-9-IN-1 是特异性的基质金属蛋白酶-9 抑制剂，选择性靶向 MMP-9 的血红素域，对其他 MMP 无影响。
T62555	MMP-2/9-IN-1
	MMP-2/9-IN-1 (Compound 4a) 是一种有效的 MMP-2 (IC50: 56 nM) 和 MMP-9 (IC50: 38 nM) 双重抑制剂。MMP-2/9-IN-1 对肿瘤生长具有抑制作用，明显诱导癌细胞凋亡 (apoptosis)，抑制细胞迁移，并抑制细胞周期进程导致 DNA 片段化。
T21512	MMP-2/MMP-9 Inhibitor I	MMP	Proteases/Proteasome
	MMP-2/MMP-9-IN-1 是一种有效的、具有高选择性和可口服的 IV 型胶原酶 (MMP-9和MMP-2) 抑制剂，对 MMP-9 和 MMP-2具有抑制作用， IC50分别为 0.24 和 0.3 1μM。MMP-2/MMP-9-IN-1 在肿瘤生长和转移的动物模型中展现出口服活性，可用于研究癌症。
T14322	ARP-100 MMP-2 Inhibitor III	MMP	Proteases/Proteasome
	ARP-100 (MMP-2 Inhibitor III) 是选择性基质金属蛋白酶MMP-2抑制剂 (IC50=12 nM)。它对 MMP-1 (>50 μM)，MMP-3 (4.5 μM)，MMP-7 (>50 μM) 和MMP-9 (0.2 μM) 的抑制活性较小。它与 MMP-2 的 S1＇口袋相互作用，并在体外对基质胶的侵袭模型中显示抗侵袭特性。
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...
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.
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.
T81777	MMP-9-IN-8
	MMP-9-IN-8（Compound 3）是MMP-9抑制剂，10 μM浓度下抑制活性为42.16%，50 μM时达58.28%。该化合物展现抗癌活性，能诱导MCF-7细胞凋亡，IC50为23.42 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.
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。
T61491	(R)-ND-336
	(R)-ND-336 is a highly potent and selective MMP-9 inhibitor, displaying a K i value of 19 nM. It also exhibits inhibitory activity against MMP-2 (K i = 127 nM) and MMP-14 (K i =119 nM). With its significant potential, (R)-ND-336 is being investigated in the field of diabetic foot ulcers (DFUs) research [1].
T27033	CKD-712 CKD 712,CKD712
	CKD-712 is a nuclear factor NF-kappa B inhibitor. CKD-712 suppressed MMP-9, but not MMP-2 and other NF-κB-regulated proteins involved in cancer metastasis such as VEGF. CKD-712 induced cell cycle arrest at G2M phase by suppressing cyclin A, cyclin B and C
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.
T63545	FAK-IN-3
	FAK-IN-3 是一种有效的粘着斑激酶 (FAK) 抑制剂。FAK-IN-3 能够减少 PA-1 细胞的迁移和侵袭，并抑制 MMP-2 和 MMP-9 的表达。FAK-IN-3 对肿瘤生长和转移具有抑制作用，且没有明显不良反应。FAK-IN-3 对卵巢癌表现出研究潜力。
T81171	SH491
	SH491（Compound 33）是一款抗骨质疏松药物。该化合物能够抑制RANKL诱导的骨髓源性单核细胞（BMM）分化为破骨细胞（IC50: 11.8 nM）。同时，SH491降低了破骨细胞形成的相关标记基因（TRAP、CTSK、MMP-9和ATPase v0d2）以及相应蛋白（TRAP、CTSK、MMP-9）的表达。
T80108	Hepcidin-1 (mouse)
	Hepcidin-1 (mouse) 是调控铁平衡的内源性多肽激素，通过上调TRAP、组织蛋白酶K和MMP-9的mRNA水平及增强TRAP-5b蛋白的分泌作用。此外，Hepcidin-1 (mouse) 降低FPN1蛋白水平并提升细胞内铁含量，且促进破骨细胞的分化。
T35701	FSL-1 TFA
	FSL-1 TFA, a bacterial-derived toll-like receptor 2/6 (TLR2/6) agonist, enhances resistance to experimental HSV-2 infection[1]. FSL-1 TFA induces MMP-9 production through TLR2 and NF-κB/AP-1 signaling pathways in monocytic THP-1 cells[2]. FSL-1 significantly reduces HSV-2 replication in human vaginal epithelial cells (EC)[1].FSL-1 induces significant resistance to experimental genital HSV-2 infection through elaboration of a specific cytokine response profile[1].FSL-1 (50 ng/mL, 24 hours) induce...
T37713	Funalenone
	Funalenone is a phenalenone originally isolated from A. niger. It inhibits HIV-1 integrase (IC50 = 10 μM) and HIV-1 replication in human peripheral blood cells transformed by murine leukemia virus (HPB-M(a); IC50 = 1.7 μM) but is less cytotoxic to mammalian HPB-M(a) cells (IC50 = 87 μM). Funalenone selectively inhibits matrix metalloproteinase-1 (MMP-1; IC50 = 170 μM) over MMP-2 and MMP-9, which it inhibits by 18.3 and 38.2%, respectively, when used at a concentration of 400 μM. It also inhibits...
T62005	Imidapril
	Imidapril (TA-6366 free base) 是口服有效的血管紧张素转换酶（ACE）和MMP-9抑制剂。Imidapril 通过抑制血管紧张素 I 向血管紧张素 II 转化从而降低总外周阻力和血压。Imidapril 在高血压、1 型糖尿病、肾病和慢性心力衰竭中有研究价值。
T79560	22-(4′-py)-JA 22-(4′-Pyridinecarbonyl) jorunnamycin A	Akt	Cytoskeletal Signaling; PI3K/Akt/mTOR signaling
	22-(4′-py)-JA是久那霉素A的半合成衍生物，源自泰国蓝海绵（Xestospongia sp.）。该化合物显示出抗转移活性，能抑制AKT/mTOR/p70S6K信号通路，并阻断人脐静脉内皮细胞（HUVEC）中肿瘤细胞侵袭及管形成作用。它通过下调金属蛋白酶（MMP-2和MMP-9）、缺氧诱导因子1α（HIF-1α）和血管内皮生长因子（VEGF）来发挥作用。此外，22-(4′-py)-JA对非小细胞肺癌（NSCLC）显示出显著的抗癌效果。
T36844	Inostamycin A
	Inostamycin A is a bacterial metabolite that has been found inStreptomycesand has anticancer activity.1It is an inhibitor of CDP-diacylglycerol:inositol 3-phosphatidyltransferase (IC50= 0.02 μg/ml in A431 cell membranes) and is selective for CDP-diacylglycerol:inositol 3-phosphatidyltransferase over phospholipase C (PLC) and phosphatidylinositol kinase at 10 μg/ml.2Inostamycin A decreases viability of YCU-T892, KCC-TC873, KB, HSC-4, and YCU-T891 oral squamous cell carcinoma (OSCC) cells in a con...
T69995	Chlorhexidine-d8 HCl
	Chlorhexidine-d8 is intended for use as an internal standard for the quantification of chlorhexidine by GC- or LC-MS. Chlorhexidine is a bis(biguanide) antimicrobial disinfectant and antiseptic agent. It inhibits growth of clinical methicillin-resistant S. aureus (MRSA) isolates (MIC90 = 4 μg/ml). It is also active against canine isolates of MRSA, methicillin-susceptible S. aureus (MSSA), methicillin-resistant S. pseudintermedius (MRSP), and methicillin-susceptible S. pseudintermedius (MSSP; MIC...
T35558	KAAD-Cyclopamine
	Cyclopamine-KAAD is a potent inhibitor of hedgehog signaling with an IC50 value of 20 nM in a Shh-LIGHT2 assay. It blocks binding of BODIPY-cyclopamine to cells expressing Smoothened (Smo) in a dose-dependent manner. Cyclopamine-KAAD is cell-permeable and binds to SmoA1 to promote its exit from the endoplasmic reticulum. It inhibits the invasion and migration (45.9 and 43.3% inhibition, respectively) of Bel-7402 hepatocarcinoma cells and decreases the expression of nuclear glioma-associated onco...
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: T8310

Target: MMP

Cat.No: T62555

MMP-2/MMP-9 Inhibitor I

Cat.No: T21512

Target: MMP

Cat.No: T14322

Synonym: MMP-2 Inhibitor III

Target: MMP

Cat.No: T37983

Cat.No: T22685

Synonym: CP 471474

Target: Others

MMP-9 Inhibitor I

Cat.No: T37726

Cat.No: T81777

CL 82198 hydrochloride

Cat.No: T41179

Cat.No: T60551

Cat.No: T61491

Cat.No: T27033

Synonym: CKD 712,CKD712

Cat.No: T41079

Synonym: MMP13-IN-2

Cat.No: T63545

Cat.No: T81171

Hepcidin-1 (mouse)

Cat.No: T80108

Cat.No: T35701

Cat.No: T37713

Cat.No: T62005

22-(4′-py)-JA

Cat.No: T79560

Synonym: 22-(4′-Pyridinecarbonyl) jorunnamycin A

Target: Akt

Cat.No: T36844

Chlorhexidine-d8 HCl

Cat.No: T69995

KAAD-Cyclopamine

Cat.No: T35558

Cat.No: T37861

Cat. No.	Product Name	Target	Signaling Pathways
T2973	Astragaloside IV AST-IV,黄芪甲苷IV,AS-IV,黄芪皂苷 IV	MMP; ERK; Estrogen/progestogen Receptor; JNK	Endocrinology/Hormones; MAPK; Proteases/Proteasome
	Astragaloside IV (AS-IV) 是从黄芪中分离得到的一种皂苷，抑制ERK1/2和JNK 激活，在乳腺癌细胞 MDA-MB-231 中，下调(MMP)-2和(MMP)-9的信号通路。
T4S0181	Hinokiflavone 日本扁柏黄酮,扁柏双黄酮	MMP; BCL; E1/E2/E3 Enzyme	Apoptosis; Proteases/Proteasome; Ubiquitination
	Hinokiflavone 是pre-mRNA 剪接活性的新型调节剂，通过抑制剪接体装配来阻止pre-mRNA 底物的剪接，特别是阻止 B complex 的形成。它是SUMO protease 蛋白酶抑制剂，能够抑制前哨蛋白特异性蛋白酶 1 的活性。
TN1879	Lucideric acid A Lucidenic acid A,赤芝酸A	MMP; p38 MAPK; JNK	MAPK; Proteases/Proteasome
	Lucideric acid A (Lucidenic acid A) 是分离自灵芝的天然产物，可抑制 PMA 诱导的MMP-9活性，具有抵抗肝癌细胞侵袭的作用。
T5S0053	Coptisine 黄连碱,Coptisin	Indoleamine 2,3-Dioxygenase (IDO)	Metabolism
	Coptisine (Coptisin) 是一种从黄连中分离到的生物碱，是非竞争性的IDO 抑制剂，Ki=为 5.8 μM，IC50=6.3 μM。
T6S1699	Shogaol [6]-Shogaol,姜烯酚,6-姜烯酚,6-Shogaol	Lipoxygenase; Autophagy	Autophagy; Metabolism
	6-Shogaol (6-Shogaol) 是从生姜中分离的一种天然产物，具有抗癌、抗炎和抗氧化的多种生物活性。

天然产物

Astragaloside IV

Cat.No: T2973

Synonym: AST-IV,黄芪甲苷IV,AS-IV,黄芪皂苷 IV

Target: MMP, ERK, Estrogen/progestogen Receptor, JNK

Cat.No: T4S0181

Synonym: 日本扁柏黄酮,扁柏双黄酮

Target: MMP, BCL, E1/E2/E3 Enzyme

Lucideric acid A

Cat.No: TN1879

Synonym: Lucidenic acid A,赤芝酸A

Target: MMP, p38 MAPK, JNK

Cat.No: T5S0053

Synonym: 黄连碱,Coptisin

Target: Indoleamine 2,3-Dioxygenase (IDO)

Cat.No: T6S1699

Synonym: [6]-Shogaol,姜烯酚,6-姜烯酚,6-Shogaol

Target: Lipoxygenase, Autophagy

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