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12

抑制剂 & 化合物

4

天然产物

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Cat. No. Product Name Target Signaling Pathways
T63155 MMP-9-IN-3

MMP-9-IN-3 是一种 MMP-9 抑制剂 (IC50: 5.56 nM),可与 MMP-9 形成氢键。MMP-9-IN-3 对 AKT 的活性具有抑制作用 (IC50: 2.11 nM)。MMP-9-IN-3 具有细胞毒性,能够诱导细胞凋亡。MMP-9-IN-3 能够用于研究癌症。
T61271 MMP2-IN-3

MMP Proteases/Proteasome
MMP2-IN-3是一种有效的基质金属蛋白酶(MMP-2)抑制剂( IC50 值:31 μM)。MMP2-IN-3 抑制 MMP-9MMP-8 ,其 IC50 分别为 26.6 和 32 μM。
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.
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。
T72719 Tubulin/MMP-IN-2

Tubulin/MMP-IN-2是一种针对微管蛋白和基质金属蛋白酶的双重抑制剂,能有效抑制微管蛋白聚合并触发细胞凋亡。该化合物对MMP-2、MMP-3MMP-9展现出明显的抑制效果,其IC50值分别为24.95 μM、31.60 μM与22.37 μM。Tubulin/MMP-IN-2主要应用于癌症研究领域。
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。
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.
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。
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...
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

MMP-9-IN-3
Cat.No: T63155
Synonym:
Target:
MMP2-IN-3
Cat.No: T61271
Synonym:
Target: MMP
ARP-100
Cat.No: T14322
Synonym: MMP-2 Inhibitor III
Target: MMP
GM 1489
Cat.No: T37983
Synonym:
Target:
CP-471474
Cat.No: T22685
Synonym: CP 471474
Target: Others
MMP-9-IN-8
Cat.No: T81777
Synonym:
Target:
Tubulin/MMP-IN-2
Cat.No: T72719
Synonym:
Target:
FAK-IN-3
Cat.No: T63545
Synonym:
Target:
MMP13-IN-2
Cat.No: T41079
Synonym: MMP13-IN-2
Target:
(Rac)-Tanomastat
Cat.No: T62090
Synonym:
Target:
Inostamycin A
Cat.No: T36844
Synonym:
Target:
Talabostat
Cat.No: T37861
Synonym:
Target:
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。
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。
TN4046 Excisanin A

MMP; FAK; PARP; GSK-3; NF-κB; Wnt/beta-catenin; Akt; Caspase; PI3K; Prostaglandin Receptor; JNK Angiogenesis; Apoptosis; Chromatin/Epigenetic; Cytoskeletal Signaling; DNA Damage/DNA Repair; GPCR/G Protein; Immunology/Inflammation; MAPK; NF-κB; PI3K/Akt/mTOR signaling; Proteases/Proteasome; Stem Cells; Tyrosine Kinase/Adaptors
ExcisaninA may be a potent inhibitor of AKT signaling pathway in tumor cells, it can inhibit invasion by suppressing MMP-2 and MMP-9 expression, it may be a potential anti-metastatic chemotherapeutic agent for the treatment of breast cancer. Excisanin A shows comparable inhibitory effects on the LPS-induced production of NO and PGE2, and activation of NF-kappaB without affecting cell viability.Excisanin A induces apoptosis in colon cancer cell line SW620 as determined by Annexin V staining, the ...

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
Coptisine
Cat.No: T5S0053
Synonym: 黄连碱,Coptisin
Target: Indoleamine 2,3-Dioxygenase (IDO)
Shogaol
Cat.No: T6S1699
Synonym: [6]-Shogaol,姜烯酚,6-姜烯酚,6-Shogaol
Target: Lipoxygenase, Autophagy
Excisanin A
Cat.No: TN4046
Synonym:
Target: MMP, FAK, PARP, GSK-3, NF-κB, Wnt/beta-catenin, Akt, Caspase, PI3K, Prostaglandin Receptor, JNK
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