24
5
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。 | |||
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... | |||
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。 | |||
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,... |
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。 |