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Cat. No. | Product Name | Target | Signaling Pathways |
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T5007 |
Benproperine phosphate
磷酸苯丙哌林,Blascorid,Pirexyl phosphate |
Others; Microtubule Associated | Cytoskeletal Signaling; Others |
Benproperine phosphate (Pirexyl phosphate) 是一种具有口服活性的,肌动蛋白相关蛋白 2/3 复合亚基 2 (ARPC2) 抑制剂。它通过削弱 Arp2/3 功能来减弱肌动蛋白的聚合反应速率。它可抑制癌细胞迁移和肿瘤转移,有用于治疗止咳的潜力。 | |||
T21314 |
Amsilarotene
TAC-101,TAC 101,TAC101 |
CDK | Cell Cycle/Checkpoint |
Amsilarotene (TAC101) 是口服有活性的合成类视黄醇,对视黄酸受体 α (RAR-α) 具有选择性亲和力,对 RAR-α 和 RAR-β 的 Ki=为 2.4 nM 和 400 nM。它可造成人胃癌、卵巢癌细胞及肝细胞癌的凋亡,可用于研究癌症。 | |||
T2613 |
Almorexant
阿莫伦特,ACT 078573 |
OX Receptor | GPCR/G Protein; Neuroscience |
Almorexant (ACT 078573) 是一种有效的竞争性食欲素 1 受体 (OX1)/食欲素 2 受体 (OX2) 双重拮抗剂,OX1 和 OX2 的 Ki 值分别为 1.3 和 0.17 nM。 | |||
T6155 |
Almorexant hydrochloride
ACT-078573 hydrochloride,Almorexant HCl |
OX Receptor | GPCR/G Protein; Neuroscience |
Almorexant hydrochloride (ACT-078573 hydrochloride) 是一种有效的竞争性食欲素 1 受体(OX1)/食欲素 2 受体 (OX2) 双重拮抗剂,OX1 和 OX2 的 Ki 值分别为 1.3 和 0.17 nM。 | |||
T78843 |
MET/PDGFRA-IN-1
|
c-Met/HGFR | Tyrosine Kinase/Adaptors |
MET/PDGFRA-IN-1 (compound 8c) 作为MET和PDGFRA蛋白的抑制剂,以36 μM对MET的IC50值显示活性。该化合物能够抑制MET磷酸化并触发细胞凋亡(apoptosis)。此外,MET/PDGFRA-IN-1有效抑止了多种MET阳性细胞系的增殖,包括AsPc-1、EBC-1、MKN-45、Mia-Paca-2、HT-29和K562,其IC50s分别为15.3、19.0、22.0、25.6、21.0、31.5 μM。 | |||
T78844 |
MET/PDGFRA-IN-2
|
c-Met/HGFR | Tyrosine Kinase/Adaptors |
MET/PDGFRA-IN-2(化合物8h)是一种针对MET和PDGFRA蛋白的抑制剂,具有诱导细胞凋亡(apoptosis)的功能。该化合物能有效抑制多种MET表达细胞系的增殖,包括AsPc-1、EBC-1、MKN-45、Mia-Paca-2、HT-29和K562细胞,其IC50分别为9.7、6.1、12.0、11.5、8.6和34.4μM。 | |||
T78784 |
RIPK3-IN-3
|
||
RIPK3-IN-3(化合物20)是一种针对受体相互作用蛋白激酶RIPK3的选择性抑制剂,其IC50为10 nM。它通过抑制p-MLKL的寡聚化作用来阻止RIPK3介导的MLKL磷酸化以及随后的坏死性凋亡。此外,RIPK3-IN-3还能降低CXCL5的分泌,并抑制AsPC-1细胞的迁移和侵袭。 | |||
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... | |||
T41070 |
LP-184
|
||
LP-184 (Compound 6), referred to as an acylfulvene analog, demonstrates the ability to inhibit tumor growth with noteworthy anti-cancer efficacy observed across multiple cell lines, including ovarian, colon, prostate, and pancreatic. |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T36179 |
Aspulvinone O
|
||
Aspulvinone O is a fungal metabolite that has been found in P. variotti and has antioxidant and anticancer activities.1,2 It scavenges 2,2-diphenyl-1-picrylhydrazyl radicals in a cell-free assay (IC50 = 11.6 μM).1 Aspulvinone O inhibits aspartate transaminase 1 (GOT1; Kd = 3.32 μM) and is cytotoxic to PANC-1, AsPC-1, and SW1990 pancreatic cancer cells (IC50s = 20.54-26.8 μM).2 It reduces the oxygen consumption rate (OCR) and induces apoptosis in SW1990 cells. Aspulvinone O (2.5 and 5 mg/kg) redu... | |||
T36954 |
Nemorosone
|
||
Nemorosone is a polycyclic polyprenylated acylphloroglucinol (PPAP) originally isolated from C. rosea that has antiproliferative properties.1 Nemorosone inhibits growth of NB69, Kelly, SK-N-AS, and LAN-1 neuroblastoma cells (IC50s = 3.1-6.3 μM), including several drug-resistant clones, but not MRC-5 human embryonic fibroblasts (IC50 = >40 μM).2 It increases DNA fragmentation in LAN-1 cells in a dose-dependent manner, and decreases N-Myc protein levels and phosphorylation of ERK1/2 by MEK1/2. Nem... |