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Cat. No. | Product Name | Target | Signaling Pathways |
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T62771 |
AKT-IN-9
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AKT-IN-9 是一种 AKT 的有效抑制剂。其中蛋白激酶 B (PKB,也称为 AKT) 是细胞中 PI3K/AKT/mTOR 信号传导的核心,在细胞生长、存活、分化和代谢中发挥着重要用处。AKT-IN-9 具有潜力进行乳腺癌和前列腺癌的研究。 | |||
T16750 |
Rigosertib
ON-01910,瑞格色替 |
Apoptosis; FLT; PLK; PI3K; Bcr-Abl; CDK; PDGFR; Src | Angiogenesis; Apoptosis; Cell Cycle/Checkpoint; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors |
Rigosertib (ON-01910) 是一种多激酶抑制剂和选择性抗癌剂,通过抑制 PI3K/Akt 途径诱导细胞凋亡,促进组蛋白 H2AX 的磷酸化并诱导细胞周期中的 G2/M 期停滞。它是一种选择性的非 ATP 竞争性PLK1抑制剂,IC50值为 9 nM。 | |||
T6070 |
(E/Z)-Rigosertib sodium
N-[2-甲氧基-5-[[[2-(2,4,6-三甲氧基苯基)乙烯基]磺酰]甲基]苯基]甘氨酸钠盐,(E/Z) ON-01910 sodium |
PLK | Cell Cycle/Checkpoint |
ON-01910 是一种非 ATP 竞争性 PLK1 抑制剂(IC50 为 9 nM,在无细胞试验中)。它对 Plk2 的选择性高出 30 倍,对 Plk3 没有活性。 Rigosertib 抑制 PI3K/Akt 通路并激活氧化应激信号。 Rigosertib 可诱导多种癌细胞凋亡。它是一种合成的苄基苯乙烯基砜类似物,具有潜在的抗肿瘤活性。 | |||
T63155 |
MMP-9-IN-3
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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。 | |||
T64083 |
MMP-9-IN-5
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MMP-9-IN-5 是一种 MMP-9 抑制剂,其 IC50 值为 4.49 nM,能够与 MMP-9 形成氢键。MMP-9-IN-5 也抑制 AKT 活性,其 IC50 值为 1.34 nM。MMP-9-IN-5 表现出细胞毒性,可诱导细胞凋亡 (apoptosis),能够用于研究癌症。 | |||
T63994 | MMP-9-IN-4 | ||
MMP-9-IN-4 是 MMP-9 抑制剂,能够与 MMP-9 形成 H-π 相互作用,IC50 值为 7.46 nM。MMP-9-IN-4 还能够抑制 AKT 活性,其 IC50 值为 8.82 nM。MMP-9-IN-4 能够诱导细胞凋亡 (apoptosis),显示出细胞毒性,能够用于研究癌症。 | |||
T17346 | 9-Decyn-1-ol | Others | Others |
9-Decyn-1-ol is an alkyl/ether-based PROTAC linker suitable for synthesizing PROTACs. It serves as a conjugation agent to combine GDC-0068 and Lenalidomide, resulting in the formation of INY-03-041. INY-03-041 is a potent and highly selective pan-Akt degrader that operates through the PROTAC mechanism. It effectively inhibits Akt1, Akt2, and Akt3 with IC50 values of 2.0 nM, 6.8 nM, and 3.5 nM, respectively[1]. | |||
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。 | |||
T36648 |
Tucatinib hemiethanolate
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Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM. Tucatinib hemiethanolate has nanomolar activity against purified HER2 enzyme and is approximately 500-fold selective for HER2 versus EGFR in cell-based assays. Tucatinib selectively inhibits the receptor tyrosine kinase HER2 relative to EGFR[1].Tucatinib blocks proliferation and the phosphorylation of HER2 and its downstream effector, Akt in HER2 overexpressing cell lines. In the ... | |||
T35897 |
ASK120067
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ASK120067 is a potent and orally active inhibitor of EGFRT790M (IC50:0.3 nM) with selectivity over EGFRWT (IC50:6.0 nM). ASK120067 is a third-generation EGFR-TKI for the research of non-small cell lung cancer (NSCLC)[1]. In the in vitro kinase assay ASK120067 potently inhibits the EGFR L858R/T790M and EGFR T790M resistant mutants with IC50 values of 0.3 nM and 0.5 nM, respectively, as well as the EGFRexon19del sensitizing mutant (IC50= 0.5 nM). The 50 of ASK120067 against wild-type EGFR (EGFRWT... |
Cat. No. | Product Name | Target | Signaling Pathways |
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T3729 |
Ethyl gallate
Nipagallin A,Phyllemblin,gallic acid ethyl ester,没食子酸乙酯 |
MMP; NF-κB; Akt; Antibacterial | Cytoskeletal Signaling; Microbiology/Virology; NF-κB; PI3K/Akt/mTOR signaling; Proteases/Proteasome |
Ethyl gallate (gallic acid ethyl ester) 是一种非类黄酮酚过氧化氢清除剂。 | |||
T4S21320 |
ISOGINKGETIN
异银杏素,4',4'''-Dimethylamentoflavone,异银杏双黄酮 |
MMP; Others | Others; Proteases/Proteasome |
ISOGINKGETIN (4',4'''-Dimethylamentoflavone) 是一种MMP9抑制剂,也是一种Pre-mRNA Splicing 抑制剂。 | |||
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
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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 ... |