T78125
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Kinesin
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PVZB1194是一种联苯型激酶Eg5(亦称KIF11)抑制剂,与细胞周期相关,可以通过抑制Eg5的ATP酶活性导致细胞周期阻滞和细胞凋亡,从而显现抗癌潜力。该化合物与α4/α6变抗袋结合,展现ATP竞争性活性。 |
T70622
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Selonsertib, also known as GS-4997, is an orally bioavailable inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with potential anti-inflammatory, antineoplastic and anti-fibrotic activities. GS-4997 targets and binds to the catalytic kinase domain of ASK1 in an ATP-competitive manner, thereby preventing its phosphorylation and activation. GS-4997 prevents the production of inflammatory cytokines, down-regulates the expression of genes involved in fibrosis, suppresses excessive apoptosis and inhibits cellular proliferation. |
T72270
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WYE-687 dihydrochloride 是一种 ATP 竞争性的 mTOR 抑制剂,IC50为 7 nM。WYE-687 dihydrochloride 抑制mTORC1和mTORC2活化。WYE-687 也抑制PI3Kα和PI3Kγ,IC50分别为 81 nM 和 3.11 μM。 |
T74001
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PROTACs
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INY-03-041 trihydrochloride 是一种有效的、高选择性的、基于PROTAC 的泛-AKT 降解剂,由ATP 竞争性AKT 抑制剂Ipatasertib 结合Lenalidomide 组成。INY-03-041 trihydrochloride 可抑制AKT1,AKT2和AKT3,IC50分别为 2.0 nM,6.8 nM 和 3.5 nM。 |
T68267
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RO5068760 , a substituted hydantoin, is a potent, highly selective, non-adenosine triphosphate (ATP)-competitive MEK1/2 inhibitors. RO5068760 shows significant efficacy in a broad spectrum of tumors with aberrant mitogen-activated protein kinase pathway activation. In vitro, RO5068760 demonstrates MEK1 kinase inhibitory activity with an IC50 of 0.025 μM in a cRaf/MEK/ERK cascade assay RO5068760 showed superior efficacy in tumors harboring B-RafV600E mutation. |
T38927
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SR-1277 is a highly potent, selective, and ATP competitive inhibitor of CK1δ/ε, with IC50 values of 49 nM and 260 nM, respectively. Additionally, SR-1277 exhibits inhibitory effects on FLT3, CDK4/cyclin D1, CDK6/cyclin D3, and CDK9/cyclin K, with IC50 values of 305 nM, 1340 nM, 311 nM, and 109 nM, respectively. Taken together, SR-1277 represents a valuable tool for cancer research. |
T71736
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AMG-628, (R)- is the R isomer of AMG-628 --- a potent, ATP-competitive inhibitor of Raf kinases. AMG-628 displays selectivity for Raf kinases and inhibits activation of tyrosine protein kinases such as VEGFR2, Lyn, Flt1 and Fms. AMG-628 has shown to inhibit growth, and induces cell cycle arrest and apoptosis in colon and melanoma cell lines with the B-RafV600E mutation. |
T38462
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PF-04577806 is a potent, selective, and ATP competitive inhibitor of the protein kinase C (PKC). It exhibits significant inhibitory activity against various isoforms of PKC, including PKCα, PKCβI, PKCβII, PKCγ, and PKCθ, with IC50 values of 2.4 nM, 8.1 nM, 6.9 nM, 45.9 nM, and 29.5 nM, respectively. Furthermore, PF-04577806 has the ability to reverse retinal vascular leakage in diabetic rats. |
T68523
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AMG-628, (S)-, is the S isomer of AMG-628 --- a potent, ATP-competitive inhibitor of Raf kinases. AMG-628 displays selectivity for Raf kinases and inhibits activation of tyrosine protein kinases such as VEGFR2, Lyn, Flt1 and Fms. AMG-628 has shown to inhibit growth, and induces cell cycle arrest and apoptosis in colon and melanoma cell lines with the B-RafV600E mutation. |
T70095
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Mps1-IN-1 dihydrochloride 是一种有效的,ATP 竞争性 Mps1激酶抑制剂,IC50为 367 nM。Mps1-IN-1 dihydrochloride 抑制 Mps1有丝分裂激酶活性并沉默纺锤体组装检查点 (SAC) 功能。Mps1-IN-1 dihydrochloride 降低癌细胞和“正常”细胞的活力。 |