Cat. No. | Product Name | Target | Signaling Pathways |
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T71167 |
Zatosetron
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Zatosetron is a serotonin antagonists. | |||
T72522 |
Aurora kinase-IN-1
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Aurora kinase-IN-1 是aurora kinase 的有效抑制剂。Aurora kinase-IN-1 上调 G1 细胞周期抑制蛋白 (包括 p21 和 p27) 以及 G1 进行性细胞周期蛋白 D1 的表达,并下调 G1-to-S 进行性细胞周期蛋白,导致细胞周期停滞在 G1/S 边界。Aurora 激酶-IN-1 还诱导细胞凋亡 (apoptosis)。Aurora 激酶-IN-1 是化疗药物的先导化合物。 | |||
T62945 |
Aurora A/PKC-IN-1
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Aurora A/PKC-IN-1 (Compound 2e) 是一种有效的 Aurora A (AurA) 和 PKC (α, β1, β2, θ) 双重抑制剂,作用于 AurA (IC50: 6.9 nM) 和 PKCα (IC50: 16.9 nM)。Aurora A/PKC-IN-1 对乳腺癌细胞表现出抗增殖和抗转移作用。 | |||
T60783 | Aurora/LIM kinase-IN-1 | ||
Aurora/LIM kinase-IN-1 (Compound F114) 是aurora 和lim 激酶的有效双重抑制剂。Aurora/LIM kinase-IN-1 可抑制胶质母细胞瘤的增殖和侵袭,可能用于胶质母细胞瘤和其他癌症相关的药物研发。Aurora 和 LIM 激酶是分别参与肿瘤细胞分裂和细胞运动的激酶。 | |||
T64338 |
AKI603
AKI 603,AKI-603 |
Aurora Kinase | Cell Cycle/Checkpoint; Chromatin/Epigenetic |
AKI603 是一种极光激酶 A 抑制剂,IC50值为 12.3 nM。它对白血病细胞具有很强的抗增殖活性,可用于克服白血病中 BCR-ABL-T315I 耐药性突变。 | |||
T71169 |
XMD-12
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XMD-12, also known as DUN57447, Aurora inhibitor (compound 1) or Aurora-IN-1, is an Auroro inhibitor, which targets Aurora A/B/C. (5.6/18.4/24.6 nM). | |||
T71112 | SAR156497 | ||
SAR156497 is an exquisitely selective Aurora A, B, and C inhibitor with in vitro and in vivo efficacy with IC50 = 0.5 nM (Aurora A); 1 nM (Aurora B / incenp); 3 nM (Aurora C / incenp) respectively SAR156497 combines high in vitro potency with satisfactory metabolic stability and limited CYP 3A4 and PDE3 inhibition. In vitro, SAR156497 displayed high antiproliferative activity on a large panel of tumor cell lines without correlation with any particular genetic signature or Aurora kinases expressi... | |||
T78753 | Aurora Kinases-IN-4 | Aurora Kinase | Cell Cycle/Checkpoint; Chromatin/Epigenetic |
Aurora Kinases-IN-4(Compound 11c)是共价ATP竞争型aurora kinaseA抑制剂,具有IC50为1.7 nM。该化合物对SJSA-1、MDA-MB-231、A549和HeLa细胞系的增殖抑制效果显著,其IC50分别为4.27、1.54、3.08和6.99 μM。Aurora Kinases-IN-4适用于三阴性乳腺癌(TNBC)的相关研究。 | |||
T74174 |
JB170
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PROTACs | PROTAC |
JB170 是一种强效且高度特异性的PROTAC 介导的AURORA-A 降解剂 (DC50=28 nM),通过将 Alisertib 连接至Cereblon 配体 Thalidomide 而形成。JB170 优先结合 AURORA-A (EC50=193 nM) 而不是 AURORA-B (EC50=1.4µM)。JB170 介导的 S 期阻滞是由 AURORA-A 耗竭引起的。JB170 对 AURORA-A 激酶的非催化功能具有很好的抑制能力。 | |||
T61527 |
GSK2646264
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GSK2646264 (Compound 44) is a highly effective and specific inhibitor of spleen tyrosine kinase (SYK) with a pIC50 of 7.1. In addition to targeting SYK, GSK2646264 also inhibits several other kinases, including LCK, LRRK2, GSK3β, JAK2, VEGFR2, Aurora B, and Aurora A, with pIC50 values of 5.4, 5.4, 5.3, 5, 4.5, <4.6 and <4.3, respectively. Notably, GSK2646264 demonstrates skin penetrability, reaching both the epidermis and dermis [1]. | |||
T36932 |
CD532 hydrochloride
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CD532 hydrochloride is a potent inhibitor of Aurora A kinase, having an IC50 of 45 nM. It not only blocks the activity of Aurora A kinase but also facilitates the degradation of the protein MYCN. Furthermore, CD532 hydrochloride interacts directly with AURKA, inducing a significant conformational change. Its utility in cancer research has been demonstrated [1][2]. | |||
T36199 |
AZD 1152 (hydrochloride)
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AZD 1152 is an orally bioavailable prodrug of AZD 1152-HQPA, a selective inhibitor of Aurora kinase B (IC50= 0.36 nM).1AZD 1152 is converted to AZD 1152-HQPA in plasma. Inhibition of Aurora B results in disruption of spindle checkpoint functions and chromosome alignment, resulting in inhibition of cytokinesis followed by apoptosis.2,3AZD 1152 inhibits tumor xenograft growthin vivo.4,5 1.Mortlock, A.A., Foote, K.M., Heron, N.M., et al.Discovery, synthesis, and in vivo activity of a new class of p... | |||
T79913 |
GRK2 Inhibitor 2
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GRK2 Inhibitor 2 (Compound 8h) 作为一种高效的抑制剂,对GRK2有显著的抑制活性(IC50: 19 nM),同样对Aurora-A也表现出抑制作用(IC50: 137 nM)。该化合物能增强GRK2过表达的HEK293细胞中β-AR介导的cAMP积累。此外,GRK2 Inhibitor 2适用于充血性心力衰竭(HF)的相关研究。 |