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Cat. No. | Product Name | Target | Signaling Pathways |
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T2082 |
CDK4-IN-1
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CDK | Cell Cycle/Checkpoint |
CDK4-IN-1 是一种新型的特异性 CDK4/Cyclin D1 抑制剂,IC50 为 10 nM;分别是 CDK1/Cyclin B (IC50>15 uM) 和 CDK2/Cyclin A (IC50=5.265 uM) 的 1500 倍和 500 倍。 | |||
T61583 | CDK/HDAC-IN-1 | ||
CDK/HDAC-IN-1 exhibits potent inhibitory activity towards CDK2/4/6 and HDAC6, with IC50 values of 60.9 ± 2.9 nM, 276 ± 22.3 nM, 27.2 ± 4.2 nM, and 128.6 ± 0.4 nM, respectively. | |||
T79729 |
EGFR/CDK2-IN-4
|
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
EGFR/CDK2-IN-4(化合物4c)是一种EGFR与CDK-2的双重抑制剂,其IC50值分别为89.6 nM和165.4 nM。该化合物在MCF-7细胞中能诱导(apoptosis)凋亡,并导致细胞周期在S期停滞。EGFR/CDK2-IN-4显示出显著的抗癌细胞毒性,对MCF-7细胞的IC50为2.74 μM。 | |||
T60583 |
CDK1/2/4-IN-1
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CDK1/2/4-IN-1 (compound 3a) 是 CDK 的有效抑制剂, 其对于 CDK1、CDK2 和 CDK4 的 IC50值分别为 1.47、0.78 和 0.87 μM。CDK1/2/4-IN-1 可用于癌症研究。CDK1/2/4-IN-1 可将细胞周期阻滞在 G2/M 期并诱导细胞凋亡。CDK1/2/4-IN-1 提高 Bax、caspase-3和 P53 的水平并降低 Bcl-2 水平。 | |||
T36967 |
LSN3106729 hydrochloride
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LSN3106729 hydrochloride, the metabolite of Abemaciclib , is a CDK inhibitor with antitumor activity. LSN3106729 hydrochloride and a CRBN ligand have been used to design PROTAC CDK4/6 degrader[1]. [1]. Edward S. Kim, et al. Abemaciclib in Combination with Single-Agent Options in Patients with Stage IV Non-Small Cell Lung Cancer: A Phase Ib Study. [2]. Nathanael Gray, et al. Degradation of cyclin-dependent kinase 4/6 (cdk4/6) by conjugation of cdk4/6 inhibitors with e3 ligase ligand and methods o... | |||
T72951 |
CDK4/6-IN-14
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CDK4/6-IN-14 是一种有效且高度选择性的 CDK4和 CDK6(CDK) 抑制剂,IC50分别为 10 nM 和 16 nM。CDK4/6-IN-14 的选择性是 CDK1、2、7 和 9 的 60 多倍,并且在其他 205 种激酶中表现出高选择性。 |
Cat. No. | Product Name | Target | Signaling Pathways |
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T38441 |
Manzamine A hydrochloride
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Manzamine A hydrochloride is an orally active beta-carboline alkaloid that exhibits specific inhibitory effects on GSK-3β (IC50 = 10.2 μM) and CDK-5 (IC50 = 1.5 μM). Additionally, it targets vacuolar ATPases, leading to the inhibition of autophagy in pancreatic cancer cells. Manzamine A hydrochloride possesses antimalarial and anticancer properties, and also demonstrates potent activity against HSV-1[4]. |