Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T79046 |
CDK4-IN-2
|
CDK | Cell Cycle/Checkpoint |
CDK4-IN-2 (A17) 作为CDK4的抑制剂,其对应的Ki和 IC50值均不超过 10 nM。 | |||
T10736 |
CDK4/6-IN-2
|
CDK | Cell Cycle/Checkpoint |
CDK4/6-IN-2 是一种CDK4和CDK6抑制剂,IC50分别为 2.7 和 16 nM。 | |||
T21720 |
GP-82996
Cdk4/6 Inhibitor IV,CINK4 |
CDK | Cell Cycle/Checkpoint |
GP-82996 (CINK4) (CINK4) 是 CDK4/6的药理学抑制剂。GP-82996 对 CDK4/cyclin D1、CDK6/cyclin D1 和 Cdk5/p35 的 IC50s 分别为 1.5、5.6 和 25 μM。GP-82996 诱导肿瘤细胞 U2OS 的凋亡,可用于癌症研究。 | |||
T72951 |
CDK4/6-IN-14
|
||
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。 | |||
T79112 |
CDK4/6-IN-17
|
CDK | Cell Cycle/Checkpoint |
CDK4/6-IN-17(compound 12)为具有口服活性的CDK4/6抑制剂,在BE(2)细胞的IC50为10-100 nM。CDK4/6-IN-17在COLO205异种移植模型中有效抑制肿瘤生长。 | |||
T36967 |
LSN3106729 hydrochloride
|
||
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... | |||
T40546 |
3-Methylthienyl-carbonyl-JNJ-7706621
|
||
3-Methylthienyl-carbonyl-JNJ-7706621 is a highly potent and selective inhibitor of cyclin-dependent kinase (CDK). It exhibits impressive IC50 values of 6.4 nM and 2 nM for CDK1/cyclin B and CDK2/cyclin A, respectively. Additionally, 3-Methylthienyl-carbonyl-JNJ-7706621 demonstrates potent inhibition against GSK-3 (IC50 = 0.041 μM) and moderate potency towards CDK4, VEGF-R2, and FGF-R2 (IC50 = 0.11 μM, 0.13 μM, and 0.22 μM, respectively). Its applications in cancer research are noteworthy. | |||
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。 | |||
T61369 |
p53 Activator 2
|
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p53 Activator 2 (compound 10ah) 插入DNA,导致显著的DNA双链断裂。该化合物通过增加p53、p-p53、CDK4、p21的表达,使细胞周期在G2/M期停滞,诱导细胞凋亡,并显著降低抗凋亡蛋白Bcl-2、Bcl-xL和cyclin B1的水平。此外,p53 Activator 2表现出对MGC-803细胞的抗增殖效果,其IC50为1.73 μM,且在MGC-803异种移植肿瘤模型中展示出有效的抗癌活性。 | |||
T79572 |
MAPK-IN-2
|
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
MAPK-IN-2 (化合物3h)是一种携带抗肿瘤活性的高效MAPK抑制剂。它在多个癌细胞系中有效抑制了细胞增殖,并对MAPK途径表现出强大的抑制效果(EGFRWT IC50=281 nM, c-MET IC50=205 nM, B-RAFWT IC50=112 nM, CDK4/6 IC50=95和184 nM),对突变型EGFR和B-RAF亦展现出高效力(EGFRT790M IC50=69 nM, B-RAFV600E IC50=83 nM)。 | |||
T69200 | CGP74514A | ||
CGP74514A is a CDK1 inhibitor with potential anticancer activity. In U937 cells, CGP74514A - induced apoptosis (5 microM) became apparent within 4 hr and approached 100% by 24 hr. The pan- caspase inhibitor Boc-fmk and the caspase-8 inhibitor lETD-fmk opposed CGP74514A -induced caspase-9 activation and PARP degradation, but not cytochrome c or Smac/DIABLO release. CGP74514A -mediated apoptosis was substantially blocked by ectopic expression of full-length Bel- 2, a loop-deleted mutant Bcl-2, and... | |||
T83911 |
CYY292
|
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CYY292是一种针对PDGFRα、PDGFRβ、FGFR1、-2和-3的抑制剂(IC50分别为5.35、4.6、28、28和78 nM)。该化合物对这些激酶的选择性高于FGFR4(IC50 > 1,000 nM),但也能抑制c-Kit、VEGFR2、VEGFR1和胰岛素样生长因子1受体(IGF-1R;IC50分别为67、33、36和75 nM),以及EGFR、布鲁顿酪氨酸激酶(BTK)、细胞周期依赖性激酶4(Cdk4)/cyclin D3和MET(IC50分别为128、198、214和396 nM)。CYY292抑制MG-63、U2OS、MNNG/HOS和Saos-2骨肉瘤细胞的增殖(IC50分别为0.84、0.76、1.36和0.72 µM)。在0.3和0.5 µM的浓度下,它抑制U87MG和LN-229胶质母细胞瘤细胞的迁移和侵袭。CYY292(30 mg/kg)在U87MG原位小鼠异种移植模型中降低肿瘤体积并增加生存率。 |