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抑制剂 & 化合物

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Cat. No.	Product Name	Target	Signaling Pathways
T63933	CDK1-IN-3
	CDK1-IN-3 (8g) 是一种选择性的 CDK1 抑制剂，能够作用于 CDK1 (IC50: 36.8 nM)，CDK2 (IC50: 305.17 nM) 和 CDK5 (IC50: 369.37 nM)。CDK1-IN-3 能够影响细胞周期，进而抑制癌细胞的生长，能够用于研究癌症。
T60583	CDK1/2/4-IN-1
	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。
T14136	AG-024322	CDK	Cell Cycle/Checkpoint
	AG-024322 is a potent ATP-competitive inhibitor of pan-CDK against cell cycle kinases CDK1, CDK2, and CDK4(Ki values in the 1-3 nM range)
T10737	CDK4/6-IN-3	CDK	Cell Cycle/Checkpoint
	CDK4/6-IN-3 is a brain-penetrant CDK4/CDK6 inhibitor (Kis: <0.3 nM and 2.2 nM) used for the treatment of glioblastoma. It inhibits CDK1 with a Ki of 110 nM.
T36349	CGP 74514 dihydrochloride
	Potent cdk1 inhibitor (IC50 = 25 nM). Reduces Akt phosphorylation and increases mitochondrial damage in leukemia cells in vitro in combination with LY 294002. Yu et al (2013) The lethal effects of pharmacological cyclin-dependent kinase inhibitors in human leukemia cells proceed through a phosphatidylinositol 3-kinase/Akt-dependent process. Cancer Res. 63 1822 PMID:12702569 \|Furet et al (2000) Structure-based design of potent CDK1 inhibitors derived from olomoucine. J.Comput.Aided Mol.Des. 14 40...
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.
T71287	CDKI-83
	CDKI-83 is a potent CDK9 inhibitor. The compound shows effective anti-proliferative activity in human tumour cell lines with GI50 <1 μM, and is capable of inducing apoptosis in A2780 human ovarian cancer cells as determined by the activated caspase-3, Annexin V/PI double staining and accumulated cells at the sub-G1 phase of cellcycle. The research results suggest that combined inhibition of CDK9 and CDK1 may result in the effective induction of apoptosis and CDKI-83 has the potential to be devel...
T83936	LL-K9-3
	LL-K9-3是一种基于选择性疏水标记技术（HyT）的CDK9-cyclin T1复合物降解剂（DC50值分别为cyclin T1的589 nM和CDK9的662 nM）。它由CDK9抑制剂SNS 032和一个糖基连接器连接到疏水标记组成。LL-K9-3不会降解其他CDKs（CDK1、2、4、5、6和7）。在22RV1细胞中，LL-K9-3通过诱导CDK9和cyclin T1的选择性和同步降解，降低雄激素受体（AR）和cMyc的表达。

化合物

CGP 74514 dihydrochloride

Cat.No: T36349

Synonym:

Target:

3-Methylthienyl-carbonyl-JNJ-7706621

Cat. No.	Product Name	Target	Signaling Pathways
T3S0737	Flavokawain A 2'-羟基-4,4',6'-三甲氧基查耳酮,Flavokavain A	Apoptosis; p38 MAPK	Apoptosis; MAPK
	Flavokawain A (Flavokavain A) 是 kava 提取物中的查耳酮，是一种抗癌试剂，具有抗肿瘤活性。它通过 Bax 蛋白依赖和线粒体依赖的凋亡途径诱导细胞凋亡，有潜力用于膀胱癌的相关研究。

天然产物

Flavokawain A

Cat.No: T3S0737

Synonym: 2'-羟基-4,4',6'-三甲氧基查耳酮,Flavokavain A

Target: Apoptosis, p38 MAPK

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