Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TQ0078 |
CDK-IN-2
CDK inhibitor II |
CDK | Cell Cycle/Checkpoint |
CDK-IN-2 (CDK inhibitor II) 是一种有效且特异性的 CDK9 抑制剂,IC50小于8 nM。 | |||
T14916 |
CDK2-IN-4
|
CDK | Cell Cycle/Checkpoint |
CDK2-IN-4 是选择性的CDK2抑制剂,对 CDK2/cyclin A 的IC50值为 44 nM,选择性高出 CDK1/cyclin B 的 2,000 倍 (IC50=86 μM)。 | |||
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。 | |||
T39752 |
CDK12-IN-2
CDK12 inhibitor 2,CDK12-IN-2 |
CDK | Cell Cycle/Checkpoint |
CDK12-IN-2 (CDK12 inhibitor 2) 是一种有效的选择性 CDK12 抑制剂,对 CDK12、CDK2、CDK7 和 CDK9 的 IC50 为 52 nM、>100 μM、>10 μM 和 16 μM。 CDK12-IN-2可用于研究CDK12的功能。 | |||
T14918 |
CDK9-IN-2
N2'-(反式-4-氨基环己基)-5'-氯-N6-[(3-氟苯基)甲基]-[2,4'-联吡啶]-2',6-二胺 |
Others; CDK | Cell Cycle/Checkpoint; Others |
CDK9-IN-2 是一种特异性CDK9抑制剂。它在 A2058 皮肤细胞系(72 小时)和 H929 多发性骨髓瘤细胞系(72小时)的IC50分别为 7 nM 和 5 nM。 | |||
T7296 |
THZ2
CDK7-IN-1 |
CDK | Cell Cycle/Checkpoint |
THZ2 (CDK7-IN-1) 是 THZ1 的类似物,是一种有效的选择性 CDK7 抑制剂 ,IC50值为 13.9 nM。它有治疗三阴性乳腺癌的潜力。 | |||
T36933 |
Cdk2 Inhibitor II
Cdk2 Inhibitor II,CDK2-IN-3 |
CDK | Cell Cycle/Checkpoint |
Cdk2 Inhibitor II 是一种具有选择性和有效性的 CDK2 抑制剂,50 为 60 nM。 | |||
T40160 |
CDK2-IN-7
CDK2-IN-7 |
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CDK2-IN-7 is a CDK2 inhibitor for treating cancer ( IC 50 < 50 nM). | |||
T39864 |
CDK7-IN-2 hydrochloride hydrate
CDK7-IN-2 hydrochloride hydrate |
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CDK7-IN-2 hydrochloride hydrate (Example 6) is a highly effective and specific inhibitor of the CDK7 enzyme. This compound exhibits significant anti-cancer properties. | |||
T63664 |
CDK/HDAC-IN-2
|
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CDK/HDAC-IN-2 是有效的 HDAC/CDK 双重抑制剂,能够作用于 HDAC1 (IC50: 6.4 nM)、HDAC2 (IC50: 0.25 nM)、HDAC3 (IC50: 45 nM)、HDAC6,8 (IC50>1000 nM)、CDK1 (IC50: 8.63 nM)、CDK2 (IC50: 0.30 nM)、CDK4,6,7 (IC50>1000 nM)。CDK/HDAC-IN-2 能够将细胞周期停滞在 G2/M 期,并诱导细胞凋亡 (apoptosis)。CDK/HDAC-IN-2 具有优异的抗增殖效果,显示出显著的抗肿瘤作用。 | |||
T21314 |
Amsilarotene
TAC-101,TAC 101,TAC101 |
CDK | Cell Cycle/Checkpoint |
Amsilarotene (TAC101) 是口服有活性的合成类视黄醇,对视黄酸受体 α (RAR-α) 具有选择性亲和力,对 RAR-α 和 RAR-β 的 Ki=为 2.4 nM 和 400 nM。它可造成人胃癌、卵巢癌细胞及肝细胞癌的凋亡,可用于研究癌症。 | |||
T78813 |
CDK2/Bcl2-IN-1
|
CDK | Cell Cycle/Checkpoint |
CDK2/Bcl2-IN-1(化合物1)为皂素类CDK-2抑制剂(IC50=117.6 nM),对癌细胞显示显著细胞毒性,并能够抑制Bcl-2,诱导A549肺癌细胞的凋亡。 | |||
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。 | |||
T36689 | KuWal151 | ||
Potent and selective CLK inhibitor (IC50 values are 28, 88 and 510 nM for CLK4, 1 and 2, respectively). Exhibits no significant activity at CLK3, DYRK, CDK or GSK3 at a concentration of 10 μM. Inhibits growth of a range of cancer cell lines in vitro at subnanomolar concentrations. Walter et al (2018) Molecular structures of cdc2-like kinases in complex with a new inhibitor chemotype. PLoS One 13 e0196761 PMID:29723265 | |||
T27033 |
CKD-712
CKD 712,CKD712 |
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CKD-712 is a nuclear factor NF-kappa B inhibitor. CKD-712 suppressed MMP-9, but not MMP-2 and other NF-κB-regulated proteins involved in cancer metastasis such as VEGF. CKD-712 induced cell cycle arrest at G2M phase by suppressing cyclin A, cyclin B and C | |||
T79728 |
EGFR/CDK2-IN-3
|
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
EGFR/CDK2-IN-3(compound 4b)是一种针对EGFR与CDK-2的双重抑制剂,分别具有71.7 nM和113.7 nM的IC50s。该化合物在MCF-7细胞中能诱导凋亡,导致细胞周期在S期停滞,并显示出对癌细胞的明显毒性,其对MCF-7细胞的IC50值为3.16 μM。 | |||
T79727 |
EGFR/CDK2-IN-2
|
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
EGFR/CDK2-IN-2(compound 6a)是一种针对EGFR和CDK-2的双重抑制剂,具有19.6 nM和87.9 nM的IC50s。该化合物能在MCF-7细胞内诱导凋亡,并在S期引发细胞周期停滞。此外,EGFR/CDK2-IN-2展现出IC50为0.39 μM的显著抗癌活性,对MCF-7细胞具有强效的细胞毒性。 | |||
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。 | |||
T40546 |
3-Methylthienyl-carbonyl-JNJ-7706621
|
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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. | |||
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... | |||
T71230 |
VMY-1-103
|
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VMY-1-103 is a potent CDK inhibitor, is also a novel dansylated analog of purvalanol B, was shown to inhibit cell cycle progression and proliferation in prostate and breast cancer cells more effectively than purvalanol B. VMY-1-103 , but not purvalanol B, significantly decreased the proportion of cells in S phase and increased the proportion of cells in G(2)/M. VMY-1-103 increased the sub G(1) fraction of apoptotic cells, induced PARP and caspase-3 cleavage and increased the levels of the Death ... | |||
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。 | |||
T37065 |
6-Chloro-2-fluoropurine
|
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6-Chloro-2-fluoropurine is a heterocyclic building block.1,2It has been used in the synthesis of purine nucleosides that inhibit cyclin-dependent kinases (CDKs)in vitro.16-Chloro-2-fluoropurine has also been used in the synthesis of purine nucleosides that are active against HIV-1 and hepatitis B virus (HBV)in vitro.2 1.Wilson, S.C., Atrash, B., Barlow, C., et al.Design, synthesis and biological evaluation of 6-pyridylmethylaminopurines as CDK inhibitorsBioorg. Med. Chem.19(22)6949-6965(2011) 2.... | |||
T36409 |
Roccellic Acid
|
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Roccellic acid is a lichen secondary metabolite that has been found in R. montagnei and has antibacterial and anticancer activities.1,2 It is active against the bacteria S. gordonii and P. gingivalis (MIC = 46.9 μg/ml for both).1 Roccellic acid (100 μg/ml) inhibits proliferation of MDA-MB-231, MCF-7, and DLD-1 cancer cells by 65.3, 75.8, and 87.9%, respectively.2 |1. Sweidan, A., Chollet-Krugler, M., Sauvager, A., et al. Antibacterial activities of natural lichen compounds against Streptococcus ... |