Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
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。 | |||
T63357 |
EGFR/HER2/CDK9-IN-2
|
||
EGFR/HER2/CDK9-IN-2 是 EGFR/HER2/CDK9 的有效抑制剂,他们的 IC50s 值分别为 145.35、129.07 和 117.13 nM,表现出明显的抗肿瘤作用。 | |||
T10742 |
CDK9-IN-10
|
CDK | Cell Cycle/Checkpoint |
CDK9-IN-10 是一种有效的 CDK9 抑制剂。CDK9-IN-10 是 PROTAC CDK9 degrader-2 的配体。 | |||
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。 | |||
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。 | |||
T17728 |
PROTAC CDK9 degrader-2
|
Others | Others |
PROTAC CDK9 degrader-2 (compounds 11c) is a potent and selective CDK9 degrader based on PROTAC, with an IC50 of 17 μM in MCF-7 cell lines. Natural product Wogonin binds ubiquitin E3 ligase cereblon (CRBN) via a linker to form PROTAC[1]. | |||
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。 | |||
T40288 |
CDK12-IN-4
CDK12-IN-4 |
||
CDK12-IN-4, a pyrazolotriazine compound, exhibits potent inhibition of CDK12 by achieving an IC50 value of 0.641 μM, utilizing high ATP levels (2 mM). Notably, CDK12-IN-4 does not impact CDK2/Cyclin E (IC50 > 20 μM) or CDK9/Cyclin T1 (IC50 > 20 μM) under the influence of high ATP (2 mM) levels (WO2021116178A1). | |||
T40290 |
CDK12-IN-5
CDK12-IN-5 |
||
CDK12-IN-5 is a pyrazolotriazine compound that effectively inhibits CDK12, with an IC50 value of 23.9 nM at a high ATP concentration of 2 mM. However, CDK12-IN-5 does not exhibit inhibitory effects on CDK2/Cyclin E (IC50 = 173 μM) and CDK9/Cyclin T1 (IC50 = 127 μM) at the same high ATP concentration of 2 mM, as stated in WO2021116178A1. | |||
T40289 |
CDK12-IN-6
CDK12-IN-6 |
||
CDK12-IN-6, a pyrazolotriazine compound, is a powerful inhibitor of CDK12. Its inhibitory activity is significant with an IC50 value of 1.19 μM when tested at high ATP concentration (2 mM). Notably, CDK12-IN-6 does not exhibit any inhibitory effect on CDK2/Cyclin E (IC50 >20 μM) and CDK9/Cyclin T1 (IC50 >20 μM) when tested under the same high ATP conditions (2 mM) (WO2021116178A1). | |||
T79287 |
SB-1295
|
Reactive Oxygen Species | Immunology/Inflammation; Metabolism; NF-κB |
SB-1295是一种口服活性CDK9/T1抑制剂,其IC50为0.17 μM。在HCT 116和MIA PaCa-2细胞中表现出抗增殖效应,并能诱导MIA PaCa-2细胞死亡,机制包括ROS生成增加、线粒体膜电位下降及细胞凋亡启动。SB-1295具备作为癌症研究工具的潜力。 |