Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T10741 | CDK9-IN-1 | CDK | Cell Cycle/Checkpoint |
CDK9-IN-1 is a novel, selective CDK9 inhibitor for the treatment of HIV infection (IC50: 39 nM for CDK9/CycT1). | |||
T118066 |
CDK9 inhibitor HH1
8019-9719 |
CDK | Cell Cycle/Checkpoint |
CDK9 inhibitor HH1 (8019-9719) 是人类 CDK2-cyclin A2复合物的抑制剂,IC50为2 μM。 | |||
T63851 | CDK9/10/GSK3β-IN-1 | ||
CDK9/10/GSK3β-IN-1 是一种激酶抑制剂 (Flavopiridol 类似物),能有效抑制 HsGSK3β、HsCDK9/CyclinT、HsCDK5/p25 和 HsCDK2/CyclinA,其 IC50 值分别为 59 nM、64 nM、1.093 μM 和 1.725 μM。CDK9/10/GSK3β-IN-1 表现出相当或高于 Flavopiridol 的抗癌细胞活性,在体外对多达七种癌细胞系表现出高抗增殖活性。 | |||
T39997 |
PROTAC CDK9 ligand-1
PROTAC CDK9 ligand-1 |
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PROTAC CDK9 ligand-1 is a CDK9 ligand that can be used in the synthesis of PROTACs. | |||
T62746 |
EGFR/HER2/CDK9-IN-1
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EGFR/HER2/CDK9-IN-1 (Compound 4) 是一种有效的 EGFR/HER2/CDK9 抑制剂,他们的 IC50 值分别为 90.17、131.39 和 67.04 nM。EGFR/HER2/CDK9-IN-1 表现出明显的抗肿瘤作用。 | |||
T36744 |
CDK9 Antagonist-1
CDK9 Antagonist-1 |
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CDK9 Antagonist-1 (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]. CDK9|17 μM (IC50, MCF-7 cells) [1]. Bian J , et al. Discovery of Wogonin-based PROTACs against CDK9 and capable of achieving antitumor activity. Bioorg Chem. 2018 Dec;81:373-381. | |||
T82758 | CDK9-Cyclin T1 PPI-IN-1 | CDK | Cell Cycle/Checkpoint |
CDK9-Cyclin T1 PPI-IN-1 (Compound B19) 是CDK9-Cyclin T1蛋白-蛋白相互作用的选择性抑制剂。该化合物能够有效抑制TNBC MDA-MB-231细胞系的细胞增殖(IC50: 0.044 μM),诱导细胞凋亡,同时降低CDK9的转录活性并减少RNA Pol II CTD ser2的磷酸化,有效地抑制了4T1移植瘤模型小鼠中肿瘤的生长。 | |||
T5438 |
PROTAC CDK9 Degrader-1
|
CDK | Cell Cycle/Checkpoint |
PROTAC CDK9 Degrader-1 是一种选择性 CDK9 降解剂,是由Cereblon 配体和CDK 配体相连的PROTAC。 | |||
T70400 |
CDK9/CycT1-IN-93
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CDK9/CycT1-IN-93 is a highly specific, ATP-competitive inhibitor of CDK9/CycT1 with antiviral activity. | |||
T79904 |
PROTAC CDK9/CycT1 Degrader-2
|
CDK | Cell Cycle/Checkpoint |
PROTACCDK9/CycT1 Degrader-2 对CDK9表现出较高的抑制效能,具有一个IC50值为45 nM。 | |||
T74707 | PROTAC FLT3/CDK9 degrader-1 | ||
PROTACFLT3/CDK9 degrader-1 是一种有效的FLT3和CDK9双PROTAC 降解剂。PROTACFLT3/CDK9 degrader-1 诱导细胞凋亡 (Apoptosis) 并有效降解靶蛋白FLT3和 CDK9。PROTACFLT3/CDK9 degrader-1具有研究 FLT3-ITD 突变型 AML 的潜力。 | |||
T9632 |
CDK9-IN-30
|
HIV Protease | Microbiology/Virology; Proteases/Proteasome |
CDK9-IN-30 是 Tat 肽衍生物之一,可抑制 HIV-1 长末端重复激活转录。 | |||
T23840 |
BUR1
BMP upregulator-1,1-{1-苯基-1H-吡唑并[3,4-D]嘧啶-4-基}哌啶,BMP upregulator 1,BUR 1,BUR-1 |
CDK | Cell Cycle/Checkpoint |
BUR1 是一种酿酒酵母细胞周期蛋白依赖性激酶 (CDK),与在转录延伸中起作用的哺乳动物 Cdk9 同源。 | |||
T10096L |
Voruciclib
|
CDK | Cell Cycle/Checkpoint |
Voruciclib 是一种具有口服活性和选择性 CDK 抑制剂,Ki 为 0.626 nM-9.1 nM。它在多种弥漫性大 B 细胞淋巴瘤模型中抑制 MCL-1 的表达。它有效阻断 MCL-1 的转录调节子 CDK9。 | |||
T79631 |
CDK9-IN-26
|
CDK | Cell Cycle/Checkpoint |
CDK9-IN-26 (化合物1d) 为CDK9抑制剂,具有0.18 µM的IC50值。 | |||
T10743 |
CDK9-IN-11
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CDK | Cell Cycle/Checkpoint |
CDK9-IN-11 是一种有效的CDK9抑制剂,可作为 PROTAC CDK9 Degrader-1 的配体。 | |||
T82757 |
CDK9-IN-29
|
CDK | Cell Cycle/Checkpoint |
CDK9-IN-29,一有效CDK9抑制剂(IC50=3.20 nM),激酶选择性佳,能抑制细胞增殖及诱导细胞凋亡。 | |||
T79367 |
CDK9-IN-27
|
CDK | Cell Cycle/Checkpoint |
CDK9-IN-27(Compound 6a)是一款针对CDK9的抑制剂,其IC50s为0.424 μM。该化合物可诱导细胞凋亡(apoptosis)及S期细胞周期停滞,并对HepG2、HCT-116及MCF-7细胞系展现出细胞毒性,其IC50s介于10.31至40.34 μM之间。CDK9-IN-27主要应用于癌症相关研究领域。 | |||
T14915 |
CDK12-IN-E9
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CDK | Cell Cycle/Checkpoint |
CDK12-IN-E9 is a potent and selective covalent CDK12 inhibitor and non-covalent CDK9 inhibitor while avoiding ABC transporter-mediated efflux. It has a weak binding ability to CDK7/CyclinH complex (IC50> 1 μM). | |||
T79704 |
CDK9-IN-28
|
CDK | Cell Cycle/Checkpoint |
CDK9-IN-28(化合物10)是一种高效CDK9抑制剂,可用作PROTAC合成中的靶蛋白配体,并在实体瘤中展现出显著的抗增殖能力。 | |||
T79037 |
CDK9-IN-23
|
CDK | Cell Cycle/Checkpoint |
CDK9-IN-23 (Example 4)作为一种CDK9抑制剂,其半抑制浓度(IC50)小于20纳摩尔(nM)。 | |||
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]. | |||
T78928 |
PROTAC CDK9 degrader-8
|
PROTACs | PROTAC |
PROTACCDK9degrader-8 (化合物21) 是具有0.01 μM IC50值的高效PROTAC CDK9降解剂,适用于癌症研究领域。 | |||
T79354 |
CDK9-IN-24
|
CDK | Cell Cycle/Checkpoint |
CDK9-IN-24(化合物21a)为高选择性CDK9抑制剂,显著抑止肿瘤生长。该化合物有效抑制细胞增殖,通过降调Mcl-1及c-Myc诱导细胞凋亡,适用于急性髓系白血病研究。 | |||
T10739 | CDK8/19-IN-1 | CDK | Cell Cycle/Checkpoint |
CDK8/19-IN-1 is a selective and oral bioavailable CDK8/19 dual inhibitor (IC50s: 0.46 nM, 0.99 nM, and 270 nM for CDK8, CDK19, and CDK9). | |||
T36743 |
CDK7/9 tide
|
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CDK7/9 tide is peptide substrate for CDK7 or CDK9[1]. [1]. Robert T, et, al. Development of a CDK10/CycM in vitro Kinase Screening Assay and Identification of First Small-Molecule Inhibitors. Front Chem. 2020 Feb 27; 8:147. | |||
T71287 |
CDKI-83
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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... | |||
T40353 |
CDK7/9-IN-1
CDK7/9-IN-1 |
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CDK7/9-IN-1 is a specific inhibitor of cyclin-dependent kinases 7/9 (CDK7/9). It specifically targets CDK7, while also displaying inhibitory activity against CDK9. CDK7/9-IN-1 demonstrates excellent inhibitory potency against CDK7, with IC50 values of 0.0656 μM and 0.00574 μM without pre-incubation and after 3 hours pre-incubation, respectively. Furthermore, CDK7/9-IN-1 inhibits CDK9 with an IC50 of 2.14 μM after 3 hours pre-incubation. Its application in cancer research makes it valuable for su... | |||
T79630 |
CDK9-IN-25
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Virus Protease | Microbiology/Virology |
CDK9-IN-25(化合物4a)为咪唑并吡嗪类 CDK9 抑制剂,其 IC50 值为0.24 μM。该化合物对 COVID-19 主要蛋白酶展现出良好的亲和力,并对人类冠状病毒 229E 表现出抗病毒活性,其 IC50 值达到 63.28 μM。 | |||
T40047 |
CDK6/9-IN-1
CDK6/9-IN-1 |
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CDK6/9-IN-1 (compound 66) is a potent dual inhibitor of CDK 6 and CDK 9 that can be administered orally. It exhibits inhibitory activity with IC 50 values of 40.5 nM and 39.5 nM against CDK6 and CDK9, respectively. | |||
T60477 | Haspin-IN-1 | ||
Haspin-IN-1 (compound 2a) 是一种haspin(单倍体生殖细胞特异性核蛋白激酶)抑制剂,IC50值为 119 nM。Haspin-IN-1 还抑制CLK1、DYRK1A 和 CDK9,IC50分别为 221 nM 、916.3 nM 和406.8 nM。Haspin-IN-1具有开发新型抗癌药物的潜力[1]。 | |||
T78837 |
CP-07
|
CDK | Cell Cycle/Checkpoint |
CP-07为高效的PROTAC CDK9选择性降解剂(DC50:43 nM),能显著抑制22RV1细胞增殖(IC50:62 nM)及集落形成,其作用机制为通过下调Mcl-1与c-Myc。此外,CP-07有效抑制22RV1异种移植肿瘤的生长,有望成为研究前列腺癌的重要化合物。 | |||
T79014 |
QR-6401
|
CDK | Cell Cycle/Checkpoint |
QR-6401是一种口服、选择性的大环CDK2抑制剂,其IC50分别针对CDK2/E1、CDK9/T1、CDK1/A2、CDK6/D3和CDK4/D1为0.37、10、22、34及45nM。在OVCAR3卵巢癌异种移植模型中,QR-6401表现出显著的抗肿瘤活性,显示出其作为癌症研究工具的潜能。 | |||
T78906 | CDK/HDAC-IN-3 | HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
CDK/HDAC-IN-3 是一种口服活性的 HDAC/CDK 双重抑制剂,对 CDK9、CDK12、CDK13 及 HDAC1、HDAC2、HDAC3 表现出有效且选择性的抑制,IC50 值分别为 98.32 nM、98.85 nM、100 nM、62.12 nM、93.28 nM 和 82.87 nM。该化合物主要用于急性髓性白血病 (AML) 的相关研究。 | |||
T70988 |
Ibulocydine
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Ibulocydine is a potent CDK inhibitor. Ibulocydine has high activity against Cdk7/cyclin H/Mat1 and Cdk9/cyclin T. Ibulocydine inhibited the growth of HCC cells more effectively than other Cdk inhibitors, including olomoucine and roscovitine, whereas ibulocydine as well as the other Cdk inhibitors and BMK-Y101 minimally influenced the growth of normal hepatocyte cells. Ibulocydine induced apoptosis in HCC cells, most likely by inhibiting Cdk7 and Cdk9. In vitro treatment of HCC cells with ibuloc... | |||
T79287 |
SB-1295
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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。 |