341
11
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。 | |||
T60869 | CDK-IN-10 | CDK | Cell Cycle/Checkpoint |
CDK-IN-10 是一种细胞周期蛋白依赖性激酶 (CDK) 抑制剂,具有潜在的抗癌活性,可用于研究癌症。 | |||
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)。 | |||
T36741 | CDK-IN-6 | ||
CDK-IN-6, a pyrazolo[1,5-a]pyrimidine compound, exhibits potent anticancer activities as a CDK inhibitor[1]. | |||
T39957 |
CDK4/6-IN-6
|
CDK | Cell Cycle/Checkpoint |
CDK4/6-IN-6 是CDK4/CDK6的有效抑制剂,结合CDK4/Cyclin D1 和 CDK6/Cyclin D3 的 Ki 为 0.6 nM 和 13.9 nM。 | |||
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。 | |||
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。 | |||
T10740 |
CDK8-IN-1
|
CDK | Cell Cycle/Checkpoint |
CDK8-IN-1 是一个有效的、CDK8 的选择性抑制剂,其 IC50 值为 3 nM。 | |||
T14914 |
Cdk1/2 Inhibitor III
|
CDK | Cell Cycle/Checkpoint |
Cdk1/2 Inhibitor III 是一种具有选择性的 Cdk1/2抑制剂,对 CDK1/cyclin B 的 IC50值为2.1μM。 | |||
T10734 |
CDK ligand for PROTAC
|
Others | Others |
CDK ligand for PROTAC is a CDK inhibitor with antitumor activity. It has been used to design PROTAC CDK4/6 degraders. | |||
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。 | |||
T10745 |
CDK9-IN-7
|
CDK | Cell Cycle/Checkpoint |
CDK9-IN-7 (compound 21e) 是一种高效选择性的,具有口服活性的 CDK9/cyclin T 抑制剂 (IC50=11 nM),与抑制其他 CDK 相比更有效 (CDK4/cyclinD=148 nM; CDK6/cyclinD=145 nM)。CDK9-IN-7 具有抗癌活性并没有明显的毒性。CDK9-IN-7 诱导非小细胞肺癌 (NSCLC) 细胞凋亡,在 G2 期阻滞细胞周期,并具有抑制非小细胞肺癌干细胞特性。 | |||
T37207L |
Cdk5 Substrate acetate
|
CDK | Cell Cycle/Checkpoint |
Cdk5 Substrate acetate 是一种丝氨酸/苏氨酸激酶,主要在神经元组织中具有活性。与 p25 或 p35 一起,Cdk5 磷酸化一系列蛋白质,包括组蛋白 H1 和 tau。 它是一种合成肽 (PKTPKKAKKL),对应于组蛋白 H1 的序列。它被 Cdk5 磷酸化,Km 值为 5 µM。 | |||
T10735 |
CDK4/6/1 Inhibitor
Crozbaciclib |
CDK | Cell Cycle/Checkpoint |
CDK4/6/1 Inhibitor (Crozbaciclib) 是一种 CDK4/6 抑制剂 (IC50s: 3 and 1 nM). CDK4/6抑制剂是一类用于治疗一些类型的激素受体阳性、her2阴性乳腺癌的化合物,可阻断了乳腺癌细胞分裂和繁殖的过程。 | |||
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。 | |||
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。 | |||
T10734L |
CDK ligand for PROTAC hydrochloride
|
Others | Others |
CDK ligand for PROTAC hydrochloride is a CDK inhibitor with antitumor activity. It has been used to design PROTAC CDK4/6 degraders. | |||
TP1875L |
CDK2 acetate(255064-79-0 free base)
|
Others | Others |
CDK2 acetate(255064-79-0 free base) 是真核生物 S/T 蛋白激酶家族的成员,其功能是催化 ATP γ-磷酸磷酸基转移到蛋白质底物中的丝氨酸或苏氨酸羟基(表示为 S0/T0)。 | |||
T75127 | CDK-IN-12 | ||
CDK-IN-12 (Example 20) 是一种CDK 抑制剂。CDK-IN-12 抑制 CDK4/6 的IC50值小于 20 nM。 | |||
T62235 | CDK-IN-9 | ||
CDK-IN-9 (compound 24) 是一种 CDK 的有效抑制剂。CDK-IN-9 也是一种能够诱导 CDK12 和 DDB1 相互作用的分子胶, 能够作用于 CDK2/E (IC50: 4 nM) 。CDK-IN-9 能够导致细胞周期蛋白 K (cyclin K) 的多泛素化及其随后的降解。CDK-IN-9 可以利用去磷酸化视网膜母细胞瘤蛋白和RNA 聚合酶 II,进而诱导细胞凋亡 (apoptosis)。 | |||
T61583 | CDK/HDAC-IN-1 | ||
CDK/HDAC-IN-1 exhibits potent inhibitory activity towards CDK2/4/6 and HDAC6, with IC50 values of 60.9 ± 2.9 nM, 276 ± 22.3 nM, 27.2 ± 4.2 nM, and 128.6 ± 0.4 nM, respectively. | |||
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。 | |||
T63664 |
CDK/HDAC-IN-2
|
||
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。 | |||
T60025 |
Eciruciclib
|
CDK | Cell Cycle/Checkpoint |
Eciruciclib 是一种具有抗肿瘤特性的 CDK 抑制剂。 | |||
T37207 |
Cdk5 Substrate
Cdk5 Substrate |
||
Cyclin-dependent kinase 5 (Cdk5) is a serine/threonine kinase that is predominantly active in neuronal tissues. With p25 or p35, Cdk5 phosphorylates a range of proteins, including histone H1 and tau. Cdk5 substrate is a synthetic peptide (PKTPKKAKKL) corresponding to a sequence of histone H1. It is phosphorylated by Cdk5 with a Km value of 5 μM. | |||
T10746 |
CDK9-IN-8
|
CDK | Cell Cycle/Checkpoint |
CDK9-IN-8 is a highly potent and selective CDK9 inhibitor (IC50: 12 nM). | |||
T7789 |
DRB
|
HIV Protease | Microbiology/Virology; Proteases/Proteasome |
DRB 是一种核苷类似物,对几种羧基末端结构域激酶(包括酪蛋白激酶 II 、细胞周期依赖性激酶)有抑制作用。它可诱导人类结肠腺癌细胞的 p53 依赖性凋亡,且不会诱发健康细胞遗传毒性应激。 | |||
T5673 |
Senexin A
|
CDK | Cell Cycle/Checkpoint |
Senexin A 是一种有效且选择性的 CDK8 抑制剂,它还抑制 CDK19,Kd 值分别为0.83μM 和0.31μM。 | |||
T40263 |
CDK5-IN-1
CDK5-IN-1 |
||
CDK5-IN-1 is a highly potent inhibitor of CDK5, displaying an inhibitory activity of less than 10 nM. This potent compound is specifically employed in scientific investigations relating to kidney diseases. | |||
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). | |||
T39247 |
CDK7-IN-5
CDK7-IN-5 |
||
CDK7-IN-5, a CDK7 inhibitor with an IC 50 value of less than 100 nM, exhibits potent anticancer properties (WO2015154022A1, Compound 104). | |||
T40160 |
CDK2-IN-7
CDK2-IN-7 |
||
CDK2-IN-7 is a CDK2 inhibitor for treating cancer ( IC 50 < 50 nM). | |||
T39354 |
CDK9-IN-12
CDK9-IN-12 |
||
CDK9-IN-12 displays the optimal CDK9 inhibitory activity with an IC 50 value of 5.41 nM. | |||
T40264 |
CDK7-IN-7
CDK7-IN-7 |
||
CDK7-IN-7, a highly potent and selective inhibitor of CDK7 kinase, exhibits remarkable activity with an IC50 of less than 50 nM. | |||
T72029 |
CDK8-IN-13
|
Apoptosis; CDK | Apoptosis; Cell Cycle/Checkpoint |
CDK8-IN-13是一种 CDK8抑制剂(IC50:51.9 nM),具有强效性、选择性和口服活性。CDK8-IN-13能诱导细胞凋亡,降低了 p-STAT1 S727和p-STAT5 S726的表达。CDK8-IN-13表现出抗肿瘤活性。 | |||
T39943 |
CDK7-IN-6
CDK7-IN-6 |
||
CDK7-IN-6 is a highly effective and specific inhibitor (IC50 ≤100 nM) of cyclin-dependent kinase 7 (CDK7). It showcases remarkable selectivity, with more than a 200-fold preference for CDK7 over CDK1, CDK2, and CDK5. This compound holds significant potential for cancer research purposes. | |||
T39372 |
CDK7-IN-1
CDK7-IN-1 |
||
CDK7-IN-1 is an analog derived from YKL-5-124 and functions as an inhibitor of cyclin-dependent kinase 7 (cdk7). It exhibits strong inhibitory activity, with an IC50 value of less than 100 nM (WO 2016105528 A2, Compound 215). | |||
T36743 |
CDK7/9 tide
|
||
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. | |||
T36744 |
CDK9 Antagonist-1
CDK9 Antagonist-1 |
||
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. | |||
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). | |||
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。 | |||
T64373 |
CDK1-IN-2
cdk1 inhibitor 2 |
CDK | Cell Cycle/Checkpoint |
CDK1-IN-2 (cdk1 inhibitor 2)是一种CDK1抑制剂,IC50为5.8μM。CDK1-IN-2的激酶谱显示了多种激酶的非选择性抑制。 | |||
T72048 |
CDK8-IN-12
|
GSK-3; CDK | Cell Cycle/Checkpoint; PI3K/Akt/mTOR signaling; Stem Cells |
CDK8-IN-12 是一种具有选择性、有效性和口服活性的 CDK8 抑制剂(Ki : 14 nM),是一种抗癌剂。CDK8-IN-12 对 GSK-3α、GSK-3β、PCK-θ 具有抑制作用,Ki 分别为 13 nM、4 nM、109 nM。CDK8-IN-12对 MV4-11 细胞显示出抗增殖活性。 | |||
T60619 |
CDK9-IN-15
|
CDK | Cell Cycle/Checkpoint |
CDK9-IN-15 是一种有效的小分子CDK9抑制剂,可通过降解、抑制 CDK9 来阻断正性转录延长因子 P-TEFb (positive transcription elongation factor b) 对 RNA Poly-II C末端区域的磷酸化,抑制转录,迅速降低细胞内 mRNA 水平,从而引起肿瘤细胞凋亡。 | |||
T2082 |
CDK4-IN-1
|
CDK | Cell Cycle/Checkpoint |
CDK4-IN-1 是一种新型的特异性 CDK4/Cyclin D1 抑制剂,IC50 为 10 nM;分别是 CDK1/Cyclin B (IC50>15 uM) 和 CDK2/Cyclin A (IC50=5.265 uM) 的 1500 倍和 500 倍。 | |||
T14901 |
CCT-251921
|
CDK | Cell Cycle/Checkpoint |
CCT-251921是一种有口服活性的选择性CDK8抑制剂;IC50值为2.3 nM。 | |||
T16391 |
ON-013100
|
CDK | Cell Cycle/Checkpoint |
ON-013100 是有丝分裂的抑制剂,具有抗肿瘤活性。ON-013100能够抑制细胞周期蛋白 D1 的表达。 | |||
T4482 |
CC-671
|
Others; CDK | Cell Cycle/Checkpoint; Others |
CC-671 是一种双重 TTK 蛋白激酶/CLK2抑制剂, 对于 TTK 和 CLK2 的IC50值分别为 0.005 和 0.006 μM。 | |||
T40047 |
CDK6/9-IN-1
CDK6/9-IN-1 |
||
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. |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T5S1467 |
Cucurbitacin E
|
CDK; Autophagy | Autophagy; Cell Cycle/Checkpoint |
Cucurbitacin E 是从黄瓜的攀缘茎中分离得到的一种天然产物。它显着抑制细胞周期蛋白B1/CDC2复合物的活性,具有预防神经变性,具有强效的抗增殖、抗肿瘤、抗炎和镇痛作用行动。 | |||
T2933 |
Wogonin
Vogonin,汉黄芩素 |
Apoptosis; Wnt/beta-catenin; CDK; Autophagy | Apoptosis; Autophagy; Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells |
Wogonin (Vogonin) 是一种具有细胞渗透性的口服类黄酮,具有抗炎和抗癌特性,能够抑制 CDK8和 Wnt 的活性。 | |||
T16324 |
Nimbolide
|
Apoptosis; NF-κB; CDK | Apoptosis; Cell Cycle/Checkpoint; NF-κB |
Nimbolide 是源自印楝叶和花的一种三萜。它抑制CDK4/CDK6激酶活性。它抑制 NF-κB,Wnt,PI3K-Akt,MAPK 和 JAK-STAT 信号通路。它通过抑制NF-κB 而诱导肿瘤细胞凋亡。 | |||
TN1673 |
Garcinone C
伽升沃 C,伽升沃C |
ATM/ATR; CDK; STAT; AChR; Antifection | Cell Cycle/Checkpoint; DNA Damage/DNA Repair; JAK/STAT signaling; Microbiology/Virology; Neuroscience; PI3K/Akt/mTOR signaling; Stem Cells |
Garcinone C 是一种从 Garcinia oblongifolia Champ 中提取的黄酮衍生物,具有抗炎、收敛和促进肉芽的活性。 Garcinone C 是一种 AChE 抑制剂,对某些癌症具有潜在的细胞毒性作用。 | |||
T7444 |
6-(Dimethylamino)purine
N,N-Dimethyladenine,6-二甲基氨基嘌呤 |
Serine/threonin kinase; CDK | Cell Cycle/Checkpoint; Metabolism |
6-(Dimethylamino)purine (N,N-Dimethyladenine) 是一种丝氨酸苏氨酸蛋白激酶和 CDK 抑制剂。 | |||
TN1299 |
Desmethylglycitein
4',6,7-三羟基异黄酮,4',6,7-三羟异黄酮,6-羟基大豆苷元,6,7,4'-Trihydroxyisoflavone |
PI3K; CDK; PKC | Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
Desmethylglycitein (6,7,4'-Trihydroxyisoflavone) 是大豆中苷元的代谢产物,具有抗氧化性和抗癌活性。它是蛋白激酶 C(PKC)α 的直接抑制剂,抑制正常人皮肤成纤维细胞中的太阳紫外线诱导的基质金属蛋白酶1。它在体内直接结合CDK1和CDK2,抑制 CDK1 和 CDK2 活性。 | |||
T17143 |
Toyocamycin
丰加霉素,Vengicide |
Apoptosis; Others; IRE1; Antibiotic; Antifungal | Apoptosis; Cell Cycle/Checkpoint; Microbiology/Virology; Others |
Toyocamycin (Vengicide) 是放线菌类产生的腺苷类似物,为 X 盒结合蛋白 1 (XBP1) 抑制剂,抑制 IRE1α 诱导的 ATP 依赖性 XBP1 mRNA 的断裂,IC50值为 80 nM。它还诱导凋亡。 | |||
T7060 |
Amantadine
1-Aminoadamantane,1-金刚烷胺,金刚烷胺,1-Adamantanamine,1-Adamantylamine |
Others | Others |
Amantadine (1-Aminoadamantane) 是抗病毒药物,也是是 NMDA 型谷氨酸受体的弱拮抗剂,能促进高多巴胺的释放,并阻断多巴胺的再摄取。 | |||
T25192 |
Butyrolactone I
Olomoucin,丁酸内酯I |
CDK | Cell Cycle/Checkpoint |
Butyrolactone I (Olomoucin) 是 CDK 和 cdc2 激酶家族的 ATP 竞争性抑制剂。 Butyrolactone I 在非小细胞肺、小细胞肺和前列腺癌细胞系中显示出抗肿瘤作用。 | |||
TN2080 |
Pinoresinol
松脂酚,松脂素,(+)-Pinoresinol |
Apoptosis; NF-κB; CDK; p53 | Apoptosis; Cell Cycle/Checkpoint; NF-κB |
Pinoresinol ((+)-Pinoresinol) 是一种植物来源的木质素,具有抗炎、保肝和杀真菌活性。它导致 CDK 抑制剂 p21(WAF1/Cip1) 在 mRNA 和蛋白质水平上调,抑制 NF-kappaB 和激活蛋白 1 。 | |||
T38441 |
Manzamine A hydrochloride
|
||
Manzamine A hydrochloride is an orally active beta-carboline alkaloid that exhibits specific inhibitory effects on GSK-3β (IC50 = 10.2 μM) and CDK-5 (IC50 = 1.5 μM). Additionally, it targets vacuolar ATPases, leading to the inhibition of autophagy in pancreatic cancer cells. Manzamine A hydrochloride possesses antimalarial and anticancer properties, and also demonstrates potent activity against HSV-1[4]. |