75
2
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
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。 | |||
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. | |||
T36742 |
CDK5 inhibitor 20-223
CDK5 inhibitor 20-223 |
||
CDK5 inhibitor 20-223, a potent inhibitor of CDK2 and CDK5, demonstrates IC50 values of 6.0 nM and 8.8 nM, respectively. It serves as an effective agent against colorectal cancer (CRC)[1]. | |||
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. | |||
T35555 |
GSK-3/CDK5/CDK2-IN-1
GSK-3/CDK5/CDK2-IN-1 |
||
GSK-3/CDK5/CDK2-IN-1 is an imidazole derivative compound that inhibits cdk5, cdk2, and GSK-3.it has demonstrated applications in cancer research and the study of neurodegenerative diseases [1]. | |||
TP1602 |
[pThr3]-CDK5 Substrate
|
||
[pThr3]-CDK5 Substrate is an effective Phospho-Thr3CDK5 Substrate.[pThr3]-CDK5 Substrate is phosphorylated by CDK5 with a Km value of 6 µM[1]. | |||
TP1660 |
[pThr3]-CDK5 Substrate (TFA)
|
||
[pThr3]-CDK5 Substrate TFA is an effective Phospho-Thr3CDK5 Substrate. [pThr3]-CDK5 Substrate is phosphorylated by CDK5 with a Km value of 6 µM. | |||
T63184 | CDK5-IN-2 | ||
CDK5-IN-2 (compound 15) 是一种高选择性的 CDK5 抑制剂,能够作用于 CDK5/p25 (IC50: 0.2 nM) 和 CDK2/CycA (IC50: 23 nM)。 | |||
T76031 |
[pThr3]-CDK5 Substrate TFA
|
||
[pThr3]-CDK5 Substrate TFA 是 Thr3 磷酸化的CDK5底物。[pThr3]-CDK5 Substrate 来自组蛋白 H1,位于组蛋白 H1 上和CDK5作用的位点。CDK5Substrate 被CDK5磷酸化为 [pThr3]-CDK5 Substrate 的 Km 为 6 μM。 | |||
T61362 |
CDK5-IN-3
|
||
CDK5-IN-3 (compound 11) is a highly potent and selective inhibitor of CDK5, demonstrating significant inhibition with IC50 values of 0.6 nM and 18 nM for CDK5/p25 and CDK2/CycA, respectively. This compound holds promise for further investigation in the context of autosomal dominant polycystic kidney disease (ADPKD) research [1]. | |||
T7426 |
ALSTERPAULLONE
|
Apoptosis; GSK-3; CDK | Apoptosis; Cell Cycle/Checkpoint; PI3K/Akt/mTOR signaling; Stem Cells |
Alsterpaullone 是高效的 CDK 抑制剂,是一种 ATP 竞争性的 GSK-3alpha/GSK-3beta 抑制剂,且作用的 IC50值都为 4 nM。它有用于神经退行性和增生性疾病的研究潜力,具有抗肿瘤活性,诱导白血病细胞凋亡。 | |||
T7167 |
Purvalanol B
NG 95,(2R)-2-[[6-[(3-氯-4-羧基苯基)氨基]-9-(1-甲基乙基)-9H-嘌呤-2-基]氨基]-3-甲基-1-丁醇 |
CDK; Parasite | Cell Cycle/Checkpoint; Microbiology/Virology |
Purvalanol B (NG 95) 是选择性可逆的 ATP 竞争性 CDK 抑制剂。它在一系列其他蛋白激酶 (IC50>1000 nM) 中显示出对 CDK 的选择性。它抑制耐氯喹菌株 P. falciparum 的生长。 | |||
T8230 |
PNU112455A hydrochloride
PNU 112455A |
CDK | Cell Cycle/Checkpoint |
PNU112455A hydrochloride 是 CDK2 和 CDK5 的 ATP 位点竞争性抑制剂,与 CDK2 和 CDK5 的 ATP 位点结合,Km 值为 3.6 和 3.2 μM。 | |||
T2440 |
IC261
SU-5607 |
Apoptosis; Casein Kinase; CDK | Apoptosis; Cell Cycle/Checkpoint; Metabolism; Stem Cells |
IC261 (SU-5607) 是一种选择性的,ATP 竞争性的CK1抑制剂,可触发有丝分裂检查点控制。对Ckiδ、Ckiε、 Ckiα1 和Cdk5的IC50值分别为 1 μM、1 μM 、16 μM 和4.5mM。 | |||
TQ0068 |
NVP-LCQ195
AT9311,LCQ-195 |
CDK | Cell Cycle/Checkpoint |
NVP-LCQ195 (LCQ-195) 是CDK 杂环类抑制剂,对CDK1,CDK2,CDK3和CDK5的IC50为1到42 nM 之间。 | |||
T2095 |
Seliciclib
Roscovitine,R-roscovitine,CYC202 |
CDK | Cell Cycle/Checkpoint |
Seliciclib (Roscovitine) 是 Cdk2/cyclin E 的有效抑制剂,IC50为0.1 µM。它还抑制 Cdk7/cyclin H、Cdk5/p35 和 Cdc2/cyclin B,IC50为 0.49、0.16和0.65 µM。 | |||
T77341 |
GSK-3 inhibitor 4
|
GSK-3; CDK | Cell Cycle/Checkpoint; PI3K/Akt/mTOR signaling; Stem Cells |
GSK-3 inhibitor 4 是一种具有口服活性和脑渗透性的 GSK-3,CDK2 和 CDK5 三重抑制剂,对 GSK-3β,GSK-3α,CDK2 和 CDK5 具有抑制作用,IC50 值分别为 0.56 nM ,0.45 nM ,0.47 μM,0.68 μM。GSK-3 inhibitor 4 可有效降低 Tau protein 水平。GSK-3 inhibitor 4 可用于研究阿尔茨海默症 。 | |||
T2247 |
KenPaullone
9-Bromopaullone,NSC-664704,9-溴-7,12-二氢吲哚并[3,2-D][1]苯并氮杂卓-6(5H)-酮 |
GSK-3; CDK | Cell Cycle/Checkpoint; PI3K/Akt/mTOR signaling; Stem Cells |
KenPaullone (9-Bromopaullone) 是一种CDK1/cyclin B 和GSK-3β抑制剂,IC50值分别为 0.4 μM 和 23 nM。它也抑制 CDK2/cyclin A、CDK2/cyclin E 和 CDK5/p25 的活性,IC50值分别为 0.68 μM、7.5 μM 和 0.85 μM。。它通过增强 TGFβ-Smad3 信号通路增加和延长 foxp3 基因的转录来促进 iTreg 细胞分化。 | |||
T1917 |
GSK 3 Inhibitor IX
BIO,GSK 3 IX,6-BIO,6-Bromoindirubin-3'-oxime,MLS 2052,6-bromoindirubin-3-oxime |
Apoptosis; GSK-3; Tyrosine Kinases; CDK | Apoptosis; Cell Cycle/Checkpoint; PI3K/Akt/mTOR signaling; Stem Cells; Tyrosine Kinase/Adaptors |
GSK 3 Inhibitor IX (6-BIO) 是一种选择性可逆的,ATP 竞争性的 GSK-3α/β和 CDK1-cyclinB 复合体抑制剂,能够抑制 (GSK-3α/β)/CDK1/CDK5 的活性,IC50值分别为 5 nM/320 nM/83 nM。 | |||
T1912 |
Dinaciclib
SCH 727965,PS-095760 |
Apoptosis; CDK | Apoptosis; Cell Cycle/Checkpoint |
Dinaciclib (SCH 727965) 是一种 CDK 抑制剂,抑制 CDK1、CDK2、CDK5 和 CDK9 (IC50分=3/1/1/4 nM),具有选择性。Dinaciclib 具有潜在的抗肿瘤活性,可以抑制胸甘 (dThd) DNA 的整合。 | |||
T5200 |
Indirubin-3'-monoxime
靛玉红-3' -单肟,Indirubin-3'-oxime |
GSK-3; Lipoxygenase; CDK | Cell Cycle/Checkpoint; Metabolism; PI3K/Akt/mTOR signaling; Stem Cells |
Indirubin-3'-monoxime (Indirubin-3'-oxime) 是一种有效的 GSK3β 抑制剂,IC50值为 22 nM。它对 CDK5/p25、CDK1/cyclin B 和CDk2/cyclin E 也有作用,IC50值分别为 100、180 和 250 nM。 | |||
T6358 |
1-Azakenpaullone
1-氮杂坎帕罗酮,azakenpaullone |
GSK-3 | PI3K/Akt/mTOR signaling; Stem Cells |
1-Azakenpaullone (azakenpaullone) 是一种 ATP 竞争性的、具有高度选择性的糖原合成酶激酶3 β (GSK-3β)的抑制剂,其 IC50=18 nM。 | |||
T21588 |
Olomoucine
|
ERK; CDK | Cell Cycle/Checkpoint; MAPK |
Olomoucine 是 Cdk2/cyclin A、Cdc2/CyclinB、CDK2/CyclinE、CDK5/p35 和 ERK1/p44 MAP 激酶的 ATP 竞争性抑制剂,IC50 分别为 7、7、7、3 和 25 µM。 Olomoucine 调节细胞周期并表现出抗黑色素肿瘤活性。 | |||
T36964 |
BML-259
CAY10554 |
CDK | Cell Cycle/Checkpoint |
BML-259 是 CDK5 和 CDK2 的抑制剂,IC50 分别为 64 和 98 nM。 BML-259 可用于癌症和神经退行性疾病治疗的研究。 | |||
T23389 |
SR1664
SR 1664 |
PPAR | DNA Damage/DNA Repair; Metabolism |
SR1664 是一种PPARγ拮抗剂,与结合PPARγ,可有效抑制 Cdk5 介导的PPARγ磷酸化,IC50为80 nM,Ki 为 28.67 nM。 | |||
T21720 |
GP-82996
Cdk4/6 Inhibitor IV,CINK4 |
CDK | Cell Cycle/Checkpoint |
GP-82996 (CINK4) (CINK4) 是 CDK4/6的药理学抑制剂。GP-82996 对 CDK4/cyclin D1、CDK6/cyclin D1 和 Cdk5/p35 的 IC50s 分别为 1.5、5.6 和 25 μM。GP-82996 诱导肿瘤细胞 U2OS 的凋亡,可用于癌症研究。 | |||
T6787 |
BIO-acetoxime
BIA,GSK-3 Inhibitor X |
Apoptosis; GSK-3; HSV | Apoptosis; Microbiology/Virology; PI3K/Akt/mTOR signaling; Stem Cells |
BIO-acetoxime (GSK-3 Inhibitor X) 是一种 GSK3α/β 抑制剂,IC50值均为 10 nM,具有抗惊厥和抗感染作用。 | |||
T2378 |
RGB-286638 free base
|
GSK-3; MEK; JAK; CDK | Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; JAK/STAT signaling; MAPK; PI3K/Akt/mTOR signaling; Stem Cells |
RGB-286638 free base 是一种新型 CDK 抑制剂,抑制cyclin T1-CDK9、cyclin B1-CDK1、cyclin E-CDK2、cyclin D1-CDK4、cyclin E-CDK3和p35-CDK5活性,IC50分别为 1、2、3、4、5 和 5 nM。它也抑制 GSK-3β、TAK1、Jak2 和 MEK1,IC50值分别为 3、5、50和 54 nM。 | |||
T61439 |
DSS30
|
Beta Amyloid; BACE; CDK | Cell Cycle/Checkpoint; Neuroscience |
DSS30 是一种 P25/CDK5抑制剂。DSS30通过抑制淀粉样前体蛋白裂解酶1 (BACEl) 磷酸化,减少 β-淀粉样蛋白 (Aβ) 的分泌发挥作用。DSS30 可用于预防和治疗阿尔茨海默病等神经退行性疾病。 | |||
T22260 |
Aminopurvalanol A
|
CDK | Cell Cycle/Checkpoint |
Aminopurvalanol A 是一种竞争性、选择性和细胞渗透性的Cyclins/Cdk 复合物抑制剂,优先靶向G2/M 期转变进而抑制癌细胞分化。它通过抑制生理获能依赖性肌动蛋白聚合而抑制精子受精能力。 | |||
T6940 |
PHA-767491 hydrochloride
CAY10572,PHA-767491,PHA767491 HCl,CAY-10572 hydrochloride |
Apoptosis; GSK-3; CDK | Apoptosis; Cell Cycle/Checkpoint; PI3K/Akt/mTOR signaling; Stem Cells |
PHA-767491 hydrochloride (CAY-10572 hydrochloride) 是一种Cdc7-Dbf4(DDK)/Cdk9的双重抑制剂,IC50值分别为 10 nM 和 34 nM。 | |||
T10898 |
Samuraciclib hydrochloride
ICEC0942 hydrochloride,CT7001 hydrochloride |
Apoptosis; CDK | Apoptosis; Cell Cycle/Checkpoint |
Samuraciclib hydrochloride (ICEC0942 hydrochloride) 是一种具有选择性,ATP 竞争性和口服活性的CDK7抑制剂,IC50为 41 nM。它以 GI50值为 0.2-0.3 µM 来抑制乳腺癌细胞系的生长,具有抗肿瘤作用。 | |||
T2506 |
AZD-5438
AZD5438 |
CDK | Cell Cycle/Checkpoint |
AZD-5438 有效抑制 CDK1,CDK2,CDK9,IC50值分别为 16 nM, 6 nM, 20 nM,但它对 GSK3β,CDK5,CDK6 的抑制作用较弱。 | |||
T2059 |
Purvalanol A
NG-60 |
Apoptosis; CDK; Autophagy | Apoptosis; Autophagy; Cell Cycle/Checkpoint |
Purvalanol A (NG-60) 是一种CDK 抑制剂,对 cdc2-cyclin B、cdc2-cyclin B、cdk2-cyclin E、cdk4-cyclin D1 和 cdk5-p35 的IC50值分别为 4、70、35、850 和 75 nM。 | |||
T14943 |
CGP60474
|
VEGFR; CDK; PKC | Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
CGP60474 是一种高效的抗内毒素药物,抑制细胞周期蛋白依赖激酶(CDK) ,抑制 CDK1/B、CDK2/E、CDK2/a、CDK4/D、CDK5/p25、CDK7/H 和 CDK9/T 的IC50分别为 26、3、4、216、10、200 和 13 nM。它是选择性和 ATP 竞争性PKC 抑制剂。 | |||
T10172 |
5-Iodo-indirubin-3'-monoxime
|
GSK-3; CDK | Cell Cycle/Checkpoint; PI3K/Akt/mTOR signaling; Stem Cells |
5-Iodo-indirubin-3'-monoxime 是一种 GSK-3β、CDK5/P25和CDK1/cyclin B 抑制剂,IC50值分别为 9、20 和 25 nM,与 ATP 竞争性地结合酶的催化位点。 | |||
T71486 |
NS-0011
|
||
NS-0011 is an inhibitor of CDK5 translocation which increases CDK5 accumulation in the nucleus, suppressing both cancer cell proliferation and xenograft tumorigenesis. | |||
T11652 |
Indirubin-3'-monoxime-5-sulphonic acid
|
Others | Others |
Indirubin-3'-monoxime-5-sulphonic acid is a potent and selective inhibitor of GSK-3β, CDK5, and CDK1 with IC50s of 80nM,5 nM, and 7 nM, respectively. | |||
T22590 |
AT7519 TFA
AT7519 trifluoroacetate |
Others | Others |
AT7519 is a kinase inhibitor (IC50: 0.19, 0.044, 0.51, 0.067, 0.66 and 0.018 μM for CDK1/cyclinB, CDK2/CyclinA, CDK2/Cyclin E, CDk4/CyclinD1, CDK6/Cyclin D3, CDk5/p35). | |||
T21377 | Aloisine A | ||
Aloisine A is a potent and selective CDK/GSK-3 inhibitor. IC50 data of Aloisine A: Cdk1/cyclin B (IC50: 150nM), Cdk2/cyclin A (IC50: 120nM), Cdk2/cyclin E (IC50: 400nM), Cdk5/p25 (IC50: 200nM), Cdk5/p35 (IC50: 160nM), GSK-3α (IC50: 500nM), GSK-3β (IC50: 6 | |||
T24734 |
RP-106
RP 106 |
||
RP-106 is an ATP-competitive inhibitor of CDK5/p25, CDK1/cyclin B, and GSK-3. | |||
T25650 |
LDN-193665
LDN 193665,LDN193665 |
||
LDN-193665 is a potent inhibitor of tau kinase. It acts by targeting CDK5/p25 and GSK3β. | |||
T61890 |
(E/Z)-BIO-acetoxime
|
||
(E/Z)-BIO-acetoxime 是有效的,选择性的GSK-3α/β 抑制剂。对于GSK-3α/β,CDK5/p25,CDK2/cyclin A 和CDK1/cyclin B 的IC50分别为10nM,2.4μM, 4.3μM, 63μM。 | |||
T62554 | PPARγ phosphorylation inhibitor 1 | ||
PPARγ phosphorylation inhibitor 1 (Compound 10) 是一种有效的 PPARγ结合剂 (IC50: 24 nM),具有抗糖尿病效果。PPARγ phosphorylation inhibitor 1 对 CDK5 介导的 PPARγ Ser273 磷酸化表现出抑制作用 (IC50: 160 nM),且几乎无 PPARγ 激动作用。 | |||
T62694 |
(S)-GFB-12811
|
||
(S)-GFB-12811 (compound 596) 是一种选择性的、选择性的 CDK5 抑制剂 (IC50<10 nM)。(S)-GFB-12811 能够用于细胞周期进程、神经元发育、肿瘤发生的研究。 | |||
T60661 |
CP681301
|
||
CP681301 是CDK5的有效抑制剂,具有抗增殖活性。CP681301 在果蝇中表现出抗肿瘤活性。CP681301 降低神经胶质瘤干细胞中 CD133、OLIG2、SOX2、KI67、pCDK5 蛋白水平的表达。CP681301 减少小鼠胶质瘤异种移植物的自我更新。 | |||
T11653 |
Indirubin-5-sulfonate
|
Others | Others |
Indirubin-5-sulfonate shows inhibitory activity against GSK-3β. Indirubin-5-sulfonate is a cyclin-dependent kinase (CDK) inhibitor, with IC50 values of 55 nM, 35 nM, 150 nM, 300 nM and 65 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK4/cyclin D1, | |||
T62695 |
GFB-12811
|
||
GFB-12811,一种具有高选择性的口服活性CDK5抑制剂,其IC50为2.3 nM。该化合物对其他CDK激酶(CDK1/2/6/7/9)表现出显著的选择性。 | |||
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。 | |||
T63080 | CDK1-IN-4 | ||
CDK1-IN-4 (10d) 是一种选择性的 CDK1 抑制剂,能够作用于 CDK1 (IC50: 44.52 nM)、CDK2 (IC50: 624.93 nM) 和 CDK5 (IC50: 135.22 nM)。CDK1-IN-4 能够影响细胞周期,进而对癌细胞的生长表现出抑制作用。CDK1-IN-4 能够用于研究癌症。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TN3673 |
Clausine Z
|
CDK | Cell Cycle/Checkpoint |
Clausine Z exhibits inhibitory activity against cyclin-dependent kinase 5 (CDK5) and shows protective effects on cerebellar granule neurons in vitro. | |||
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]. |