38
2
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
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。 | |||
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。 | |||
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。 | |||
T2028 |
NG 52
NG52,NG-52,Compound 52 |
CDK | Cell Cycle/Checkpoint |
NG 52 (NG-52) 是可逆和 ATP 相容性且具有口服活性的Cdc28p 和Pho85p 激酶抑制剂,IC50分别为 7 μM 和 2 μM。它还抑制磷酸甘油酸激酶 1 的活性,IC50值为 2.5 μM。 | |||
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。 | |||
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。 | |||
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。 | |||
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)。 | |||
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。 | |||
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。 | |||
T69188 |
Aloisine B
AloisineB |
GSK-3; CDK | Cell Cycle/Checkpoint; PI3K/Akt/mTOR signaling; Stem Cells |
Aloisine B (AloisineB) inhibited cyclin-dependent kinase and glycogen synthase kinase with IC50 values of 0.85 µM and 0.75 µM, respectively. Aloisine B has antiviral activity and can be used to study Alzheimer's, diabetes, HIV and Parkinson's. | |||
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。 | |||
T2679 |
BMS-265246
BMS265246 |
CDK | Cell Cycle/Checkpoint |
BMS-265246 是一种有效的选择性 CDK1/2 抑制剂,对 CDK1/cyclin B 和 CDK2/cyclin E 的 IC50分别为6 nM 和9 nM。 | |||
T16359 |
NU6140
|
CDK; Aurora Kinase | Cell Cycle/Checkpoint; Chromatin/Epigenetic |
NU6140 是选择性CDK2-cyclin A 抑制剂,IC50为0.41 μM。它显示出比其他 CDK 高 10 到 36 倍的选择性。它还抑制Aurora A 和Aurora B 的活性,IC50值分别为 67 和 35 nM。它还增强细胞凋亡作用并具有抗癌活性。 | |||
T15732 |
Ribociclib succinate
LEE011 琥珀酸盐,瑞博西尼琥珀酸盐,LEE011 succinate |
CDK | Cell Cycle/Checkpoint |
Ribociclib succinate (LEE011 succinate) 是一种高度特异性的CDK4/6抑制剂,IC50值分别为 10 nM 和 39 nM。它对细胞周期蛋白 B/CDK1 复合物的效力低 1000 倍。 | |||
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。 | |||
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。 | |||
T6312 |
R547
Ro 4584820 |
Apoptosis; GSK-3; PKA; CDK | Apoptosis; Cell Cycle/Checkpoint; PI3K/Akt/mTOR signaling; Stem Cells; Tyrosine Kinase/Adaptors |
R547 (Ro 4584820) 是一种口服有效,选择性, ATP 竞争性CDK 抑制剂,对 CDK1/cyclin B、 CDK2/cyclin E 和 CDK4/cyclin D1 作用的Ki 值分别为 2 nM、3 nM、1 nM。 | |||
T6187 |
TDZD-8
GSK-3β Inhibitor I,NP 01139 |
GSK-3 | PI3K/Akt/mTOR signaling; Stem Cells |
TDZD-8 (NP 01139) 是抑制GSK-3β的抑制剂,其 IC50=2 μM。它对 Cdk-1/cyclin B,CK-II,PKA 和 PKC 的作用较弱,IC50值均 >100 μM。 | |||
T35610 |
2,5-dimethyl Celecoxib
|
Apoptosis; Wnt/beta-catenin; Prostaglandin Receptor | Apoptosis; Cytoskeletal Signaling; GPCR/G Protein; Immunology/Inflammation; Stem Cells |
2,5-dimethyl Celecoxib 是塞来昔布衍生物和微粒体前列腺素 E 合酶 1 (mPGES-1) 的靶向抑制剂,mPGES-1 是炎症介质 PGE2 合成途径中的关键酶。 | |||
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。 | |||
T24734 |
RP-106
RP 106 |
||
RP-106 is an ATP-competitive inhibitor of CDK5/p25, CDK1/cyclin B, and GSK-3. | |||
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, | |||
T68555 |
Alsterpaullone, 2-Cyanoethyl
|
||
Alsterpaullone, 2-Cyanoethyl is a selective dual inhibitor of Cdk1/cyclin B and GSK-3β. | |||
T27033 |
CKD-712
CKD 712,CKD712 |
||
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 | |||
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 | |||
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。 | |||
T15730 |
Ribociclib hydrochloride
LEE011 hydrochloride,瑞博西尼盐酸盐 |
CDK | Cell Cycle/Checkpoint |
Ribociclib hydrochloride is a highly specific CDK4/6 inhibitor (IC50: 10 nM and 39 nM, respectively). It is over 1,000-fold less potent against the cyclin B/CDK1 complex. | |||
T13454 |
(S)-Purvalanol B
(S)-NG 95 |
BCL | Apoptosis |
(S)-Purvalanol B 是 Purvalanol B 的 S 对映体,Purvalanol B 是一种细胞周期蛋白依赖性激酶(CDK)抑制剂。 | |||
T21950 |
K 00546
|
||
K00546 是一种有效的细胞周期蛋白依赖性激酶CDK1和CDK2抑制剂,对CDK1/cyclin B 和CDK2/cyclin A 的IC50分别为 0.6 nM 和 0.5 nM。K00546 也是一种有效的 CDC2 样激酶 1 (CLK1) 和CLK3抑制剂,IC50分别为 8.9 nM 和 29.2 nM。 | |||
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。 | |||
T15731 |
Ribociclib succinate hydrate
LEE011 succinate hydrate |
CDK | Cell Cycle/Checkpoint |
Ribociclib succinate hydrate is a highly specific CDK4/6 inhibitor (IC50s: 10 nM and 39 nM, respectively). It also is over 1,000-fold less potent against the cyclin B/CDK1 complex. | |||
T40546 |
3-Methylthienyl-carbonyl-JNJ-7706621
|
||
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. | |||
T10436L |
AZD4573 HCl (2057509-72-3 free base)
AZD4573 hydrochloride,AZD4573,AZD4573 HCl,AZD-4573,AZD 4573 |
||
AZD-4573 is a selective and short-acting inhibitor of the serine/threonine cyclin-dependent kinase 9, the catalytic subunit of the RNA polymerase II elongation factor positive transcription elongation factor b. It also has a potential antineoplastic activ | |||
T69091 |
CBP501
|
||
CBP501 is a peptide with G2 checkpoint-abrogating activity. G2 checkpoint inhibitor CBP501 inhibits multiple serine/threonine kinases, including MAPKAP-K2, C-Tak1, and CHK1, that phosphorylate serine 216 of the dual-specific phosphatase Cdc25C (cell division checkpoint 25 C); disruption of Cdc25C activity results in the inhibition of Cdc25C dephosphorylation of the mitotic cyclin-dependent kinase complex Cdc2/cyclin B, preventing entry into the mitotic phase of the cell cycle. | |||
T37065 |
6-Chloro-2-fluoropurine
|
||
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.... | |||
T83890 |
Flavokawain 1i
Flavokavain 1i |
||
Flavokawain 1i是chalcones的派生物,包括flavokawain A、flavokawain B和flavokawain C,具有抗癌和抗病毒活性。在30 µM浓度下,Flavokawain 1i能够抑制gefitinib抵抗性的H1975非小细胞肺癌(NSCLC)细胞的增殖率达到36%,同时降低热休克蛋白90(Hsp90)客体蛋白EGFR、c-Met、HER2、Akt和细胞周期依赖性激酶4(Cdk4)的蛋白水平,并提高Hsp70蛋白水平,这是Hsp90抑制的标志。肌肉内给药的Flavokawain 1i能够降低感染猪生殖与呼吸综合征病毒(PRRSV)猪只的病毒滴度。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T6169 |
Indirubin
Indigopurpurin,Indigo red,NSC 105327,Couroupitine B,靛玉红 |
Apoptosis; Raf; GSK-3; CDK | Apoptosis; Cell Cycle/Checkpoint; MAPK; PI3K/Akt/mTOR signaling; Stem Cells |
Indirubin (Couroupitine B) 是一种具有抗炎症和抗癌活性的天然产物。 | |||
T6S1917 |
Schisandrol B
Gomisin A,TJN-101,Besigomsin,五味子醇乙,Gamma-Schisandrin,戈米辛A,Schizandrol B,Wuweizi alcohol-B |
P450; Reactive Oxygen Species; Autophagy | Autophagy; Immunology/Inflammation; Metabolism; NF-κB |
Schisandrol B (Besigomsin) 是华中五味子的主要活性成分,具有保肝、抗炎、抗糖尿病和抗氧化的作用。它抑制活性氧的产生,也抑制 P-糖蛋白和CYP3A 的活性。 |