CDK(细胞周期蛋白依赖性激酶)
CDKs (Cyclin-dependent kinases) are serine-threonine kinases first discovered for their role in regulating the cell cycle. They are also involved in regulating transcription, mRNA processing, and the differentiation of nerve cells. CDKs are relatively small proteins, with molecular weights ranging from 34 to 40 kDa, and contain little more than the kinase domain. In fact, yeast cells can proliferate normally when their CDK gene has been replaced with the homologous human gene. By definition, a CDK binds a regulatory protein called a cyclin. Without cyclin, CDK has little kinase activity; only the cyclin-CDK complex is an active kinase.
There are around 20 Cyclin-dependent kinases (CDK1-20) known till date. CDK1, 4 and 5 are involved in cell cycle, and CDK 7, 8, 9 and 11 are associated with transcription.
CDK levels remain relatively constant throughout the cell cycle and most regulation is post-translational. Most knowledge of CDK structure and function is based on CDKs of S. pombe (Cdc2), S. cerevisia (CDC28), and vertebrates (CDC2 and CDK2). The four major mechanisms of CDK regulation are cyclin binding, CAK phosphorylation, regulatory inhibitory phosphorylation, and binding of CDK inhibitory subunits (CKIs).
Products for CDK
- Cat.No. 产品名称 Information
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GC11401
Roscovitine (Seliciclib,CYC202)
细胞周期蛋白B激酶抑制剂,Roscovitine; CYC202; R-roscovitine
A potent inhibitor of cyclin-dependent kinase 2 -
GC11396
SNS-032 (BMS-387032)
BMS-387032
A Cdk2, Cdk7, and Cdk9 inhibitor -
GC15571
SU 9516
A pro-apoptotic Cdk2/cyclin A inhibitor
-
GC12064
SB1317
14-甲基-20-氧杂-5,7,14,27-四氮杂四环[19.3.1.1(2,6).1(8,12)]二十七碳-1(25),2,4,6(27),8,10,12(26),16,21,23-十烯,TG02;SB 1317;TG 02;SB-1317;TG-02
A multi-kinase inhibitor -
GC11324
PHA-767491
CAY10572;PHA767491;PHA 767491;CAY-10572;CAY 10572
A potent Cdc7 kinase inhibitor -
GC16959
NVP-LCQ195
4-(2,6-二氯苯甲酰基氨基)-1H-吡唑-3-羧酸N-[1-(甲基磺酰基)哌啶-4-基]酰胺,LCQ-195;AT-9311;NVP LCQ195;LCQ 195;AT9311;AT 9311
NVP-LCQ195 (AT9311; LCQ195) 是 CDK1、CDK2、CDK3 和 CDK5 的小分子杂环抑制剂,IC50 为 1-42 nM。 -
GC11823
LY2835219 free base
阿贝西利,CDK4/6 dual inhibitor;LY 2835219 (free base);LY-2835219 (free base)
LY2835219 free base是 CDK4 和 CDK6 的强效选择性抑制剂,在非细胞实验中的 IC50 分别为 2nM 和 10nM。 -
GC16063
Flavopiridol
夫拉平度; HMR-1275; Alvocidib; L86-8275
An inhibitor of cyclin-dependent kinases -
GC18028
CVT-313
CVT 313;NG 26;CVT313;NG26;NG-26
A Cdk2 inhibitor -
GC17359
CDK9 inhibitor 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
CDK9 inhibitor 2 是一种特殊的细胞周期蛋白依赖性激酶 9 (CDK9) 抑制剂,提取自专利 WO/2012131594A1,化合物 CDKI(8),在 H929 多发性骨髓瘤 (MM) 细胞系中的 IC50 分别为 5 nM 和 7 nM(72 小时) ) 和 A2058 皮肤细胞系(72 小时)。 -
GC12871
CDK9 inhibitor
N-[5-[[6-[3-(1,3-二氧代异吲哚-2-基)苯基]嘧啶-4-基]氨基]-2-甲基苯基]甲烷磺酰胺
CDK9 inhibitor 是一种新型的选择性 CDK9 抑制剂,用于治疗 HIV 感染,对 CDK9/CycT1 的 IC50 为 39 nM,从参考化合物 87 中提取。 -
GC12425
CDK inhibitor II
CDK inhibitorII
CDK inhibitor II 是一种有效且特异性的 CDK9 抑制剂,IC50 <8 nM,取自参考文献 1,实施例 4。 -
GC12001
BS-181
N5-(6-氨基己基)-3-异丙基-N7-苄基吡唑并[1,5-A]嘧啶-5,7-二胺,BS 181; BS181
A selective Cdk7 inhibitor -
GC15597
AT7519 trifluoroacetate
4-[(2,6-二氯苯甲酰基)氨基]-N-4-哌啶基-1H-吡唑-3-甲酰胺三氟乙酸盐,AT 7519 trifluoroacetate;AT-7519 trifluoroacetate
AT7519 (AT7519M) TFA 作为一种有效的 CDK 抑制剂,对 CDK1、CDK2、CDK4 到 CDK6 和 CDK9 的 IC50 分别为 210、47、100、13、170 和 <10 nM。 -
GC13998
AT7519 Hydrochloride
N-(4-哌啶基)-4-(2,6-二氯苄氨基)-1H-吡唑-3-羧胺盐酸盐,AT 7519 Hydrochloride;AT-7519 Hydrochloride
A Cdk inhibitor -
GC12612
JNJ-7706621
JNJ7706621, JNJ 7706621
A dual inhibitor of CDKs and Aurora kinases -
GN10696
Garcinone C
伽升沃 C
Garcinone C 是一种黄酮衍生物,是一种从 Garcinia oblongifolia Champ 中提取的天然化合物,用作抗炎、收敛和促进肉芽的药物,对某些癌症具有潜在的细胞毒性作用。 Garcinone C 刺激 ATR 和 4E-BP1 的表达水平,同时有效抑制 cyclin B1、cyclin D1、cyclin E2、cdc2、Stat3 和 CDK7 的表达水平。 Garcinone C 以时间和剂量依赖性方式显着抑制人鼻咽癌 (NPC) 细胞系 CNE1、CNE2、HK1 和 HONE1 的细胞活力。 -
GN10526
Cucurbitacin E
葫芦素 E; α-Elaterin; α-Elaterine
A natural triterpene -
GN10017
Wogonin
汉黄芩素
A flavonoid with anti-inflammatory and antitumor activities